Abstract

Provided is a cocrystal of a compound (I) and glutaric acid useful for treating cancer and a process for the preparation thereof, pharmaceutical compositions thereof and use for the treatment of cancer comprising administering the cocrystal described herein to a patient in need thereof.

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia
• A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone

Abstract

Provided are solid forms of a compound useful for treating cancer, such as pharmaceutically acceptable salts and cocrystals, pharmaceutical compositions thereof, and use for the treatment cancer comprising administering the solid forms described herein to a patient in need thereof.

IPC Classes  ?

• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07C 309/25 - Sulfonic acids having sulfo groups bound to carbon atoms of rings other than six-membered aromatic rings of a carbon skeleton
• C07C 309/28 - Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
• A61P 35/00 - Antineoplastic agents

Abstract

Crystalline forms of Compound A: Crystalline forms of Compound A: Crystalline forms of Compound A: characterized by its X-ray powder diffraction diagram, solid-state 13C NMR spectrum, MIR spectrum and Raman spectrum and pharmaceutical compositions containing it.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems

Abstract

A salt and related crystalline forms of Compound A: A salt and related crystalline forms of Compound A: A salt and related crystalline forms of Compound A: wherein the salt is the hydrogen sulfate salt, A salt and related crystalline forms of Compound A: wherein the salt is the hydrogen sulfate salt, characterised by its X-ray powder diffraction diagram, method for preparing the same via crystallization, and pharmaceutical compositions containing it.

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Abstract

The present invention relates to a recombinant microorganism which is modified to be capable of producing diosmin and hesperidin and to the use thereof for producing diosmin and/or hesperidin.

IPC Classes  ?

• C12P 19/60 - Preparation of O-glycosides, e.g. glucosides having an oxygen of the saccharide radical directly bound to a non-saccharide heterocyclic ring or a condensed ring system containing a non-saccharide heterocyclic ring, e.g. coumermycin, novobiocin
• C12N 9/00 - Enzymes, e.g. ligases (6.)ProenzymesCompositions thereofProcesses for preparing, activating, inhibiting, separating, or purifying enzymes
• C12N 9/02 - Oxidoreductases (1.), e.g. luciferase
• C12N 9/10 - Transferases (2.)
• C12N 9/88 - Lyases (4.)
• C12N 9/90 - Isomerases (5.)

Abstract

The present invention relates to a novel recombinant antibody or antigen-binding portion thereof targeting MET, as well as ADCs comprising this antibody or antigen-binding portion thereof, compositions comprising this antibody or antigen- binding portion thereof, compositions comprising ADCs comprising said anti-MET antibody or antigen-binding portion thereof, the use of said antibody or antigen- binding portion thereof or of said ADCs or of said compositions comprising anti- MET antibody or anti-MET ADC.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents

Abstract

The present disclosure provides PROTAC compounds represented by Formula (A): D-L-DSM (A), or an enantiomer, a diastereoisomer, and/or a pharmaceutically acceptable salt of any one of the foregoing, wherein: DSM is a degradation signaling compound {e.g., an E3 ubiquitin ligase recruitment ligand, such as a CRBN ligand or a VHL ligand) covalently attached to a linker L; L is a linker that covalently attaches DSM to D; and D is a Bcl-xL inhibitor compound of Formula (I) or Formula (II) covalently attached to the linker L: (I); (II) wherein the definitions for the variables are described herein. Also provided are pharmaceutical compositions comprising the PROTAC compounds of the present disclosure and methods of use and methods of making thereof. The present disclosure provides PROTAC compounds represented by Formula (A): D-L-DSM (A), or an enantiomer, a diastereoisomer, and/or a pharmaceutically acceptable salt of any one of the foregoing, wherein: DSM is a degradation signaling compound {e.g., an E3 ubiquitin ligase recruitment ligand, such as a CRBN ligand or a VHL ligand) covalently attached to a linker L; L is a linker that covalently attaches DSM to D; and D is a Bcl-xL inhibitor compound of Formula (I) or Formula (II) covalently attached to the linker L: (I); (II) wherein the definitions for the variables are described herein. Also provided are pharmaceutical compositions comprising the PROTAC compounds of the present disclosure and methods of use and methods of making thereof.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• A61P 35/00 - Antineoplastic agents
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings

Abstract

Process for the preparation of diosmin and flavonoid fraction by direct oxidation of hesperidin.

IPC Classes  ?

• C07H 17/07 - Benzo[b]pyran-4-ones

Abstract

The present invention relates to novel trimetazidine solid phases, leading to a reduced formation of trimetazidine nitrosamine in presence of nitrites.

IPC Classes  ?

• A61K 9/19 - Particulate form, e.g. powders lyophilised
• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/14 - Particulate form, e.g. powders
• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
• A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• A61K 35/06 - Mineral oils, e.g. paraffinic oils or aromatic oils based on aromatic hydrocarbons
• A61K 47/38 - CelluloseDerivatives thereof
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

This invention relates to anti-NKG2A antibodies and methods of using them in enhancing immunity in a patient in need thereof and in treating cancer.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 35/00 - Antineoplastic agents

Abstract

This invention relates to combination therapies targeting two or all of PD-1, TIM-3, and LAG-3 using antibodies specific for these targets in patients who are in need of enhanced immunity. Also included in the invention are compositions useful in the therapies. The therapies are useful in treating diseases such as cancers.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61K 39/00 - Medicinal preparations containing antigens or antibodies
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 35/00 - Antineoplastic agents

Abstract

Antibody-drug conjugates that bind to human oncology targets are disclosed. The antibody-drug conjugates comprise a Bcl-xL inhibitor drug moiety. The disclosure farther relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising Bcl-xL inhibitor drug moiety and methods of making same are also disclosed.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents

Abstract

Compounds of formula (I): Compounds of formula (I): Compounds of formula (I): wherein A1, A2, Ra, Rb, Rc, Rd, R3, R4, R5 and T are as defined in the description. Compounds of formula (I): wherein A1, A2, Ra, Rb, Rc, Rd, R3, R4, R5 and T are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.

IPC Classes  ?

• A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
• A61K 9/20 - Pills, lozenges or tablets
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 471/04 - Ortho-condensed systems
• C07D 491/10 - Spiro-condensed systems
• C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
• C07D 498/04 - Ortho-condensed systems
• C07D 498/14 - Ortho-condensed systems

Abstract

Compounds of formula (I) are useful as LRRK2 kinase inhibitors. Compounds of formula (I) are useful as LRRK2 kinase inhibitors.

IPC Classes  ?

• C07D 491/16 - Peri-condensed systems
• A61K 9/20 - Pills, lozenges or tablets
• A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
• A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
• A61K 31/4192 - 1,2,3-Triazoles
• A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
• A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• C07D 491/06 - Peri-condensed systems
• C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
• C07D 498/06 - Peri-condensed systems
• C07D 498/16 - Peri-condensed systems

Goods & Services

Business administration of patient reimbursement programs, namely, programs to provide patients reimbursement for insurance co-payments for medications Financial administration of patient reimbursement programs, namely, programs to provide patients reimbursement for insurance co-payments for medications

Goods & Services

Business administration of patient reimbursement programs, namely, programs to provide patients reimbursement for insurance co-payments for medications Financial administration of patient reimbursement programs, namely, programs to provide patients reimbursement for insurance co-payments for medications

Abstract

The present invention relates to a new process for preparing 5-{5-chloro-2-[(38)-3-[(morpholin-4-yl)methyl]-3.4-dihydr oisoquinoline-2(1H)-carbonyl]phenyl}-1,2-dimethyl-1/H-pyrrole-3-carboxylic acid derivatives and its application for the production of pharmaceutical compounds.

IPC Classes  ?

• C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 207/50 - Nitrogen atoms
• C07K 1/10 - General processes for the preparation of peptides using coupling agents

Goods & Services

Pharmaceutical preparations, medicated and veterinary preparations; Sanitary preparations for medical purposes; Foodstuffs and dietetic substances for medical or veterinary purposes, Food for babies for medical use; Adhesive tapes for medical purposes, Materials prepared for bandages (dressings) For medical purposes; Material for stopping teeth, dental wax; Disinfectants for medical use; vermin destroying preparations for medical purposes; Fungicides for medical use, Weedicides; Natural remedies for medical purposes; Probiotic preparations for medical purposes; Dietary fibre for medical purposes; Stem cells; Pharmaceuticals for use in regenerative medicine; Enzymes for medical and veterinary purposes; Phytotherapy preparations for medical purposes; Patches for pharmaceutical purposes. Scientific, optical, weighing, measuring, signalling, checking (supervision), life-saving and teaching apparatus and instruments; Apparatus and instruments for conducting, switching, transforming, accumulating, regulating or controlling electricity; Apparatus for recording, transmission or reproduction of sound or images; Recording substrates [magnetic]; Digital recording media; Phonograph records; Apparatus and equipment for processing data and information; Software; Computers; Computer programs, downloadable; Data-processing equipment; Computer software recorded on magnetic media or downloaded from a remote computer network; Computer software applications, downloadable; Downloadable applications for use with mobile devices and Downloadable applications for mobile apparatus; Digital applications; Telecommunications hardware for use with mobile networks; Transmitters of electronic signals; Computer software for monitoring physiological signals; Computer software for analysing, storing and monitoring physiological data, including predictive medicine, diagnosis, monitoring and warning software; Software for algorithms; Artificial intelligence software; Computer platforms in the form of computer software for sharing information; Analysis systems based on artificial intelligence (computer software); Computer software for updating and exchanging data on a virtual platform for exchanging information between patients and healthcare professionals; Computer software for teleconsultation and video consultation; Computer software for online data management in the field of cloud computing networks and applications; Computer software for medical purposes, for collecting and processing patient data and managing diagnostic and therapeutic methods using medico-technical apparatus; Medical imaging software; PDAs (personal digital assistants); Smart bracelets; Smart scales, Connected bracelets (measuring instruments); Smart self-measurement tools; Spectacles, contact lenses; Camcorders; Wearable activity trackers; Augmented reality software; Virtual reality computer programs; Electronic chips connected to information systems; Virtual reality headsets; pressure measurement apparatus; Pressure indicators; In-ear headphones; Information display terminals; Position fixing apparatus; Electronic tags; Travel distance monitors; Personal electronic apparatus for displaying, measuring, recording, organising, handling, analysing and receiving data, text, images and audio files relating to health and wellbeing; Receivers used for detecting, storing and processing electronic data transmitted by a sensor that records data relating to health. Surgical, medical, dental and veterinary apparatus and instruments; Orthopedic articles; Artificial limbs, eyes and teeth; Suture materials; Medical device; Diagnostic and tracking devices for medical purposes; compression socks, Compression panty hose and Compression calf supports; Stockings, tights and socks for varicose veins; Compression dressing strips; Medical apparatus, instruments and equipment for introducing pharmaceutical preparations into the human body; Infusion devices and syringes for medical purposes; Diagnostic tools and instruments for medical purposes; Apparatus for blood analysis [for medical use]; Medical apparatus for use in endoscopy; Inhalers; Physiological monitoring and measuring apparatus for medical purposes; Telemetry apparatus for medical use; Acupuncture instruments; Hearing aids; automated analyzers for medical purposes; Medical imaging apparatus; Massage apparatus; Computer-aided medical apparatus and instruments; Control and monitoring apparatus for healthcare, both for medical purposes; Sensors, monitors and display screens in the field of healthcare, both for medical purposes; Electric or electronic sensors for use in detecting, measuring, processing, collecting, recording and transmitting health-related variables, both for medical purposes; Medical image analysis systems based on artificial intelligence. Assistance in the operation or management of a commercial business; Business management assistance services; Commercial assistance in the creation of businesses; Computerized file management; Management of databases and computer files on virtual data exchange platforms; Business intermediary services relating to the matching of potential private investors with entrepreneurs needing funding; Recording, transcription, composition, compilation or systematisation of written communications, recordings and information into databases; Collating mathematical or statistical data; Computerized file management; Compilation of information into computer databases; Updating and maintenance of data in computer databases; Management and processing of data, in particular medical, surgical and pharmacological data, for others; Business management and organization consultancy; Business management consultancy; business data analytics; Market studies; Market research information; Establishment of relationships between investors, natural or legal persons, and companies seeking own funds; Business efficiency expert services; Retail or wholesale services for pharmaceutical, veterinary and sanitary preparations, medical and surgical apparatus and instruments and medical supplies; Sales promotion to others; Public relations services; Sponsorship search; Auctioneering services; Organisation of events for commercial or advertising purposes; Subsidy administration and management (business management assistance); Supply of personnel; Collecting information for business; Data processing verification; Data retrieval services. Business advice and consultancy relating to financing; Providing funding for commercial entities and entrepreneurs; Information and consultancy in relation to financial and monetary affairs; Setting up of financial transactions and investments; Financial studies and consultancy relating to capital structuring and industrial strategy; Investing of capital in young businesses; Project financing; Mutual funds and capital investments; Financial sponsorship; Capital investment. Education providing of training; Arranging and conducting of colloquiums, events, congresses, seminars, conferences, symposiums, competitions and exhibitions; Publication of texts; Online publication of specialist magazines and books; Entertainment services; Sporting and cultural activities; Organization of competitions [education or entertainment]; Physical fitness consultation; Coaching [training]. Scientific and technological services and research and design relating thereto; Industrial analysis and research services; Scientific research for medical purposes; Design and development of computer hardware and software; Research, design and development of monitoring and diagnostic tools; Clinical trials; Scientific laboratory services; Evaluation and study of scientific and technical projects; Cloud computing; Rental of computer software; Updating of computer software; Computer programming; Research and development of new products for others; Scientific research; Electronic data storage; Hosting services of data on internet platforms, Hosting web portals, Providing of temporary use of non-downloadable software applications accessible via a website; Design of websites on the internet, in particular collaborative platforms; Engineering services relating to robotics; Development of computer software for patients; Platforms (services) for the exchange of information between patients and healthcare professionals; Software as a service [SaaS]; Biological analysis; Conversion of data or documents from physical to electronic media. Medical services; Animal healthcare services; Medical services, hygienic and beauty care for human beings or animals; Medical consultancy in the field of health care; Pharmacy advice; Healthcare, medical assistance; Telemedicine services; Therapy services; Medical diagnostic services; Medical diagnostic services via electronic and telematic means; Medical services, namely: Provision of health care services in domestic homes; Individualised medical prescriptions; Online medical prescriptions; Consultancy in relation to medical treatment in the home; Medical advice on self-medication; Medical information for patients; Remote medical examinations; Medical advice regarding personal well-being [health]; Medical monitoring of patients, including provided remotely; Providing medical support in the monitoring of patients receiving treatments; Medical information retrieval services; Medical services, namely: health check services. Providing personal support services for families of patients with life threatening disorders; Social networking services.

Goods & Services

(1) Préparations pharmaceutiques pour le traitement de maladies cardio-vasculaires, de troubles immunoinflammatoires, de troubles neuro-psychiatriques, pour le traitement du cancer et du diabète; produits hygiéniques pour la médecine, nommément savons désinfectants et lingettes désinfectants; aliments et substances diététiques à usage médical, nommément aliments pour diabétiques, aliments pour bébés; compléments alimentaires minéraux et vitaminés pour l'état général de la santé; emplâtres en tant que matériel pour pansements; matières pour plomber les dents et pour empreintes dentaires; désinfectants pour instruments et appareils dentaires et médicaux; produits pour la destruction d'animaux nuisibles; fongicides, herbicides; patchs de diagnostic à appliquer sur la peau pour dépister les allergies. (2) Appareils pour l'enregistrement, la transmission, la reproduction du son et des images, nommément récepteurs et transmetteurs audio, vidéo et stéréo, amplificateurs optiques et sonores, webcam; logiciels pour le traitement de données physiques et physiologiques provenant d'un dispositif médical nommément moniteur d'activité cardiaque, moniteur d'oxygène à usage médical, moniteur de tension artérielle, moniteur de pouls, déployant ces données sur le réseau informatique mondial et gérant ces données sur une plateforme informatique en nuage; logiciels pour utilisation dans la gestion d'informations médicales sur les patients; logiciels informatiques enregistré et téléchargeables pour le suivi et la gestion des dossiers médicaux des patients; logiciels enregistrés sur supports magnétiques ou téléchargés d'un réseau informatique distant pour le diagnostic, la surveillance, la prévention et le traitement des troubles cardiovasculaires, immuno-inflammatoires, neuropsychiatriques; logiciels enregistrés sur supports magnétiques ou téléchargés d'un réseau informatique distant pour le diagnostic, la surveillance, la prévention et le traitement du cancer et du diabète; applications téléchargeables pour téléphones mobiles et tablettes électroniques pour le diagnostic, la surveillance, la prévention et le traitement du cancer et du diabète; ordinateurs; programmes du système d'exploitation pour ordinateurs; logiciels enregistrés sur un disque pour le diagnostic, la surveillance, la prévention et le traitement des troubles cardiovasculaires, immuno-inflammatoires, neuropsychiatriques, du cancer et du diabète; logiciels enregistré sur une bande pour le diagnostic, la surveillance, la prévention et le traitement des troubles cardiovasculaires, immuno inflammatoires, neuropsychiatriques, du cancer et du diabète; émetteurs récepteurs; logiciels de contrôle de signaux physiologiques; logiciels de contrôle d'analyse, de mémorisation et de traitement des données physiologiques dans le domaine de la médecine; logiciels contenant des algorithmes mathématiques pour l'analyse et l'évaluation de la santé; logiciels de reconnaissance faciale, logiciels de reconnaissance vocale; logiciels pour le partage d'informations et de données par ordinateurs et réseaux de communication relatifs à la gestion d'informations médicales; logiciels pour mise à jour et échange de données sur une plateforme virtuelle d'échange d'informations entre patients et professionnels de santé; logiciel de téléconsultation et de vidéo consultation; logiciels de gestion de données en ligne dans le domaine des applications et des réseaux d'informatique dans le nuage (cloud computing); logiciels à usage médical, servant à la collecte et au traitement de données concernant les patients et à la commande de méthodes de diagnostic et thérapeutiques à l'aide d'appareils médico-techniques; logiciels d'imagerie médicale; assistant numérique personnel; émetteurs récepteurs; caméras vidéos; montres intelligentes; capteurs d'activité à porter sur soi; bracelets connectés à usage médical; balances connectées à usage médical; montres connectées pour le traitement, la surveillance et l'analyse médicale de signes vitaux; montres intelligentes; lunettes, lentilles de contact; caméras vidéo; capteurs d'activité à porter sur soi; logiciels de réalité augmentée pour permettre aux médecins d'effectuer des essais chirurgicaux; logiciels de réalité virtuelle pour permettre aux médecins d'effectuer des essais chirurgicaux; puces électroniques reliées à un système d'information; casques de réalité virtuelle; indicateurs de pression artérielle; écouteurs intra-auriculaires; terminaux à écran, terminaux intelligents; système mondial de localisation (GPS) consistant en ordinateurs, logiciels, transmetteurs, récepteurs et unités d'interfaces réseau; étiquettes électroniques; application mobile téléchargeable destinée à faciliter le suivi des données relatives à la santé et au bien-être des patients atteints troubles cardiovasculaires, immuno-inflammatoires, neuropsychiatriques, de cancers et de diabète, application mobile téléchargeable permettant de définir, de suivre et de contrôler les objectifs de santé et de bien-être des utilisateurs; récepteurs de signaux électroniques sans fil à savoir récepteurs d'ondes radioélectriques et d'ondes électromagnétiques, émetteurs-récepteurs de signaux électroniques sans fil à savoir émetteurs récepteurs d'ondes radioélectriques et d'ondes électromagnétiques, émetteurs-récepteurs de signaux électroniques sans fil avec port USB à savoir émetteurs-récepteurs d'ondes radioélectriques et d'ondes électromagnétiques avec port USB pour la détection, le stockage, le traitement de données électroniques émanant d'un capteur qui enregistre les données liées à la santé. (3) Instruments chirurgicaux à usage médical, instruments chirurgicaux à usage vétérinaire, instruments dentaires à usage médical; membres, yeux et dents artificiels; articles orthopédiques, nommément attelles, ceintures, chaussures, corsets, genouillères; instruments chirurgicaux destinés à la chirurgie orthopédique; implants médicaux, chirurgicaux et orthopédiques faits de matériaux artificiels; matériel de suture; bas, collants et chaussettes de contention; bas, collants et chaussettes à varices; bandes de pansement de contention; appareils médicaux pour l'administration intraveineuse de fluides, nommément, réchauffeurs de fluides; dispositifs implantables pour la libération sous-cutanée de substances médicamenteuses; pompes à perfusion à usage médical ainsi que pièces et accessoires connexes, seringues à usage médical; instruments de mesure médicaux, nommément thermomètres pour la fièvre, moniteurs cardiaques; appareils, instruments et équipements issus de la robotique à usage médical, nommément combinaisons exosquelettes robotisées à usage médical, bras robotisés à des fins chirurgicales; robots chirurgicaux; appareils, instruments et équipements issus de la bionique à usage médical, nommément bras bioniques pour usage prothétique, jambes bioniques à usage orthopédique, mains bioniques pour usage prothétique; appareils de prélèvement d'échantillons de sang; processeurs vidéo endoscopiques à des fins médicales et chirurgicales; appareils médicaux pour mesurer les changements biochimiques dans le sang; appareils diagnostic médical pour la détection de biomarqueurs dans le sang; caméras d'endoscopie à usage médical, équipement d'endoscopie; inhalateurs à usage médical vendus vides, inhalateurs dotés d'une chambre de maintien à valve utilisé pour améliorer l'administration de médicaments aux poumons, inhalateurs pour l'administration de médicaments en aérosol au système respiratoire d'un patient; tensiomètres artériels; appareils de mesure et de surveillance physiologique à usage médical, nommément appareils de mesure de la pression artérielle, appareils pour la mesure de la pression intracrânienne, dispositifs de mesure de la glycémie; appareils de télémétrie à usage médical, nommément appareils de mesure du rythme cardiaque; matériel d'acupuncture; appareils auditifs; processeurs d'imagerie médicale; lits de massage à usage médical, tapis de massage avec appareil de massage intégré. (1) Services scientifiques et technologiques ainsi que services de recherches et de conception y relatifs dans le domaine médical; services d'analyses et de recherches industrielles dans le domaine médical; services de recherche scientifique à buts médicaux; conception et développement d'ordinateurs et de logiciels; services de recherche, conception et développement d'équipements de suivi, de diagnostic, de prédiction et d'analyse dans le domaine médical; essais cliniques; laboratoires de recherche scientifique pour mener des recherches dans le domaine des troubles cardiovasculaires, immuno-inflammatoire, neuro-dégénératifs, et reliés à l'oncologie, au métabolisme et au système nerveux central; analyse et étude de projets scientifiques et techniques dans le domaine des troubles cardiovasculaires, immuno-inflammatoire, neuro-dégénératifs, et reliés à l'oncologie, au métabolisme et au système nerveux central; informatique en nuage offrant des logiciels de gestion de bases de données; location de logiciels informatiques; mise à jour de logiciels; programmation pour ordinateurs; recherche et développement de nouveaux produits pour des tiers; stockage électronique de données pour l'archivage de documents d'entreprise, fournisseur d'informatique en nuage pour le stockage de données; hébergement de portails web, fourniture d'une utilisation temporaire d'une application non téléchargeable pour le diagnostic, la surveillance et le suivi des troubles cardiovasculaires, immuno-inflammatoire, respiratoires, neurodégénératifs, et reliés à l'oncologie, au métabolisme et au système nerveux central; services de conception de sites web sur Internet, notamment de plateformes collaboratives; services d'ingénierie en matière de robotique; développement de logiciels à destination des patients. (2) Services d'examens médicaux, services médicaux dans le domaine des troubles cardiovasculaires, immuno-inflammatoire, neuro-dégénératifs, et reliés à l'oncologie, au métabolisme et au système nerveux central; services vétérinaires; fourniture d'informations et de conseils dans le domaine de soins médicaux et de soins pharmaceutiques; consultation en matière de pharmacie; services de santé dans le domaine des troubles immuno-inflammatoires et du diabète; services de télémédecine; services de loisirs thérapeutiques; services d'analyses médicales fournis par des laboratoires médicaux à des fins diagnostiques et thérapeutiques; services de diagnostic médical; services de soin médicaux à domicile; préparation d'ordonnances par des pharmaciens; préparation de prescriptions en pharmacie; services d'information, de conseil et de consultation dans le domaine des services de traitement médical; offre d'information aux patients dans le domaine de l'administration de médicaments; fourniture d'informations médicales dans le domaine des troubles cardiovasculaires, immuno-inflammatoire, neuro-dégénératifs, et reliés à l'oncologie, l'ostéoporose, au métabolisme et au système nerveux central; services d'examen médical à distance; services de conseil dans les domaines de la santé et du bien-être en général, de la nutrition et du bien-être par le mode de vie, y compris le bien-être physique, mental et spirituel; services de tests de diagnostic médical, de surveillance et de rapports; services transtéléphoniques de surveillance cardiaque..

Abstract

The present disclosure concerns dosages for the treatment of human patients susceptible to or diagnosed with a disease, such as cancer. Provided are methods for administering chimeric antigen receptor (CAR)-T cells. Also provided are compositions and articles of manufacture for use in the methods.

IPC Classes  ?

• A61K 35/17 - LymphocytesB-cellsT-cellsNatural killer cellsInterferon-activated or cytokine-activated lymphocytes
• A61K 31/664 - Amides of phosphorus acids
• A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61K 39/00 - Medicinal preparations containing antigens or antibodies
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents
• C07K 14/705 - ReceptorsCell surface antigensCell surface determinants
• C07K 14/725 - T-cell receptors
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
• C12N 5/0783 - T cellsNK cellsProgenitors of T or NK cells

Abstract

12344 and are as defined in the description. Medicaments.

IPC Classes  ?

• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 215/233 - Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

e.ge.g., the antigen expressed on a tumor or other cancer cells. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising Bcl-xL inhibitor drug moiety and methods of making the same are also disclosed.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

Abstract

Anti-Met antibody-drug conjugates that bind to human oncology targets are disclosed. The antibody-drug conjugates comprise a Bcl-xL inhibitor drug moiety and an anti-Met antibody or antigen-binding fragment thereof that binds the antigen target, e.g., the antigen expressed on a tumor or other cancer cells. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising Bcl-xL inhibitor drug moiety and methods of making same are also disclosed.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

Abstract

Antibody-drug conjugates that bind to human oncology targets are disclosed. The antibody-drug conjugates comprise an antibody or an antigen-binding fragment thereof covalently linked to two antineoplastic payloads through a dual linker, wherein at least one antineoplastic payload is a BH3 mimetic. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising at least one BH3 mimetic and methods of making the same are also disclosed.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents

Abstract

Compounds of Formula (I): Compounds of Formula (I): wherein R, X1, X2, X3, Z1, Z2, Z3, A and Ra are as defined in the description.

IPC Classes  ?

• C07D 498/18 - Bridged systems
• C07D 498/08 - Bridged systems
• C07D 513/18 - Bridged systems

Abstract

Process for the preparation of diosmin.

IPC Classes  ?

• C07H 17/07 - Benzo[b]pyran-4-ones
• C07H 1/00 - Processes for the preparation of sugar derivatives

Abstract

This invention relates to anti-Gal3 antibodies and methods of using them in treating diseases and conditions that benefit from modulating Gal3 activity, e.g., fibrotic disease, inflammatory disease, autoimmune disease, 5 immune-mediated disorder, cancer, neurodegenerative disease, metabolic disease or infectious disease.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 11/00 - Drugs for disorders of the respiratory system

Goods & Services

Medical services; veterinary services; hygienic and beauty care for human beings or animals; health counseling services; pharmacy advice; health services; telemedicine services; therapeutic services; medical diagnosis services; home care services; individualized medical prescription services; online medical prescription services; advice relating to home medical treatment; advice relating to self-medication; provision of medical information to patients; remote medical examination services; advice related to personal well-being [health]; medical monitoring of patients including remote monitoring.

Abstract

3456122 and T are as defined in the description. Medicaments.

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems
• C07D 487/10 - Spiro-condensed systems
• C07D 495/10 - Spiro-condensed systems
• C07D 498/04 - Ortho-condensed systems
• A61P 35/00 - Antineoplastic agents
• A61K 31/472 - Non-condensed isoquinolines, e.g. papaverine

Abstract

The present invention relates to the field of oncology, particularly the early diagnostic of lung cancer, the monitoring of lung cancer patients and the prediction of the clinical outcome of patients. The invention relates to a method for diagnosing lung cancer or diagnosing relapse of lung cancer in patients by determination of the level of methylation of gene(s) and the kit to implement said method.

IPC Classes  ?

• C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer

Goods & Services

Consultation in the pharmaceutical field; information services concerning pharmaceutical products; medical information services.

Abstract

This invention relates to anti-CD73 antibodies and methods of using them in treating diseases and conditions related to CD73 activity, e.g., cancer.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to para-amino-benzyl linker compounds useful for linking drug moieties to antibodies, to linker-drug compounds in which said para-amino-benzyl linker compounds are covalently linked to drug moieties, and to antibody-drug conjugates in which said para-amino-benzyl linker compounds are covalently linked to drug wherein said drug is enzymatically cleaved from the conjugate at a particular cell or tissue type targeted by said antibody.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment

Abstract

A combination comprising (a) an anti-EGFR antibody component comprising one or two anti-EGFR antibodies or antigen-binding portions thereof and (b) a trifluridine/tipiracil component.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61K 31/00 - Medicinal preparations containing organic active ingredients
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents

Abstract

The disclosure provides fusion proteins specific for both OX40 and PD-L1, which fusion proteins can be used to co-stimulate lymphocyte activation in a PD-L1-target-dependent manner. Such fusion proteins can be used in many pharmaceutical applications, for example, as anti-cancer agents and/or immune modulators. The present disclosure also concerns methods of making the fusion proteins described herein as well as compositions comprising such fusion proteins. The present disclosure further relates to nucleic acid molecules encoding such fusion proteins. In addition, the application discloses therapeutic and/or diagnostic uses of such fusion proteins.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C12N 15/62 - DNA sequences coding for fusion proteins

Abstract

The present invention relates to novel trimetazidine salts, leading to a reduced formation of trimetazidine nitrosamine in presence of nitrites.

IPC Classes  ?

• C07D 295/096 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine

Abstract

The present invention relates to novel trimetazidine salts, leading to a reduced formation of trimetazidine nitrosamine in presence of nitrites.

IPC Classes  ?

• C07D 295/096 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

This invention relates to anti-NKG2A antibodies, optionally in combination with anti-PD-1 or anti-PD-L1 antibodies and/or anti-EGFR or anti-HER2 antibodies, and methods of using the antibodies or antibody combinations in enhancing immunity in a patient in need thereof and in treating cancer.

IPC Classes  ?

• C07K 16/46 - Hybrid immunoglobulins
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
• C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes

Abstract

This invention relates to anti-NKG2A antibodies, optionally in combination with anti-PD-1 or anti-PD-L1 antibodies and/or anti-EGFR or anti-HER2 antibodies, and methods of using the antibodies or antibody combinations in enhancing immunity in a patient in need thereof and in treating cancer.

IPC Classes  ?

• C07K 16/46 - Hybrid immunoglobulins
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
• C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum

Abstract

This invention relates to anti-TIM-3 antibodies and antibody compositions and their use in enhancing immunity in a patient, e.g., to treat cancer.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• C07K 16/46 - Hybrid immunoglobulins

Abstract

A compound of formula (I): A compound of formula (I): A compound of formula (I): wherein Z, Y1, Y2, A compound of formula (I): wherein Z, Y1, Y2, A compound of formula (I): wherein Z, Y1, Y2, R1 to R7 are as defined in the description, its optical isomers, and addition salts thereof with a pharmaceutically acceptable base. A compound of formula (I): wherein Z, Y1, Y2, R1 to R7 are as defined in the description, its optical isomers, and addition salts thereof with a pharmaceutically acceptable base. Medicaments.

IPC Classes  ?

• A61K 31/547 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame spiro-condensed or forming part of bridged ring systems
• C07D 515/18 - Bridged systems
• A61K 9/20 - Pills, lozenges or tablets
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

Antibody-drug conjugates that bind to human oncology targets are disclosed. The antibody-drug conjugates comprise an Mcl-1 inhibitor drug moiety. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising an Mcl-1 inhibitor drug moiety and methods of making same are also disclosed.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61K 47/65 - Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61P 35/00 - Antineoplastic agents

Abstract

Anti-CD74 antibody-drug conjugates are disclosed. The anti-CD74 antibody-drug conjugates comprise an Mcl-1 inhibitor drug moiety and an anti-CD74 antibody or antigen-binding fragment thereof that binds an antigen target, e.g., an antigen expressed on a tumor or other cancer cell. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising an Mcl-1 inhibitor drug moiety and methods of making same are also disclosed.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment

Goods & Services

Pharmaceutical products, medical and veterinary preparations; sanitary products for medicine; dietetic substances and foodstuffs for medical or veterinary use, food for babies; dietary supplements for humans and animals; plasters, materials for dressings; materials for dental fillings and dental impressions; disinfectants; products for destroying vermin; fungicides, herbicides; biomaterials in the form of biological tissue for medical use. Scientific, optical, weighing, measuring, signaling, checking (inspecting), life-saving and teaching apparatus and instruments; apparatus and instruments for conducting, switching, transforming, accumulating, regulating or controlling electricity; apparatus for sound or image recording, transmission and reproduction; magnetic recording media; sound recording disks; digital recording media; data and information processing apparatus and equipment; software; computer programs; computers; software recorded on magnetic media or downloaded from a remote computer network; downloadable computer software applications; telecommunication equipment for use with mobile networks; personal digital assistant; electronic signal transmitters; connected bracelets (measuring instruments); connected scales; connected watches (measuring instruments); video cameras; electronic sensors; mobile applications; digital applications; algorithms (software); artificial intelligence software; computer platforms in the form of information sharing software; connected self-measurement instruments; electronic chips connected to an information system; downloadable applications for mobile devices; spectacles; contact lenses; smart glasses; in-ear headphones; downloadable telemedicine applications for mobile devices; augmented reality software; virtual reality computer programs; analysis systems based on artificial intelligence (software); medical image analysis systems based on artificial intelligence; virtual reality headsets. Medical, surgical, dental and veterinary apparatus, instruments and equipment, artificial limbs, organs, eyes and teeth; orthopedic articles; surgical instruments for use in orthopedic surgery; medical, surgical and orthopedic implants made of artificial materials; suture materials; compression stockings, tights and socks; stockings, tights and socks for varicose veins; bandages for compression dressing; medical apparatus, instruments and equipment for introducing pharmaceutical preparations into the human body, particularly for prolonged, controlled or immediate release of active substances; infusion devices and syringes for medical use; medical measuring instruments, in particular instruments able to directly transmit data to a database, in particular instruments to measure fevers, heart rate monitors; apparatus, instruments and equipment derived from robotics for medical use; nanobots for medical use; apparatus, instruments and equipment derived from bionics for medical use; medical devices, namely, connected materials for medical use; medical devices, namely, smart materials for medical use; medical diagnostic apparatus for allergy tests; blood testing apparatus; medical devices intended for ingestion; endoscopic video capsules; medical apparatus for measuring biochemical changes in blood; blood biomarker devices; medical endoscopy apparatus; inhalers; blood pressure monitors; physiological monitoring and measuring apparatus for medical use; telemetry apparatus for medical use; acupuncture instruments; hearing aids; automatic analyzers for medical use; medical imaging apparatus; massage apparatus. Scientific and technological services as well as research and design services relating thereto; industrial analysis and research services; scientific research services for medical purposes; design and development of computer hardware and software; research, design and development of tools for monitoring, diagnosis, prediction, analysis; clinical trials; scientific laboratory services; evaluation, scientific and technical project studies; cloud computing; rental of computer software; updating of software; programming for computers; research and development of new products for third parties; electronic data storage; hosting platforms on the Internet, hosting Web portals, temporary provision of non-downloadable software applications accessible via an Internet site; web site design services on the Internet, especially collaborative platforms; engineering services relating to robotics; development of software directed at patients. Medical services; veterinary services; hygienic and beauty care for human beings or animals; advice with respect to health; consultation with respect to pharmacy; health services; telemedicine services; therapeutic services; medical diagnosis services; home care services; individualized medical prescription services; online medical prescription services; providing support in the monitoring of patients receiving medical treatment; consultancy in relation to medical treatment in the home; consultancy regarding self-medication; medical information services for patients; remote medical examination services; advice concerning personal well-being [health]; medical monitoring of patients including provided remotely.

Goods & Services

Pharmaceutical products, medical and veterinary preparations; sanitary products for medicine; dietetic substances and foodstuffs for medical or veterinary use, food for babies; dietary supplements for humans and animals; plasters, materials for dressings; materials for dental fillings and dental impressions; disinfectants; products for destroying vermin; fungicides, herbicides; biomaterials in the form of biological tissue for medical use. Scientific, optical, weighing, measuring, signaling, checking (inspecting), life-saving and teaching apparatus and instruments; apparatus and instruments for conducting, switching, transforming, accumulating, regulating or controlling electricity; apparatus for sound or image recording, transmission and reproduction; magnetic recording media; sound recording disks; digital recording media; data and information processing apparatus and equipment; software; computer programs; computers; software recorded on magnetic media or downloaded from a remote computer network; downloadable computer software applications; telecommunication equipment for use with mobile networks; personal digital assistant; electronic signal transmitters; connected bracelets (measuring instruments); connected scales; connected watches (measuring instruments); video cameras; electronic sensors; mobile applications; digital applications; algorithms (software); artificial intelligence software; computer platforms in the form of information sharing software; connected self-measurement instruments; electronic chips connected to an information system; downloadable applications for mobile devices; spectacles; contact lenses; smart glasses; in-ear headphones; downloadable telemedicine applications for mobile devices; augmented reality software; virtual reality computer programs; analysis systems based on artificial intelligence (software); medical image analysis systems based on artificial intelligence; virtual reality headsets. Medical, surgical, dental and veterinary apparatus, instruments and equipment, artificial limbs, organs, eyes and teeth; orthopedic articles; surgical instruments for use in orthopedic surgery; medical, surgical and orthopedic implants made of artificial materials; suture materials; compression stockings, tights and socks; stockings, tights and socks for varicose veins; bandages for compression dressing; medical apparatus, instruments and equipment for introducing pharmaceutical preparations into the human body, particularly for prolonged, controlled or immediate release of active substances; infusion devices and syringes for medical use; medical measuring instruments, in particular instruments able to directly transmit data to a database, in particular instruments to measure fevers, heart rate monitors; apparatus, instruments and equipment derived from robotics for medical use; nanobots for medical use; apparatus, instruments and equipment derived from bionics for medical use; medical devices, namely, connected materials for medical use; medical devices, namely, smart materials for medical use; medical diagnostic apparatus for allergy tests; blood testing apparatus; medical devices intended for ingestion; endoscopic video capsules; medical apparatus for measuring biochemical changes in blood; blood biomarker devices; medical endoscopy apparatus; inhalers; blood pressure monitors; physiological monitoring and measuring apparatus for medical use; telemetry apparatus for medical use; acupuncture instruments; hearing aids; automatic analyzers for medical use; medical imaging apparatus; massage apparatus. Scientific and technological services as well as research and design services relating thereto; industrial analysis and research services; scientific research services for medical purposes; design and development of computer hardware and software; research, design and development of tools for monitoring, diagnosis, prediction, analysis; clinical trials; scientific laboratory services; evaluation, scientific and technical project studies; cloud computing; rental of computer software; updating of software; programming for computers; research and development of new products for third parties; electronic data storage; hosting platforms on the Internet, hosting Web portals, temporary provision of non-downloadable software applications accessible via an Internet site; web site design services on the Internet, especially collaborative platforms; engineering services relating to robotics; development of software directed at patients. Medical services; veterinary services; hygienic and beauty care for human beings or animals; advice with respect to health; consultation with respect to pharmacy; health services; telemedicine services; therapeutic services; medical diagnosis services; home care services; individualized medical prescription services; online medical prescription services; providing support in the monitoring of patients receiving medical treatment; consultancy in relation to medical treatment in the home; consultancy regarding self-medication; medical information services for patients; remote medical examination services; advice concerning personal well-being [health]; medical monitoring of patients including provided remotely.

Abstract

The present application relates to a method for preparing a substantially and diastereomerically pure crystalline ethanol solvate of Compound IIa and its use for synthesizing Ivosidenib.

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Abstract

Disclosed is a process preparing diosmin and flavonoid fraction by direct oxidation of hesperidin.

IPC Classes  ?

• C07H 1/00 - Processes for the preparation of sugar derivatives
• C07H 17/07 - Benzo[b]pyran-4-ones

Abstract

Disclosed is a process preparing diosmin and flavonoid fraction by direct oxidation of hesperidin.

IPC Classes  ?

• C07H 1/00 - Processes for the preparation of sugar derivatives
• C07H 17/07 - Benzo[b]pyran-4-ones

Abstract

This invention relates to anti-NKG2A antibodies and methods of using them in enhancing immunity in a patient in need thereof and in treating cancer.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 35/00 - Antineoplastic agents

Abstract

This invention relates to anti-NKG2A antibodies and methods of using them in enhancing immunity in a patient in need thereof and in treating cancer.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

Goods & Services

Pharmaceuticals, namely, pharmaceutical preparations for the treatment of cardiovascular diseases, pharmaceutical preparations for preventing and treating disorders of the central nervous system, cytostatic pharmaceutical preparations for use in the treatment of cancer, pharmaceutical preparations for preventing and treating metabolism disorders, pharmaceutical preparations for the treatment and prevention of obesity, pharmaceutical preparations for the treatment and prevention of diabetes, pharmaceutical preparations for treating blood and blood forming organs to aid in blood clotting, pharmaceutical preparations for the treatment and prevention of disorders of the respiratory system, pharmaceutical preparations for the treatment and prevention of disorders of the musculo-skeletal system, pharmaceutical preparations for the treatment and prevention of disorders of the genitourinary system, anti-infective pharmaceutical preparations, pharmaceutical preparations for the treatment and prevention of disorders of the ophthalmological system Scientific, optical, weighing, measuring, signaling, checking, inspecting, life-saving and teaching apparatus and instruments, namely, computers and microscopes; apparatus and instruments for conducting, switching, transforming, accumulating, regulating or controlling electricity, namely, electric current transformers, electrical power distribution units; apparatus for sound or image recording, transmission and reproduction; magnetic recording media, namely, blank magnetic disks; data and data information processing apparatus and equipment, namely, couplers; sound recording disks, namely, blank audio discs; digital recording media, namely, blank magnetic disks; data and data information processing apparatus and equipment; software, namely, downloadable software for processing digital images of the anatomy for diagnostic and treatment; downloadable computer programs for managing electronic data and databases, database administration, managing cloud applications, and self-automation of database-management activities; computers; software recorded on magnetic media or downloaded from a remote computer network for the analysis, storage and monitoring of medical data; downloadable computer software applications for providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; telecommunication equipment for use with mobile networks, namely, telecommunication exchangers, telecommunications transmitters; personal digital assistant; electronic signal transmitters; connected bracelets being measuring instruments, namely, wearable activity trackers; connected scales being electronic scales; connected watches as measuring instruments, namely, smart watches; video cameras; electronic proximity sensors; downloadable mobile applications for providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; digital applications, namely, downloadable mobile applications for assisting with patient diagnosis, providing surveillance of patient health data, and providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; software incorporating algorithms, namely, downloadable computer software for assisting with patient diagnosis, providing surveillance of patient health data, and providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; artificial intelligence software, namely, downloadable computer software using artificial intelligence for assisting with patient diagnosis, providing surveillance of patient health data, and providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; downloadable computer software platforms in the form of information sharing software for providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; connected self-measurement instruments being scales; encoded electronic chip cards connected to an information system containing programming used for assisting with patient diagnosis, providing surveillance of patient health data, and providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; downloadable applications for mobile devices for assisting with patient diagnosis, providing surveillance of patient health data, and providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; spectacles; contact lenses; smart glasses; in-ear headphones; downloadable telemedicine applications for mobile devices; downloadable augmented reality software for assisting with patient diagnosis, providing surveillance of patient health data, and providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; downloadable virtual reality computer programs for assisting with patient diagnosis, providing surveillance of patient health data, and providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; analysis systems based on artificial intelligence, namely, downloadable computer software using artificial intelligence for assisting with patient diagnosis, providing surveillance of patient health data, and providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; medical image analysis systems based on artificial intelligence, namely, downloadable computer software using artificial intelligence for medical imaging; virtual reality headsets Medical, surgical, dental and veterinary apparatus, instruments and equipment for the prevention and treatment of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; artificial limbs, organs being artificial hearts, eyes and teeth; orthopedic articles, namely, orthopedic braces, orthopedic belts; surgical instruments for use in orthopedic surgery; medical, surgical and orthopedic implants made of artificial materials; suture materials; compression stockings, tights and socks; stockings, tights and socks for varicose veins; bandages for compression dressing; medical apparatus, instruments and equipment for introducing pharmaceutical preparations into the human body, particularly for prolonged, controlled or immediate release of active substances; infusion devices for administering drugs and syringes for medical use; medical measuring instruments, in particular instruments able to directly transmit data to a database, in particular instruments to measure fevers, heart rate monitors; apparatus, instruments and equipment derived from robotics for medical use, namely, surgical robots; nanobots for medical use in the nature of surgical robots; apparatus, instruments and equipment derived from bionics for medical use for the prevention and treatment of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; medical devices, namely, connected materials for medical use in the nature of suture materials; medical devices, namely, smart materials for medical use in the nature of implants consisting primarily of artificial materials and also including biological materials; medical diagnostic apparatus for allergy tests; blood testing apparatus; medical devices intended for ingestion, namely, endoscopy camera for medical purposes; endoscopic equipment for medical purposes in the nature of video capsules; medical apparatus for measuring biochemical changes in blood; blood biomarker devices in the nature of blood testing apparatus; medical endoscopy apparatus, namely, medical instruments for use in endoscopy procedures; inhalers for medical purposes, sold empty; blood pressure monitors; physiological monitoring and measuring apparatus for medical use, namely, for measuring and monitoring blood pressure, lung capacity for use in the field of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; telemetry apparatus for medical use; acupuncture instruments; hearing aids; automatic analyzers for medical use, namely, hematology analyzers for medical diagnostic uses; medical imaging apparatus; massage apparatus Scientific and technological services as well as research and design services relating thereto, namely, scientific research, technological research, and new product design services in the fields of pharmaceuticals and bio-chemicals for the prevention and treatment of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; industrial analysis and research services, namely, industrial research in the fields of pharmaceuticals and bio-chemicals for the prevention and treatment of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; scientific research services for medical research purposes; design and development of computer hardware and software; research, design and development of new products for others, namely, medical tools for monitoring, diagnosis, prediction, analysis; medical and scientific research, namely, conducting clinical trials for others; scientific laboratory services; evaluation, scientific and technical project studies in the nature of technical research in the field of pharmaceutical studies; providing virtual computer systems through cloud computing; rental of computer software for medical research and collaboration; updating of computer software; programming for computers; research and development of new products for third parties; electronic data storage; hosting platforms on the Internet, hosting of web sites; temporary provision of non-downloadable software applications accessible via an Internet site, namely, providing temporary use of a web-based software application for medical research and collaboration; web site design services on the Internet, especially collaborative platforms; engineering design services relating to robotics; development of software directed at patients Medical services; veterinary services; hygienic and beauty care for human beings or animals; advice with respect to health, namely, advisory services relating to heath; consultation with respect to pharmacy, namely, pharmaceutical consultation; health services, namely, healthcare; telemedicine services; therapeutic services, namely, physical therapy; medical diagnosis of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; home health care care services; individualized medical prescription services, namely, preparation of prescriptions by pharmacists; online medical prescription services, namely, preparation of prescriptions by pharmacists; providing support in the monitoring of patients receiving medical treatment, namely, remote monitoring of medical data for medical diagnosis and treatment; consultancy in relation to medical treatment in the home; consultancy regarding self-medication; medical information services for patients; remote medical examination services; advice concerning personal well-being in the nature of advisory services relating to health; medical monitoring of patients including provided remotely for medical diagnosis and treatment purposes

Goods & Services

Pharmaceutical products, medical and veterinary preparations all for the prevention and the treatment of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; sanitary products for medicine, namely, sanitary preparations for medical purposes; dietetic substances and foodstuffs for medical or veterinary use, namely, food for babies; dietary supplements for humans and animals; medical plasters; materials for dressings, namely, medical dressings; materials for dental fillings and dental impressions; disinfectants; products for destroying vermin, namely, vermin destroying preparations; fungicides, herbicides; biomaterials in the form of biological tissue cultures for medical use Scientific, optical, weighing, measuring, signaling, checking, inspecting, life-saving and teaching apparatus and instruments, namely, computers and microscopes; apparatus and instruments for conducting, switching, transforming, accumulating, regulating or controlling electricity, namely, electric current transformers, electrical power distribution units; apparatus for sound or image recording, transmission and reproduction; magnetic recording media, namely, blank magnetic disks; data and data information processing apparatus and equipment, namely, couplers; sound recording disks, namely, blank audio discs; digital recording media, namely, blank magnetic disks; data and data information processing apparatus and equipment; software, namely, downloadable software for processing digital images of the anatomy for diagnostic and treatment; downloadable computer programs for managing electronic data and databases, database administration, managing cloud applications, and self-automation of database-management activities; computers; software recorded on magnetic media or downloaded from a remote computer network for the analysis, storage and monitoring of medical data; downloadable computer software applications for providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; telecommunication equipment for use with mobile networks, namely, telecommunication exchangers, telecommunications transmitters; personal digital assistant; electronic signal transmitters; connected bracelets being measuring instruments, namely, wearable activity trackers; connected scales being electronic scales; connected watches as measuring instruments, namely, smart watches; video cameras; electronic proximity sensors; downloadable mobile applications for providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; digital applications, namely, downloadable mobile applications for assisting with patient diagnosis, providing surveillance of patient health data, and providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; software incorporating algorithms, namely, downloadable computer software for assisting with patient diagnosis, providing surveillance of patient health data, and providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; artificial intelligence software, namely, downloadable computer software using artificial intelligence for assisting with patient diagnosis, providing surveillance of patient health data, and providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; downloadable computer software platforms in the form of information sharing software for providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; connected self-measurement instruments being scales; encoded electronic chip cards connected to an information system containing programming used for assisting with patient diagnosis, providing surveillance of patient health data, and providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; downloadable applications for mobile devices for assisting with patient diagnosis, providing surveillance of patient health data, and providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; spectacles; contact lenses; smart glasses; in-ear headphones; downloadable telemedicine applications for mobile devices; downloadable augmented reality software for assisting with patient diagnosis, providing surveillance of patient health data, and providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; downloadable virtual reality computer programs for assisting with patient diagnosis, providing surveillance of patient health data, and providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; analysis systems based on artificial intelligence, namely, downloadable computer software using artificial intelligence for assisting with patient diagnosis, providing surveillance of patient health data, and providing prevention and treatment information in the fields of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; medical image analysis systems based on artificial intelligence, namely, downloadable computer software using artificial intelligence for medical imaging; virtual reality headsets Medical, surgical, dental and veterinary apparatus, instruments and equipment for the prevention and treatment of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; artificial limbs, organs being artificial hearts, eyes and teeth; orthopedic articles, namely, orthopedic braces, orthopedic belts; surgical instruments for use in orthopedic surgery; medical, surgical and orthopedic implants made of artificial materials; suture materials; compression stockings, tights and socks; stockings, tights and socks for varicose veins; bandages for compression dressing; medical apparatus, instruments and equipment for introducing pharmaceutical preparations into the human body, particularly for prolonged, controlled or immediate release of active substances; infusion devices for administering drugs and syringes for medical use; medical measuring instruments, in particular instruments able to directly transmit data to a database, in particular instruments to measure fevers, heart rate monitors; apparatus, instruments and equipment derived from robotics for medical use, namely, surgical robots; nanobots for medical use in the nature of surgical robots; apparatus, instruments and equipment derived from bionics for medical use for the prevention and treatment of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; medical devices, namely, connected materials for medical use in the nature of suture materials; medical devices, namely, smart materials for medical use in the nature of implants consisting primarily of artificial materials and also including biological materials; medical diagnostic apparatus for allergy tests; blood testing apparatus; medical devices intended for ingestion, namely, endoscopy camera for medical purposes; endoscopic equipment for medical purposes in the nature of video capsules; medical apparatus for measuring biochemical changes in blood; blood biomarker devices in the nature of blood testing apparatus; medical endoscopy apparatus, namely, medical instruments for use in endoscopy procedures; inhalers for medical purposes, sold empty; blood pressure monitors; physiological monitoring and measuring apparatus for medical use, namely, for measuring and monitoring blood pressure, lung capacity for use in the field of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; telemetry apparatus for medical use; acupuncture instruments; hearing aids; automatic analyzers for medical use, namely, hematology analyzers for medical diagnostic uses; medical imaging apparatus; massage apparatus Scientific and technological services as well as research and design services relating thereto, namely, scientific research, technological research, and new product design services in the fields of pharmaceuticals and bio-chemicals for the prevention and treatment of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; industrial analysis and research services, namely, industrial research in the fields of pharmaceuticals and bio-chemicals for the prevention and treatment of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; scientific research services for medical research purposes; design and development of computer hardware and software; research, design and development of new products for others, namely, medical tools for monitoring, diagnosis, prediction, analysis; medical and scientific research, namely, conducting clinical trials for others; scientific laboratory services; evaluation, scientific and technical project studies in the nature of technical research in the field of pharmaceutical studies; providing virtual computer systems through cloud computing; rental of computer software for medical research and collaboration; updating of computer software; programming for computers; research and development of new products for third parties; electronic data storage; hosting platforms on the Internet, hosting of web sites; temporary provision of non-downloadable software applications accessible via an Internet site, namely, providing temporary use of a web-based software application for medical research and collaboration; web site design services on the Internet, especially collaborative platforms; engineering design services relating to robotics; development of software directed at patients Medical services; veterinary services; hygienic and beauty care for human beings or animals; advice with respect to health, namely, advisory services relating to heath; consultation with respect to pharmacy, namely, pharmaceutical consultation; health services, namely, healthcare; telemedicine services; therapeutic services, namely, physical therapy; medical diagnosis of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; home health care care services; individualized medical prescription services, namely, preparation of prescriptions by pharmacists; online medical prescription services, namely, preparation of prescriptions by pharmacists; providing support in the monitoring of patients receiving medical treatment, namely, remote monitoring of medical data for medical diagnosis and treatment; consultancy in relation to medical treatment in the home; consultancy regarding self-medication; medical information services for patients; remote medical examination services; advice concerning personal well-being in the nature of advisory services relating to health; medical monitoring of patients including provided remotely for medical diagnosis and treatment purposes

Abstract

Compounds of formula (I): Compounds of formula (I): Compounds of formula (I): wherein Het, Het1, Het2, A4, A5, Z1, R1, R2 and R3 are as defined in the description. Medicaments.

IPC Classes  ?

• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems
• A61P 35/02 - Antineoplastic agents specific for leukemia
• A61P 35/00 - Antineoplastic agents

Goods & Services

Pharmacy advice; Provision of pharmaceutical information; Information of a medical nature.

Abstract

SHHH-pyrrole-3 -carboxylic acid derivatives and its application for the production of pharmaceutical compounds.

IPC Classes  ?

• C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 217/16 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
• C07D 217/14 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
• C07D 207/34 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms

Goods & Services

Pharmaceutical preparations, medicated and veterinary preparations; Sanitary preparations for medical purposes; Dietetic food and substances adapted for medical or veterinary use, food for babies; Dietary supplements for humans and animals; Plasters, materials for dressings; Material for stopping teeth, dental wax; Disinfectants; Preparations for destroying vermin; Fungicides, herbicides. Scientific, optical, weighing, measuring, signalling, checking (supervision), life-saving and teaching apparatus and instruments; Apparatus and instruments for conducting, switching, transforming, accumulating, regulating or controlling electricity; Apparatus for recording, transmission or reproduction of sound or images; Recording substrates [magnetic]; Phonograph records; Digital recording media; Apparatus and equipment for processing data and information; Software; Computer programs; Computers; Computer software recorded on magnetic media or downloaded from a remote computer network; Computer software applications, downloadable; Telecommunications hardware for use with mobile networks; Personal digital assistant; Transmitters of electronic signals; Connected bracelets [measuring instruments]; Smart scales; Connected watches (measuring instruments); Camcorders; Electronic sensors; mobile applications; Digital applications; Algorithms (computer software); Artificial intelligence software; Computer platforms in the form of computer software for sharing information; Smart self-measurement tools; Electronic chips connected to information systems; Downloadable applications for use with mobile devices; Artificial intelligence apparatus; Spectacles; Contact lenses; Smartglasses; Earpieces for remote communication; Downloadable telemedicine applications for mobile devices; Augmented reality software; Virtual reality computer programs; Analysis systems based on artificial intelligence (computer software); Medical image analysis systems based on artificial intelligence; Virtual reality headsets. Surgical, medical, dental and veterinary equipment, instruments and apparatus; Artificial limbs, eyes and teeth; Orthopedic articles; Surgical instruments for use in orthopedic surgery; Medical, surgical and orthopaedic implants made of artifical materials; Suture materials; Support stockings, tights and socks; Stockings, tights and socks for varicose veins; Compression dressing strips; Medical apparatus, instruments and equipment for introducing pharmaceuticals into the human body, in particular for extended, controlled or immediate release of active substances; Infusion devices and syringes for medical purposes; Measuring instruments for medical purposes, in particular measuring instruments capable of directly transmitting data to a database, in particular fever measuring instruments, Heart rate monitors; Apparatus, instruments and equipment derived from robotics, for medical purposes; Nanorobots for medical purposes; Apparatus, instruments and equipment derived from bionics, for medical purposes; Biomaterial for medical purposes; Textiles equipped with connected chips, both for medical purposes; Textiles equipped with smart chips, both for medical purposes; Allergy testing tools; Blood testing apparatus; Medical devices intended for ingestion; Endoscopic video capsules; Medical apparatus for measuring biochemical changes in the blood; Blood biomarker devices; Medical apparatus for use in endoscopy; Inhalers; Tensiometers; Physiological monitoring and measuring apparatus for medical purposes; Telemetry apparatus for medical use; Acupuncture instruments; Hearing aids; automated analyzers for medical purposes; Medical imaging apparatus; Massage apparatus. Assistance in the operation or management of a commercial business; Business management assistance services; Computerized file management; Collating mathematical or statistical data; database management; Compilation of information into computer databases; Updating and maintaining of computer databases; Business management and organization consultancy; Business management consultancy; business data analytics; Market studies; Market research information; Business intermediary services relating to the matching of potential private investors with entrepreneurs needing funding; Business efficiency expert services; Retailing or wholesaling of pharmaceutical, veterinary and sanitary preparations, and medical and surgical instruments; Sales promotion to others; Public relations services; Sponsorship search; Auctioneering services; Organisation of events for commercial or advertising purposes; Subsidy administration and management (business management assistance); Providing of available personnel directories; Collecting information for business. Education, provision of training; Arranging and conducting of colloquiums, competitions, conferences, congresses and exhibitions; Publication of texts; Online publication of specialist magazines and books; Entertainment services; Sporting and cultural activities; Publication of the results of clinical trials. Scientific and technological services and research and design relating thereto; Industrial analysis and research services; Scientific research for medical purposes; Design and development of computer hardware and software; Research, design and development of monitoring, diagnostic, predictive and analysis tools; Clinical trials; Scientific laboratory services; Evaluation and study of scientific and technical projects; Cloud computing; Rental of computer software; Updating of computer software; Computer programming; Research and development of new products for others; Electronic data storage; Internet hosting platforms, web portal hosting, providing of temporary use of non-downloadable computer software applications accessible via a website; Design of websites on the internet, in particular collaborative platforms; Engineering services relating to robotics; Development of computer software for patients. Medical services; Animal healthcare services; Hygienic and beauty care for human beings or animals; Health counselling; Pharmacy advice; Health services; Telemedicine services; Therapy services; Medical diagnostic services; Providing of nursing services in the home; Individualised medical prescriptions; Online medical prescriptions; Providing medical support in the monitoring of patients receiving medical treatments; Consultancy in relation to medical treatment in the home; Self-medication consultancy; Medical information for patients; Remote medical examinations; Advice relating to the personal welfare and wellbeing [health]; Medical monitoring of patients, including provided remotely.

Goods & Services

Pharmaceutical preparations, medicated and veterinary preparations; Sanitary preparations for medical purposes; Dietetic food and substances adapted for medical or veterinary use, food for babies; Dietary supplements for humans and animals; Plasters, materials for dressings; Material for stopping teeth, dental wax; Disinfectants; Preparations for destroying vermin; Fungicides, herbicides. Medical apparatus and instruments; Medical apparatus, instruments and equipment used for diagnosing, treating or curing people's activities or health, diagnosis, examination and monitoring Scientific, optical, weighing, measuring, signalling, checking (supervision), life-saving and teaching apparatus and instruments; Apparatus and instruments for conducting, switching, transforming, accumulating, regulating or controlling electricity; Apparatus for recording, transmission or reproduction of sound or images; Recording substrates [magnetic]; Phonograph records; Digital recording media; Apparatus and equipment for processing data and information; Software; Computer programs; Computers; Computer software recorded on magnetic media or downloaded from a remote computer network; Computer software applications, downloadable; Telecommunications hardware for use with mobile networks; Personal digital assistant; Transmitters of electronic signals; Connected bracelets [measuring instruments]; Smart scales; Connected watches (measuring instruments); Camcorders; Electronic sensors; mobile applications; Digital applications; Algorithms (computer software); Artificial intelligence software; Computer platforms in the form of computer software for sharing information; Smart self-measurement tools; Electronic chips connected to information systems; Downloadable applications for use with mobile devices; Artificial intelligence apparatus; Spectacles; Contact lenses; Smartglasses; Earpieces for remote communication; Downloadable telemedicine applications for mobile devices; Augmented reality software; Virtual reality computer programs; Analysis systems based on artificial intelligence (computer software); Medical image analysis systems based on artificial intelligence; Virtual reality headsets. Surgical, medical, dental and veterinary equipment, instruments and apparatus; Artificial limbs, eyes and teeth; Orthopedic articles; Surgical instruments for use in orthopedic surgery; Medical, surgical and orthopaedic implants made of artifical materials; Suture materials; Support stockings, tights and socks; Stockings, tights and socks for varicose veins; Compression dressing strips; Medical apparatus, instruments and equipment for introducing pharmaceuticals into the human body, in particular for extended, controlled or immediate release of active substances; Infusion devices and syringes for medical purposes; Measuring instruments for medical purposes, in particular measuring instruments capable of directly transmitting data to a database, in particular fever measuring instruments, Heart rate monitors; Apparatus, instruments and equipment derived from robotics, for medical purposes; Nanorobots for medical purposes; Apparatus, instruments and equipment derived from bionics, for medical purposes; Biomaterial for medical purposes; Textiles equipped with connected chips, both for medical purposes; Textiles equipped with smart chips, both for medical purposes; Allergy testing tools; Blood testing apparatus; Medical devices intended for ingestion; Endoscopic video capsules; Medical apparatus for measuring biochemical changes in the blood; Blood biomarker devices; Medical apparatus for use in endoscopy; Inhalers; Tensiometers; Physiological monitoring and measuring apparatus for medical purposes; Telemetry apparatus for medical use; Acupuncture instruments; Hearing aids; automated analyzers for medical purposes; Medical imaging apparatus; Massage apparatus. Assistance in the operation or management of a commercial business; Business management assistance services; Database management; Collating mathematical or statistical data; Computerized file management; Compilation of information into computer databases; Updating and maintaining of computer databases; Business management and organization consultancy; Business management consultancy; business data analytics; Market studies; Market research information; Business intermediary services relating to the matching of potential private investors with entrepreneurs needing funding; Business efficiency expert services; Retailing or wholesaling of pharmaceutical, veterinary and sanitary preparations, and medical and surgical instruments; Sales promotion to others; Public relations services; Sponsorship search; Auctioneering services; Organisation of events for commercial or advertising purposes; Subsidy administration and management (business management assistance); Providing of available personnel directories; Collecting information for business. Education, provision of training; Arranging and conducting of colloquiums, competitions, conferences, congresses and exhibitions; Publication of texts; Online publication of specialist magazines and books; Entertainment services; Sporting and cultural activities; Publication of the results of clinical trials. Scientific and technological services and research and design relating thereto; Industrial analysis and research services; Scientific research for medical purposes; Design and development of computer hardware and software; Research, design and development of monitoring, diagnostic, predictive and analysis tools; Clinical trials; Scientific laboratory services; Evaluation and study of scientific and technical projects; Cloud computing; Rental of computer software; Updating of computer software; Computer programming; Research and development of new products for others; Electronic data storage; Internet hosting platforms, web portal hosting, providing of temporary use of non-downloadable computer software applications accessible via a website; Design of websites on the internet, in particular collaborative platforms; Engineering services relating to robotics; Development of computer software for patients. Medical services; Animal healthcare services; Hygienic and beauty care for human beings or animals; Health counselling; Pharmacy advice; Health services; Telemedicine services; Therapy services; Medical diagnostic services; Providing of nursing services in the home; Individualised medical prescriptions; Online medical prescriptions; Providing medical support in the monitoring of patients receiving medical treatments; Consultancy in relation to medical treatment in the home; Self-medication consultancy; Medical information for patients; Remote medical examinations; Advice relating to the personal welfare and wellbeing [health]; Medical monitoring of patients, including provided remotely.

Abstract

The present invention relates to a new process for preparing 5-{5-chloro-2-[(3S)-3- [(morpholin-4-yl)methyl]-3,4-dihydroisoquinoline-2(1H)-carbonyl]phenyl}-1,2-dimethyl- 1H-pyrrole-3 -carboxylic acid derivatives and its application for the production of pharmaceutical compounds.

IPC Classes  ?

• C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 207/34 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
• C07D 217/14 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
• C07D 217/16 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Abstract

Compounds of formula (I) are useful as LRRK2 kinase inhibitors.

IPC Classes  ?

• C07D 491/08 - Bridged systems
• A61K 9/20 - Pills, lozenges or tablets
• A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
• A61K 31/4192 - 1,2,3-Triazoles
• A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/16 - Anti-Parkinson drugs
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• A61P 35/00 - Antineoplastic agents
• A61P 37/00 - Drugs for immunological or allergic disorders
• C07D 491/18 - Bridged systems
• C07D 498/08 - Bridged systems
• C07D 498/18 - Bridged systems
• C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
• C07D 513/18 - Bridged systems

Abstract

Compounds of formula (I) are useful as LRRK2 kinase inhibitors.

IPC Classes  ?

• C07D 491/08 - Bridged systems
• C07D 491/18 - Bridged systems
• C07D 498/08 - Bridged systems
• C07D 498/18 - Bridged systems
• C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
• C07D 513/18 - Bridged systems
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/16 - Anti-Parkinson drugs
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• A61P 35/00 - Antineoplastic agents
• A61P 37/00 - Drugs for immunological or allergic disorders
• A61K 9/20 - Pills, lozenges or tablets
• A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
• A61K 31/4192 - 1,2,3-Triazoles
• A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine

Abstract

The present disclosure provides antisense oligonucleotides for regulating expression of alpha-synuclein and use thereof to treat synucleinopathies.

IPC Classes  ?

• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides

Abstract

Compounds of formula (I): Compounds of formula (I): Compounds of formula (I): wherein Het1, Het2, R1, R2 and R3 are as defined in the description.

IPC Classes  ?

• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

The present disclosure provides antisense oligonucleotides for regulating expression of alpha-synuclein and use thereof to treat synucleinopathies.

IPC Classes  ?

• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides

Abstract

Compounds of formula (I)

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• A61P 5/48 - Drugs for disorders of the endocrine system of the pancreatic hormones
• A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline

Abstract

Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a purified compound described herein.

IPC Classes  ?

• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61P 35/00 - Antineoplastic agents
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Abstract

The present disclosure provides for compounds according to Formula I, Formula II, and their pharmaceutically acceptable salts, tautomers, and/or isotopologues as described in the disclosure. The compounds are inhibitors of methionine adenosyltransferase isoform 2A (MAT2A). Also provided are pharmaceutical compositions and methods of using the compounds for treating cancers, including some cancers in which the gene encoding methylthioadenosine phosphorylase (MTAP) is deleted. The present disclosure provides for compounds according to Formula I, Formula II, and their pharmaceutically acceptable salts, tautomers, and/or isotopologues as described in the disclosure. The compounds are inhibitors of methionine adenosyltransferase isoform 2A (MAT2A). Also provided are pharmaceutical compositions and methods of using the compounds for treating cancers, including some cancers in which the gene encoding methylthioadenosine phosphorylase (MTAP) is deleted.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
• A61P 35/00 - Antineoplastic agents

Abstract

The present disclosure provides PROTAC compounds represented by Formula (A): D-L-DSM (A), or an enantiomer, a diastereoisomer, and/or a pharmaceutically acceptable salt of any one of the foregoing, wherein: DSM is a degradation signaling compound {e.g., an E3 ubiquitin ligase recruitment ligand, such as a CRBN ligand or a VHL ligand) covalently attached to a linker L; L is a linker that covalently attaches DSM to D; and D is a Bcl-xL inhibitor compound of Formula (I) or Formula (II) covalently attached to the linker L: (I); (II) wherein the definitions for the variables are described herein. Also provided are pharmaceutical compositions comprising the PROTAC compounds of the present disclosure and methods of use and methods of making thereof.

IPC Classes  ?

• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 471/04 - Ortho-condensed systems

Abstract

The present disclosure provides PROTAC compounds represented by Formula (A): D-L-DSM (A), or an enantiomer, a diastereoisomer, and/or a pharmaceutically acceptable salt of any one of the foregoing, wherein: DSM is a degradation signaling compound {e.g., an E3 ubiquitin ligase recruitment ligand, such as a CRBN ligand or a VHL ligand) covalently attached to a linker L; L is a linker that covalently attaches DSM to D; and D is a Bcl-xL inhibitor compound of Formula (I) or Formula (II) covalently attached to the linker L: (I); (II) wherein the definitions for the variables are described herein. Also provided are pharmaceutical compositions comprising the PROTAC compounds of the present disclosure and methods of use and methods of making thereof.

IPC Classes  ?

• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 471/04 - Ortho-condensed systems
• A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
• A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
• A61P 35/00 - Antineoplastic agents

Abstract

Compounds of Formula (I) wherein R1, R3, R11, R12, X, Y1, Y2, Y3, Y4 and formula (II) are as defined in the description. Medicaments.

IPC Classes  ?

• C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
• A61K 31/404 - Indoles, e.g. pindolol
• A61P 35/00 - Antineoplastic agents
• C07C 49/697 - Unsaturated compounds containing a keto group being part of a ring containing halogen containing six-membered aromatic rings
• C07C 71/00 - Esters of oxyacids of halogens
• C07C 229/50 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms being part of the same condensed ring system
• C07C 233/52 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
• C07C 323/61 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
• C07D 213/72 - Nitrogen atoms
• C07D 215/233 - Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
• C07D 221/20 - Spiro-condensed ring systems
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
• C07D 495/04 - Ortho-condensed systems

Abstract

13111212344 and formula (II) are as defined in the description. Medicaments.

IPC Classes  ?

• C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
• C07C 71/00 - Esters of oxyacids of halogens
• C07D 213/72 - Nitrogen atoms
• C07D 215/233 - Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
• C07D 221/20 - Spiro-condensed ring systems
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
• C07D 495/04 - Ortho-condensed systems
• A61K 31/404 - Indoles, e.g. pindolol
• A61P 35/00 - Antineoplastic agents
• C07C 49/697 - Unsaturated compounds containing a keto group being part of a ring containing halogen containing six-membered aromatic rings
• C07C 233/52 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
• C07C 229/50 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms being part of the same condensed ring system
• C07C 323/61 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton

Abstract

The present disclosure is directed to progastrin monoclonal antibodies, fragments thereof, compositions comprising progastrin monoclonal antibodies, and methods of making and using progastrin monoclonal antibodies and compositions thereof. The present disclosure is directed to methods of treating colorectal cancer with progastrin monoclonal antibodies and compositions comprising progastrin monoclonal antibodies or fragments thereof. The present disclosure is further directed to methods comprising detection of progastrin, including methods of diagnosing colorectal cancer and methods of monitoring efficacy of anti-cancer therapy in subjects suffering from colorectal cancer.

IPC Classes  ?

• C07K 16/26 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against hormones
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer

Abstract

Antibody-drug conjugates that bind to human oncology targets are disclosed. The antibody- drug conjugates comprise a Bcl-xL inhibitor drug moiety. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody- drug conjugates provided herein. Linker-drug conjugates comprising Bcl-xL inhibitor drug moiety and methods of making same are also disclosed.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment

Abstract

Anti-CD48 antibody-drug conjugates are disclosed. The anti-CD48 antibody-drug conjugates comprise an Mcl-1 inhibitor drug moiety and an anti-CD48 antibody or antigen-binding fragment thereof that binds an antigen target, e.g., an antigen expressed on a tumor or other cancer cell. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising an Mcl-1 inhibitor drug moiety and methods of making same are also disclosed.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents

Abstract

Anti-CD48 antibody-drug conjugates are disclosed. The anti-CD48 antibody-drug conjugates comprise an Mcl-1 inhibitor drug moiety and an anti-CD48 antibody or antigen-binding fragment thereof that binds an antigen target, e.g., an antigen expressed on a tumor or other cancer cell. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising an Mcl-1 inhibitor drug moiety and methods of making same are also disclosed.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents

Abstract

Antibody-drug conjugates that bind to human oncology targets are disclosed. The antibody- drug conjugates comprise a Bcl-xL inhibitor drug moiety. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody- drug conjugates provided herein. Linker-drug conjugates comprising Bcl-xL inhibitor drug moiety and methods of making same are also disclosed.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents

Abstract

The present disclosure provides for compounds according to Formula I and their pharmaceutically acceptable salts, tautomers, and/or isotopologues as described in the disclosure. The compounds are inhibitors of methionine adenosyltransferase isoform 2A (MAT2A). Also provided are pharmaceutical compositions and methods of using the compounds for treating cancers, including some cancers in which the gene encoding methylthioadenosine phosphorylase (MTAP) is deleted.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• A61P 35/00 - Antineoplastic agents
• C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

Abstract

SHNHNHdd]pyrimidin-4-yl]oxy}-3-(2-{[2-(2-methoxyphenyl)pyrimidin-4- yl]methoxy}phenyl)propanoic acid, or a pharmaceutically acceptable salt thereof, for use in the treatment of cancer, wherein Compound A and Compound B are administered as defined in the invention.

IPC Classes  ?

• A61P 35/00 - Antineoplastic agents
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 35/02 - Antineoplastic agents specific for leukemia
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Goods & Services

Pharmaceutical products, medical and veterinary preparations; sanitary products for medicine; dietetic substances and foodstuffs for medical or veterinary use, food for babies; food supplements for humans and animals; plasters, materials for dressings; material for dental fillings and dental impressions; disinfectants; products for destroying vermin; fungicides, herbicides. Medical services; veterinary services; hygiene and beauty care for human beings or animals; health advice; pharmacy consultation; health services; telemedicine services; therapeutic services; medical diagnostic services; home care services; individualized medical prescription services; online medical prescription services; providing support in the follow-up of patients receiving medical treatment; advice with respect to home medical treatment; advice on self-medication; provision of medical information to patients; remote medical examination services; advice concerning personal well-being [health]; medical monitoring of patients including remote monitoring.

Abstract

Provided herein are method of treating lymphomas using an anti-cancer agent and an anti-cancer therapy, wherein the first anti-cancer agent is represented by Formula (I) or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 31/4192 - 1,2,3-Triazoles
• A61K 31/475 - QuinolinesIsoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
• A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
• A61K 39/00 - Medicinal preparations containing antigens or antibodies
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to a recombinant microorganism which is modified to be capable of producing diosmin and hesperidin and to the use thereof for producing diosmin and/or hesperidin.

IPC Classes  ?

• C12P 19/60 - Preparation of O-glycosides, e.g. glucosides having an oxygen of the saccharide radical directly bound to a non-saccharide heterocyclic ring or a condensed ring system containing a non-saccharide heterocyclic ring, e.g. coumermycin, novobiocin
• C12N 9/00 - Enzymes, e.g. ligases (6.)ProenzymesCompositions thereofProcesses for preparing, activating, inhibiting, separating, or purifying enzymes
• C12N 9/02 - Oxidoreductases (1.), e.g. luciferase
• C12N 9/10 - Transferases (2.)
• C12N 9/88 - Lyases (4.)
• C12N 9/90 - Isomerases (5.)

Goods & Services

Pharmaceutical products, medical and veterinary preparations; hygienic products for medicine; dietetic substances and foodstuffs for medical or veterinary use, food for babies; food supplements for humans and animals; plasters, materials for dressings; material for dental fillings and dental impressions; disinfectants; products for destroying vermin; fungicides, herbicides. Scientific, optical, weighing, measuring, signaling, checking (inspecting), life-saving and teaching apparatus and instruments; apparatus and instruments for conducting, switching, transforming, accumulating, regulating or controlling electricity; apparatus for recording, transmission or reproduction of sound or images; magnetic recording media; sound recording disks; digital recording media; data and information processing apparatus and equipment; software; computer programs; computers; software recorded on magnetic media or downloaded from a remote computer network; downloadable computer software applications; telecommunication equipment for use with mobile networks; personal digital assistant; electronic signal transmitters; connected bracelets (measuring instruments); connected scales; connected watches (measuring instruments); video cameras; electronic sensors; mobile applications; digital applications; algorithms (software); artificial intelligence software; computer platforms in the form of information sharing software; connected self-measurement tools; electronic chips connected to an information system; downloadable applications for mobile devices; artificial intelligence software; spectacles; contact lenses; smart glasses; in-ear headphones; downloadable telemedicine applications for mobile devices; augmented reality software; virtual reality computer programs; analysis systems based on artificial intelligence (software); medical image analysis systems based on artificial intelligence; virtual reality headsets. Medical, surgical, dental and veterinary apparatus, instruments and equipment, artificial limbs, organs, eyes and teeth; orthopedic articles; surgical instruments for use in orthopedic surgery; medical, surgical and orthopedic implants made of artificial materials; suture material; compression stockings, tights and socks; stockings, tights and socks for varicose veins; bandages for compression dressing; medical apparatus, instruments and equipment for introduction of pharmaceutical preparations into the human body, particularly for the prolonged, controlled or immediate release of active substances; infusion devices and syringes for medical use; medical measuring instruments, in particular instruments able to directly transmit data to a database, in particular instruments to measure fevers, heart rate monitors; apparatus, instruments and equipment derived from robotics for medical use; nanobots for medical use; apparatus, instruments and equipment derived from bionics for medical use; bio-materials for medical use; connected materials for medical use; smart materials for medical use; allergy testing tools; blood testing apparatus; medical devices intended for ingestion; endoscopic video capsules; medical apparatus for measuring biochemical changes in blood; blood biomarker devices; medical endoscopy apparatus; inhalers; blood pressure monitors; physiological monitoring and measuring apparatus for medical use; telemetry apparatus for medical use; acupuncture equipment; hearing aids; automatic analyzers for medical use; medical imaging apparatus; massage apparatus. Scientific and technological services as well as research and design services relating thereto; industrial analysis and research services; scientific research services for medical purposes; design and development of computer hardware and software; research, design and development of tools for monitoring, diagnosis, prediction, analysis; clinical trials; scientific laboratory services; evaluation, scientific and technical project studies; cloud computing; rental of computer software; updating of software; programming for computers; research and development of new products for third parties; electronic data storage; hosting platforms on the Internet, hosting Web portals, temporary provision of non-downloadable software applications accessible via an Internet site; design of websites on the Internet, particularly collaborative platforms; engineering services relating to robotics; development of software intended for patients. Medical services; veterinary services; hygienic and beauty care for human beings or animals; health counseling; pharmacy consultation; health services; telemedicine services; therapeutic services; medical diagnosis services; home care services; individualized medical prescription services; online medical prescription services; providing support in the monitoring of patients receiving medical treatment; advice relating to home medical treatment; advice relating to self-medication; provision of medical information to patients; remote medical examination services; advice related to personal wellbeing [health]; medical monitoring of patients including remote monitoring.

Abstract

A combination comprising a Bcl-2 inhibitor with a hypomethylating agent, uses in the treatment of cancers and pharmaceutical compositions thereof. The Bcl-2 inhibitor is 5-(5-chloro-2- {[(3S)-3-(morpholin-4-ylmethyl)-3,4-dihydroisoquinolin-2(1H)-yl]carbonyl}phenyl)-N-(5- cyano-1,2-dimethyl-1H-pyrrol-3-yl)-N-(4-hydroxyphenyl)-1,2-dimethyl-1H-pyrrole-3- carboxamide and the hypomethylating agent is selected from decitabine, azacitidine and guadecitabine.

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
• A61K 31/708 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

The present invention relates to the field of oncology, particularly the early diagnostic of lung cancer, the monitoring of lung cancer patients and the prediction of the clinical outcome of patients. The invention relates to a method for diagnosing lung cancer or diagnosing relapse of lung cancer in patients by determination of the level of methylation of gene(s) and the kit to implement said method.

IPC Classes  ?

• C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer

Abstract

A combination comprising a Bcl-2 inhibitor with a hypomethylating agent, uses in the treatment of cancers and pharmaceutical compositions thereof. The Bcl-2 inhibitor is 5-(5-chloro-2- {[(3S)-3-(morpholin-4-ylmethyl)-3,4-dihydroisoquinolin-2(1H)-yl]carbonyl}phenyl)-N-(5- cyano-1,2-dimethyl-1H-pyrrol-3-yl)-N-(4-hydroxyphenyl)-1,2-dimethyl-1H-pyrrole-3- carboxamide and the hypomethylating agent is selected from decitabine, azacitidine and guadecitabine.

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
• A61K 31/708 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

A combination of (a) Midostaurin, or a pharmaceutically acceptable salt thereof, or a complex thereof, or a co-crystal thereof, or a solvate, including hydrate, thereof, and (b) a Mcl-1 inhibitor and compositions and uses thereof.

IPC Classes  ?

• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
• A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
• A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

Crystalline forms of Compound A: 13C NMR spectrum, MIR spectrum and Raman spectrum and pharmaceutical compositions containing it.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems

Goods & Services

(1) Préparations pharmaceutiques pour le traitement de maladies cardio-vasculaires, de troubles immunoinflammatoires, de troubles neuro-psychiatriques, pour le traitement du cancer et du diabète; produits hygiéniques pour la médecine, nommément savons désinfectants et lingettes désinfectants; aliments et substances diététiques à usage médical, nommément aliments pour diabétiques, aliments pour bébés; compléments alimentaires minéraux et vitaminés pour l'état général de la santé; emplâtres en tant que matériel pour pansements; matières pour plomber les dents et pour empreintes dentaires; désinfectants pour instruments et appareils dentaires et médicaux; produits pour la destruction d'animaux nuisibles; fongicides, herbicides. (1) Services d'examens médicaux, services médicaux dans le domaine des troubles cardiovasculaires, immuno-inflammatoire, neuro-dégénératifs, et reliés à l'oncologie, au métabolisme et au système nerveux central; services vétérinaires; fourniture d'informations et de conseils dans le domaine, de soins médicaux,et de soins pharmaceutiques; consultation en matière de pharmacie; services de santé dans le domaine des troubles immuno-inflammatoires et du diabète; services de télémédecine; services de loisirs thérapeutiques; services d'analyses médicales fournis par des laboratoires médicaux à des fins diagnostiques et thérapeutiques; services de diagnostic médical; services de soin médicaux à domicile; préparation d'ordonnances par des pharmaciens; préparation de prescriptions en pharmacie; services d'information, de conseil et de consultation dans le domaine des services de traitement médical; offre d'information aux patients dans le domaine de l'administration de médicaments; fourniture d'informations médicales dans le domaine des troubles cardiovasculaires, immuno-inflammatoire, neuro-dégénératifs, et reliés à l'oncologie, l'ostéoporose, au métabolisme et au système nerveux central; services d'examen médical à distance; services de conseil dans les domaines de la santé et du bien-être en général, de la nutrition et du bien-être par le mode de vie, y compris le bien-être physique, mental et spirituel; services de tests de diagnostic médical, de surveillance et de rapports; services transtéléphoniques de surveillance cardiaque.

Goods & Services

Pharmaceuticals, namely, pharmaceutical preparations for the treatment of cardiovascular diseases, pharmaceutical preparations for preventing and treating disorders of the central nervous system, cytostatic pharmaceutical preparations for use in the treatment of cancer, pharmaceutical preparations for preventing and treating metabolism disorders, pharmaceutical preparations for the treatment and prevention of obesity, pharmaceutical preparations for the treatment and prevention of diabetes, pharmaceutical preparations for treating blood and blood forming organs to aid in blood clotting, pharmaceutical preparations for the treatment and prevention of disorders of the respiratory system, pharmaceutical preparations for the treatment and prevention of disorders of the musculo-skeletal system, pharmaceutical preparations for the treatment and prevention of disorders of the genitourinary system, anti-infective pharmaceutical preparations, pharmaceutical preparations for the treatment and prevention of disorders of the ophthalmological system Providing health Information; medical services; veterinary services; health advice, namely, providing advice in the field of human health and pet health; pharmaceutical advice; health services, namely, medical services, health assessment services; medical diagnosis of cardiovascular, immune-inflammatory, neurodegenerative, respiratory, oncological, metabolic and osteoporosis diseases and disorders; individualized medical prescription refill reminder services, online prescription refill reminder services; interactive medical monitoring services for reminding patients of medicinal dosage, allergic sensitivity, and prescription refills for medical treatment purposes; advice relating to home medical treatment, namely, residential medical advice services; Residential medical advice services relating to self-medication; provision of medical information to patients; providing medical advice in the field of personal health wellbeing; remote medical monitoring of data indicative of the health condition of an individual for medical diagnosis and treatment purposes

Abstract

Diosmin preparation method.

IPC Classes  ?

• C07H 1/00 - Processes for the preparation of sugar derivatives
• C07H 17/07 - Benzo[b]pyran-4-ones

Abstract

Diosmin preparation method.

IPC Classes  ?

• C07H 1/00 - Processes for the preparation of sugar derivatives
• C07H 17/07 - Benzo[b]pyran-4-ones

Abstract

Process of ortho-halogenation of phenylalanine compounds by C-H activation.

IPC Classes  ?

• C07C 227/14 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
• C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Abstract

Provided herein are method of treating cancers using a first anti-cancer agent and at least one second anti-cancer agent, wherein the first anti-cancer agent is represented by Formula (I): or a pharmaceutically acceptable salt thereof. Compositions comprising the disclosed first anti-cancer agent and at least one second anti-cancer agent are also provided.

IPC Classes  ?

• A61K 31/4192 - 1,2,3-Triazoles
• A61K 31/635 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide having a heterocyclic ring, e.g. sulfadiazine
• A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
• A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

Process for the industrial synthesis of the compound of formula (I):

IPC Classes  ?

• C07D 295/08 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
• C07D 295/088 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain

Goods & Services

Pharmaceutical products, medical and veterinary preparations; hygienic products for medicine; dietetic food and substances for medical or veterinary use, food for babies for medical use; plasters, materials for dressings for medical use; material for dental fillings and dental impressions; disinfectants for medical use; preparations for destroying vermin for medical use; fungicides for medical use, herbicides; natural remedies for medical use; probiotic preparations for medical use; dietary fibers for medical use; stem cells; pharmaceutical products for regenerative medicine; enzymes for medical and veterinary use; phytotherapy preparations for medical use; patches for pharmaceutical use. Scientific, optical, weighing, measuring, signaling, checking (supervision), life-saving and teaching apparatus and instruments; apparatus and instruments for conducting, switching, transforming, accumulating, regulating or controlling electricity; apparatus for recording, transmission or reproduction of sound or images; magnetic recording media; digital recording media; sound recording disks; data and information processing apparatus and equipment; software; computers; computer programs; data processing equipment; software recorded on magnetic media or downloaded from a remote computer network; downloadable computer software applications; downloadable applications for mobile devices and portable apparatus; digital applications; telecommunication equipment for use with mobile networks; electronic signal transmitters; software for monitoring physiological signals; software for analyzing, storing and monitoring physiological data, including predictive medicine, diagnosis, monitoring and warning software; software for algorithms; artificial intelligence software; computer platforms in the form of information sharing software; analysis systems based on artificial intelligence (software); software for updating and exchanging data on a virtual exchange platform for information between patients and healthcare professionals; teleconsultation and video consultation software; software for online data management in the field of cloud computing networks and applications; software for medical purposes, used for the collection and processing of data regarding patients and the control of diagnostic and therapeutic methods using medical-technical devices; medical imaging software; personal digital assistant; connected bracelets; connected scales, connected watches (measuring instruments); connected self-measurement tools; spectacles, contact lenses; video cameras; wearable activity trackers; augmented reality software; virtual reality computer programs; medical image analysis systems in the nature of software, based on artificial intelligence; electronic chips connected to an information system; virtual reality headsets; pressure indicators; in-ear headphones; information display terminals; tracking apparatus; electronic labels; travel distance monitor; personal electronic devices for displaying, measuring, recording, organizing, handling, analysing and receiving data, texts, images and audio files related to health and wellbeing; receivers for the detection, storage, processing of electronic data from a sensor which records data in connection with health. Surgical, medical, dental and veterinary apparatus and instruments; orthopedic articles; artificial limbs, eyes and teeth; suture material; diagnostic and monitoring devices for medical use; compression stockings, tights and socks; stockings, tights and socks for varicose veins; bandages for compression dressing; medical apparatus, instruments and equipment for introducing pharmaceutical preparations into the human body; infusion devices and syringes for medical use; diagnostic tools and instruments for medical use; blood analysis apparatus for medical use; medical endoscopy apparatus; inhalers; physiological monitoring and measuring apparatus for medical use; telemetry apparatus for medical use; acupuncture equipment; hearing aids; automatic analyzers for medical use; medical imaging apparatus; massage apparatus; computer-aided medical apparatus and instruments; health monitoring and testing apparatus; sensors, monitors and display screens in the field of health; electric or electronic sensors for use in detecting, measuring, processing, collecting, recording and transmitting health-related variables; apparatus for measuring blood and arterial pressure. Support services in running or managing a commercial company; business management assistance services; business start-up assistance; database management; management of computer files and databases on a virtual data exchange platform; commercial intermediation services in the framework of matching potential private investors with entrepreneurs in search of funding; recording, transcription, composition, compilation or systematization of written communications, recordings and information in a database; compilation of mathematical or statistical data; computer file management; compilation of information into computer databases; updating and maintenance of data in computer databases; management and processing of data, particularly medical, surgical, pharmacological data, on behalf of third parties; business management and organization consultancy; business management consultancy; analysis of commercial data; market studies; information relating to market research; establishment of relations between investors, natural persons or legal entities and businesses seeking equity; expertise services regarding company productivity; retail sale or wholesale services for pharmaceutical, veterinary and sanitary preparations as well as medical, surgical apparatus and instruments, medical supplies; sales promotion services for third parties; public relations; sponsorship search; auctioneering; organization of events for commercial or advertising purposes; subsidy administration and management (business management assistance); provision of personnel; collection of information for companies; data processing verification; data retrieval services. Advice and assistance to companies relating to financing; providing funding for commercial entities and businesses; information, consultancy relating to monetary and financial affairs; arranging of financial investments and transactions; advice and consultancy in structuring capital and industrial strategy; capital investment in start-ups; financing of projects; raising or investing capital; financial sponsorship; capital investments. Education, training; organizing and conducting colloquiums, congresses, seminars, conferences, symposiums, organizing and conducting events, contests, exhibitions for cultural, educational or entertainment purposes; publication of texts other than advertising texts; online publication of books and specialized journals; entertainment; sporting and cultural activities; organization of competitions (education or entertainment); consultancy services related to fitness; coaching (training). Scientific and technological services as well as research and design services relating thereto; industrial analysis and research services; scientific research services for medical purposes; design and development of computer hardware and software; research, design and development services for monitoring and diagnostic tools; clinical trials; scientific laboratory services; evaluation, scientific and technical project studies; cloud computing; rental of computer software; updating of software; programming for computers; research and development of new products for third parties; scientific research; electronic data storage; data hosting platforms on the Internet, hosting of Web portals, providing temporary use of non-downloadable software applications accessible via a website; website design services on the Internet, in particular collaborative platforms; engineering services relating to robotics; development of software directed at patients; platform (as a service) for the exchange of information between patients and healthcare professionals; software as a service [SaaS]; biological analyses; conversion of data or documents from physical to electronic media. Medical services; veterinary services; medical, hygiene and beauty care for human beings or animals; advice regarding health; pharmacy advice; health services; telemedicine services; therapeutic services; medical diagnosis services; medical diagnostic services via electronic and telematic means; home healthcare services; individualized medical prescription services; online medical prescription services; consultancy in relation to medical treatment in the home; consultancy regarding self-medication; medical information services for patients; remote medical examination services; advice concerning personal well-being [health]; medical monitoring of patients including provided remotely; providing medical support in the monitoring of patients receiving medical treatments; medical information retrieval services; medical health assessment services. Providing individual support services to families of patients with serious illnesses; social networking services.

Abstract

The disclosure provides fusion proteins specific for both CD 137 and PD-L1, which fusion protein can be used to co-stimulate lymphocyte activation in a PD-L1-target-dependent manner. Such fusion proteins can be used in many pharmaceutical applications, for example, as anti-cancer agents and/or immune modulators for the treatment or prevention of human diseases such as a variety of tumors. The present disclosure also concerns methods of making the fusion proteins described herein as well as compositions comprising such fusion proteins. The present disclosure further relates to nucleic acid molecules encoding such fusion proteins and to methods for generation of such fusion proteins and nucleic acid molecules. In addition, the application discloses therapeutic and/or diagnostic uses of such fusion proteins as well as compositions comprising one or more of such fusion proteins.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to para-amino-benzyl linker compounds useful for linking drug moieties to antibodies, to linker-drug compounds in which said para-amino-benzyl linker compounds are covalently linked to drug moieties, and to antibody-drug conjugates in which said para-amino-benzyl linker compounds are covalently linked to drug wherein said drug is enzymatically cleaved from the conjugate at a particular cell or tissue type targeted by said antibody.

IPC Classes  ?

• C07K 5/062 - Dipeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala
• A61K 47/65 - Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• C07K 5/06 - Dipeptides
• C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies

Abstract

The present invention relates to para-amino-benzyl linker compounds useful for linking drug moieties to antibodies, to linker-drug compounds in which said para-amino-benzyl linker compounds are covalently linked to drug moieties, and to antibody-drug conjugates in which said para-amino-benzyl linker compounds are covalently linked to drug wherein said drug is enzymatically cleaved from the conjugate at a particular cell or tissue type targeted by said antibody.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment

Abstract

Novel salt and related crystalline forms of Compound A: Novel salt and related crystalline forms of Compound A: wherein the salt is the hydrogen sulfate salt, characterised by its X-ray powder diffraction diagram, method for preparing the same and pharmaceutical compositions containing it.

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Abstract

Compounds of formula (I): wherein R, X1, X2, X3, Z1, Z2, Z3, A and Ra are as defined in the description. Medicaments.

IPC Classes  ?

• C07D 498/16 - Peri-condensed systems
• C07D 498/18 - Bridged systems
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems

Abstract

Compounds of formula (I): wherein R, X1, X2, X3, Z1, Z2, Z3, A and Ra are as defined in the description. Medicaments.

IPC Classes  ?

• C07D 498/18 - Bridged systems
• A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• C07D 498/04 - Ortho-condensed systems
• C07D 515/18 - Bridged systems