In one aspect of the subject invention, a labeling shell is provided for a drug vial having a glass reservoir and an opening sealed by an elastomeric stopper, the labeling shell including: a polymeric tubular body formed to accommodate the reservoir of the drug vial, the tubular body having a first open end defining a first opening smaller than a diameter of the reservoir of the drug vial so as to prevent passage therethrough of the reservoir, wherein the elastomeric stopper is exposed through the first end with the reservoir being accommodated in the tubular body; and, a polymeric cap removably mountable to the tubular body to selectively cover the elastomeric stopper of the drug vial with the reservoir being accommodated in the tubular body. Advantageously, the subject invention provides a labeling surface for a drug vial, while also providing restricted access to the drug vial to limit tampering therewith.
A pneumatic tablet collection device including a tablet collector, a pneumatic rotary actuator, and a rotatable base operatively connected to the tablet collector and the pneumatic rotary actuator. The rotatable base includes a housing having an outer shell that includes ratchet teeth, and a central shaft having a pawl. The device further includes an annular shaft housed within the housing between the outer shell and the central shaft, wherein the annular shaft includes ratchet teeth operatively engaging the housing.
B65D 83/04 - Containers or packages with special means for dispensing contents for dispensing annular, disc-shaped, spherical or like small articles, e.g. tablets or pills
B65B 1/10 - Methods of, or means for, filling the material into the containers or receptacles by rotary feeders
Compounds of Formula (I) or their pharmaceutically acceptable salts can inhibit the G12C, G12D, G12V, and/or G13D mutants of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of bone, cardiovascular, central nervous system, dermatological, endocrine, hematological, hepatological, immunological, gastrointestinal, genitourinary, gynecological, metabolic, musculoskeletal, nephrological, neurological, oncological, ophthalmic, psychiatric, pulmonary, renal, respiratory, and urological diseases and disorders; Pharmaceutical preparations for the treatment and prevention of autoimmune diseases, asthma, cancer and tumors, chronic cough, diabetes, hypertension, insomnia, intestinal infections, skin disorders, and urinary incontinence; Inhalers filled with pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; Antibacterial pharmaceuticals; Antibiotics; Antifungal preparations; Anti-infectives; Anti-inflammatories; Antiparasitics; Antivirals; Human vaccine preparations
5.
METHODS FOR TREATING CANCER, OR VON-HIPPEL LINDAU DISEASE USING A COMBINATION OF A TIGIT ANTAGONIST, A PD-1 ANTAGONIST, AND A HIF-2-ALPHA INHIBITOR
Provided herein are methods of treating cancer, or von-Hippel Lindau disease, which comprise administering to a human patient in need thereof: (a) a TIGIT antagonist; (b) a PD-1 antagonist; and an HIF-2α inhibitor. Also provided are kits containing such agents and uses of therapeutic combinations of such agents for the treatment of cancer, or von-Hippel Lindau disease.
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 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
A61K 39/00 - Medicinal preparations containing antigens or antibodies
The instant invention is directed to an efficient and scalable process for synthesizing Compound 5, (aminomethyl phenylalanine), or a salt thereof. The process utilizes an engineered PAL enzyme to prepare Compound 4 via an enantioselective hydroamination of readily accessible 3-cyanocinnamic acid, which is optimal for industrial scale manufacturing. In the instant invention, Compound 4 then undergoes a hydrogenation step to make Compound 5, or a salt thereof.
C07C 255/49 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
C07C 255/58 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of bone, cardiovascular, central nervous system, dermatological, endocrine, hematological, hepatological, immunological, gastrointestinal, genitourinary, gynecological, metabolic, musculoskeletal, nephrological, neurological, oncological, ophthalmic, psychiatric, pulmonary, renal, respiratory, and urological diseases and disorders; Pharmaceutical preparations for the treatment and prevention of autoimmune diseases, asthma, cancer and tumors, chronic cough, diabetes, hypertension, insomnia, intestinal infections, skin disorders, and urinary incontinence; Inhalers filled with pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; Antibacterial pharmaceuticals; Antibiotics; Antifungal preparations; Anti-infectives; Anti-inflammatories; Antiparasitics; Antivirals; Human vaccine preparations
The invention is directed to compounds of Formula (I) and their pharmaceutically acceptable salts, which may be suitable for imaging Granzyme B activity and hence are useful in binding and imaging Granzyme B in patients with cancer or inflammatory diseases.
C07K 5/097 - Tripeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp, e.g. thyroliberin, melanostatin
C07D 207/10 - 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 no 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
The present disclosure provides polypeptides (e.g., PAL polypeptides), polynucleotides and expression vectors comprising the same, methods of producing polypeptides (e.g., PAL polypeptides), and methods of converting heterocyclic cinnamic acids (e.g., 3-cyanocinnamic acid) into L-phenylalanines (e.g., 3-cyano-L-phenylalanine).
The present disclosure is directed to certain functionalized dual substituted arene derivatives (e.g., arenesulfonamide, arenesulfamide, areneoxalamide and areneamide derivatives) of Formula I; and pharmaceutically acceptable salts thereof, wherein X1, X2, Y, Z, G, R1, R2, R3, R4, and R5 are as defined herein, which are potent inhibitors of MsbA and may be useful in the treatment of infections caused by any multi-drug resistant (MDR) Gram-negative bacteria. The disclosure is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of infections in which MsbA is involved.
The present disclosure is directed to certain functionalized dual substituted arene derivatives (e.g., arenesulfonamide, arenesulfamide, areneoxalamide and areneamide derivatives) of Formula I; and pharmaceutically acceptable salts thereof, wherein X1, X2, Y, Z, G, R1, R2, R3, R4, and R5 are as defined herein, which are potent inhibitors of MsbA and may be useful in the treatment of infections caused by any multi-drug resistant (MDR) Gram-negative bacteria. The disclosure is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of infections in which MsbA is involved.
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 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07C 311/21 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07D 307/16 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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 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 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 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 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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 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
Described herein are compounds of Formula 1 or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as RIPK1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for RIPK1-related diseases.
Described herein are compounds of Formula 1 or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as RIPK1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for RIPK1-related diseases.
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 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of bone, cardiovascular, central nervous system, dermatological, endocrine, hematological, hepatological, immunological, gastrointestinal, genitourinary, gynecological, metabolic, musculoskeletal, nephrological, neurological, oncological, ophthalmic, psychiatric, pulmonary, renal, respiratory, and urological diseases and disorders; Pharmaceutical preparations for the treatment and prevention of autoimmune diseases, asthma, cancer and tumors, chronic cough, diabetes, hypertension, insomnia, intestinal infections, skin disorders, and urinary incontinence; Inhalers filled with pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; Antibacterial pharmaceuticals; Antibiotics; Antifungal preparations; Anti-infectives; Anti-inflammatories; Antiparasitics; Antivirals; Human vaccine preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of bone, cardiovascular, central nervous system, dermatological, endocrine, hematological, hepatological, immunological, gastrointestinal, genitourinary, gynecological, metabolic, musculoskeletal, nephrological, neurological, oncological, ophthalmic, psychiatric, pulmonary, renal, respiratory, and urological diseases and disorders; Pharmaceutical preparations for the treatment and prevention of autoimmune diseases, asthma, cancer and tumors, chronic cough, diabetes, hypertension, insomnia, intestinal infections, skin disorders, and urinary incontinence; Inhalers filled with pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; Antibacterial pharmaceuticals; Antibiotics; Antifungal preparations; Anti-infectives; Anti-inflammatories; Antiparasitics; Antivirals; Human vaccine preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of bone, cardiovascular, central nervous system, dermatological, endocrine, hematological, hepatological, immunological, gastrointestinal, genitourinary, gynecological, metabolic, musculoskeletal, nephrological, neurological, oncological, ophthalmic, psychiatric, pulmonary, renal, respiratory, and urological diseases and disorders; Pharmaceutical preparations for the treatment and prevention of autoimmune diseases, asthma, cancer and tumors, chronic cough, diabetes, hypertension, insomnia, intestinal infections, skin disorders, and urinary incontinence; Inhalers filled with pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; Antibacterial pharmaceuticals; Antibiotics; Antifungal preparations; Anti-infectives; Anti-inflammatories; Antiparasitics; Antivirals; Human vaccine preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of bone, cardiovascular, central nervous system, dermatological, endocrine, hematological, hepatological, immunological, gastrointestinal, genitourinary, gynecological, metabolic, musculoskeletal, nephrological, neurological, oncological, ophthalmic, psychiatric, pulmonary, renal, respiratory, and urological diseases and disorders; Pharmaceutical preparations for the treatment and prevention of autoimmune diseases, asthma, cancer and tumors, chronic cough, diabetes, hypertension, insomnia, intestinal infections, skin disorders, and urinary incontinence; Inhalers filled with pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; Antibacterial pharmaceuticals; Antibiotics; Antifungal preparations; Anti-infectives; Anti-inflammatories; Antiparasitics; Antivirals; Human vaccine preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of bone, cardiovascular, central nervous system, dermatological, endocrine, hematological, hepatological, immunological, gastrointestinal, genitourinary, gynecological, metabolic, musculoskeletal, nephrological, neurological, oncological, ophthalmic, psychiatric, pulmonary, renal, respiratory, and urological diseases and disorders; Pharmaceutical preparations for the treatment and prevention of autoimmune diseases, asthma, cancer and tumors, chronic cough, diabetes, hypertension, insomnia, intestinal infections, skin disorders, and urinary incontinence; Inhalers filled with pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; Antibacterial pharmaceuticals; Antibiotics; Antifungal preparations; Anti-infectives; Anti-inflammatories; Antiparasitics; Antivirals; Human vaccine preparations
18.
MACROCYCLES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF
The present invention is directed to certain 2-aminoquinzaoline derivatives of Formula (I) and (Ia); and pharmaceutically acceptable salts thereof, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
The present invention is directed to certain 2-aminoquinzaoline derivatives of Formula (I) and (Ia); and pharmaceutically acceptable salts thereof, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
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
A61K 31/529 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring systems
A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
The application provides modified immune effector cells wherein a Lysine Demethylase 4A (KDM4A) gene or gene product is modified in the cell so that the expression and/or function of KDM4A in the cell is reduced or eliminated. The application also provides related pharmaceutical compositions and the methods for generating such modified immune effector cells. The application further provides uses of such modified immune effector cells for treating diseases such as cancers, infectious diseases and autoimmune diseases.
The disclosure provides live attenuated measles vectors encoding in their genome one or more heterologous genes for herpes simplex virus (HSV) proteins, e.g., glycoprotein B, glycoprotein C, glycoprotein D, and variants thereof, as well as nucleic acid constructs encoding such measles vectors. The disclosure also relates to immunogenic compositions comprising live attenuated measles vectors encoding HSV proteins, immunogenic compositions comprising such measles vectors, and use of such measles vectors and immunogenic compositions to induce an immune response to HSV in subjects.
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
The integrin family of cell adhesion molecules has emerged as key mediators of tissue fibrosis. A pharmacological inhibitor of multiple integrin subtypes is required to produce meaningful effects on delaying or inhibiting the progression of fibrosis. Monoclonal antibodies recognizing multiple integrins with potent neutralizing activity and having human and mouse cross-reactivity are described. In particular, monoclonal antibodies that bind human αvβ1, αvβ3, αvβ5, αvβ36, αvβ38, and α5β1 integrins and mouse αvβ1, αvβ3, αvβ5, αvβ6, and αvβ8 integrins are described.
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
23.
INHIBITORS OF MsbA AS ANTIBIOTICS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF
The present disclosure is directed to certain functionalized dual substitute arene derivatives joined by a cyclic or heterocyclic linker of Formula (I); and pharmaceutically acceptable salts thereof, wherein X1, X2, Y, Z, G1, G2, R1, R2, R3, and R4 are as defined herein, which are potent inhibitors of MsbA and may be useful in the treatment of infections caused by any multi-drug resistant (MDR) Gram-negative bacteria. The disclosure is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of infections in which MsbA is involved.
The present disclosure is directed to certain functionalized dual substitute arene derivatives joined by a cyclic or heterocyclic linker of Formula (I); and pharmaceutically acceptable salts thereof, wherein X1, X2, Y, Z, G1, G2, R1, R2, R3, and R4 are as defined herein, which are potent inhibitors of MsbA and may be useful in the treatment of infections caused by any multi-drug resistant (MDR) Gram-negative bacteria. The disclosure is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of infections in which MsbA is involved.
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
C07C 273/02 - Preparation of urea or its derivatives, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups of urea, its salts, complexes or addition compounds
C07C 311/21 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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 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 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
The present disclosure relates to methods of treating gastric cancer in a patient, said methods comprising administering to the patient an Immunoconjugate of Formula (I) wherein: Ab is an antibody that binds to Trop-2; and n is an integer from 1 to 10, and wherein the amount of Immunoconjugate (I) administered is effective to treat gastric cancer.
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
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 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
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
25.
PROCESS FOR PREPARING BETA 3 AGONISTS AND INTERMEDIATES
The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.
C07C 215/30 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings containing hydroxy groups and carbon atoms of six-membered aromatic rings bound to the same carbon atom of the carbon skeleton
C07D 207/08 - 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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
Crystals of an antibody that specifically binds to human tau protein phosphorylated at serine 413 are provided, as well as methods of producing such antibody crystals, compositions comprising the crystals, and uses of such compositions for treating a disease, e.g., Alzheimer's disease. Crystals suitable for X-ray diffraction are also provided, and the inventors herein have used such crystals to solve the three-dimensional structure of the antibody to 2.76 Å resolution.
C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
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
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of bone, cardiovascular, central nervous system, dermatological, endocrine, hematological, hepatological, immunological, gastrointestinal, genitourinary, gynecological, metabolic, musculoskeletal, nephrological, neurological, oncological, ophthalmic, psychiatric, pulmonary, renal, respiratory, and urological diseases and disorders; Pharmaceutical preparations for the treatment and prevention of autoimmune diseases, asthma, cancer and tumors, chronic cough, diabetes, hypertension, insomnia, intestinal infections, skin disorders, and urinary incontinence; Inhalers filled with pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; Antibacterial pharmaceuticals; Antibiotics; Antifungal preparations; Anti-infectives; Anti-inflammatories; Antiparasitics; Antivirals; Human vaccine preparations
Disclosed are polypeptides that can be used for bioconjugation. The polypeptides have transglutaminase activity, and they can be used to make biomolecule-compound conjugates, for example to conjugate a compound to a specific lysine or glutamine of an antibody.
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 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
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
29.
System for Medicinal Supply Monitoring and Management with Controlled Packaging of Medicinal Product
A medicinal supply management system manages distribution of medicinal supply. The system may implement a pooling algorithm for pooling studies together, across different countries, with different protocol labeling parameters and/or blinding parameters. The system may allocate unique identifiers for the pooled studies. The system may implement digital display labels on the medicinal product for up-to-date presentation of relevant information to healthcare providers administering the medicinal product. The system may further implement controlled packaging for maintaining proper storage of the medicinal product, e.g., during transport to the treatment site. The controlled packaging may further include sensors for monitoring the internal environment of the controlled packaging, to maintain proper storage of the medicinal product.
G16H 20/10 - ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance relating to drugs or medications, e.g. for ensuring correct administration to patients
G16H 70/40 - ICT specially adapted for the handling or processing of medical references relating to drugs, e.g. their side effects or intended usage
30.
ANTI-CANCER COMBINATION THERAPIES COMPRISING CTLA-4 AND PD-1 BLOCKING AGENTS
Anti-cancer combination therapies comprising a CTLA-4 blocking agent and a PD-1 blocking agent are disclosed. In particular, combination therapies are disclosed wherein the CTLA-4 blocking agent is an effector-silent anti-CTLA-4 antibody or effector-silent anti-CTLA-4 antibody fragment and the PD-1 blocking agent is an anti-PD-1 or anti-PD-L1 antibody, or antibody fragment thereof.
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
The present disclosure is directed to N-oxide derivatives of Formula I (I) and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV naïve cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).
A medicinal supply management system manages distribution of medicinal supply. The system may implement a pooling algorithm for pooling studies together, across different countries, with different protocol labeling parameters and/or blinding parameters. The system may allocate unique identifiers for the pooled studies. The system may implement digital display labels on the medicinal product for up-to-date presentation of relevant information to healthcare providers administering the medicinal product. The system may further implement controlled packaging for maintaining proper storage of the medicinal product, e.g., during transport to the treatment site. The controlled packaging may further include sensors for monitoring the internal environment of the controlled packaging, to maintain proper storage of the medicinal product.
G16H 40/40 - ICT specially adapted for the management or administration of healthcare resources or facilitiesICT specially adapted for the management or operation of medical equipment or devices for the management of medical equipment or devices, e.g. scheduling maintenance or upgrades
G16H 10/20 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for electronic clinical trials or questionnaires
33.
System for Medicinal Supply Monitoring and Management for Pooled Medicinal Product Across Studies
A medicinal supply management system manages distribution of medicinal supply. The system may implement a pooling algorithm for pooling studies together, across different countries, with different protocol labeling parameters and/or blinding parameters. The system may allocate unique identifiers for the pooled studies. The system may implement digital display labels on the medicinal product for up-to-date presentation of relevant information to healthcare providers administering the medicinal product. The system may further implement controlled packaging for maintaining proper storage of the medicinal product, e.g., during transport to the treatment site. The controlled packaging may further include sensors for monitoring the internal environment of the controlled packaging, to maintain proper storage of the medicinal product.
G16H 10/20 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for electronic clinical trials or questionnaires
G16H 30/40 - ICT specially adapted for the handling or processing of medical images for processing medical images, e.g. editing
G16H 40/67 - ICT specially adapted for the management or administration of healthcare resources or facilitiesICT specially adapted for the management or operation of medical equipment or devices for the operation of medical equipment or devices for remote operation
34.
MODULATION OF CELL GROWTH AND VIABILITY USING NUCLEOSIDE TRANSPORT INHIBITORS, INHIBITORS OF ADENOSINE UPTAKE, ADENOSINE KINASE INHIBITORS AND INHIBITORS OF EXTRACELLULAR SYNTHESIS
Provided is a cell culture medium for the production of a product of interest using a fed-batch process wherein the cell culture medium comprises an extracellular adenosine modulator comprising one or more of a nucleoside transport inhibitor, an inhibitor of adenosine uptake, an adenosine kinase inhibitor or an inhibitor of extracellular synthesis of adenosine.
A medicinal supply management system manages distribution of medicinal supply. The system may implement a pooling algorithm for pooling studies together, across different countries, with different protocol labeling parameters and/or blinding parameters. The system may allocate unique identifiers for the pooled studies. The system may implement digital display labels on the medicinal product for up-to-date presentation of relevant information to healthcare providers administering the medicinal product. The system may further implement controlled packaging for maintaining proper storage of the medicinal product, e.g., during transport to the treatment site. The controlled packaging may further include sensors for monitoring the internal environment of the controlled packaging, to maintain proper storage of the medicinal product.
G16H 20/10 - ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance relating to drugs or medications, e.g. for ensuring correct administration to patients
G16H 40/20 - ICT specially adapted for the management or administration of healthcare resources or facilitiesICT specially adapted for the management or operation of medical equipment or devices for the management or administration of healthcare resources or facilities, e.g. managing hospital staff or surgery rooms
H04W 12/47 - Security arrangements using identity modules using near field communication [NFC] or radio frequency identification [RFID] modules
G06K 19/06 - Record carriers for use with machines and with at least a part designed to carry digital markings characterised by the kind of the digital marking, e.g. shape, nature, code
G06Q 10/08 - Logistics, e.g. warehousing, loading or distributionInventory or stock management
36.
3-SULFAMOYL BENZOATE ESTER AND BENZAMIDE COMPOUNDS AS TEAD MODULATORS
Provided are compounds of Formula I: and a pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising them and methods of using such compounds and pharmaceutically acceptable salts thereof.
The present disclosure provides methods, compositions, uses, and kits for treatment of a cancer, e.g., a cancer having a PD-L1 CPS <10 (e.g., a TNBC having a PD-L1 CPS <10) using an anti-CD27 antibody or antigen-binding fragment thereof, alone or in combination with one or more additional therapeutic agents (e.g., an anti-PD-1 antibody or antigen-binding fragment thereof and/or one or more chemotherapeutic agents).
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
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
The present invention is directed to compounds of Formula I which are agonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
The present invention is directed to compounds of Formula I which are agonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
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
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
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 405/06 - 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 carbon chain containing only aliphatic carbon atoms
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 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 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/06 - 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 carbon chain containing only aliphatic carbon atoms
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
39.
COMBINATION THERAPIES FOR THE TREATMENT OF HR+/HER2- METASTATIC OR LOCALLY ADVANCED BREAST CANCER
The present disclosure relates to methods of treating HR+/HER2- metastatic or locally advanced breast cancer in a patient, the methods comprising administering to the patient: (a) an anti-human PD-1 antibody or antigen binding fragment thereof; and (b) an Immunoconjugate of Formula (I): wherein: Ab is an antibody that binds to Trop-2; and n is an integer from 1 to 10.
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 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
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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 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
Provided are compounds of Formula I: and a pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising them and methods of using such compounds or the pharmaceutically acceptable salts thereof.
The process of the present invention is used to prepare agglomerated, crystalline particles of medium chain fatty acid sodium salts, such as sodium caprate. This process comprises the steps of: a) dissolving a medium chain fatty acid in a first solvent to produce a first solution, wherein the first solvent comprises an aprotic polar solvent; b) adding to the first solution (i) a second solvent, wherein the second solvent comprises a medium chain aliphatic hydrocarbon solvent, and (ii) a solution comprising a sodium salt of a short chain alcohol to create a resulting slurry; and c) isolating agglomerated crystals from the resulting slurry. The first solvent may comprise acetonitrile, and the second solvent may comprise heptane. Further provided are products generated by this process, including sodium caprate products having superior flowability and compression properties.
The invention relates to stable coformulations of antibodies or antigen-binding fragments thereof that bind to human immunoglobulin-like transcript 4 (ILT4) and PD-1. Also provided are methods of treating various cancers using the formulations disclosed herein.
S. pneumoniae S. pneumoniaeS. pneumoniaeS. pneumoniaeS. pneumoniaeS. pneumoniae including pneumococcal pneumoniae, invasive pneumococcal disease and acute otitis media.
A system and method are disclosed for evaluating neural network prediction by leveraging generative reconstructions of a test image to assess confidence in the prediction. The system obtains a test image of a tissue histology slide. The system generates seeds from applying a dropout filter to the test image. The system generates, for each seed, a synthetic image by applying an image generator model to the seed. The system applies a prediction model (e.g., a neural network) to the test image to generate a prediction for the test image of whether the tissue is normal or anormal. The system applies the prediction model to each synthetic image to generate a prediction for the synthetic image of whether the tissue is normal or anormal. The system determines a final prediction for the test image and a confidence associated with the final prediction based on the predictions for the test image and the synthetic images. The system may augment the test image with a label indicating the final prediction and the confidence associated with the final prediction.
G06V 10/26 - Segmentation of patterns in the image fieldCutting or merging of image elements to establish the pattern region, e.g. clustering-based techniquesDetection of occlusion
G06V 10/36 - Applying a local operator, i.e. means to operate on image points situated in the vicinity of a given pointNon-linear local filtering operations, e.g. median filtering
G06V 10/74 - Image or video pattern matchingProximity measures in feature spaces
G06V 10/774 - Generating sets of training patternsBootstrap methods, e.g. bagging or boosting
G06V 10/82 - Arrangements for image or video recognition or understanding using pattern recognition or machine learning using neural networks
G06V 20/70 - Labelling scene content, e.g. deriving syntactic or semantic representations
46.
PNEUMOCOCCAL CONJUGATE VACCINES AND METHODS OF USE THEREOF
The invention is related to 26-valent immunogenic compositions comprising 26 different S. pneumoniae polysaccharide carrier protein conjugates, wherein each of the conjugates comprises a polysaccharide from an S. pneumoniae serotype conjugated to a carrier protein, wherein the serotypes of S. pneumoniae are as defined herein. The 26-valent immunogenic compositions are useful for providing protection against S. pneumoniae infection and/or pneumococcal diseases caused by S. pneumoniae including pneumococcal pneumoniae, invasive pneumococcal disease and acute otitis media.
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
Provided herein, in certain aspects, are methods for inhibiting a TNFR1 -mediated activity using a compound that binds to a binding pocket of TNFR1 between CRD3 and CRD4 of TNFR1.
C07K 7/56 - Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
Disclosed herein are short interfering RNA (siRNA) molecules that downregulate expression of PNPLA3 or variants thereof. The siRNA molecules comprise modified nucleotides and uses thereof. The siRNA molecules may be double stranded and comprise modified nucleotides, such as 2′-O-methyl nucleotides and 2′-fluoro nucleotides, and ligands.
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 47/54 - 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 organic compound
A device includes a camera, a display and a computer-based analysis subsystem. The computer-based analysis subsystem is configured to perform operations including receiving images captured by the camera, the images including a first image depicting a subject performing an ongoing task, analyzing the first image by applying a machine-learned model to segment the images, isolate segments depicting the subject, and extract features from the segments, determining, based on the analyzing, that the subject's performance of the ongoing task is not in accordance with a compliance requirement of the ongoing task, and causing the display to display an indication of why the subject's performance of the ongoing task is not in accordance with the compliance requirement.
G06V 40/20 - Movements or behaviour, e.g. gesture recognition
G06T 7/70 - Determining position or orientation of objects or cameras
G06V 10/26 - Segmentation of patterns in the image fieldCutting or merging of image elements to establish the pattern region, e.g. clustering-based techniquesDetection of occlusion
G06V 20/52 - Surveillance or monitoring of activities, e.g. for recognising suspicious objects
A multi-cartridge injector includes a plunger having a main brace and a pair of stems, each of the pair of stems having a coupler, a pair of stoppers coupled to each coupler of the pair of stems, a containment unit having a pair of barrels, and a Y-shaped conduit having a pair of branches and a common shaft, and a passageway that extends through the common shaft and the pair of branches, each of the pair of branches being in communication with an interior of one of the pair of barrels.
A61M 5/315 - PistonsPiston-rodsGuiding, blocking or restricting the movement of the rodAppliances on the rod for facilitating dosing
A61M 5/32 - NeedlesDetails of needles pertaining to their connection with syringe or hubAccessories for bringing the needle into, or holding the needle on, the bodyDevices for protection of needles
52.
METHODS OF SEPARATING HOST CELL LIPASES FROM A PRODUCTION PROTEIN IN CHROMATOGRAPHIC PROCESSES
Provided herein are methods of separating host cell lipases from a production protein in chromatographic processes and methods of improving polysorbate-80 stability in a production protein formulation by separating host cell lipases from the production protein using chromatographic processes. Also provided are pharmaceutical compositions comprising less than 1 ppm of
C07K 1/22 - Affinity chromatography or related techniques based upon selective absorption processes
B01D 15/16 - Selective adsorption, e.g. chromatography characterised by constructional or operational features relating to the conditioning of the fluid carrier
B01D 15/32 - Bonded phase chromatography, e.g. with normal bonded phase, reversed phase or hydrophobic interaction
B01D 15/36 - Selective adsorption, e.g. chromatography characterised by the separation mechanism involving ionic interaction, e.g. ion-exchange, ion-pair, ion-suppression or ion-exclusion
B01D 15/38 - Selective adsorption, e.g. chromatography characterised by the separation mechanism involving specific interaction not covered by one or more of groups , e.g. affinity, ligand exchange or chiral chromatography
B01D 15/42 - Selective adsorption, e.g. chromatography characterised by the development mode, e.g. by displacement or by elution
C07K 16/06 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies from serum
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of bone, cardiovascular, central nervous system, dermatological, endocrine, hematological, hepatological, immunological, gastrointestinal, genitourinary, gynecological, metabolic, musculoskeletal, nephrological, neurological, oncological, ophthalmic, psychiatric, pulmonary, renal, respiratory, and urological diseases and disorders; Pharmaceutical preparations for the treatment and prevention of autoimmune diseases, asthma, cancer and tumors, chronic cough, diabetes, hypertension, insomnia, intestinal infections, skin disorders, and urinary incontinence; Inhalers filled with pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; Antibacterial pharmaceuticals; Antibiotics; Antifungal preparations; Anti-infectives; Anti-inflammatories; Antiparasitics; Antivirals; Human vaccine preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of bone, cardiovascular, central nervous system, dermatological, endocrine, hematological, hepatological, immunological, gastrointestinal, genitourinary, gynecological, metabolic, musculoskeletal, nephrological, neurological, oncological, ophthalmic, psychiatric, pulmonary, renal, respiratory, and urological diseases and disorders; Pharmaceutical preparations for the treatment and prevention of autoimmune diseases, asthma, cancer and tumors, chronic cough, diabetes, hypertension, insomnia, intestinal infections, skin disorders, and urinary incontinence; Inhalers filled with pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; Antibacterial pharmaceuticals; Antibiotics; Antifungal preparations; Anti-infectives; Anti-inflammatories; Antiparasitics; Antivirals; Human vaccine preparations
55.
PROTEASE INHIBITORS FOR TREATING OR PREVENTING CORONAVIRUS INFECTION
The present invention provides a compound of Formula I wherein A, M, R1, R2, R3a, R3b, and subscripts m and n are as described herein and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for the treatment, inhibition, or amelioration of one or more disease states that could benefit from inhibition of a coronavirus, including SARS-CoV, MERS-CoV and SARS-CoV-2. The compounds of this invention could further be used in combination with other therapeutically effective agents, including but not limited to, other drugs useful for the treatment of coronavirus infection. The invention furthermore relates to processes for preparing compounds of Formula I, and pharmaceutical compositions which comprise compounds of Formula I and pharmaceutically acceptable salts thereof.
The present invention provides a compound of Formula I wherein A, M, R1, R2, R3a, R3b, and subscripts m and n are as described herein and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for the treatment, inhibition, or amelioration of one or more disease states that could benefit from inhibition of a coronavirus, including SARS-CoV, MERS-CoV and SARS-CoV-2. The compounds of this invention could further be used in combination with other therapeutically effective agents, including but not limited to, other drugs useful for the treatment of coronavirus infection. The invention furthermore relates to processes for preparing compounds of Formula I, and pharmaceutical compositions which comprise compounds of Formula I and pharmaceutically acceptable salts thereof.
C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 31/438 - 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 being spiro-condensed with carbocyclic or heterocyclic ring systems
The present invention relates to viral fusion inhibitors, as well as use of these viral fusion inhibitors in the treatment or prevention of infectious disease or infection.
Novel compounds of Formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of NLRP3 and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by NLPR3. The compounds of the present invention may be useful in the treatment, prevention or management of diseases, disorders and conditions mediated by NLRP3 such as, but not limited to, obesity, gout, pseudogout, CAPS, NASH, MASH, fibrosis, heart failure, idiopathic pericarditis, atopic dermatitis, inflammatory bowel disease, Alzheimer's Disease, Parkinson's Disease, dementia with Lewy bodies (DLB), and traumatic brain injury.
Novel compounds of Formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of NLRP3 and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by NLPR3. The compounds of the present invention may be useful in the treatment, prevention or management of diseases, disorders and conditions mediated by NLRP3 such as, but not limited to, obesity, gout, pseudogout, CAPS, NASH, MASH, fibrosis, heart failure, idiopathic pericarditis, atopic dermatitis, inflammatory bowel disease, Alzheimer's Disease, Parkinson's Disease, dementia with Lewy bodies (DLB), and traumatic brain injury.
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 31/439 - 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
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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
58.
PROCESS FOR PREPARING ((1S,2S)-2-(5-METHYLPYRIDIN-2-YL)CYCLOPROPYL)-METHANOL
The present invention relates to an efficient scalable synthesis of compounds such as (1S,2S)-2-(5-methylpyridin-2-yl)cyclopropyl)methanol, which contains a disubstituted cyclopropane with two stereogenic centers and represents a significant challenging synthetic target.
C07D 405/06 - 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 carbon chain containing only aliphatic carbon atoms
The present disclosure provides enzymes derived from the fungi Fusarium oxysporum c8D (“FoPip4H enzymes”) having improved properties as compared to a naturally occurring wild-type enzyme including the capability of hydroxylating certain substituted indanones to provide optically pure 3-hydroxyindanones. Also provided are polynucleotides encoding the FoPip4H enzymes, host cells capable of expressing the FoPip4H enzymes, and processes for using the FoPip4H enzymes to synthesize (R)-4-fluoro-3-hydroxy-7-(methylsulfonyl)-2, 3-dihydro-1H-inden-1-one, a useful intermediate in the synthesis of belzutifan.
The present disclosure is directed to pyridinone derivatives of Formula I
The present disclosure is directed to pyridinone derivatives of Formula I
The present disclosure is directed to pyridinone derivatives of Formula I
and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV naïve cells, and for the treatment of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).
C07D 401/06 - 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 only aliphatic carbon atoms
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
Disclosed are compounds of Formula I, or a salt thereof:
Disclosed are compounds of Formula I, or a salt thereof:
Disclosed are compounds of Formula I, or a salt thereof:
where A, B, D, X, R1, R2 and R8 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.
Provided are novel Substituted Isoquinoline Derivative of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1, R2, and X are as defined herein, as well as compositions comprising at least one Substituted Isoquinoline Derivative, and methods of using the Substituted Isoquinoline Derivatives for treating or preventing cancer in a patient.
C07D 217/12 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
The present invention relates to processes useful in the synthesis of aminohexyl compounds, such as a compound of Formula I or a salt, hydrate and/or solvate thereof, as well as methods for the preparing a compound of Formula I and intermediates used to make a compound of Formula I. The present invention presents a novel method for the selective alkylation of tryptophan analogues, eliminating the need for protecting groups and advancing the field of tryptophan analogue synthesis.
The present disclosure is directed to compounds of Formula (I) and their use as TREM2 agonists for treatment and prevention of a neurodegenerative disorder associated with a loss of function of human TREM2. The disclosed TREM2 agonists may be useful for the treatment of Alzheimer's Disease and associated neurological conditions.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
C07D 239/70 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or 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
The present disclosure is directed to compounds of Formula I and their use as TREM2 agonists for treatment and prevention of a neurodegenerative disorder associated with a loss of function of human TREM2. The disclosed TREM2 agonists may be useful for the treatment of Alzheimer's Disease and associated neurological conditions.
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
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 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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
Therapies comprising administering at least one antiviral nucleoside, and the use of such therapies in the treatment of viral infections, such as infection by Eastern equine encephalitis virus, Western equine encephalitis virus, Venezuelan equine encephalitis virus, Chikungunya virus, Ross River virus, orthomyxoviridae virus, paramyxoviridae virus, RSV, influenza A virus, influenza B virus, filoviridae virus, human coronavirus, SARS-CoV-1, MERS-CoV, SARS-CoV-2, Ebola virus, or Zika virus, are disclosed herein.
A61K 31/7072 - 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 having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
The present disclosure provides, among other things, a vaccine composition that includes HPV virus-like particles (VLPs) of at least one type of human papillomavirus (HPV) selected from the group consisting of HPV types: 6, 11, 16, 18, 26, 31, 33, 35, 39, 45, 51, 52, 53, 55, 56, 58, 59, 66, 68, 73, and 82, where the vaccine composition provides enhanced or comparable HPV vaccine response in comparison to a similar multiple-dose vaccine.
Described is an efficient, scalable synthesis of compounds such as ((1S,2S)-2-(5-methylpyridin-2-yl)cyclo-propyl)m ethanol, which contains a disubstituted cyclopropane with two stereogenic centers and represents a significant challenging synthetic target.
C12N 9/04 - Oxidoreductases (1.), e.g. luciferase acting on CHOH groups as donors, e.g. glucose oxidase, lactate dehydrogenase (1.1)
69.
PROCESS FOR PREPARING (S)-1-((S)-2-AMINO-3-(4-METHOXYPHENYL)PROPANOYL)-N-(4-(HYDROXYMETHYL)PHENETHYL)-2-METHYLPYRROLIDINE-2-CARBOXAMIDE AND ITS INTERMEDIATES
C07C 213/00 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
C07D 263/02 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
C07D 263/16 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
C07C 215/28 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
70.
METHODS OF TREATING A PATIENT WITH A PD-1 ANTAGONIST
The invention relates to a method of treating cancer in a patient in need thereof comprising co-expression of PD-L1 and/or PD-L2. In one aspect, the present disclosure provides a method of treating cancer in a patient comprising determine if a sample from a tumor from the patient expresses a level of PD-L1 or is predicted to express a level of PD-L1 that exceeds a first pre-determined threshold and expresses a level of PD-L2 or is predicted to express a level of PD-L2 that exceeds a second pre-determined threshold; and administering a PD-1 antagonist to the patient if the level or the predicted level of PD-L1 exceeds the first pre-determined threshold and the level or the predicted level of PD-L2 exceeds the second pre-determined threshold.
C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
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
G16H 20/10 - ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance relating to drugs or medications, e.g. for ensuring correct administration to patients
71.
INDAZOLE DERIVATIVES USEFUL AS INHIBITORS OF NOD-LIKE RECEPTOR PROTEIN 3
Novel compounds of Formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of NLRP3 and may be useful in the treatment, prevention, management, amelioration, control, and suppression of diseases mediated by NLPR3. The compounds of the present invention may be useful in the treatment, prevention or management of diseases, disorders and conditions mediated by NLRP3 such as, but not limited to, obesity, gout, pseudogout, CAPS, NASH, MASH, fibrosis, osteoarthritis, atherosclerosis, heart failure, idiopathic pericarditis, myocarditis, atopic dermatitis, hidradenitis suppurativa, inflammatory bowel disease, cancer, Alzheimer's Disease, Parkinson's Disease, dementia with Lewy bodies (DLB), and traumatic brain injury.
Novel compounds of Formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of NLRP3 and may be useful in the treatment, prevention, management, amelioration, control, and suppression of diseases mediated by NLPR3. The compounds of the present invention may be useful in the treatment, prevention or management of diseases, disorders and conditions mediated by NLRP3 such as, but not limited to, obesity, gout, pseudogout, CAPS, NASH, MASH, fibrosis, osteoarthritis, atherosclerosis, heart failure, idiopathic pericarditis, myocarditis, atopic dermatitis, hidradenitis suppurativa, inflammatory bowel disease, cancer, Alzheimer's Disease, Parkinson's Disease, dementia with Lewy bodies (DLB), and traumatic brain injury.
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
B01D 15/16 - Selective adsorption, e.g. chromatography characterised by constructional or operational features relating to the conditioning of the fluid carrier
B01D 15/20 - Selective adsorption, e.g. chromatography characterised by constructional or operational features relating to the conditioning of the sorbent material
B01D 15/32 - Bonded phase chromatography, e.g. with normal bonded phase, reversed phase or hydrophobic interaction
B01D 15/36 - Selective adsorption, e.g. chromatography characterised by the separation mechanism involving ionic interaction, e.g. ion-exchange, ion-pair, ion-suppression or ion-exclusion
B01D 15/38 - Selective adsorption, e.g. chromatography characterised by the separation mechanism involving specific interaction not covered by one or more of groups , e.g. affinity, ligand exchange or chiral chromatography
B01D 15/42 - Selective adsorption, e.g. chromatography characterised by the development mode, e.g. by displacement or by elution
C07K 1/22 - Affinity chromatography or related techniques based upon selective absorption processes
73.
COMBINATION THERAPY OF A PD-1 ANTAGONIST AND LAG3 ANTAGONIST AND ALL-TRANS RETINOIC ACID OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF FOR TREATING PATIENTS WITH CANCER
The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1), a Lymphocyte-Activation Gene 3 (LAG3) antagonist, and all-trans retinoic acid or a pharmaceutically acceptable salt thereof and the use of the combination therapies for the treatment of cancer.
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
Novel compounds of Formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of NLRP3 and may be useful in the treatment, prevention, management, amelioration, control, and suppression of diseases mediated by NLPR3. The compounds of the present invention may be useful in the treatment, prevention or management of diseases, disorders and conditions mediated by NLRP3 such as, but not limited to, obesity, gout, pseudogout, CAPS, NASH, MASH, fibrosis, osteoarthritis, atherosclerosis, heart failure, idiopathic pericarditis, myocarditis, atopic dermatitis, hidradenitis suppurativa, inflammatory bowel disease, cancer, Alzheimer's Disease, Parkinson's Disease, dementia with Lewy bodies (DLB), and traumatic brain injury.
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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 37/06 - Immunosuppressants, e.g. drugs for graft rejection
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
75.
AZAINDAZOLE DERIVATIVES USEFUL AS INHIBITORS OF NOD-LIKE RECEPTOR PROTEIN 3
Novel compounds of Formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of NLRP3 and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by NLPR3. The compounds of the present invention may be useful in the treatment, prevention or management of diseases, disorders and conditions mediated by NLRP3 such as, but not limited to, obesity, gout, pseudogout, CAPS, NASH, MASH, fibrosis, heart failure, idiopathic pericarditis, atopic dermatitis, inflammatory bowel disease, Alzheimer's Disease, Parkinson's Disease, dementia with Lewy bodies (DLB), and traumatic brain injury.
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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 37/06 - Immunosuppressants, e.g. drugs for graft rejection
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
76.
A CYCLIC PEPTIDE IL-1BETA TRAP FOR THE TREATMENT OF ATHEROSCLEROSIS AND INFLAMMATORY DISORDERS
Provided are compounds of the Formula (I), or their pharmaceutically acceptable salts, wherein L1, L2, X1-X3, CPC, A1, A2, and R1-R8 are as herein described. (I) The compounds and their pharmaceutically acceptable salts can trap IL-1β and are expected to have utility as therapeutic agents, for example, for treating cardiovascular disease and inflammatory disorders. The disclosure also provides pharmaceutical compositions which comprise the compounds disclosed herein or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cardiovascular disease and inflammatory disorders and for preparing pharmaceuticals for this purpose.
In some examples, a tubing assembly for an injection device includes a tubing having a first end and a second end, the tubing defining a lumen having a constant inner diameter and a constant outer diameter from the first end to the second end, a first connector coupled to the first end, the first connector having a first enlarged section, a first tapered section and a first narrowed section, and a second connector coupled to the second end, the second connector having a second enlarged section, a second tapered section and a second narrowed section.
A61M 39/08 - TubesStorage means specially adapted therefor
A61M 5/00 - Devices for bringing media into the body in a subcutaneous, intra-vascular or intramuscular wayAccessories therefor, e.g. filling or cleaning devices, arm rests
A61M 5/14 - Infusion devices, e.g. infusing by gravityBlood infusionAccessories therefor
In some examples, a tubing assembly for an injection device includes a tubing having a first end and a second end, the tubing defining a lumen having a constant inner diameter and a constant outer diameter from the first end to the second end, a first connector coupled to the first end, the first connector having a first enlarged section, a first tapered section and a first narrowed section, and a second connector coupled to the second end, the second connector having a second enlarged section, a second tapered section and a second narrowed section.
This invention relates to therapies useful for the treatment of pulmonary arterial hypertension. In particular, the invention relates to a method for treating pulmonary arterial hypertension which comprises administering to a patient in need thereof an ActRIIA-Fc fusion protein or a variant thereof, using the dosage regimens specified herein.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 9/00 - Medicinal preparations characterised by special physical form
A61P 11/00 - Drugs for disorders of the respiratory system
The present invention relates to Compounds of Formula I: and pharmaceutically acceptable salts or prodrug thereof. The present invention also relates to compositions comprising at least one compound of Formula I, and methods of using the compounds of Formula I for treatment or prophylaxis of lysosomal storage diseases, neurodegenerative disease, cystic disease, cancer, or a diseases or disorders associated with elevated levels of glucosylceramide (GlcCer), glucosylsphingosine (GlcSph) and/or other glucosylceramide-based glycosphingolipids (GSLs).
The present invention relates to Compounds of Formula I: and pharmaceutically acceptable salts or prodrug thereof. The present invention also relates to compositions comprising at least one compound of Formula I, and methods of using the compounds of Formula I for treatment or prophylaxis of lysosomal storage diseases, neurodegenerative disease, cystic disease, cancer, or a diseases or disorders associated with elevated levels of glucosylceramide (GlcCer), glucosylsphingosine (GlcSph) and/or other glucosylceramide-based glycosphingolipids (GSLs).
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/527 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
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
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 403/04 - 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 directly linked by a ring-member-to-ring- member bond
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 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 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 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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 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
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
The present disclosure provides methods for the acute treatment of migraine with or without aura, comprising the administration of ubrogepant. In particular, the present disclosure provides methods for the acute treatment of migraine in patients having hepatic impairment; in patients with renal impairment; and in patients concurrently taking CYP3A4 modulators or BCRP and/or P-gp only inhibitors.
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
The present disclosure provides methods for the acute treatment of migraine with or without aura, comprising the administration of ubrogepant. In particular, the present disclosure provides methods for the acute treatment of migraine in patients having hepatic impairment; in patients with renal impairment; and in patients concurrently taking CYP3A4 modulators or BCRP and/or P-gp only inhibitors.
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
The present disclosure relates to methods of treating metastatic non-small cell lung cancer in a patient, said methods comprising administering to the patient: (a) an anti-human PD-1 antibody or antigen binding fragment thereof; and (b) an Immunoconjugate of Formula (I) wherein: Ab is an antibody that binds to Trop-2; and n is an integer from 1 to 10.
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 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
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
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 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
84.
PHARMACEUTICAL COMBINATIONS AND METHODS OF USE OF AMINO-PYRROLOPYRIMIDINONE COMPOUND
The application relates to a pharmaceutical combination or combinational therapy comprising a therapeutically effective amount of the compound of Formula (I), or a pharmaceutically acceptable salt thereof, and at least one second agent, or a pharmaceutically acceptable salt thereof, for use in the treatment of a BTK-mediated disease or disorder.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/635 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide having a heterocyclic ring, e.g. sulfadiazine
A61P 35/02 - Antineoplastic agents specific for leukemia
85.
ADENOSINE RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE THEREOF
In its many embodiments, the invention provides compounds of structural Formula (I): (I), and pharmaceutically acceptable salts thereof, wherein, ring A, R1, R2 and R3 are as defined herein, and pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents). The invention further provides methods for the preparation and use of the compounds of the invention, or a pharmaceutically acceptable salt thereof, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.
In its many embodiments, the invention provides compounds of structural Formula (I): (I), and pharmaceutically acceptable salts thereof, wherein, ring A, R1, R2 and R3 are as defined herein, and pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents). The invention further provides methods for the preparation and use of the compounds of the invention, or a pharmaceutically acceptable salt thereof, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
86.
FUSED PYRAZOLE AMIDE ANALOGS AS GLUCOSYLCERAMIDE SYNTHASE INHIBITORS
The present invention relates to Compounds of Formula I: and pharmaceutically acceptable salts or prodrug thereof. The present invention also relates to compositions comprising at least one compound of Formula I, and methods of using the compounds of Formula I for treatment or prophylaxis of lysosomal storage diseases, neurodegenerative disease, cystic disease, cancer, or a diseases or disorders associated with elevated levels of glucosylceramide (GlcCer), glucosylsphingosine (GlcSph) and/or other glucosylceramide-based glycosphingolipids (GSLs).
The present invention relates to Compounds of Formula I: and pharmaceutically acceptable salts or prodrug thereof. The present invention also relates to compositions comprising at least one compound of Formula I, and methods of using the compounds of Formula I for treatment or prophylaxis of lysosomal storage diseases, neurodegenerative disease, cystic disease, cancer, or a diseases or disorders associated with elevated levels of glucosylceramide (GlcCer), glucosylsphingosine (GlcSph) and/or other glucosylceramide-based glycosphingolipids (GSLs).
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
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of bone, cardiovascular, central nervous system, dermatological, endocrine, hematological, hepatological, immunological, gastrointestinal, genitourinary, gynecological, metabolic, musculoskeletal, nephrological, neurological, oncological, ophthalmic, psychiatric, pulmonary, renal, respiratory, and urological diseases and disorders; Pharmaceutical preparations for the treatment and prevention of autoimmune diseases, asthma, cancer and tumors, chronic cough, diabetes, hypertension, insomnia, intestinal infections, skin disorders, and urinary incontinence; Inhalers filled with pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; Antibacterial pharmaceuticals; Antibiotics; Antifungal preparations; Anti-infectives; Anti-inflammatories; Antiparasitics; Antivirals; Human vaccine preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of bone, cardiovascular, central nervous system, dermatological, endocrine, hematological, hepatological, immunological, gastrointestinal, genitourinary, gynecological, metabolic, musculoskeletal, nephrological, neurological, oncological, ophthalmic, psychiatric, pulmonary, renal, respiratory, and urological diseases and disorders; Pharmaceutical preparations for the treatment and prevention of autoimmune diseases, asthma, cancer and tumors, chronic cough, diabetes, hypertension, insomnia, intestinal infections, skin disorders, and urinary incontinence; Inhalers filled with pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; Antibacterial pharmaceuticals; Antibiotics; Antifungal preparations; Anti-infectives; Anti-inflammatories; Antiparasitics; Antivirals; Human vaccine preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of bone, cardiovascular, central nervous system, dermatological, endocrine, hematological, hepatological, immunological, gastrointestinal, genitourinary, gynecological, metabolic, musculoskeletal, nephrological, neurological, oncological, ophthalmic, psychiatric, pulmonary, renal, respiratory, and urological diseases and disorders; Pharmaceutical preparations for the treatment and prevention of autoimmune diseases, asthma, cancer and tumors, chronic cough, diabetes, hypertension, insomnia, intestinal infections, skin disorders, and urinary incontinence; Inhalers filled with pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; Antibacterial pharmaceuticals; Antibiotics; Antifungal preparations; Anti-infectives; Anti-inflammatories; Antiparasitics; Antivirals; Human vaccine preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of bone, cardiovascular, central nervous system, dermatological, endocrine, hematological, hepatological, immunological, gastrointestinal, genitourinary, gynecological, metabolic, musculoskeletal, nephrological, neurological, oncological, ophthalmic, psychiatric, pulmonary, renal, respiratory, and urological diseases and disorders; Pharmaceutical preparations for the treatment and prevention of autoimmune diseases, asthma, cancer and tumors, chronic cough, diabetes, hypertension, insomnia, intestinal infections, skin disorders, and urinary incontinence; Inhalers filled with pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; Antibacterial pharmaceuticals; Antibiotics; Antifungal preparations; Anti-infectives; Anti-inflammatories; Antiparasitics; Antivirals; Human vaccine preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of bone, cardiovascular, central nervous system, dermatological, endocrine, hematological, hepatological, immunological, gastrointestinal, genitourinary, gynecological, metabolic, musculoskeletal, nephrological, neurological, oncological, ophthalmic, psychiatric, pulmonary, renal, respiratory, and urological diseases and disorders; Pharmaceutical preparations for the treatment and prevention of autoimmune diseases, asthma, cancer and tumors, chronic cough, diabetes, hypertension, insomnia, intestinal infections, skin disorders, and urinary incontinence; Inhalers filled with pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; Antibacterial pharmaceuticals; Antibiotics; Antifungal preparations; Anti-infectives; Anti-inflammatories; Antiparasitics; Antivirals; Human vaccine preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of bone, cardiovascular, central nervous system, dermatological, endocrine, hematological, hepatological, immunological, gastrointestinal, genitourinary, gynecological, metabolic, musculoskeletal, nephrological, neurological, oncological, ophthalmic, psychiatric, pulmonary, renal, respiratory, and urological diseases and disorders; Pharmaceutical preparations for the treatment and prevention of autoimmune diseases, asthma, cancer and tumors, chronic cough, diabetes, hypertension, insomnia, intestinal infections, skin disorders, and urinary incontinence; Inhalers filled with pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; Antibacterial pharmaceuticals; Antibiotics; Antifungal preparations; Anti-infectives; Anti-inflammatories; Antiparasitics; Antivirals; Human vaccine preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of bone, cardiovascular, central nervous system, dermatological, endocrine, hematological, hepatological, immunological, gastrointestinal, genitourinary, gynecological, metabolic, musculoskeletal, nephrological, neurological, oncological, ophthalmic, psychiatric, pulmonary, renal, respiratory, and urological diseases and disorders; Pharmaceutical preparations for the treatment and prevention of autoimmune diseases, asthma, cancer and tumors, chronic cough, diabetes, hypertension, insomnia, intestinal infections, skin disorders, and urinary incontinence; Inhalers filled with pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; Antibacterial pharmaceuticals; Antibiotics; Antifungal preparations; Anti-infectives; Anti-inflammatories; Antiparasitics; Antivirals; Human vaccine preparations
94.
PEPTIDE CONJUGATE VACCINE COMPOSITIONS AND METHODS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
The invention provides compositions and methods for the treatment of diseases associated with amyloid deposits of Aβ in the brain of a patient, such as Alzheimer's Disease. Such methods entail administering a pharmaceutical composition comprising an immunogenic fragment of Aβ capable of inducing a beneficial immune response in the form of antibodies to Aβ. The immunogenic fragments comprise linear or multivalent peptides of Aβ. Pharmaceutical compositions comprise the immunogenic fragment chemically linked to a carrier molecule which may be administered with an adjuvant.
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/385 - Haptens or antigens, bound to carriers
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
95.
CLOGGING PREVENTION OF NEEDLE-BASED DELIVERY DEVICES
An injection device includes a reservoir for containing a medicament, a needle having a needle fluid path in communication with the reservoir and configured to deliver the medicament to a patient's body at a needle tip, and an anti-clogging substance disposed within the needle fluid path, the anti-clogging substance being configured and arranged to form a fluid barrier between the medicament and the needle tip.
B05D 7/22 - Processes, other than flocking, specially adapted for applying liquids or other fluent materials to particular surfaces or for applying particular liquids or other fluent materials to internal surfaces, e.g. of tubes
C23C 16/44 - Chemical coating by decomposition of gaseous compounds, without leaving reaction products of surface material in the coating, i.e. chemical vapour deposition [CVD] processes characterised by the method of coating
96.
PYRROLIDINYL DERIVATIVES USEFUL AS HCN1/HCN 2 MODULATORS
The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of, pain, such as, inflammatory and/or neuropathic pain, central nervous system (CNS) and psychiatric disorders, mood disorders, and tinnitus, and for preparing pharmaceuticals for this purpose.
The present disclosure provides isolated antibodies that specifically bind to human Nectin-4, antigen-binding fragments of such antibodies, and kits comprising the anti-Nectin-4 antibodies or binding fragments and a set of reagents for detecting a complex of the antibody or antigen-binding fragment thereof bound to human Nectin-4. The antibodies and antigen-binding fragments of this disclosure are useful for detection of human Nectin-4 expression in tissue samples and for treating cancer in a subject. Nucleic acid molecules encoding the antibodies and antigen-binding fragments of this disclosure, expression vectors, and host cells for expressing the antibodies and antigen-binding fragments are also provided.
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
G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
Described herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. The compounds of Formula (I) act as RIPK1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for RIPK1-related diseases.
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
Provided are compounds of the Formula (I), or their pharmaceutically acceptable salts, wherein X1, X2, X3, R1-R9, RA, RB, RD, A1, A2, and subscripts t and w are as herein described. Formula (I),(I). The compounds and their pharmaceutically acceptable salts can trap IL-1β and are expected to have utility as therapeutic agents, for example, for treating cardiovascular disease and inflammatory disorders. The disclosure also provides pharmaceutical compositions which comprise the compounds disclosed herein or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cardiovascular disease and inflammatory disorders and for preparing pharmaceuticals for this purpose.
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
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
C07K 7/64 - Cyclic peptides containing only normal peptide links
The invention provides compositions and methods for the treatment of diseases associated with amyloid deposits of Aβ in the brain of a patient, such as Alzheimer's Disease. Such methods entail administering a pharmaceutical composition comprising an immunogenic fragment of Aβ capable of inducing a beneficial immune response in the form of antibodies to Aβ. The immunogenic fragments comprise linear or multivalent peptides of Aβ. Pharmaceutical compositions comprise the immunogenic fragment chemically linked to a carrier molecule which may be administered with an adjuvant.
A61K 39/00 - Medicinal preparations containing antigens or antibodies
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
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
