Abrégé

The present invention provides novel SMNDC1 inhibitors, specifically the compounds of formula (I), (I) as well as pharmaceutical compositions containing these compounds. The SMNDC1 inhibitors provided herein exhibit particularly beneficial properties in terms of potency and selectivity, which renders these compounds highly advantageous for use in therapy, including, e.g., in the treatment or prevention of cancer or diabetes.

Classes IPC  ?

• A61K 31/4436 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle
• C07D 417/04 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
• C07D 277/46 - Radicaux amino ou imino acylés par les acides carboxyliques ou par leurs analogues du soufre ou de l'azote
• C07D 417/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
• C07D 487/04 - Systèmes condensés en ortho
• C07D 491/10 - Systèmes condensés en spiro
• C07K 5/097 - Tripeptides le premier amino-acide étant hétérocyclique, p. ex. Pro, His, Trp, p. ex. thyrolibérine, mélanostatine
• A61P 5/50 - Médicaments pour le traitement des troubles du système endocrinien des hormones pancréatiques pour augmenter ou potentialiser l'activité de l'insuline
• A61P 35/00 - Agents anticancéreux

Abrégé

The present invention relates to compounds of the formula (I) as bifunctional protein targeting chimeras (PROTACs), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. These compounds, pharmaceutically acceptable salts, and pharmaceutical compositions thereof are useful in the treatment or prophylaxis of a cancer, an autoimmune disease, or an inflammatory disease, in paticular, associated with and/or caused by PDEdelta (PDEδ) / K-Ras or B lymphoid kinase (BLK) /Bruton´s tyrosine kinase (BTK) or cyclin-dependent kinase 9 (CDK9).

Classes IPC  ?

• C07D 487/04 - Systèmes condensés en ortho
• C07D 401/12 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
• C07D 417/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
• A61P 35/00 - Agents anticancéreux
• A61K 31/5025 - PyridazinesPyridazines hydrogénées condensées en ortho ou en péri avec des systèmes hétérocycliques

Abrégé

The invention relates to a method for sequencing oligonucleotides comprising RNA, wherein two indexing sequences are introduced in RNA oligonucleotides. The invention furthermore relates to uses of such methods and devices used for such methods. Further provided are kits comprising one or more components used in the methods of the invention.

Classes IPC  ?

• C12Q 1/6869 - Méthodes de séquençage

Abrégé

The present invention provides 1,2,4-triazolo[1,5-a]pyrimidine-based compounds of formula (I), Formula (I) and pharmaceutically acceptable salts thereof, which have been found to be advantageously potent and selective inhibitors of SLC16A3, as well as their use in the treatment or prevention of SLC16A3-associated diseases/disorders such as cancer.

Classes IPC  ?

• C07D 487/04 - Systèmes condensés en ortho
• A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
• A61K 31/55 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole
• A61P 35/00 - Agents anticancéreux

Abrégé

in vitro in vivo inviroviro, e.g., for adoptive cell transfer. Combinations of a RHOG modulator according to the invention and synthetic antigen receptors such as CARs are also encompassed by the present invention. Furthermore, the present invention provides specific CRISPR gRNAs and specific combinations of CRISPR gRNAs and CRISPR modifiers.

Classes IPC  ?

• A61K 35/17 - LymphocytesLymphocytes BLymphocytes TCellules tueuses naturellesLymphocytes activés par un interféron ou une cytokine

Abrégé

The present invention relates to a method for monitoring the effect of an environmental factor on the proteome of a cell. Furthermore, cell populations are provided that comprise multiple cells each comprising an inserted tag sequence in an intron of said cell, wherein the tag is inserted in-frame with the preceding exonic sequence and wherein the intron into which the tag is inserted is different between cells.

Classes IPC  ?

• C12Q 1/6897 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques faisant intervenir des gènes rapporteurs liés de façon fonctionnelle à des promoteurs
• C12N 15/10 - Procédés pour l'isolement, la préparation ou la purification d'ADN ou d'ARN
• G01N 33/50 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique

Abrégé

The present invention relates to a compound of formula (I) or its pharmaceutically acceptable salt. The present invention further relates to a pharmaceutical composition comprising the compound of formula (I) or its pharmaceutically acceptable salt, and at least one pharmaceutically acceptable carrier. The compounds of formula (I) are useful as medicaments, for use in treatment or prevention of an autoimmune disorder or inflammatory condition, in particular an autoimmune disorder being systemic lupus erythematosus, or an inflammatory condition selected from inflammatory bowel disease, psoriasiform dermatitis, and endosomal TLR-dependent inflammation. Preferably, the autoimmune disorder to be treated with the compound of formula (I) is a disorder associated with SLC15 peptide transporter. The compound of formula (I) has been demonstrated to inhibit SLC15 peptide transporter.

Classes IPC  ?

• A61P 37/02 - Immunomodulateurs
• A61K 31/4709 - Quinoléines non condensées contenant d'autres hétérocycles
• C07D 215/16 - Composés hétérocycliques contenant les systèmes cycliques de la quinoléine ou de la quinoléine hydrogénée ne comportant pas de liaison entre l'atome d'azote du cycle et un chaînon non cyclique ou ne comportant que des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
• C07D 401/12 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
• C07D 401/14 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant au moins trois hétérocycles

Abrégé

The present invention relates to an antibody, or an antigen-binding fragment thereof, specifically binding to APRIL for use in the prevention and/or treatment of hypertriglyceridemia, metabolic syndrome, non-alcoholic steatohepatitis, diabetes mellitus type 2, abdominal aortic aneurysm, atherogenic dyslipidemia, cardiovascular events (e.g., myocardial infarction and stroke) and/or atherosclerosis. The invention further relates to a polynucleotide that encodes and/or a pharmaceutical composition that comprises the antibody or an antigen-binding fragment of the invention. The invention also relates to a kit and/or method for quantifying the concentration of nc-APRIL, canonical APRIL or total APRIL in a sample. Further, the invention relates to a nephelometric assay for quantifying nc-APRIL. Further, the invention relates to a method for predicting mortality risk in subjects suffering from, and/or for determining whether a subject is susceptible to the treatment of hypertriglyceridemia, metabolic syndrome, abdominal aortic aneurysm, non-alcoholic steatohepatitis, diabetes mellitus type 2, atherogenic dyslipidemia, cardiovascular events and/or atherosclerosis.

Classes IPC  ?

• C07K 16/28 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire
• A61P 3/06 - Antihyperlipémiants
• G01N 33/543 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet avec un support insoluble pour l'immobilisation de composés immunochimiques
• G01N 33/68 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique faisant intervenir des protéines, peptides ou amino-acides

Abrégé

The present invention relates to compounds of formula compounds of formulae (I) by which transmembrane proteins such as SLC transporters can be unlocked to chemically-induced degradation, whereby a multitude of diseases can be addressed for the first time. Particularly, the present invention relates to compounds with the ability to induce degradation of SLC transporters via the ubiquitin-proteasome pathway. The invention also relates to the compounds and composition for use as medicaments as well as pharmaceutical compositions comprising these compounds, particularly for use as degraders of SLC transporters which are, e.g., associated with cancer and for use in the treatment of various diseases such as cancer. Furthermore, the present invention relates to a method for treating a disease or condition, such as cancer, comprising administering the compound of the present invention.

Classes IPC  ?

• A61K 47/55 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p. ex. les supports ou les additifs inertesAgents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p. ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un composé organique l’agent de modification étant aussi un agent pharmacologiquement ou thérapeutiquement actif, c.-à-d. le conjugué entier étant un co-médicament, p. ex. un dimère, un oligomère ou un polymère de composés pharmacologiquement ou thérapeutiquement actifs
• A61K 47/54 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p. ex. les supports ou les additifs inertesAgents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p. ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un composé organique
• A61P 35/02 - Agents anticancéreux spécifiques pour le traitement de la leucémie

Abrégé

The present invention relates to a method for obtaining an intron-tagged pool of cells representing and/or comprising tagged introns. Furthermore, the present invention relates to a pool of cells that may be obtainable by said method, in particular an intron-tagged pool of cells. The present invention furthermore provides for a method for automated recognition of the identity of the tagged intron(s) comprised in the genome of an intron- tagged cell within an intron-tagged pool of cells and a method for assessing the effect of a perturbation on the proteome and/or gene expression levels of an intron-tagged cell within an intron-tagged pool of cells.

Classes IPC  ?

• C12N 9/22 - Ribonucléases
• C12N 15/113 - Acides nucléiques non codants modulant l'expression des gènes, p. ex. oligonucléotides anti-sens
• C12N 15/10 - Procédés pour l'isolement, la préparation ou la purification d'ADN ou d'ARN
• C12Q 1/6897 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques faisant intervenir des gènes rapporteurs liés de façon fonctionnelle à des promoteurs

Abrégé

The present invention provides 1,2,4-triazolo[1,5-a]pyrimidine-based compounds of formula (I), Formula (I) and pharmaceutically acceptable salts thereof, which have been found to be advantageously potent and selective inhibitors of SLC16A3, as well as their use in the treatment or prevention of SLC16A3-associated diseases/disorders such as cancer.

Classes IPC  ?

• A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
• A61P 35/00 - Agents anticancéreux
• C07D 487/00 - Composés hétérocycliques contenant des atomes d'azote comme uniques hétéro-atomes dans le système condensé, non prévus par les groupes
• C07D 487/04 - Systèmes condensés en ortho

Abrégé

The present invention provides 3-(phthalazin-1-yl)benzenesulfonamide-based compounds of formula (I), Formula (I) and pharmaceutically acceptable salts thereof, which have been found to be advantageously potent and selective inhibitors of SLC16A3, as well as their use in the treatment or prevention of SLC16A3-associated diseases/disorders such as cancer.

Classes IPC  ?

• A61K 31/502 - PyridazinesPyridazines hydrogénées condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. cinnoline, phtalazine
• A61K 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
• A61P 9/00 - Médicaments pour le traitement des troubles du système cardiovasculaire
• A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p. ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
• A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
• A61P 35/00 - Agents anticancéreux
• A61P 43/00 - Médicaments pour des utilisations spécifiques, non prévus dans les groupes

Abrégé

The present invention relates to a method for diagnosing myeloid malignancy comprising determining the presence of a mutant allele of the calreticulin gene. Also genomic sequences, cDNA sequences, mRNA sequences and protein sequences of the mutant calreticulin are subject of the present invention. Further, the invention relates to medical uses of inhibitors of mutant calreticulin.

Classes IPC  ?

• C12Q 1/6886 - Produits d’acides nucléiques utilisés dans l’analyse d’acides nucléiques, p. ex. amorces ou sondes pour les maladies provoquées par des altérations du matériel génétique pour le cancer
• G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer
• A61K 39/00 - Préparations médicinales contenant des antigènes ou des anticorps
• C07K 14/47 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains provenant de vertébrés provenant de mammifères
• C07K 16/18 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains
• C12N 15/113 - Acides nucléiques non codants modulant l'expression des gènes, p. ex. oligonucléotides anti-sens

Abrégé

The present invention relates to an antibody, or an antigen-binding fragment thereof, specifically binding to APRIL for use in the prevention and/or treatment of hypertriglyceridemia, metabolic syndrome, non-alcoholic steatohepatitis, diabetes mellitus type 2, abdominal aortic aneurysm, atherogenic dyslipidemia, cardiovascular events (e.g., myocardial infarction and stroke) and/or atherosclerosis. The invention further relates to a polynucleotide that encodes and/or a pharmaceutical composition that comprises the antibody or an antigen-binding fragment of the invention. The invention also relates to a kit and/or method for quantifying the concentration of nc-APRIL, canonical APRIL or total APRIL in a sample. Further, the invention relates to a nephelometric assay for quantifying nc-APRIL. Further, the invention relates to a method for predicting mortality risk in subjects suffering from, and/or for determining whether a subject is susceptible to the treatment of hypertriglyceridemia, metabolic syndrome, abdominal aortic aneurysm, non- alcoholic steatohepatitis, diabetes mellitus type 2, atherogenic dyslipidemia, cardiovascular events and/or atherosclerosis.

Classes IPC  ?

• C07K 16/28 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire
• A61P 3/06 - Antihyperlipémiants

Abrégé

The present invention relates to an antibody, or an antigen-binding fragment thereof, specifically binding to APRIL for use in the prevention and/or treatment of hypertriglyceridemia, metabolic syndrome, non-alcoholic steatohepatitis, diabetes mellitus type 2, abdominal aortic aneurysm, atherogenic dyslipidemia, cardiovascular events (e.g., myocardial infarction and stroke) and/or atherosclerosis. The invention further relates to a polynucleotide that encodes and/or a pharmaceutical composition that comprises the antibody or an antigen-binding fragment of the invention. The invention also relates to a kit and/or method for quantifying the concentration of nc-APRIL, canonical APRIL or total APRIL in a sample. Further, the invention relates to a nephelometric assay for quantifying nc-APRIL. Further, the invention relates to a method for predicting mortality risk in subjects suffering from, and/or for determining whether a subject is susceptible to the treatment of hypertriglyceridemia, metabolic syndrome, abdominal aortic aneurysm, non- alcoholic steatohepatitis, diabetes mellitus type 2, atherogenic dyslipidemia, cardiovascular events and/or atherosclerosis.

Classes IPC  ?

• C07K 16/28 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire
• A61P 3/06 - Antihyperlipémiants
• G01N 33/68 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique faisant intervenir des protéines, peptides ou amino-acides

Abrégé

The present invention relates to compounds with the ability to stimulate/induce ubiquitination of a target protein/target proteins. The compounds of the present invention may stimulate/induce ubiquitination of a target protein/target proteins; i.e. via degradation of a target protein/target proteins by the cullin-RING ubiquitin ligase (CRL). Such target protein/ target proteins may be proteins involved in diseases, like cancer, metabolic disorder, infectious disease and/or neurological disorder. The invention also relates to the compounds and composition for use as medicaments as well as pharmaceutical compositions comprising these compounds. Particularly, the compounds of the present invention may degrade proteins associated with cancer, metabolic disorder, infectious disease and/or neurological disorder. Furthermore, the present invention relates the compounds for use as a medicament, such as for use in treating cancer, metabolic disorder, infectious disease and/or neurological disorder and to a method for treating a disease, such as cancer, metabolic disorder, infectious disease and/or neurological disorder, comprising administering the compound of the present invention.

Classes IPC  ?

• C07D 213/74 - Radicaux amino ou imino substitués par des radicaux hydrocarbonés ou par des radicaux hydrocarbonés substitués
• C07D 213/75 - Radicaux amino ou imino, acylés par un acide carboxylique, par l'acide carbonique ou par leurs analogues du soufre ou de l'azote, p. ex. des carbamates
• C07D 277/46 - Radicaux amino ou imino acylés par les acides carboxyliques ou par leurs analogues du soufre ou de l'azote
• C07D 401/12 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
• C07D 403/12 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
• C07D 405/12 - Composés hétérocycliques contenant à la fois un ou plusieurs hétérocycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle et un ou plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
• C07D 417/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
• C07D 471/04 - Systèmes condensés en ortho
• C07D 513/04 - Systèmes condensés en ortho
• A61P 3/00 - Médicaments pour le traitement des troubles du métabolisme
• A61P 25/00 - Médicaments pour le traitement des troubles du système nerveux
• A61P 31/00 - Agents anti-infectieux, c.-à-d. antibiotiques, antiseptiques, chimiothérapeutiques
• A61P 35/00 - Agents anticancéreux
• A61K 31/4155 - 1,2-Diazoles non condensés et contenant d'autres hétérocycles
• A61K 31/427 - Thiazoles non condensés et contenant d'autres hétérocycles

Abrégé

A computer-implemented method for semi-automatic segmentation of medical imaging data, the method comprising steps of a) obtaining from the medical imaging data a sequence of slices in which at least one anatomical structure appears; b) for each of the slices, performing a thresholding to identify a plurality of anatomical structure pixels and delineating an initial contour of the anatomical structures, thereby defining a plurality of anatomical structure regions; c) interactively selecting a reference slice in which the anatomical structure regions sufficiently correspond to the anatomical structures appearing therein and/or interactively refining the reference slice by modifying at least one of the anatomical structure regions so that the at least one modified organ region corresponds more closely to the respective anatomical structure; and d) correcting the definition of the anatomical structure regions of at least one of the remaining slices based on information acquired for the reference slice.

Classes IPC  ?

• G06T 7/11 - Découpage basé sur les zones
• G06T 7/136 - DécoupageDétection de bords impliquant un seuillage
• G06T 7/155 - DécoupageDétection de bords impliquant des opérateurs morphologiques

Abrégé

The present invention relates to a method for monitoring the effect of an environmental factor on the proteome of a cell. Furthermore, cell populations are provided that comprise multiple cells each comprising an inserted tag sequence in an intron of said cell, wherein the tag is inserted in-frame with the preceding exonic sequence and wherein the intron into which the tag is inserted is different between cells.

Classes IPC  ?

• C12Q 1/6806 - Préparation d’acides nucléiques pour analyse, p. ex. pour test de réaction en chaîne par polymérase [PCR]
• C12N 15/10 - Procédés pour l'isolement, la préparation ou la purification d'ADN ou d'ARN
• C12Q 1/6897 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques faisant intervenir des gènes rapporteurs liés de façon fonctionnelle à des promoteurs

Abrégé

The present invention relates to compounds with the ability to stimulate/induce ubiquitination of a target protein/target proteins. The compounds of the present invention may stimulate/induce ubiquitination of a target protein/target proteins; i.e. via degradation of a target protein/target proteins by the cullin-RING ubiquitin ligase (CRL). Such target protein/ target proteins may be proteins involved in diseases, like cancer, metabolic disorder, infectious disease and/or neurological disorder. The invention further relates to a method for identifying/obtaining and/or testing a compound able to induce ubiquitination of a target protein/target proteins. The invention also relates to the compounds and composition for use as medicaments as well as pharmaceutical compositions comprising these compounds. Particularly, the compounds of the present invention may degrade proteins associated with cancer, metabolic disorder, infectious disease and/or neurological disorder. Furthermore, the present invention relates the compounds for use as a medicament, such as for use in treating cancer, metabolic disorder, infectious disease and/or neurological disorder and to a method for treating a disease, such as cancer, metabolic disorder, infectious disease and/or neurological disorder, comprising administering the compound of the present invention.

Classes IPC  ?

• A61P 35/00 - Agents anticancéreux
• C07D 487/04 - Systèmes condensés en ortho
• A61K 31/53 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec trois azote comme seuls hétéro-atomes d'un cycle, p. ex. chlorazanil, mélamine

Abrégé

The present invention relates to compounds of formula compounds of formulae (I) by which transmembrane proteins such as SLC transporters can be unlocked to chemically-induced degradation, whereby a multitude of diseases can be addressed for the first time. Particularly, the present invention relates to compounds with the ability to induce degradation of SLC transporters via the ubiquitin-proteasome pathway. The invention also relates to the compounds and composition for use as medicaments as well as pharmaceutical compositions comprising these compounds, particularly for use as degraders of SLC transporters which are, e.g., associated with cancer and for use in the treatment of various diseases such as cancer. Furthermore, the present invention relates to a method for treating a disease or condition, such as cancer, comprising administering the compound of the present invention.

Classes IPC  ?

• C07D 401/14 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant au moins trois hétérocycles
• A61K 31/4545 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un cycle à six chaînons avec l'azote comme hétéro-atome du cycle, p. ex. pipampérone, anabasine
• A61P 35/00 - Agents anticancéreux

Abrégé

The present invention relates to compounds of formula compounds of formulae (I) by which transmembrane proteins such as SLC transporters can be unlocked to chemically-induced degradation, whereby a multitude of diseases can be addressed for the first time. Particularly, the present invention relates to compounds with the ability to induce degradation of SLC transporters via the ubiquitin-proteasome pathway. The invention also relates to the compounds and composition for use as medicaments as well as pharmaceutical compositions comprising these compounds, particularly for use as degraders of SLC transporters which are, e.g., associated with cancer and for use in the treatment of various diseases such as cancer. Furthermore, the present invention relates to a method for treating a disease or condition, such as cancer, comprising administering the compound of the present invention.

Classes IPC  ?

• C07D 401/14 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant au moins trois hétérocycles
• A61K 47/54 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p. ex. les supports ou les additifs inertesAgents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p. ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un composé organique
• A61K 31/4545 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un cycle à six chaînons avec l'azote comme hétéro-atome du cycle, p. ex. pipampérone, anabasine
• A61P 35/00 - Agents anticancéreux
• A61P 35/02 - Agents anticancéreux spécifiques pour le traitement de la leucémie

Abrégé

The present invention relates to compounds with the ability to stimulate/induce ubiquitination of a target protein/target proteins. The compounds of the present invention may stimulate/induce ubiquitination of a target protein/target proteins; i.e. via degradation of a target protein/target proteins by the cullin-RING ubiquitin ligase (CRL). Such target protein/target proteins may be proteins involved in diseases, like cancer, metabolic disorder, infectious disease and/or neurological disorder. The invention further relates to a method for identifying/obtaining and/or testing a compound able to induce ubiquitination of a target protein/target proteins. The invention also relates to the compounds and composition for use as medicaments as well as pharmaceutical compositions comprising these compounds. Particularly, the compounds of the present invention may degrade proteins associated with cancer, metabolic disorder, infectious disease and/or neurological disorder. Furthermore, the present invention relates the compounds for use as a medicament, such as for use in treating cancer, metabolic disorder, infectious disease and/or neurological disorder and to a method for treating a disease, such as cancer, metabolic disorder, infectious disease and/or neurological disorder, comprising administering the compound of the present invention.

Classes IPC  ?

• A61P 3/00 - Médicaments pour le traitement des troubles du métabolisme
• A61K 31/4184 - 1,3-Diazoles condensés avec des carbocycles, p. ex. benzimidazoles
• A61K 31/427 - Thiazoles non condensés et contenant d'autres hétérocycles
• A61K 31/53 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec trois azote comme seuls hétéro-atomes d'un cycle, p. ex. chlorazanil, mélamine
• A61P 25/00 - Médicaments pour le traitement des troubles du système nerveux
• A61P 31/00 - Agents anti-infectieux, c.-à-d. antibiotiques, antiseptiques, chimiothérapeutiques
• A61P 35/00 - Agents anticancéreux
• C07D 401/12 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
• C07D 411/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'oxygène et de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
• C07D 411/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'oxygène et de soufre comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
• C07D 487/06 - Systèmes condensés en péri

Abrégé

The invention relates to a method for sequencing oligonucleotides comprising RNA, wherein two indexing sequences are introduced in RNA oligonucleotides. The invention furthermore relates to uses of such methods and devices used for such methods. Further provided are kits comprising one or more components used in the methods of the invention.

Classes IPC  ?

• C12Q 1/6869 - Méthodes de séquençage
• C12Q 1/6806 - Préparation d’acides nucléiques pour analyse, p. ex. pour test de réaction en chaîne par polymérase [PCR]

Abrégé

The invention relates to a method for sequencing oligonucleotides comprising RNA, wherein two indexing sequences are introduced in RNA oligonucleotides. The invention furthermore relates to uses of such methods and devices used for such methods. Further provided are kits comprising one or more components used in the methods of the invention.

Classes IPC  ?

• C12Q 1/6806 - Préparation d’acides nucléiques pour analyse, p. ex. pour test de réaction en chaîne par polymérase [PCR]
• C12Q 1/6869 - Méthodes de séquençage

Produits et services

Data networks; Virtual reality software for education; Virtual reality software; Artificial intelligence apparatus; Virtual reality software for medical teaching; Virtual reality software for playing virtual reality games; Audiovisual teaching apparatus; Artificial intelligence software for healthcare; Virtual reality glasses; Virtual reality models; Databases; Artificial intelligence software; Virtual reality games software; Data engines.; Virtual reality headsets; Virtual reality goggles; Virtual reality hardware. Development services relating to virtual reality software; Development of virtual reality software; Medical and pharmacological research services; Advisory services relating to technological research.; Science and technology services; Data mining; Research and development services in the field of gene expression systems; Design and development of computer game software and virtual reality software; Laboratory research in the field of gene expression; Design of virtual reality software; Genetic research; Genetic fingerprinting; Design and development of virtual reality software. RNA or DNA analysis for cancer diagnosis and prognosis; Pharmaceutical services; Medical services; Medical analysis for the diagnosis and treatment of persons.; Consultancy and information services relating to biopharmaceutical products; Human healthcare services; Provision of pharmaceutical information; Consultancy and information services provided via the Internet relating to pharmaceutical products; Providing health information; Genetic counseling; Professional consultancy relating to health; Health care consultancy services [medical]; Health advice and information services; Consultancy and information services relating to pharmaceutical products; Performing diagnosis of diseases; Health screening; Pharmaceutical advice; Medical testing services relating to the diagnosis and treatment of disease.

Abrégé

The present invention relates to a method for identifying compounds or agents able to induce ubiquitination of a protein of interest. Further, the present invention relates to compounds/agents obtainable by the method of the present invention. Furthermore, the present invention relates to a method for treating cancer or other diseases comprising administering the chemical compound or agent obtainable by the method of the present invention. Moreover, the present invention relates to a eukaryotic cell comprising enhanced cullin-RING ubiquitin ligase (CRL) activity and/or constantly neddylated cullin-RING ubiquitin ligases/CRLs.

Classes IPC  ?

• G01N 33/50 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique

Abrégé

The present invention relates to a method for diagnosing myeloid malignancy comprising determining the presence of a mutant allele of the calreticulin gene. Also genomic sequences, cDNA sequences, mRNA sequences and protein sequences of the mutant calreticulin are subject of the present invention. Further, the invention relates to medical uses of inhibitors of mutant calreticulin.

Classes IPC  ?

• C12Q 1/6886 - Produits d’acides nucléiques utilisés dans l’analyse d’acides nucléiques, p. ex. amorces ou sondes pour les maladies provoquées par des altérations du matériel génétique pour le cancer
• G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer
• A61K 39/00 - Préparations médicinales contenant des antigènes ou des anticorps
• C07K 14/47 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains provenant de vertébrés provenant de mammifères
• C07K 16/18 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains
• C12N 15/113 - Acides nucléiques non codants modulant l'expression des gènes, p. ex. oligonucléotides anti-sens

Produits et services

Chemical preparations for use in RNA analysis and/or DNA analysis [other than medical]; Reagents for use in scientific apparatus for chemical or biological analysis; Biomolecule labelling kits comprising reagents for use in scientific research; Chemicals for use in immuno-assay testing [other than medical or veterinary]; ln-vivo diagnostic reagents for scientific use; Diagnostic testing materials, other than for medical use; Diagnostic preparations, other than for medical or veterinary purposes; Diagnostic reagents, other than for medical laboratory use; Diagnostic reagents, except for medical or veterinary use; Diagnostic reagents for in-vitro use [other than medical]; Diagnostic chemicals [other than for medical or veterinary use]; Clinical diagnostics, other than for medical or veterinary use; Diagnostic reagents and preparations, except for medical or veterinary use; Diagnostic reagents, other than for medical use for sale in kit form; Diagnostic reagents for in vitro use in biochemistry, clinical chemistry and microbiology; Diagnostic preparations for scientific or research use other than for medical use; Reagents for use in diagnostic tests [other than for medical or veterinary purposes]; Chemical reagents for use in diagnostic tests, other than for medical or veterinary use; Diagnostic substances, other than for medical use; Diagnostic reagents for scientific or research use; Diagnostic preparations for scientific or research use; Biochemicals, namely biochemicals for industrial and scientific purposes, in particular biochemicals for industrial and scientific purposes for the investigation of cells, chromatin, proteins, nucleic acids, in particular of RNA and/or DNA, protein nucleic acid reactions; Biochemical reagents or Chemical reagents, in particular biochemical reagents or chemical reagents for in-vitro use in laboratories for scientific use. Apparatus, namely column or magnet-based apparatus for chromatin immunoprecipitation, chromatin analysis, chromatin purification, nucleic acid purification and analysis, in particular of RNA and/or DNA; Scientific, electric, photographic, optical, measuring apparatus, namely sequencers for next generation sequencing; scientific, electric apparatus preparing nucleic acids for sequencing; computer hardware and computer software for processing and displaying and interpreting data, in particular for scientific purposes; Diagnostic apparatus, not for medical purposes. Treatment of nucleic acids, proteins and chromatin; treatment of nucleic acids with enzymatic reactions; treatment of chromatin with enzymatic reactions; Treatment of nucleic acids for sequencing, in particular for sequencing of RNA and/or DNA. Research and development services; industrial research in the field of biology; industrial development in the field of human biology and diseases like cancer and inflammation/ immune disorders; Laboratory services for detecting protein-DNA interactions and/or for detecting protein-RNA interactions; Scientific services for the analysis of laboratory results; Computer programming; DNA and RNA testing for purposes of scientific research; Biochemical analysis; Biological analysis; Preparation of biological samples for analysis in research laboratories; Preparation of biological samples for testing and analysis in research laboratories; Research and development in the field of diagnostic preparations. Blood bank services; Medical assistance; Hospitals; Animal healthcare services; Advisory services relating to health; Medical analysis services for diagnostic and treatment purposes provided by medical laboratories; Medical screening, in particular for diagnostic and therapeutic purposes; Nucleic acids screening for medical use; Genetic and molecular biological analysis, in particular with tissues, cells, nucleic acids for medical purposes.

Produits et services

Chemical preparations for use in RNA analysis and/or DNA analysis [other than medical]; Reagents for use in scientific apparatus for chemical or biological analysis; Biomolecule labelling kits comprising reagents for use in scientific research; Chemicals for use in immuno-assay testing [other than medical or veterinary]; ln-vivo diagnostic reagents for scientific use; Diagnostic testing materials, other than for medical use; Diagnostic preparations, other than for medical or veterinary purposes; Diagnostic reagents, other than for medical laboratory use; Diagnostic reagents, except for medical or veterinary use; Diagnostic reagents for in-vitro use [other than medical]; Diagnostic chemicals [other than for medical or veterinary use]; Clinical diagnostics, other than for medical or veterinary use; Diagnostic reagents and preparations, except for medical or veterinary use; Diagnostic reagents, other than for medical use for sale in kit form; Diagnostic reagents for in vitro use in biochemistry, clinical chemistry and microbiology; Diagnostic preparations for scientific or research use other than for medical use; Reagents for use in diagnostic tests [other than for medical or veterinary purposes]; Chemical reagents for use in diagnostic tests, other than for medical or veterinary use; Diagnostic substances, other than for medical use; Diagnostic reagents for scientific or research use; Diagnostic preparations for scientific or research use; Biochemicals, namely biochemicals for industrial and scientific purposes, in particular biochemicals for industrial and scientific purposes for the investigation of cells, chromatin, proteins, nucleic acids, in particular of RNA and/or DNA, protein nucleic acid reactions; Biochemical reagents or Chemical reagents, in particular biochemical reagents or chemical reagents for in-vitro use in laboratories for scientific use; none of the aforesaid goods for the treatment of human infertility, reproductive medicine and the treatment of sterility via assisted reproduction techniques. Apparatus, namely column or magnet-based apparatus for chromatin immunoprecipitation, chromatin analysis, chromatin purification, nucleic acid purification and analysis, in particular of RNA and/or DNA; Scientific, electric, photographic, optical, measuring apparatus, namely sequencers for next generation sequencing; scientific, electric apparatus preparing nucleic acids for sequencing; computer hardware and computer software for processing and displaying and interpreting data, in particular for scientific purposes; Diagnostic apparatus, not for medical purposes. Treatment of nucleic acids, proteins and chromatin; treatment of nucleic acids with enzymatic reactions; treatment of chromatin with enzymatic reactions; Treatment of nucleic acids for sequencing, in particular for sequencing of RNA and/or DNA. Research and development services; industrial research in the field of biology; industrial development in the field of human biology and diseases like cancer and inflammation/ immune disorders; Laboratory services for detecting protein-DNA interactions and/or for detecting protein-RNA interactions; Scientific services for the analysis of laboratory results; Computer programming; DNA and RNA testing for purposes of scientific research; Biochemical analysis; Biological analysis; Preparation of biological samples for analysis in research laboratories; Preparation of biological samples for testing and analysis in research laboratories; Research and development in the field of diagnostic preparations; none of the aforesaid services for the treatment of human infertility, reproductive medicine and the treatment of sterility via assisted reproduction techniques. Blood bank services; Medical assistance; Hospitals; Animal healthcare services; Advisory services relating to health; Medical analysis services for diagnostic and treatment purposes provided by medical laboratories; Medical screening, in particular for diagnostic and therapeutic purposes; Nucleic acids screening for medical use; Genetic and molecular biological analysis, in particular with tissues, cells, nucleic acids for medical purposes; none of the aforesaid services for the treatment of human infertility, reproductive medicine and the treatment of sterility via assisted reproduction techniques.

Produits et services

Chemical preparations for use in RNA analysis and/or DNA analysis [other than medical]; Reagents for use in scientific apparatus for chemical or biological analysis; Biomolecule labelling kits comprising reagents for use in scientific research; Chemicals for use in immuno-assay testing [other than medical or veterinary]; ln-vivo diagnostic reagents for scientific use; Diagnostic testing materials, other than for medical use; Diagnostic preparations, other than for medical or veterinary purposes; Diagnostic reagents, other than for medical laboratory use; Diagnostic reagents, except for medical or veterinary use; Diagnostic reagents for in-vitro use [other than medical]; Diagnostic chemicals [other than for medical or veterinary use]; Clinical diagnostics, other than for medical or veterinary use; Diagnostic reagents and preparations, except for medical or veterinary use; Diagnostic reagents, other than for medical use for sale in kit form; Diagnostic reagents for in vitro use in biochemistry, clinical chemistry and microbiology; Diagnostic preparations for scientific or research use other than for medical use; Reagents for use in diagnostic tests [other than for medical or veterinary purposes]; Chemical reagents for use in diagnostic tests, other than for medical or veterinary use; Diagnostic substances, other than for medical use; Diagnostic reagents for scientific or research use; Diagnostic preparations for scientific or research use; Biochemicals, namely biochemicals for use in industry and science, in particular biochemicals for use in industry and science for the investigation of cells, chromatin, proteins, nucleic acids, in particular of RNA and/or DNA, protein nucleic acid reactions; Biochemical reagents or Chemical reagents, in particular biochemical reagents or chemical reagents for in-vitro use in laboratories for scientific use. Apparatus, namely column or magnet-based apparatus for chromatin immunoprecipitation, chromatin analysis, chromatin purification, nucleic acid purification and analysis, in particular of RNA and/or DNA; Scientific, electric, photographic, optical, measuring apparatus, namely sequencers for next generation sequencing; scientific, electric apparatus preparing nucleic acids for sequencing; computer hardware and computer software for processing and displaying and interpreting data, in particular for scientific purposes; Diagnostic apparatus, not for medical purposes. Treatment of nucleic acids, proteins and chromatin; treatment of nucleic acids with enzymatic reactions; treatment of chromatin with enzymatic reactions; Treatment of nucleic acids for sequencing, in particular for sequencing of RNA and/or DNA. Research and development services; industrial research in the field of biology; industrial development in the field of human biology and diseases like cancer and inflammation/ immune disorders; Laboratory services for detecting protein-DNA interactions and/or for detecting protein-RNA interactions; Scientific services for the analysis of laboratory results; Computer programming; DNA and RNA testing for purposes of scientific research; Biochemical analysis; Biological analysis; Preparation of biological samples for analysis in research laboratories; Preparation of biological samples for testing and analysis in research laboratories; Research and development in the field of diagnostic preparations.

Abrégé

The invention relates to methods for determining the selectivity of a test compound and related methods such as methods for determining whether a subject suffering from cancer will respond or is responsive to treatment with a test compound or compositions comprising more than one test compound.

Classes IPC  ?

• G01N 33/50 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique
• C12N 5/078 - Cellules du sang ou du système immunitaire
• C12N 5/077 - Cellules mésenchymateuses, p. ex. cellules osseuses, cellules de cartilage, cellules stromales médulaires, cellules adipeuses ou cellules musculaires

Abrégé

The present invention relates to a sulfonylurea compound for use in the treatment and/or amelioration of a disease that is associated with UV-induced DNA damage, wherein the subject to be treated expresses enzymatically active mutY homolog (MUTYH), wherein the sufonylurea compound preferably is acetohexamide or a derivative thereof, or glimepiride or a derivative thereof. The invention furthermore relates to pharmaceutical compositions comprising a sulfonylurea compound for use in the treatment and/or amelioration of a disease that is associated with UV-induced DNA damage. Also, a screening method for identifying a compound that treats and/or ameliorates a disease that is associated with UV-induced DNA damage in a subject that expresses enzymatically active MUTYH is provided. The invention also relates to a method for monitoring the therapeutic success during the treatment of a disease that is associated with UV-induced DNA damage in a subject and a method for identifying a subject which responds to a treatment with a sulfonylurea compound.

Classes IPC  ?

• A61K 31/64 - Sulfonylurées, p. ex. glibenclamide, tolbutamide, chlorpropamide
• A61P 43/00 - Médicaments pour des utilisations spécifiques, non prévus dans les groupes
• C12Q 1/00 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions

Abrégé

The present invention relates to methods for determining the propensity of cells to interact in a population of cells comprising at least two distinguishable subpopulations of cells. In addition, the present invention provides methods for diagnosing a disease or predisposition to a disease of a cell donor, wherein the method comprises the determination of the propensity of cells to interact in a population of cells obtained from the donor, wherein the population of cells comprises at least two distinguishable subpopulations of cells. The invention also provides methods for determining whether a subject suffering from or predisposed to a disease will respond or is responsive to treatment with a therapeutic agent by determining the alteration of the propensity of cells to interact in a population of ceils obtained from the subject, wherein the population of cells comprises at least two distinguishable subpopulations of cells. The invention also relates to methods for screening for a therapeutic agent comprising the determination whether one or more test substances alter the propensity of cells to interact.

Classes IPC  ?

• G01N 33/569 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour micro-organismes, p. ex. protozoaires, bactéries, virus
• G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer

Abrégé

The present invention relates to methods for determining the propensity of cells to interact in a population of cells comprising at least two distinguishable subpopulations of cells. In addition, the present invention provides methods for diagnosing a disease or predisposition to a disease of a cell donor, wherein the method comprises the determination of the propensity of cells to interact in a population of cells obtained from the donor, wherein the population of cells comprises at least two distinguishable subpopulations of cells. The invention also provides methods for determining whether a subject suffering from or predisposed to a disease will respond or is responsive to treatment with a therapeutic agent by determining the alteration of the propensity of cells to interact in a population of ceils obtained from the subject, wherein the population of cells comprises at least two distinguishable subpopulations of cells. The invention also relates to methods for screening for a therapeutic agent comprising the determination whether one or more test substances alter the propensity of cells to interact.

Classes IPC  ?

• G01N 33/569 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour micro-organismes, p. ex. protozoaires, bactéries, virus
• G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer

Abrégé

The present invention provides a novel method for preparing a sequencing library and studying molecular interactions involving a nucleic acid. In particular, the invention relates to a method for preparing a sequencing library, the method comprising the addition of an agent binding to chromatin to a sample comprising a nucleic acid; isolating chromatin bound by said agent; addition of transposase to the isolated chromatin; isolating nucleic acid from chromatin; and obtaining a sequencing library. Moreover, the present invention relates to a method for mapping of molecular interactions involving a nucleic acid, the method comprising the addition of an agent binding to chromatin to a sample comprising a nucleic acid; isolating chromatin bound by said agent; addition of transposase to the isolated chromatin; isolating nucleic acid from chromatin; amplification of nucleic acid; sequencing of amplified nucleic acid; and identifying molecular interactions.

Classes IPC  ?

• C40B 50/06 - Procédés biochimiques, p. ex. utilisant des enzymes ou des micro-organismes viables entiers
• C12Q 1/6806 - Préparation d’acides nucléiques pour analyse, p. ex. pour test de réaction en chaîne par polymérase [PCR]
• C07K 16/44 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel non prévu ailleurs
• C40B 50/04 - Procédés de création de bibliothèques, p. ex. synthèse combinatoire utilisant des techniques de chimie combinatoire dynamique
• C40B 50/08 - Synthèse en phase liquide, c.-à-d. dans laquelle tous les blocs servant à créer la bibliothèque sont en phase liquide ou en solution au cours de la création de la bibliothèqueProcédés particuliers de clivage à partir du support liquide

Abrégé

The present invention relates to the combination of an antiandrogen with a vitamin K antagonist or with a γ-glutamyl carboxylase inhibitor for use in the treatment or prevention of an androgen receptor positive cancer, such as prostate cancer, or a hyperactive androgen receptor signaling disease/disorder. The invention also relates to a vitamin K antagonist or a γ-glutamyl carboxylase inhibitor for use in resensitizing an antiandrogen-resistant prostate cancer to the treatment with an antiandrogen. The invention further provides a pharmaceutical composition comprising an antiandrogen, a vitamin K antagonist or a γ-glutamyl carboxylase inhibitor, and a pharmaceutically acceptable excipient.

Classes IPC  ?

• A61K 31/37 - Coumarines, p. ex. psoralène
• A61K 31/167 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome d'azote d'un groupe carboxamide lié directement au cycle aromatique, p. ex. lidocaïne, paracétamol
• A61P 35/00 - Agents anticancéreux
• A61K 31/4166 - 1,3-Diazoles ayant des groupes oxo liés directement à l'hétérocycle, p. ex. phénytoïne

Abrégé

The present invention relates to the combination of a BRD4 inhibitor with an antifolate (particularly an MTHFD1 inhibitor) for use in the treatment or prevention of cancer. The invention also relates to an antifolate (particularly an MTHFD1 inhibitor) for use in resensitizing a BRD4 inhibitor-resistant cancer to the treatment with a BRD4 inhibitor. The invention further provides a pharmaceutical composition comprising a BRD4 inhibitor, an antifolate (particularly an MTHFD1 inhibitor), and a pharmaceutically acceptable excipient. Moreover, the invention provides a method of assessing the susceptibility or responsiveness of a subject to the treatment with a BRD4 inhibitor, wherein the subject has been diagnosed as suffering from cancer or is suspected of suffering from cancer, the method comprising determining the level of nuclear folate and/or the level of expression of MTHFD1 in a sample obtained from the subject.

Classes IPC  ?

• A61K 31/5025 - PyridazinesPyridazines hydrogénées condensées en ortho ou en péri avec des systèmes hétérocycliques
• A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
• A61K 31/551 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant deux atomes d'azote comme hétéro-atomes d'un cycle, p. ex. clozapine, dilazèpe
• A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
• G01N 33/00 - Recherche ou analyse des matériaux par des méthodes spécifiques non couvertes par les groupes
• G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer

Abrégé

The invention relates to a multiwell imaging plate and a method for incubating non- adherent cells. The multiwell imaging plate includes multiple wells, at least some of the wells having a first chamber, a second chamber arranged on top of the first chamber, and a disturbance blocking structure provided between the first chamber and the second chamber. The first chamber is formed by one or more first sidewalls and a bottom wall while the second chamber is formed by one or more second sidewalls and includes an opening for introducing liquids. The disturbance blocking structure includes at least one through hole that provides a liquid connection between the first and second chambers.

Classes IPC  ?

• B01L 3/00 - Récipients ou ustensiles pour laboratoires, p. ex. verrerie de laboratoireCompte-gouttes
• C12M 3/00 - Appareillage pour la culture de tissus, de cellules humaines, animales ou végétales, ou de virus

Abrégé

The present invention relates to lactam derivatives of formula (I) for use as medicaments as well as pharmaceutical compositions comprising these compounds, particularly for use as inhibitors of the bromodomain-containing protein TAF1 (i.e., transcription initiation factor TFIID subunit 1) and for use in the treatment or prevention of cancer.

Classes IPC  ?

• C07D 217/26 - Atomes de carbone comportant trois liaisons à des hétéro-atomes avec au plus une liaison à un halogène
• C07D 401/12 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
• C07D 407/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
• C07D 413/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
• A61K 31/4725 - Isoquinoléines non condensées, p. ex. papavérine contenant d'autres hétérocycles
• A61P 35/00 - Agents anticancéreux

Produits et services

Chemical preparations for use in medical diagnostics, in particular preparations for personalised medicine and/or gene analysis and/or genome sequencing; diagnostic and analytical preparations for medical purposes, in particular for personalised medicine and/or gene analysis and/or genome sequencing. Scientific and technological services and research and design relating thereto, in particular for personalised medicine and/or gene analysis and/or genome sequencing; industrial analysis and research services. Medical and veterinary services, in particular treatment methods for personalised medicine and/or gene analysis and/or genome sequencing; medical analysis, in particular test methods for personalised medicine and/or gene analysis and/or genome sequencing; medical services.

Abrégé

ROS1 inhibitor for use in the treatment of a subject suffering from ROS1 positive cancer, wherein the inhibitor is tivozanib.

Classes IPC  ?

• A61K 31/4709 - Quinoléines non condensées contenant d'autres hétérocycles
• A61P 35/00 - Agents anticancéreux

Abrégé

The present invention provides a novel method for preparing a sequencing library and studying molecular interactions involving a nucleic acid. In particular, the invention relates to a method for preparing a sequencing library, the method comprising the addition of an agent binding to chromatin to a sample comprising a nucleic acid; isolating chromatin bound by said agent; addition of transposase to the isolated chromatin; isolating nucleic acid from chromatin; and obtaining a sequencing library. Moreover, the present invention relates to a method for mapping of molecular interactions involving a nucleic acid, the method comprising the addition of an agent binding to chromatin to a sample comprising a nucleic acid; isolating chromatin bound by said agent; addition of transposase to the isolated chromatin; isolating nucleic acid from chromatin; amplification of nucleic acid; sequencing of amplified nucleic acid; and identifying molecular interactions.

Classes IPC  ?

• C12Q 1/68 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques
• G01N 33/68 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique faisant intervenir des protéines, peptides ou amino-acides

Abrégé

The present invention provides a novel method for preparing a sequencing library and studying molecular interactions involving a nucleic acid. In particular, the invention relates to a method for preparing a sequencing library, the method comprising the addition of an agent binding to chromatin to a sample comprising a nucleic acid; isolating chromatin bound by said agent; addition of transposase to the isolated chromatin; isolating nucleic acid from chromatin; and obtaining a sequencing library. Moreover, the present invention relates to a method for mapping of molecular interactions involving a nucleic acid, the method comprising the addition of an agent binding to chromatin to a sample comprising a nucleic acid; isolating chromatin bound by said agent; addition of transposase to the isolated chromatin; isolating nucleic acid from chromatin; amplification of nucleic acid; sequencing of amplified nucleic acid; and identifying molecular interactions.

Classes IPC  ?

• C12Q 1/68 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques
• G01N 33/68 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique faisant intervenir des protéines, peptides ou amino-acides

Abrégé

The present invention relates to the combination of an antiandrogen with a vitamin K antagonist or with a γ-glutamyl carboxylase inhibitor for use in the treatment or prevention of an androgen receptor positive cancer, such as prostate cancer, or a hyperactive androgen receptor signaling disease/disorder. The invention also relates to a vitamin K antagonist or a γ-glutamyl carboxylase inhibitor for use in resensitizing an antiandrogen-resistant prostate cancer to the treatment with an antiandrogen. The invention further provides a pharmaceutical composition comprising an antiandrogen, a vitamin K antagonist or a γ-glutamyl carboxylase inhibitor, and a pharmaceutically acceptable excipient.

Classes IPC  ?

• A61K 31/167 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome d'azote d'un groupe carboxamide lié directement au cycle aromatique, p. ex. lidocaïne, paracétamol
• A61K 31/37 - Coumarines, p. ex. psoralène
• A61K 31/4166 - 1,3-Diazoles ayant des groupes oxo liés directement à l'hétérocycle, p. ex. phénytoïne
• A61P 5/28 - Antiandrogènes
• A61P 35/00 - Agents anticancéreux

Abrégé

The present invention relates to substituted 4-(phenylamino)quinoline derivatives of formula (I) for use as medicaments as well as pharmaceutical compositions comprising these compounds, particularly for use as inhibitors of MTH1 and for use in the treatment or prevention of cancer.

Classes IPC  ?

• A61K 31/4706 - 4-Aminoquinoléines8-Aminoquinoléines, p. ex. chloroquine, primaquine
• A61P 35/00 - Agents anticancéreux

Abrégé

The present invention relates to a method for diagnosing myeloid malignancy comprising determining the presence of a mutant allele of the calreticulin gene. Also genomic sequences, cDNA sequences, mRNA sequences and protein sequences of the mutant calreticulin are subject of the present invention. Further, the invention relates to medical uses of inhibitors of mutant calreticulin.

Classes IPC  ?

• C12Q 1/68 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques
• C12Q 1/6886 - Produits d’acides nucléiques utilisés dans l’analyse d’acides nucléiques, p. ex. amorces ou sondes pour les maladies provoquées par des altérations du matériel génétique pour le cancer
• G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer
• A61K 39/00 - Préparations médicinales contenant des antigènes ou des anticorps
• C07K 14/47 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains provenant de vertébrés provenant de mammifères
• C07K 16/18 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains
• C12N 15/113 - Acides nucléiques non codants modulant l'expression des gènes, p. ex. oligonucléotides anti-sens

Abrégé

The present invention relates to oxoquinoline derivatives of formula (I) for use as medicaments as well as pharmaceutical compositions comprising these compounds, particularly for use as inhibitors of MTH1 and for use in the treatment or prevention of cancer.

Classes IPC  ?

• A61K 31/473 - QuinoléinesIsoquinoléines condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. acridines, phénantridines
• A61P 35/00 - Agents anticancéreux

Abrégé

The present invention relates to 2,3-dihydrocyclopenta[bJquinoline derivatives of formula (I) as well as pharmaceutical compositions comprising these compounds for use in the treatment or prevention of cancer, and particularly for use as inhibitors of MTH1.

Classes IPC  ?

• A61K 31/473 - QuinoléinesIsoquinoléines condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. acridines, phénantridines
• A61P 35/00 - Agents anticancéreux

Abrégé

The present invention relates to 4-aminoquinazoline derivatives of formula (I) for use as medicaments as well as pharmaceutical compositions comprising these compounds, particularly for use as inhibitors of MTH1 and for use in the treatment or prevention of cancer.

Classes IPC  ?

• A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
• A61K 35/00 - Préparations médicinales contenant des substances ou leurs produits de réaction de constitution non déterminée

Abrégé

The present disclosure relates to an antibody that specifically binds to a mutant calreticulin protein, wherein the variable region of the heavy chain of said antibody comprises a CDR-H3 region having an amino acid sequence as depicted in SEQ ID NO.: 3, or a CDR sequence having 75% or more amino acid identity to said CDR; or wherein the variable region of the heavy chain of said antibody comprises a CDR-H3 region having an amino acid sequence as depicted in SEQ ID NO.: 6, or a CDR sequence having 75% or more amino acid identity to said CDR. Hybridoma 8B2-H6-10.7 deposited under accession number DSM ACC3249 with the depositary institute DSMZ on September 12, 2014 as well as antibodies obtainable therefrom are subject of the present disclosure. The antibodies provided herein can be used in the diagnosis of or therapeutic intervention in myeloid malignancies.

Classes IPC  ?

• C07K 16/30 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire provenant de cellules de tumeurs

Abrégé

The present invention relates to an antagonist of the methyltransferase Setdb2 for use in treating an infection. Also provided herein are methods for treating, preventing or ameliorating infections comprising the administration of an antagonist of Setdb2 to a subject in need of such treatment. Herein preferred is the treatment of superinfections, in particular bacterial superinfections. The infection, in particular the bacterial superinfection, can be preceded by a viral infection.

Classes IPC  ?

• A61K 31/352 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à six chaînons avec un oxygène comme seul hétéro-atome d'un cycle condensés avec des carbocycles, p. ex. cannabinols, méthanthéline
• A61K 31/404 - Indoles, p. ex. pindolol
• A61K 31/4155 - 1,2-Diazoles non condensés et contenant d'autres hétérocycles
• A61K 31/4184 - 1,3-Diazoles condensés avec des carbocycles, p. ex. benzimidazoles
• A61K 31/428 - Thiazoles condensés avec des carbocycles
• A61K 31/433 - Thiadiazoles
• A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
• A61K 31/496 - Pipérazines non condensées contenant d'autres hétérocycles, p. ex. rifampine, thiothixène ou sparfloxacine
• A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
• A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
• A61K 31/52 - Purines, p. ex. adénine
• A61K 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
• A61K 31/538 - 1,4-Oxazines, p. ex. morpholine condensées en ortho ou en péri avec des systèmes carbocycliques
• A61K 31/548 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec au moins un azote et au moins un soufre comme hétéro-atomes d'un cycle, p. ex. sulthiame ayant plusieurs atomes de soufre dans le même cycle
• A61K 31/5513 - 1,4-Benzodiazépines, p. ex. diazépam

Produits et services

Chemical preparations for use in DNA analysis [other than medical]; reagents for use in scientific apparatus for chemical or biological analysis; biomolecule labeling kits comprising reagents for use in scientific research; chemicals for use in immuno-assay testing [other than medical or veterinary]; in-vivo diagnostic reagents for scientific use; diagnostic testing materials, other than for medical use; diagnostic preparations, except for medical or veterinary use; diagnostic reagents, other than for medical laboratory use; diagnostic reagents, except for medical or veterinary use; diagnostic reagents for in-vitro use [other than medical]; diagnostic chemicals [other than for medical or veterinary use]; diagnostic preparations, other than for medical or veterinary purposes; clinical diagnostics, other than for medical or veterinary use; diagnostic reagents and preparations, except for medical or veterinary use; diagnostic reagents, other than for medical use for sale in kit form; diagnostic reagents for in-vitro use in biochemistry, clinical chemistry and microbiology; diagnostic preparations for scientific or research use other than for medical use; reagents for use in diagnostic tests [other than for medical or veterinary purposes]; chemical reagents for use in diagnostic tests, other than for medical or veterinary use; diagnostic substances, other than for medical use; diagnostic reagents for scientific or research use; diagnostic preparations for scientific or research use; biochemical products, in particular biochemical products used in industry and science, in particular biochemical products used in industry and science to study cells, chromatin, proteins, nucleic acids, protein-nucleic acid interactions; biochemical reagents or chemical reagents, in particular biochemical reagents or chemical reagents for in-vitro use in laboratories for scientific use. Apparatus, namely column- or magnet-based apparatus for chromatin immunoprecipitation, chromatin analysis, chromatin purification, nucleic acid purification and analysis; scientific, electric, photographic, optical, measuring apparatus, namely sequencers for next generation sequencing; scientific, electric apparatus preparing nucleic acids for sequencing; computer hardware and computer software for processing and displaying and interpreting data, in particular for scientific purposes; testing apparatus for diagnostic purposes [other than medical]. Treatment of nucleic acids, proteins and chromatin; treatment of nucleic acids with enzymatic reactions; treatment of chromatin with enzymatic reactions; treatment of nucleic acids for sequencing. Research and development services; industrial research in the field of biology; industrial development in the field of human biology and diseases like cancer and inflammation/ immune disorders; laboratory services for detecting protein-DNA interactions; services for analysis relating thereto; computer programming; DNA screening for scientific research purposes; biochemical analysis; biological analysis; preparation of biological samples for analysis in research laboratories; preparation of biological samples for testing and analysis in research laboratories; research and development in the field of diagnostic preparations.

Abrégé

The invention relates to peripheral blood mononuclear cell (PBMC) monolayers or bone-marrow cell monolayers and methods for its culture and corresponding uses of said monolayers. The present invention also relates, in some aspects, to screening methods comprising the PBMC monolayer or bone-marrow cell monolayer of the invention for determination of response or lack of response of a disease to a therapeutic agent and/or drug screening methods. In some aspects, the invention further relates to methods for diagnosing a disease or predisposition to a disease in a PBMC donor or bone-marrow cell donor comprising the PBMCs/bone-marrow cells cultured according to the method of the invention and/or to methods for determining whether the disease is likely to respond or is responsive to treatment with a therapeutic agent.

Classes IPC  ?

• G01N 33/569 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour micro-organismes, p. ex. protozoaires, bactéries, virus
• C12N 5/078 - Cellules du sang ou du système immunitaire
• G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer

Abrégé

The invention relates to peripheral blood mononuclear cell (PBMC) monolayers or bone-marrow cell monolayers and methods for its culture and corresponding uses of said monolayers. The present invention also relates, in some aspects, to screening methods comprising the PBMC monolayer or bone-marrow cell monolayer of the invention for determination of response or lack of response of a disease to a therapeutic agent and/or drug screening methods. In some aspects, the invention further relates to methods for diagnosing a disease or predisposition to a disease in a PBMC donor or bone-marrow cell donor comprising the PBMCs/bone-marrow cells cultured according to the method of the invention and/or to methods for determining whether the disease is likely to respond or is responsive to treatment with a therapeutic agent.

Classes IPC  ?

• G01N 33/569 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour micro-organismes, p. ex. protozoaires, bactéries, virus
• C12N 5/078 - Cellules du sang ou du système immunitaire
• A61K 35/14 - SangSang artificiel
• C12M 3/04 - Appareillage pour la culture de tissus, de cellules humaines, animales ou végétales, ou de virus comportant des moyens fournissant des couches minces
• C12Q 1/02 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des micro-organismes viables
• G01N 33/15 - Préparations médicinales
• G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer

Produits et services

[ Treatment of nucleic acids, proteins and chromatin; treatment of nucleic acids with enzymatic reactions; treatment of chromatin with enzymatic reactions; treatment of nucleic acids for sequencing ] Chemical preparations for use in DNA analysis other than for medical use; reagents for use in scientific apparatus for chemical or biological analysis; biomolecule labeling kits comprising reagents for use in scientific research; chemicals for use in immuno-assay testing other than for medical or veterinary use; in-vivo diagnostic reagents for scientific use; diagnostic testing preparations, other than for medical use; diagnostic preparations, except for medical or veterinary use; diagnostic reagents, other than for medical laboratory use; diagnostic reagents, except for medical or veterinary use; diagnostic reagents for in-vitro use, other than for medical use; diagnostic chemicals, other than for medical or veterinary use; diagnostic preparations, other than for medical or veterinary purposes; clinical diagnostic preparations, other than for medical or veterinary use; diagnostic reagents and preparations, except for medical or veterinary use; diagnostic reagents, other than for medical use for sale in kit form; diagnostic reagents for in-vitro use in biochemistry, clinical chemistry and microbiology; diagnostic preparations for scientific or research use other than for medical use; reagents for use in diagnostic tests, other than for medical or veterinary purposes; chemical reagents for use in diagnostic tests, other than for medical or veterinary use; diagnostic substances in the nature of chemicals and preparations, other than for medical use; diagnostic reagents for scientific or research use; diagnostic preparations for scientific or research use; biochemical products, in particular biochemicals used in industry and science to study cells, chromatin, proteins, nucleic acids, protein-nucleic acid interactions, other than for medical use; biochemical reagents and chemical reagents, in particular biochemical reagents and chemical reagents for in-vitro use in laboratories for scientific use [ Apparatus, namely, column- and magnet-based apparatus for chromatin immunoprecipitation, chromatin analysis, chromatin purification, nucleic acid purification and analysis for laboratory use; scientific, electric, photographic, optical, measuring apparatus, namely, sequencers for next generation genetic sequencing for laboratory use; scientific, electric apparatus preparing nucleic acids for sequencing for laboratory use; computer hardware and computer software for processing and displaying and interpreting data, in particular for scientific purposes; testing apparatus for testing samples comprising a nucleic acid for for diagnostic purposes, other than medical purposes ] [ Scientific research and development services; industrial research in the field of biology; industrial research in the field of human biology and diseases like cancer and inflammation and immune disorders; laboratory services for detecting protein-DNA interactions; Laboratory analysis relating to protein-DNA interactions; computer programming; DNA screening for scientific research purposes; biochemical analysis; biological analysis; preparation of biological samples for analysis in research laboratories; preparation of biological samples for testing and analysis in research laboratories; research and development in the field of diagnostic preparations ]

Abrégé

The present invention relates to an antagonist or modulator of SLC38A9 for use in treating a disease associated with mTORC1 activation, like a proliferative disease (e.g. a cancerous disease or benign proliferative disease), a metabolic disorder, a disorder of the immune system, a disorder causing premature aging, an ophthalmic disorder or a neurological disorder. Exemplary diseases to be treated are cancerous diseases like lung cancer, breast cancer, bladder cancer, pancreatic cancer, ovarian cancer, colon carcinoma, leukemia, lymphoma, melanoma, esophageal cancer and stomach cancer; or metabolic disorders like overweight (pre-obesity), obesity or diabetes. Also provided herein are methods for treating, preventing or ameliorating such diseases comprising the administration of an antagonist of SLC38A9 to a subject in need of such a treatment, prevention or amelioration. Furthermore, the present invention provides methods for assessing the activity of a candidate molecule suspected of being an antagonist of SLC38A9 and identification of such antagonists.

Classes IPC  ?

• C12N 15/113 - Acides nucléiques non codants modulant l'expression des gènes, p. ex. oligonucléotides anti-sens
• C07K 14/705 - RécepteursAntigènes de surface cellulaireDéterminants de surface cellulaire

Abrégé

The invention refers to BTBD9 binders and gephyrin binders for medical use and in particular an artemisinin compound of general formula I for use in the treatment of a diabetes patient, as well as a method of identifying suitable lead candidates.

Classes IPC  ?

• A61K 31/357 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant plusieurs atomes d'oxygène dans le même cycle, p. ex. éthers en couronne, guanadrel
• A61K 31/366 - Lactones ayant des cycles à six chaînons, p. ex. delta-lactones
• A61P 3/10 - Médicaments pour le traitement des troubles du métabolisme de l'homéostase du glucose de l'hyperglycémie, p. ex. antidiabétiques
• A61P 5/48 - Médicaments pour le traitement des troubles du système endocrinien des hormones pancréatiques
• C12N 5/071 - Cellules ou tissus de vertébrés, p. ex. cellules humaines ou tissus humains

Produits et services

Chemical preparations for use in DNA analysis [other than medical]; Reagents for use in scientific apparatus for chemical or biological analysis; Biomolecule labeling kits comprising reagents for use in scientific research; Chemicals for use in immuno-assay testing [other than medical or veterinary]; ln-vivo diagnostic reagents for scientific use; Diagnostic testing materials, other than for medical use; Diagnostic preparations, except for medical or veterinary use; Diagnostic reagents, other than for medical laboratory use; Diagnostic reagents, except for medical or veterinary use; Diagnostic reagents for in-vitro use [other than medical]; Diagnostic chemicals [other than for medical or veterinary use]; Diagnostic preparations, other than for medical or veterinary purposes; Clinical diagnostics, other than for medical or veterinary use; Diagnostic reagents and preparations, except for medical or veterinary use; Diagnostic reagents, other than for medical use for sale in kit form; Diagnostic reagents for in-vitro use in biochemistry, clinical chemistry and microbiology; Diagnostic preparations for scientific or research use other than for medical use; Reagents for use in diagnostic tests [other than for medical or veterinary purposes]; Chemical reagents for use in diagnostic tests, other than for medical or veterinary use; Diagnostic substances, other than for medical use; Diagnostic reagents for scientific or research use; Diagnostic preparations for scientific or research use; Biochemical products, in particular biochemical products used in industry and science, in particular biochemical products used in industry and science to study cells, chromatin, proteins, nucleic acids, protein-nucleic acid interactions; biochemical reagents or chemical reagents, in particular biochemical reagents or chemical reagents for in-vitro use in laboratories for scientific use. Apparatus, namely column- or magnet-based apparatus for chromatin immunoprecipitation, chromatin analysis, chromatin purification, nucleic acid purification and analysis; Scientific, electric, photographic, optical, measuring apparatus, namely sequencers for next generation sequencing; scientific, electric apparatus preparing nucleic acids for sequencing; computer hardware and computer software for processing and displaying and interpreting data, in particular for scientific purposes; Testing apparatus for diagnostic purposes [other than medical]. Treatment of nucleic acids, proteins and chromatin; treatment of nucleic acids with enzymatic reactions; treatment of chromatin with enzymatic reactions; treatment of nucleic acids for sequencing. Research and development services; industrial research in the field of biology; industrial development in the field of human biology and diseases like cancer and inflammation/ immune disorders; laboratory services for detecting protein-DNA interactions; services for analysis relating thereto; computer programming; DNA screening for scientific research purposes; Biochemical analysis; Biological analysis; Preparation of biological samples for analysis in research laboratories; Preparation of biological samples for testing and analysis in research laboratories; Research and development in the field of diagnostic preparations.

Abrégé

Mutations in calreticulin are discovered to be linked to myeloid malignancies. Disclosed are genomic sequences, cDNA sequences, mRNA sequences and protein sequences of mutant calreticulin that are linked to myeloid malignancies. Also disclosed are methods for diagnosing myeloid malignancy comprising determining the presence of a mutant allele of the calreticulin gene. Also disclosed are related compositions, kits and methods, including the medical use of inhibitors of mutant calreticulin.

Classes IPC  ?

• G01N 33/53 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet
• C12Q 1/68 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques
• G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer

Abrégé

The present invention relates to a method for diagnosing myeloid malignancy comprising determining the presence of a mutant allele of the calreticulin gene. Also genomic sequences, cDNA sequences, mRNA sequences and protein sequences of the mutant calreticulin are subject of the present invention. Further, the invention relates to medical uses of inhibitors of mutant calreticulin.

Classes IPC  ?

• C12N 15/12 - Gènes codant pour des protéines animales
• C12N 15/113 - Acides nucléiques non codants modulant l'expression des gènes, p. ex. oligonucléotides anti-sens
• C12Q 1/6886 - Produits d’acides nucléiques utilisés dans l’analyse d’acides nucléiques, p. ex. amorces ou sondes pour les maladies provoquées par des altérations du matériel génétique pour le cancer
• A61K 39/00 - Préparations médicinales contenant des antigènes ou des anticorps
• A61P 35/00 - Agents anticancéreux
• C07K 14/47 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains provenant de vertébrés provenant de mammifères
• C07K 16/18 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains
• C12P 21/02 - Préparation de peptides ou de protéines comportant une séquence connue de plusieurs amino-acides, p. ex. glutathion
• C12Q 1/68 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques
• G01N 33/48 - Matériau biologique, p. ex. sang, urineHémocytomètres

Abrégé

The present invention relates to a method for diagnosing myeloid malignancy comprising determining the presence of a mutant allele of the calreticulin gene. Also genomic sequences, cDNA sequences, mRNA sequences and protein sequences of the mutant calreticulin are subject of the present invention. Further, the invention relates to medical uses of inhibitors of mutant calreticulin.

Classes IPC  ?

• C07K 14/47 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains provenant de vertébrés provenant de mammifères
• C12Q 1/68 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques

Produits et services

Biochemical or chemical products for use in industry and science; biochemicals or chemical reagents for in vitro use in laboratories for scientific use, in particular for cell culture, testing and/or detecting effects of drugs on cell types, in particular cells originating from blood or tissues; in vitro diagnostic agents for scientific use; biochemical or chemical products for use in medical science; pharmaceutical and biochemical substances and preparations, in particular reagents for medical research applications and medical diagnosis; biochemicals or chemical reagents for in vitro use in laboratories for medical purposes; biochemicals or chemical reagents for in vitro use in laboratories for medical purposes, in particular for cell culture, testing and/or detecting effects of drugs on cell types, in particular cells originating from blood or tissues. Diagnostic products for medical purposes. Apparatus for cell culture, testing and/or detecting effects of drugs on cell types, in particular cells originating from blood or tissues; scientific, optical, measuring and monitoring apparatus and instruments; electric apparatus and instruments for use in laboratories for medical purposes, in particular for testing and/or detecting effects of drugs on cell types, in particular cells originating from blood or tissues; computer-aided analysis apparatus and installations constructed therefrom, in particular for analysing the effects of drugs on cell types, in particular cells originating from blood or tissues; computer hardware and computer software, in particular for scientific and medical purposes; accessories, namely test microtiter plates. Medical and pharmaceutical research and development; scientific and industrial research and development services; services for cell culture, testing and/or detecting effects of drugs on cell types, in particular cells originating from blood or tissues; professional consultancy services relating to biotechnology, biochemistry, and biomedical science; contract research services; computer programming.

Abrégé

he present invention relates to an (S)-enantiomer of an aminoheteroaryl compound for use in treating and/or preventing cancer in a subject. The invention further relates to a pharmaceutical composition comprising said compound. Another aspect of the invention is directed to an in vitro method for determining the effectiveness of said (S)-enantiomer of an aminoheteroaryl compound, or said pharmaceutical composition, the method comprising the steps of: (a) obtaining a cell or tissue sample from a subject; and (b) determining the subject's NUDT1/MTH1 -status; wherein a NUDT1/MTH1-positive cell or tissue sample is indicative of an effective treatment and/or prevention of cancer. In addition, provided herein is a screening method for identifying a target of an (S)-enantiomer of an aminoheteroaryl compound. Furthermore, in context of this invention, the herein described compounds inhibit the biological activity of MTH1.

Classes IPC  ?

• A61K 31/4545 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un cycle à six chaînons avec l'azote comme hétéro-atome du cycle, p. ex. pipampérone, anabasine
• A61P 35/00 - Agents anticancéreux

Produits et services

Biochemical or chemical products for use in industry and science; biochemicals or chemical reagents for in vitro use in laboratories for scientific use, in particular for cell culture, testing and/or detecting effects of drugs on cell types, in particular cells originating from blood or tissues; in vitro diagnostic agents for scientific use. Biochemical or chemical products for use in medical science; pharmaceutical and biochemical substances and preparations, in particular reagents for medical research applications and medical diagnosis; biochemicals or chemical reagents for in vitro use in laboratories for medical purposes, in particular for cell culture, testing and/or detecting effects of drugs on cell types, in particular cells originating from blood or tissues; diagnostic products for medical purposes. Apparatus for cell culture, testing and/or detecting effects of drugs on cell types, in particular cells originating from blood or tissues; scientific, optical, measuring and monitoring apparatus and instruments; electric apparatus and instruments for use in laboratories for medical purposes; computer-aided analysis apparatus and installations constructed therefrom; computer hardware and computer software, in particular for scientific and medical purposes; accessories, namely test microtiter plates. Medical and pharmaceutical research and development; scientific and industrial research and development services; services for cell culture, testing and/or detecting effects of drugs on cell types, in particular cells originating from blood or tissues; professional consultancy services; contract research services; computer programming.

Produits et services

Chemical, biochemical and biological products used in industry and science; in-vitro diagnostic preparations (not for medical or veterinary purposes); in-vitro diagnostic preparations for identifying blood malignances, in particular myeloproliferative neoplasms; control reagents used in scientific apparatus and equipment. Pharmaceutical and veterinary preparations; pharmaceutical preparations and substances for the prevention and treatment of blood malignances, in particular myeloproliferative neoplasms; preparations, chemical substances, reagents and agents for diagnostic and medical purposes; sanitary preparations for medical use. Medical services; veterinary services; services in the field of blood malignancies; services and advice related to medical and pharmaceutical preparations and substances; medical clinical services; medical treatment services; therapeutic treatment services; healthcare services; medical services related to blood malignancies and pharmaceuticals; providing for medical and medicinal information in the field of diagnostic, medicine, pharmaceuticals, disorders, diseases, treatments and prevention.

Produits et services

Chemical preparations for use in medical diagnostics, in particular preparations for personalised medicine and/or gene analysis and/or genome sequencing; Diagnostic and analytical preparations for medical purposes, in particular for personalised medicine and/or gene analysis and/or genome sequencing. Scientific and technological services and research and design relating thereto, in particular for personalised medicine and/or gene analysis and/or genome sequencing; Industrial analysis and research services. Medical and veterinary services, in particular treatment methods for personalised medicine and/or gene analysis and/or genome sequencing; Medical analysis, in particular test methods for personalised medicine and/or gene analysis and/or genome sequencing; Medical services.

Abrégé

The present invention relates to a specific sphingomyelinase for use in inhibiting immune response. Another aspect of the invention relates to a pharmaceutical composition comprising said sphingomyelinase for use in treating an autoimmune disorder or a pro-inflammatory response. In addition, another pharmaceutical composition comprising a specific inhibitor of said sphingomyelinase for use in treating an immunodeficiency disorder is comprised. The invention also relates to a diagnostic composition comprising a binding molecule which specifically binds said sphingomyelinase for use in diagnosing an immunodeficiency disorder, an autoimmune disorder or a pro-inflammatory response. The invention further relates to the use of said diagnostic composition for diagnosing an immunodeficiency disorder, an autoimmune disorder or a pro-inflammatory response. Furthermore, the present invention relates an antigen presenting cell that is inhibited in TLR signalling by said sphingomyelinase. In one aspect of the invention, said antigen presenting cell is a macrophage, a dendritic cell or a B cell. The present invention further relates to a non-human animal, wherein the activity and/or the expression of said sphingomyelinase is reduced to boost the immune system of said non-human animal. In addition, the invention relates to a method for producing antibodies against an antigen comprising the administration of said antigen to said non non-human animal. Finally, the invention relates to said method for producing antibodies, wherein said non-human animal is a knock out mouse for the gene encoding said sphingomyelinase, wherein said antibodies are high affinity antibodies.

Classes IPC  ?

• A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
• C12N 9/16 - Hydrolases (3.) agissant sur les liaisons esters (3.1)

Abrégé

A method for determining the responsiveness of a mammalian tumor cell to treatment with an inhibitor of the phosphoinosite 3-kinase (PI3K) and/or mammalian target of rapamycin (mTOR) pathway, said method comprising determining the c-MYC and/or NOTCH1 level in said tumor cell, wherein said level is indicative of whether the cell is likely to respond or is responsive to the treatment. It further refers to an in vitro method for the identification of a resistance to treatment or of predicting or monitoring the efficacy of treatment, of solid tumor cancer with an inhibitor of the PI3K and/or mTOR pathway in a patient suffering from said cancer. It further refers to a combination comprising an amount of an inhibitor of the PI3K and/or mTOR pathway, and an amount of a c-MYC and/or NOTCH 1 inhibitor.

Classes IPC  ?

• C12Q 1/68 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques

Abrégé

The invention relates to complement Factor H for use in the prevention and treatment of oxidative stress disease conditions in a patient, the use of Factor H in the preparation of a pharmaceutical preparation, and methods of determining the specific binding of Factor H to MDA and/or MAA in a sample.

Classes IPC  ?

• A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains

Abrégé

The present invention refers to a synthetic microsphere based on malondialdehyde (MDA) coupled to a backbone, with a size ranging between 500 nm and 500 µm, its use for analytic, diagnostic or pharmaceutic purposes, and specifically its use in a method of selecting antagonists of oxidative stress disease from a repertoire of agents possibly binding to oxidation epitopes.

Classes IPC  ?

• A61K 47/08 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant de l'oxygène
• G01N 33/50 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique