Crystalline forms of N-(4-(4-amino-6-ethynyl-5-(quinolin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-7- yl)bicyclo[2.2.1]heptan-1-yl)-5-methylpyrazine-2-carboxamide (TAS3351), a compound having an inhibitory effect against EGFR and an acid. The crystalline forms have advantageous physical properties including stability, hygroscopicity, and oral absorption. The crystalline forms have peaks in a powder X-ray diffraction spectrum at specific diffraction angles (2θ ± 0.2°).
A61K 31/395 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines
A61K 31/505 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/166 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome de carbone d'un groupe carboxamide lié directement au cycle aromatique, p. ex. procaïnamide, procarbazine, métoclopramide, labétalol
The present disclosure relates to methods of treating a cancer in a subject in need thereof, comprising administering to the subject futibatinib or a pharmaceutically acceptable salt thereof, pembrolizumab or a pharmaceutically acceptable salt thereof, and at least one additional anti-cancer therapy agent or a pharmaceutically acceptable salt thereof. In some embodiments, the at least one additional anti-cancer therapy agent is a chemotherapeutic agent.
A61K 31/4025 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil non condensés et contenant d'autres hétérocycles, p. ex. cromakalim
A61K 31/407 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil condensés avec des systèmes hétérocycliques, p. ex. kétorolac, physostigmine
A61K 31/7115 - Acides nucléiques ou oligonucléotides ayant des bases modifiées, c.-à-d. autres que l'adénine, la guanine, la cytosine, l'uracile ou la thymine
The present disclosure relates to methods of treating a cancer in a subject in need thereof, comprising administering to the subject futibatinib or a pharmaceutically acceptable salt thereof, pembrolizumab or a pharmaceutically acceptable salt thereof, and at least one additional anti-cancer therapy agent or a pharmaceutically acceptable salt thereof. In some embodiments, the at least one additional anti-cancer therapy agent is a chemotherapeutic agent.
A61K 31/4025 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil non condensés et contenant d'autres hétérocycles, p. ex. cromakalim
A61K 31/407 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil condensés avec des systèmes hétérocycliques, p. ex. kétorolac, physostigmine
A61K 31/7115 - Acides nucléiques ou oligonucléotides ayant des bases modifiées, c.-à-d. autres que l'adénine, la guanine, la cytosine, l'uracile ou la thymine
The present disclosure relates to a juniper pollen protein selected from (a)-(c) below. (a) A protein comprising an amino acid sequence represented by SEQ ID NO: 2. (b) A protein comprising an amino acid sequence represented by SEQ ID NO: 2 with one or several amino acids substituted, deleted, or added, and having a juniper pollen allergen activity. (c) A protein having at least 90% amino acid identity with the amino acid sequence represented by SEQ ID NO: 2, and having a juniper pollen allergen activity.
C07K 16/16 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant de végétaux
C12N 15/63 - Introduction de matériel génétique étranger utilisant des vecteursVecteurs Utilisation d'hôtes pour ceux-ciRégulation de l'expression
C12P 21/02 - Préparation de peptides ou de protéines comportant une séquence connue de plusieurs amino-acides, p. ex. glutathion
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
5.
CANCER THERAPY USING 3,5-DISUBSTITUTED BENZENE ALKYNYL COMPOUND AND IMMUNE CHECKPOINT INHIBITOR
The problem to be solved by the present invention is to provide a novel combination therapy exhibiting an excellent antitumor effect. The present invention provides an antitumor agent (that does not contain pemblolizumab as an active ingredient) that contains, as an active ingredient, futibatinib or a salt thereof that is administered to a cancer patient in combination with an immune checkpoint inhibitor (excluding CD155/TIGIT pathway antagonist) and at least one or more other antitumor agents.
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
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 31/4745 - QuinoléinesIsoquinoléines condensées en ortho ou en péri avec des systèmes hétérocycliques condensées avec des systèmes cycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. phénanthrolines
A61K 31/475 - QuinoléinesIsoquinoléines ayant un cycle indole, p. ex. yohimbine, réserpine, strychnine, vinblastine
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
A61K 31/513 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime ayant des groupes oxo liés directement à l'hétérocycle, p. ex. cytosine
A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p. ex. leucoglucosane, hespéridine, érythromycine, nystatine
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
A61K 31/7072 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique ayant deux groupes oxo liés directement au cycle pyrimidine, p. ex. uridine, acide uridylique, thymidine, zidovudine
A61K 31/7076 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées contenant des purines, p. ex. adénosine, acide adénylique
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
The present invention addresses the problem of providing a novel combination therapy having an excellent antitumor effect. The present invention provides an antitumor agent that is administered to a cancer patient in combination with an immune checkpoint inhibitor (other than CD155/TIGIT pathway antagonist) and at least one other antitumor agent and that contains futibatinib or a salt thereof as an active ingredient (but does not contain pembrolizumab as an active ingredient).
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
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 31/4745 - QuinoléinesIsoquinoléines condensées en ortho ou en péri avec des systèmes hétérocycliques condensées avec des systèmes cycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. phénanthrolines
A61K 31/475 - QuinoléinesIsoquinoléines ayant un cycle indole, p. ex. yohimbine, réserpine, strychnine, vinblastine
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
A61K 31/513 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime ayant des groupes oxo liés directement à l'hétérocycle, p. ex. cytosine
A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p. ex. leucoglucosane, hespéridine, érythromycine, nystatine
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
A61K 31/7072 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique ayant deux groupes oxo liés directement au cycle pyrimidine, p. ex. uridine, acide uridylique, thymidine, zidovudine
A61K 31/7076 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées contenant des purines, p. ex. adénosine, acide adénylique
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
The present invention attempts to solve the problem of providing a novel combination therapy that exhibits an excellent antitumor effect. The present invention provides an antitumor agent (the antitumor agent does not contain pembrolizumab as an active ingredient) containing, as an active ingredient, futibatinib or a salt thereof that is administered to a cancer patient in combination with an immune checkpoint inhibitor (excluding CD155/TIGIT pathway antagonists) and at least one other antitumor agent.
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
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 31/475 - QuinoléinesIsoquinoléines ayant un cycle indole, p. ex. yohimbine, réserpine, strychnine, vinblastine
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
A61K 31/513 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime ayant des groupes oxo liés directement à l'hétérocycle, p. ex. cytosine
A61K 31/4745 - QuinoléinesIsoquinoléines condensées en ortho ou en péri avec des systèmes hétérocycliques condensées avec des systèmes cycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. phénanthrolines
A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p. ex. leucoglucosane, hespéridine, érythromycine, nystatine
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
A61K 31/7072 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique ayant deux groupes oxo liés directement au cycle pyrimidine, p. ex. uridine, acide uridylique, thymidine, zidovudine
A61K 31/7076 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées contenant des purines, p. ex. adénosine, acide adénylique
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
An object of the present disclosure is to provide a crystalline form of 3-(15-methoxypentadecyl)-2,4,4- trimethylcyclohex-2-en-1-one, the crystalline form having excellent stability and being preferable in terms of production. The present disclosure provides a crystalline form having characteristic peaks at diffraction angles (20+0.2°) of 7.0°, 14.0°, 17.5°, 19.5°, 21.0°, 23.7°, and 24.8° in a powder X-ray diffraction spectrum (CuKa).
A61K 31/122 - Cétones ayant l'atome d'oxygène lié directement à un cycle, p. ex. quinones, vitamine K1, anthraline
A61P 13/02 - Médicaments pour le traitement des troubles du système urinaire de l'urine ou des voies urinaires, p. ex. acidificateurs d'urine
A61P 25/04 - Analgésiques centraux, p. ex. opioïdes
A61P 29/02 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS] sans effet anti-inflammatoire
C07C 49/603 - Composés non saturés comportant un groupe cétone faisant partie d'un cycle d'un cycle à six chaînons, p. ex. méthides de quinones
9.
CANCER COMBINATION THERAPY USING AZA BICYCLIC COMPOUND AND ANTIANDROGEN AGENT
Provided is a novel method for treating castration resistant prostate cancer (CRPC), particularly CRPC that has acquired resistance to antiandrogen agents. This antitumor agent is characterized by the co-administration of an antiandrogen agent and 3-ethyl-4-{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide or a salt thereof.
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 31/568 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes non substitués en position 17 bêta par un atome de carbone, p. ex. œstrane, œstradiol substitués en positions 10 et 13 par une chaîne ayant au moins un atome de carbone, p. ex. androstane, testostérone
A61K 31/4155 - 1,2-Diazoles non condensés et contenant d'autres hétérocycles
A61K 31/4439 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. oméprazole
A61K 45/00 - Préparations médicinales contenant des ingrédients actifs non prévus dans les groupes
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology.
21.
PROCESS FOR PREPARING A BENZOATE SALT OF A 1-(3-AMINOPYRROLIDINE-1-CARBONYL)-3,4-DIPHENYLBENZENE COMPOUND
A process for preparation of benzoate salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile, designated herein as Compound (A), and methods of using Compound (A) are provided. (I)
A process for preparation of benzoate salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile, designated herein as Compound (A), and methods of using Compound (A) are provided. (I)
A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
A61K 31/4025 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil non condensés et contenant d'autres hétérocycles, p. ex. cromakalim
C07C 67/52 - SéparationPurificationStabilisationEmploi d'additifs par modification de l'état physique, p. ex. par cristallisation
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology..
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Anti-cancer preparations; pharmaceutical preparations for the treatment of tumor; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of immune disorders; pharmaceutical preparations for the treatment of hematological disorders.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Anti-cancer preparations; pharmaceutical preparations for the treatment of tumor; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of immune disorders; pharmaceutical preparations for the treatment of hematological disorders.
25.
TREATMENT METHODS FOR SUBJECTS WITH NON-SMALL CELL LUNG CANCER HAVING AN ABERRATION IN EGFR
A method of treating a subject with a cancer having at least one aberration in EGFR, whereby the subject is administered (S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl)acrylamide (also known as zipalertinib and as TAS6417) or a pharmaceutically acceptable salt thereof, to a subject who has previously been treated with a molecularly targeted therapeutic. The molecularly targeted therapeutic may be an EGFR-targeting therapeutic other than Compound (1) or a non-EGFR-targeting therapeutic. The method may optionally involve administering to the subject an additional therapeutic agent.
A method of treating a subject with cancer having a dysregulated MAPK and/or PI3K pathway, whereby the subject is administered an effective amount of 4-(4-(3-((2-(tert-butylamino)ethyl)amino)-6-(5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl)pyridin-2-yl)piperidin-1-yl)-5,5-dimethyl-5H-pyrolo[2,3-d]pyrimidin-6(7H)-one or a pharmaceutically acceptable salt thereof.
The present invention addresses the problem of providing a crystal of a compound having EGFR inhibition ability or a salt thereof, said crystal being excellent in the characteristic of stability (heat, purity) and/or low hygroscopicity. One aspect of the present invention provides a crystal form of (S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl)acrylamide that has a peak at a prescribed angle as the diffraction angle (2θ±0.2°) in a powder X-ray diffraction spectrum.
In one embodiment, the present invention provides an antibody specifically binding to human GH or an antigen-binding fragment thereof. In one embodiment, the present invention relates to an antibody specifically binding to human GH or an antigen-binding fragment thereof, comprising a heavy chain variable region (VH) and a light chain variable region (VL), wherein the VH comprises an amino acid sequence set forth in SEQ ID NO: 5 as a VH complementarity-determining region (CDR) 1 (VHCDR1), an amino acid sequence set forth in SEQ ID NO: 6 as a VHCDR2, and an amino acid sequence set forth in SEQ ID NO: 7 as a VHCDR3, and the VL comprises an amino acid sequence set forth in SEQ ID NO: 8 as a VL complementarity-determining region (CDR) 1 (VLCDR1), an amino acid sequence set forth in SEQ ID NO: 9 as a VLCDR2, and an amino acid sequence set forth in SEQ ID NO: 10 as a VLCDR3.
The purpose of the present invention is to provide a pharmaceutical composition containing naproxen or a salt thereof and acetaminophen or a salt thereof and having excellent storage stability. For this purpose, provided is a composition in which at least one selected from the group consisting of a specific basic compound and glycine or a salt thereof is used.
A61K 31/192 - Acides carboxyliques, p. ex. acide valproïque ayant des groupes aromatiques, p. ex. sulindac, acides 2-aryl-propioniques, acide éthacrynique
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 47/18 - AminesAmidesUréesComposés d’ammonium quaternaireAcides aminésOligopeptides ayant jusqu’à cinq acides aminés
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations; medicinal drinks; tonics (medicines); vitamin preparations; nutritional preparations for medical use; nutritional additives for medical purposes; nutritional supplements for medical purposes; food supplements for medical purposes; drugs for medical purposes; dental materials; bracelets for medical purposes; oiled paper for medical purposes; sanitary masks; pharmaceutical wafer; gauze for dressings; capsules for pharmaceutical purposes; capsules for medicines; eye patches for medical purposes; ear bandages; incontinence diapers; semen for artificial insemination; menstruation bandages; menstruation tampons; sanitary napkins; menstruation pads; sanitary pads; sanitary panties; sanitary knickers; menstruation knickers; absorbent cotton; absorbent wadding; lacteal flour for babies; lactose (milk sugar); fly catching paper; adhesive plaster; court plaster; sticking plasters; bandages for dressings; collodion for pharmaceutical purposes; mothproofing paper; breast-nursing pads; dietetic foods adapted for medical purposes; dietetic beverages adapted for medical purposes.
32.
SMALL MOLECULE INHIBITORS OF KRAS MUTATED PROTEINS
Compounds of Formula (I) or their pharmaceutically acceptable salts can inhibit the G12C, G12D and/or G12V mutants of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/541 - Thiazines non condensées contenant d'autres 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 31/553 - 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 au moins un azote et au moins un oxygène comme hétéro-atomes d'un cycle, p. ex. loxapine, staurosporine
A61K 31/554 - 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 au moins un azote et au moins un soufre comme hétéro-atomes d'un cycle, p. ex. clothiapine, diltiazem
C07D 519/00 - Composés hétérocycliques contenant plusieurs systèmes de plusieurs hétérocycles déterminants condensés entre eux ou condensés avec un système carbocyclique commun non prévus dans les groupes ou
33.
PROPHYLACTIC DRUG/THERAPEUTIC DRUG FOR PROGRESSIVE SUPRANUCLEAR PALSY
Provided is a novel prophylactic drug and/or a novel therapeutic drug useful for progressive supranuclear palsy (PSP), the prophylactic drug and/or the therapeutic drug containing, as an active ingredient, a growth arrest and DNA damage-inducible protein 34 (GADD34) inhibitor including guanabenz that is a compound represented by formula [I-1].
A61K 31/4706 - 4-Aminoquinoléines8-Aminoquinoléines, p. ex. chloroquine, primaquine
A61P 25/00 - Médicaments pour le traitement des troubles du système nerveux
A61P 25/14 - Médicaments pour le traitement des troubles du système nerveux pour traiter les mouvements anormaux, p. ex. chorée, dyskinésie
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
Provided is an antibody-drug conjugate (ADC) that specifically binds to CD138 and exhibits an excellent antitumor effect. In the ADC, monomethyl auristatin E is bound via a linker to an anti-CD138 antibody having a specific amino acid sequence.
A61K 47/68 - 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 anticorps, une immunoglobuline ou son fragment, p. ex. un fragment Fc
A61K 38/08 - Peptides ayant de 5 à 11 amino-acides
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
Provided are: an anti-tumor agent having a high anti-tumor effect and fewer side effects; and others. The present invention relates to: a combination preparation containing trifluridine and tipiracil hydrochloride at a molar ratio of 1:0.5; an anti-tumor agent containing a PD-1 pathway antagonist, which is used in such a manner that the anti-tumor agent is administered in combination with a VEGF pathway antagonist; and others.
A61K 31/7072 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique ayant deux groupes oxo liés directement au cycle pyrimidine, p. ex. uridine, acide uridylique, thymidine, zidovudine
A61P 43/00 - Médicaments pour des utilisations spécifiques, non prévus dans les groupes
C07D 403/06 - 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 carbonée ne contenant que des atomes de carbone aliphatiques
C07H 19/073 - Radicaux pyrimidine avec un désoxy-2 ribosyle comme radical saccharide
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
37.
TREATMENT METHODS FOR SUBJECTS WITH CANCER HAVING AN ABERRATION IN EGFR AND/OR HER2
A method of treating a subject with cancer having an aberration in EGFR and/or HER2, whereby the subject is administered 7-((3R,5S)-1-acryloyl-5-methylpyrrolidin-3-yl)-4-amino-6-(cyclopropylethynyl)-N—((R)-1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide or a pharmaceutically acceptable salt thereof.
Forms of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile, designated herein as Compound I, were prepared and characterized in the solid state. Also provided are processes of manufacture and methods of using the forms of Compound I.
C07D 207/14 - Atomes d'azote ne faisant pas partie d'un radical nitro
A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
The present invention provides I form crystals of 4-piperidinyl 2,2-diphenyl-2-(propoxy-1,1,2,2,3,3,3-d7)acetate hydrochloride having at least one diffraction angle (2θ±0.2°) selected from group (a) below and at least one diffraction angle (2θ±0.2°) selected from group (b) below in a powder x-ray diffraction spectrum (CuKα). (a) 11.3°, 11.4°, and 17.2° (b) 12.7°, 15.9°, 16.1°, 20.5°, 20.7°, 23.1°, 23.2°, 25.9°, and 28.4°
The present invention provides a substituted polypeptide having the effect of inhibiting MMP2 and represented by formula [I′], or a pharmaceutically acceptable salt thereof.
The present invention provides a substituted polypeptide having the effect of inhibiting MMP2 and represented by formula [I′], or a pharmaceutically acceptable salt thereof.
A61K 38/08 - Peptides ayant de 5 à 11 amino-acides
C07K 5/02 - Peptides ayant jusqu'à quatre amino-acides dans une séquence entièrement déterminéeLeurs dérivés contenant au moins une liaison peptidique anormale
41.
TREATING CANCER IN PATIENT HAVING CO-OCCURRING GENETIC ALTERATION IN FGFR2 AND A CANCER DRIVER GENE
A method of treating a subject with cholangiocarcinoma having a co-occurring genetic alteration in FGFR2 and a cancer driver gene selected from TP53, BAP1, ARID1A, MLL2, PIK3C2B, IKBKE, MCL1, MDM4, and MYC, whereby the subject is administered (S)-1-[(3)-[4-amino-3-[(3,5-dimethoxyphenyl)ethynyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-pyrrolidinyl]-2-propen-1-one or a pharmaceutically acceptable salt thereof.
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
42.
COMBINATION THERAPY USING AZABICYCLO COMPOUND FOR CANCER
Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect.
Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect.
An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent(s).
Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect.
An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent(s).
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 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
A61K 31/454 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. pimozide, dompéridone
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
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 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
A61K 31/555 - Composés hétérocycliques contenant des métaux lourds, p. ex. hémine, hématine, mélarsoprol
A61K 31/704 - Composés ayant des radicaux saccharide liés à des composés non-saccharide par des liaisons glycosidiques liés à un composé carbocyclique, p. ex. phloridzine liés à un système carbocyclique condensé, p. ex. sennosides, thiocolchicosides, escine, daunorubicine, digitoxine
A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p. ex. leucoglucosane, hespéridine, érythromycine, nystatine
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
A method for treating cancer in patients with creatinine clearance of 15 mL/min or more and less than 30 mL/min, including dividing a combination drug containing α,α,α-trifluorothymidine (FTD) and 5-chloro-6-[(2-iminopyrrolidine-1-yl)methyl]pyrimidine-2,4(1H,3H)-dione hydrochloride in a molar ratio of 1:0.5, in a dose of 30 to 40 mg/m2/day as FTD-equivalent, into two to four times a day, and orally administering it to the patient.
A61K 31/513 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime ayant des groupes oxo liés directement à l'hétérocycle, p. ex. cytosine
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
A61K 31/7072 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique ayant deux groupes oxo liés directement au cycle pyrimidine, p. ex. uridine, acide uridylique, thymidine, zidovudine
A61P 13/12 - Médicaments pour le traitement des troubles du système urinaire des reins
An antitumor agent comprising a compound selected from the group consisting of Compounds A to D described in the specification, or a salt thereof, for treating a malignant tumor patient expressing EGFR having exon 20 insertion mutation.
A method of treating a subject with a cancerous tumor exhibiting an inactivating mutation in the PTEN gene including administering to the subject trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenylcyclobutanol or a pharmaceutically acceptable salt thereof.
A61K 31/5365 - 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 oxygène comme hétéro-atomes d'un cycle, p. ex. 1,2-oxazines condensées en ortho ou en péri avec des systèmes hétérocycliques
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
54.
BRAIN-MIGRATING TUMOR THERAPEUTIC AGENT CONTAINING FUSED PYRIMIDINE COMPOUND AS ACTIVE INGREDIENT
An object to be solved of the present invention is to provide a brain-penetrable antitumor agent showing an excellent brain penetration property and RET inhibitory activity.
An object to be solved of the present invention is to provide a brain-penetrable antitumor agent showing an excellent brain penetration property and RET inhibitory activity.
The present invention provides brain-penetrable antitumor agent including a compound represented by Formula (I) below or a salt thereof as an active ingredient:
An object to be solved of the present invention is to provide a brain-penetrable antitumor agent showing an excellent brain penetration property and RET inhibitory activity.
The present invention provides brain-penetrable antitumor agent including a compound represented by Formula (I) below or a salt thereof as an active ingredient:
An object to be solved of the present invention is to provide a brain-penetrable antitumor agent showing an excellent brain penetration property and RET inhibitory activity.
The present invention provides brain-penetrable antitumor agent including a compound represented by Formula (I) below or a salt thereof as an active ingredient:
wherein R1, R2, and R3 are as described in Specification.
Crystalline Forms of 4-amino-N-[4-(methoxymethyl)phenyl]-7-(1-methylcyclopropyl)-6-(3-morpholinoprop-1-yn-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide
Provided herein are various crystalline forms of 4-amino-N-[4-(methoxymethyl)phenyl]-7-(1-methylcyclopropyl)-6-(3-morpholinoprop-1-yn-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide, methods of producing same, and methods of using same to for RET inhibition.
Provided is a type-I crystal of a free form of 4-(4-(3-((2-(tert-butylamino)ethyl)amino)-6-(5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl)piperidin-2-yl)piperidin-1-yl)-5,5-dimethyl-5H-pyrrolo[2,3-d]pyrimidin-6(7H)-one that has, in a powder X-ray diffraction spectrum (CuKα), peaks at at least two diffraction angles (2θ±0.2°) selected from the following (a) and at least two diffraction angles (2θ±0.2°) selected from the following (b). (a) 6.2°, 9.3°, 9.7°, 11.1°, 15.4°, and 25.1° (b) 6.7°, 8.3°, 8.7°, 13.0°, 13.7°, 16.3°, 16.9°, 17.7°, 18.7°, 19.4°, 20.3°, 25.9°, and 26.5°
Methods of Using 4-Amino-N-[4-(Methoxymethyl)Phenyl]-7-(1-Methylcyclopropyl)-6-(3-Morpholinoprop-1-YN-1-YL)-7H-Pyrrolo[2,3-D]Pyrimidine-5-Carboxamide for the Treatment of Tumors
The present invention relates to compositions and methods for treating patients with cancer having a RET gene abnormality comprising administering HM06/TAS0953, for example patients with non-small cell lung cancer (NSCLC), and that may also have brain and/or leptomeningeal metastases, or another solid tumor; where the patient is administered an effective amount of HM06/TAS0953, where the HM06/TAS0953 can be formulated in a composition and administered orally in a single or multiple doses; and where the patients may have previously received and/or have developed resistance to another RET-selective or multi-kinase inhibitor.
Provided are novel compounds which are analogues to be removed from APIs and formulations. Also provided are standard products of analogues to be used in controlling the qualities of medicines. Analogue 1: 3-ethyl-4-\{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3,3'-di(propan-2-yl)-1'H-[1,4'-bipyrazolo[3,4-b]pyridin]-1'-yl\}benzamide. Analogue 2: 3-ethyl-4-fuluorobenzamide. Analogue 3: N-[1-(4-carbamoyl-2-ethylphenyl)-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-4-yl]-3-ethyl-4-\{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl\}benzamide. Analogue 4: 3-ethyl-4-\{14-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-13,23,33-tri(propan-2-yl)-31H-[11,24:21, 34-terpyrazolo[3,4-b]pyridin]-31-yl\}benzamide. Analogue 5: 4,4'-(1H,1'H-[4,4'-biimidazol]-1,1'-diylbis\{[3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-4,1-diyl]\})bis(3-ethylbenzamide). Analogue 6: 4-\{4,6-bis[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin]-1-yl\}-3-ethylbenzonitrile. Analogue 7: 4-\{4,6-bis[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl\}-3-ethylbenzamide. Analogue 8: 4-[4-ethoxy-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl]-3-ethylbenzamide. Analogue 9: 3-ethyl-4-[4-methoxy-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl]benzamide.
C07C 233/65 - Amides d'acides carboxyliques ayant des atomes de carbone de groupes carboxamide liés à des atomes de carbone de cycles aromatiques à six chaînons ayant les atomes d'azote des groupes carboxamide liés à des atomes d'hydrogène ou à des atomes de carbone de radicaux hydrocarbonés non substitués
A61K 31/166 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome de carbone d'un groupe carboxamide lié directement au cycle aromatique, p. ex. procaïnamide, procarbazine, métoclopramide, labétalol
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
C07D 519/00 - Composés hétérocycliques contenant plusieurs systèmes de plusieurs hétérocycles déterminants condensés entre eux ou condensés avec un système carbocyclique commun non prévus dans les groupes ou
Provided is a pharmaceutical composition containing compound 1 and having excellent disintegrability and bioavailability. This pharmaceutical composition contains crystalline cellulose and a granulated substance containing 3-ethyl-4-{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridine-1-yl}benzamide or a pharmaceutically acceptable salt thereof, and has a disintegration time of 360 seconds or less in a coated tablet state.
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 9/36 - Revêtements organiques contenant des hydrates de carbone ou leurs dérivés
The present invention provides a pharmaceutical composition for preventing and/or treating an RNR-related disease in a patient in need thereof, wherein the pharmaceutical composition comprises 5-chloro-2-(N-((1S,2R)-2-(6-fluoro-2,3-dimetylphenyl)-1-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)propyl)sulfamoyl)benzamide or a salt thereof, and is administered to the patient on an intermittent administration schedule for two weeks comprising dosing 1 to 5 days per week. The present invention also provides a method of treating an RNR-related diseases in a patient in need thereof, the method comprising administering an effective amount of 5-chloro-2-(N-((1S,2R)-2-(6-fluoro-2,3-dimetylphenyl)-1-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)propyl)sulfamoyl)benzamide or a salt thereof to the patient on an intermittent administration schedule for two weeks comprising dosing 1 to 5 days per week.
The present invention relates to a compound having inhibitory activity against KRAS G12D mutation or a salt thereof, and relates to a pharmaceutical composition comprising the compound as an active ingredient.
C07D 519/00 - Composés hétérocycliques contenant plusieurs systèmes de plusieurs hétérocycles déterminants condensés entre eux ou condensés avec un système carbocyclique commun non prévus dans les groupes ou
The present invention provides a pharmaceutical composition for preventing and/or treating an RNR-related disease in a patient in need thereof, wherein the pharmaceutical composition comprises 5-chloro-2-(N-((1S,2R)-2-(6-fluoro-2,3-dimetylphenyl)-1-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)propyl)sulfamoyl)benzamide or a salt thereof, and is administered to the patient on an administration schedule comprising continuous, daily dosing for one week, followed by a resting period of one week. The present invention also provides a method of treating an RNR-related diseases in a patient in need thereof, the method comprising administering an effective amount of 5-chloro-2-(N-((1S,2R)-2-(6-fluoro-2,3-dimetylphenyl)-1-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)pr opyl)sulfamoyl)benzamide or a salt thereof to the patient on an administration schedule comprising daily dosing for one week, followed by a resting period of one week.
Provided is a novel therapeutic agent useful for the prevention or treatment of lung inflammation and fibrosis, the agent containing, as an active ingredient, a compound which has an MMP2 inhibitory activity and is represented by formula [IX], or a pharmaceutically acceptable salt thereof.
Provided is a crystal of a compound having EGFR inhibition ability or a salt thereof, said crystal being excellent in one or more characteristics of stability, hygroscopicity and oral absorbability. One aspect of the present invention provides a crystal form of N-(4-(4-amino-6-ethynyl-5-(quinolin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)bicyclo[2.2.1]heptan-1-yl)-5-methylpyrazine-2-carboxamide the diffraction angle (2θ±0.2°) of which has a peak at a preset angle in the X-ray powder diffraction spectrum.
A crystal of 7-((3R,5S)-1-acryloyl-5-methylpyrrolidin-3-yl)-4-amino-6-(cyclopropylethynyl)-N-((R)-1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide (compound (I)), and a crystal thereof with an acid (salt crystal or co-crystal) are provided.
A crystal of 7-((3R,5S)-1-acryloyl-5-methylpyrrolidin-3-yl)-4-amino-6-(cyclopropylethynyl)-N-((R)-1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide (compound (I)), and a crystal thereof with an acid (salt crystal or co-crystal) are provided.
There are provided: a type II crystal of compound (I) with fumaric acid, having characteristic peaks at three or more diffraction angles (2θ ± 0.2 °) selected from 5.5°, 6.8°, 9.3°, 13.4°, 15.3°, 16.3°, 18.5°, 19.8°, 22.0°, and 24.5° in a powder X-ray diffraction spectrum;
a (free-form) type II crystal of compound (I) having characteristic peaks at three or more diffraction angles selected from 8.3°, 14.8°, 17.3°, 18.0°, 19.1°, 20.3°, 21.0°, 22.5°, 23.0°, and 26.2° in a powder X-ray diffraction spectrum;
a (free-form) type I crystal of compound (I) having characteristic peaks at three or more diffraction angles selected from 9.9°, 11.7°, 13.2°, 17.7°, 18.1°, 18.8°, and 20.8° in a powder X-ray diffraction spectrum;
a type V crystal of compound (I) with fumaric acid, having characteristic peaks at four or more diffraction angles selected from 6.9°, 9.4°, 10.2°, 13.7°, 21.1°, 23.6°, and 26.5° in a powder X-ray diffraction spectrum; and
a type I crystal of compound (I) with fumaric acid, having characteristic peaks at four or more diffraction angles selected from 6.4°, 10.3°, 12.8°, 15.0°, 20.7°, 23.4°, and 26.6° in a powder X-ray diffraction spectrum.
Provided is an antibody that exhibits pH dependence and specifically binds to a sulfated glycosaminoglycan (sGAG). An antibody specifically binding to a sulfated glycosaminoglycan that is at least one selected from the group consisting of the following (1) to (3): (1) an antibody that contains a heavy chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 1, CDR2 comprising an amino acid sequence represented by SEQ ID NO: 2 and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 3, and a light chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 4, CDR2 comprising an amino acid sequence represented by LGS and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 6; (2) an antibody that contains a heavy chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 7, CDR2 comprising an amino acid sequence represented by SEQ ID NO: 8 and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 9, and a light chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 10, CDR2 comprising an amino acid sequence represented by AAS and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 12; and (3) an antibody that contains a heavy chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 13, CDR2 comprising an amino acid sequence represented by SEQ ID NO: 14 and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 15, and a light chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 16, CDR2 comprising an amino acid sequence represented by WAS and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 18.
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
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
A61K 47/68 - 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 anticorps, une immunoglobuline ou son fragment, p. ex. un fragment Fc
The invention relates to methods of synthesizing 2′-deoxy-2′,2′-difluorotetrahydrouridine with increased purity and uniform particle size distribution. In particular, methods of the invention include crystallization and isolation procedures rendering synthetic reaction intermediates. The invention further includes compositions comprising the final compound in highly pure form, including lower number of impurities and lower levels of individual and total impurities.
The present invention addresses the problem of providing: an injectable formulation that contains fosnetupitant or a pharmaceutically acceptable salt in a stable form as a medicinal product; and a method for producing the same. The present invention provides an injectable formulation containing a) fosnetupitant or a pharmaceutically acceptable salt thereof, b) trehalose, and c) a nonionic surfactant.
A61K 9/19 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p. ex. poudres lyophilisées
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61P 1/08 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif des nausées, du mal des transports ou des vertigesAntiémétiques
Provided are a compound represented by formula (I) or a salt thereof, a nerve growth promoter containing the compound or a salt thereof as an active ingredient, a pharmaceutical composition containing the compound or a salt thereof, a therapeutic agent for neurodegenerative diseases containing the compound or a salt thereof as an active ingredient, a therapeutic agent for amyotrophic lateral sclerosis containing the compound or a salt thereof as an active ingredient, a therapeutic agent for pain containing the compound or a salt thereof as an active ingredient, and a therapeutic agent for lower urinary tract dysfunction containing the compound or a salt thereof as an active ingredient.
C07C 49/753 - Composés non saturés comportant un groupe cétone faisant partie d'un cycle contenant des groupes éther, des groupes , des groupes ou des groupes
Provided is a therapeutic agent for a disease associated with EGFR, the agent comprising a compound that has EGFR inhibitory activity and has brain penetration properties as an active ingredient. The present invention provides a compound represented by the formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the present specification, or a salt thereof, and a therapeutic agent for a disease associated with EGFR, the agent comprising a compound represented by the following formula (I), or a salt thereof as an active ingredient.
Provided is a therapeutic agent for a disease associated with EGFR, the agent comprising a compound that has EGFR inhibitory activity and has brain penetration properties as an active ingredient. The present invention provides a compound represented by the formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the present specification, or a salt thereof, and a therapeutic agent for a disease associated with EGFR, the agent comprising a compound represented by the following formula (I), or a salt thereof as an active ingredient.
2 administered as a one hour (1 h) infusion. Also provided are methods of treatment using a solid oral dosage form according to an embodiment of the invention.
A61K 31/706 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
A61K 31/20 - Acides carboxyliques, p. ex. acide valproïque ayant un groupe carboxyle lié à une chaîne acyclique d'au moins sept atomes de carbone, p. ex. acides stéarique, palmitique ou arachidique
A61K 31/7016 - Disaccharides, p. ex. lactose, lactulose
The present invention addresses the problem of providing a voiding symptom therapeutic agent for lower urinary tract disorders accompanied by residual urine. The present invention provides a voiding symptom therapeutic agent for lower urinary tract disorders with a residual urine volume of 50 mL or more, the therapeutic agent containing 3-(15-hydroxypentadecyl)-2,4,4-trimethyl-2-cyclohexen-1-one or a salt thereof as an active ingredient.
Provided is a tumor treatment method using a pyrimidine compound or a salt thereof. An antitumor agent that contains a pyrimidine compound represented by general formula (I) or a salt thereof, said antitumor agent being to be administered in combination with another antitumor agent. (In the formula, R1 represents a C1-C4 alkyl group optionally having a C1-C4 alkoxy group as a substituent, or a C3-C4 cycloalkyl group; R2 represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group optionally having, as a substituent(s), one to five C1-C4 alkoxy groups or one to five fluorine atoms, or a C1-C6 alkoxy group; R3 represents a hydrogen atom, or a C1-C4 alkyl group optionally having, as a substituent(s), one to five fluorine atoms; R4 represents a hydrogen atom or a C1-C4 alkyl group; and R5 represents a phenyl group optionally having one to three substituents selected from fluorine atoms and chlorine atoms.)
Provided is a tumor treatment method using a pyrimidine compound or a salt thereof. An antitumor agent that contains a pyrimidine compound represented by general formula (I) or a salt thereof, said antitumor agent being to be administered in combination with another antitumor agent. (In the formula, R1 represents a C1-C4 alkyl group optionally having a C1-C4 alkoxy group as a substituent, or a C3-C4 cycloalkyl group; R2 represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group optionally having, as a substituent(s), one to five C1-C4 alkoxy groups or one to five fluorine atoms, or a C1-C6 alkoxy group; R3 represents a hydrogen atom, or a C1-C4 alkyl group optionally having, as a substituent(s), one to five fluorine atoms; R4 represents a hydrogen atom or a C1-C4 alkyl group; and R5 represents a phenyl group optionally having one to three substituents selected from fluorine atoms and chlorine atoms.)
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
A61K 31/513 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime ayant des groupes oxo liés directement à l'hétérocycle, p. ex. cytosine
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
A61K 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
A61K 31/565 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes non substitués en position 17 bêta par un atome de carbone, p. ex. œstrane, œstradiol
A61K 31/4745 - QuinoléinesIsoquinoléines condensées en ortho ou en péri avec des systèmes hétérocycliques condensées avec des systèmes cycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. phénanthrolines
A61K 31/436 - 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 six chaînons ayant l'oxygène comme hétéro-atome du cycle, p. ex. rapamycine
A61K 31/553 - 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 au moins un azote et au moins un oxygène comme hétéro-atomes d'un cycle, p. ex. loxapine, staurosporine
A61K 31/4375 - 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 six chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. quinolizines, naphtyridines, berbérine, vincamine
The purpose of the present disclosure is to provide a crystal form of 3-(15-methoxypentadecyl)-2,4,4-trimethylcyclohexa-2-en-1-one, this crystal form being of superior stability and desirable in terms of production. The present disclosure provides a crystal form which, in the powder X-ray diffraction spectrum (CuKα), demonstrates diffraction angles (2θ ± 0.2°) that have characteristic peaks at 7.0°, 14.0°, 17.5°, 19.5°, 21.0°, 23.7°, and 24.8°.
C07C 49/603 - Composés non saturés comportant un groupe cétone faisant partie d'un cycle d'un cycle à six chaînons, p. ex. méthides de quinones
A61K 31/122 - Cétones ayant l'atome d'oxygène lié directement à un cycle, p. ex. quinones, vitamine K1, anthraline
A61P 13/02 - Médicaments pour le traitement des troubles du système urinaire de l'urine ou des voies urinaires, p. ex. acidificateurs d'urine
A61P 25/00 - Médicaments pour le traitement des troubles du système nerveux
A61P 25/04 - Analgésiques centraux, p. ex. opioïdes
A61P 29/02 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS] sans effet anti-inflammatoire
77.
ANTICANCER COMBINATION THERAPY WITH N-(1-ACRYLOYL-AZETIDIN-3-YL)-2-((1H-INDAZOL-3-YL)AMINO)METHYL)-1H-IMIDAZOLE-5-CARBOXAMIDE INHIBITOR OF KRAS-G12C
A method of treating cancer comprises administering: (a) a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof; and (b) a therapeutically effective amount of an additional anti-cancer agent, to a subject in need of such treatment, the compound of Formula (I) being:
A method of treating cancer comprises administering: (a) a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof; and (b) a therapeutically effective amount of an additional anti-cancer agent, to a subject in need of such treatment, the compound of Formula (I) being:
A method of treating cancer comprises administering: (a) a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof; and (b) a therapeutically effective amount of an additional anti-cancer agent, to a subject in need of such treatment, the compound of Formula (I) being:
where X, R1, R2, ring A, L1, L2, L3, and R5 are as defined in this disclosure.
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
A61K 31/427 - Thiazoles non condensés et contenant d'autres hétérocycles
A61K 31/416 - 1,2-Diazoles condensés avec des systèmes carbocycliques, p. ex. indazole
A61K 31/422 - Oxazoles non condensés et contenant d'autres hétérocycles
A61K 31/454 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. pimozide, dompéridone
A61K 31/496 - Pipérazines non condensées contenant d'autres hétérocycles, p. ex. rifampine, thiothixène ou sparfloxacine
A61K 31/4439 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. oméprazole
A61P 11/00 - Médicaments pour le traitement des troubles du système respiratoire
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
A61K 31/166 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome de carbone d'un groupe carboxamide lié directement au cycle aromatique, p. ex. procaïnamide, procarbazine, métoclopramide, labétalol
A61K 31/5365 - 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 oxygène comme hétéro-atomes d'un cycle, p. ex. 1,2-oxazines condensées en ortho ou en péri avec des systèmes hétérocycliques
A61P 1/18 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif des troubles pancréatiques, p. ex. enzymes pancréatiques
A61P 1/00 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif
A61P 13/10 - Médicaments pour le traitement des troubles du système urinaire de la vessie
A61N 5/10 - RadiothérapieTraitement aux rayons gammaTraitement par irradiation de particules
Compounds and pharmaceutically acceptable salts thereof inhibit the G12D mutant of KRAS protein and are expected to have utility as therapeutic agents, for example, for the treatment of cancer.
C07D 403/14 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
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
79.
SMALL MOLECULE INHIBITORS OF KRAS MUTATED PROTEINS
Compounds of Formula (I) or their pharmaceutically acceptable salts can inhibit the G12C, G12D and/or G12V mutants of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.
A61K 31/395 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
A61K 31/505 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime
80.
CANCER THERAPY USING 3,5-DISUBSTITUTED BENZENE ALKYNYL COMPOUND AND MEK INHIBITOR
Provided is a novel combination therapy that exhibits excellent antitumor effects, and that uses an FGFR-inhibiting compound and an MEK inhibitor. An antitumor agent contains (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof as an active ingredient and is administered in combination with an MEK inhibitor.
The present invention provides a combination drug for the treatment of a malignant tumor comprising 2-((1R,2R,4S)-2-amino-7-azabicyclo[2.2.1]heptan-7-yl)-5-(3,4-dichloro-2-methyl-2H-indazol-5-yl)-3-methyl-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one or a pharmaceutically acceptable salt thereof, and at least one additional compound having an antitumor effect or at least one pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising both the active ingredients.
A process for preparation of benzoate salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile, designated herein as Compound (A), and methods of using Compound (A) are provided.(I)
A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
36 - Services financiers, assurances et affaires immobilières
41 - Éducation, divertissements, activités sportives et culturelles
Produits et services
Advertising and publicity services; business management analysis and business consultancy; business management; market analysis and research services; providing business information concerning commercial sales; preparation of financial statements; providing information, advice and consultation relating to preparation, auditing and attesting of financial statements; import-export agency services; office reception services in the nature of greeting visitors in offices; providing consumer information and advice regarding the selection of products and items to be purchased; providing employment counseling information on how to successfully transition jobs; providing business information about newspaper articles via the Internet; market research, namely, market canvassing, research and analysis services; providing business information, advice and consultation relating to market research, market analysis and marketing services; business marketing services, namely, presentation of companies and their goods and services on the Internet; providing and rental of advertising space on the Internet; business consultancy relating to business management, sales, acquisitions and mergers; business marketing research services relating to market trends and actions; business research, analysis and advice relating to the company establishment; business investigations, evaluations, expert appraisals, information and research; market research services featuring market trend and action research and market analysis, studies and evaluation; conducting marketing studies; compilation of business statistics and commercial information for commercial purposes; providing business management information; business intermediary services relating to the matching of potential private investors with entrepreneurs needing funding; business intermediary services relating to business tie-up and business cooperation, namely, business intermediary services relating to the matching of various professionals with clients; business advisory services in the field of business intermediary and advisory services; providing business assistance in the field of business promotion; providing business information relating to articles published in newspapers, magazines and books via the Internet; commercial intermediation services featuring matching of potential private investors with entrepreneurs needing funding; work analysis to determine worker skill sets and other worker requirements; business planning and consulting services relating to public offering of stocks; business appraisals relating to stock valuation; market investigation being business investigations for obtaining basic data necessary for the development of new products and the preparation of sales plans through temporary staff, and organization and analysis of the investigation results; accountancy services; providing office functions; office functions in the nature of classifying and filing documents or magnetic-tapes; business management in the form of computerized data input and data management services; compilation of information into computer databases for pharmaceutical research; management and compilation of computerized databases; providing business information on articles relating to research papers in scientific field; providing business information on research paper articles via the Internet; news clipping services; retail stores and wholesale store services featuring food and beverages; retail stores and wholesale store services featuring confectionery; retail stores and wholesale store services featuring soft drinks; retail stores and wholesale store services featuring cosmetics, toiletries, dentifrices, soaps and detergents; retail and wholesale store services featuring deodorants for body care; retail and wholesale store services featuring fragrancing preparations; retail and wholesale store services featuring medical apparatus; retail stores and wholesale store services featuring dietary and nutritional supplements; retail and wholesale store services featuring pharmaceutical, veterinary and sanitary preparations and medical supplies; promoting the goods and services of others; retail stores and wholesale store services featuring nutritional supplement drinks; retail stores and wholesale store services featuring nutritional supplements; retail stores and wholesale store services featuring tonics being medicines; retail stores and wholesale store services featuring vitamin preparations and substances; retail stores and wholesale store services featuring bacteria removal agents, other than for industrial purposes and laundry use; retail stores and wholesale store services featuring deodorants, other than for industrial purposes; retail stores and wholesale store services featuring body sprays for cosmetic use; promoting public awareness of cancer research, treatment, and information, and promoting public awareness of support resources for cancer patients and families of cancer patients; business consulting services in the fields of business management, labor management, human resources, and business organizational design; human resource analysis and consulting services; human resources management; labor management, namely, personnel management; consulting services in the field of human resources development, namely, for the promotion of employee retention, career growth, and increased productivity for employees and employers; business consulting services in the field of employee training, engagement, development; employee administration services; serving as a human resources department for others Acceptance of deposits including substitute bond issuance and acceptance of fixed interval installment deposits, namely, securities deposit services; financing loans and discounting of bills; business credit reporting services; financial credit rating services and credit reporting services; financial advice, information and consultancy services of tax and taxation; charitable fund raising; venture capital funding services for emerging and start-up companies; financing of medical research of others; investment advice based on an investment advisory agreement and capital investment based on a discretionary investment agreement; investment services in the field of venture capital funds, private equity funds and investment funds; capital investment services; funds investment; financial consultancy relating to investment services; investment consultancy, brokerage and management services; providing financial information on values of securities; rental of business premises, namely, rental of office space and buildings; rental of commercial premises being commercial properties, office space, and buildings; providing financial information relating to financial assessment of company credit; charitable fundraising, namely, accepting and administering monetary charitable contributions to fund medical research; providing research grants in the field of artificial intelligence, pharmaceuticals, biotechnology, medical device, diagnostics and digital health; providing and managing monetary research grants and providing information and consultancy relating thereto; financial services, namely, business fundraising, relating to joint ventures, business acquisitions, and mergers for others, and providing financial information and consultancy relating thereto; venture capital fund management; financial information, advisory, consultancy and research services relating to finance and investments; mutual funds investment, distribution and planning services; financial advisory services relating to credit and debit control, investment, grants and financing of loans; financial consultancy and information services relating to insurance, pensions, asset management and financial management; financial evaluation services for insurance, banking and real estate purposes; financial advisory and consultancy services relating to venture capital; financial advice; financial analysis; financial advisory and consultancy services; providing financial assessment services of company credit and financial information relating thereto Education, teaching and training, namely, conducting classes, seminars and workshops in the field of sports, arts, investment, finance, business development, artificial intelligence, biotechnology, pharmaceuticals, medical device, diagnostics, digital health, medical and scientific research, clinical trials, healthcare and cancer patient support, and providing educational information relating thereto; providing information in the field of medical education relating to the donation of human corpses for medical education; medical education services, namely, arranging of donation of human corpses for use in medical education courses of instruction; arranging, conducting and organization of seminars in the field of sports, arts, investment, finance, business development, artificial intelligence, biotechnology, pharmaceuticals, medical device, diagnostics, digital health, medical and scientific research, clinical trials, healthcare and cancer patient support; providing electronic publications, namely, online, non-downloadable books and magazines in the fields of investment, finance, medicine and healthcare; reference libraries of literature and documentary records; book rental; art exhibitions; publication of books; organization and arrangement of showing movies, shows, plays or musical performances; movie showing; production and distribution of films; production of radio and television programs; production of videotapes and films in the field of education, culture, entertainment or sports, not for movies or television programs and not for advertising or publicity; organization, arranging and conducting of sports competitions; organization, arranging and conducting of social entertainment events excluding movies, shows, plays, musical performances, sports, horse races, bicycle races, boat races and auto races; providing facilities for movies, shows, plays, music or educational training; educational training services for pharmaceutical representatives, business ventures, and people who are interested in business ventures in the field of clinical trials for pharmaceuticals; medical training and teaching; education services, namely, providing training in the field of medical science, medical technology and pharmaceutical preparations, and providing information relating thereto; educational services, namely, conducting classes, seminars and workshops in the fields of investment and finance; business education and training services, namely, providing business education programs to employees and executives; consulting services about education and providing information about education relating thereto; education, teaching and training, namely, conducting classes, seminars and workshops in the field of pharmaceuticals, and providing educational information relating thereto; online academic library services; rental of printed matter, namely, books; publication of printed matter and texts, other than publicity texts; publication of online electronic books and periodicals; copy editing of printed matter and texts, other than publicity texts; video production; entertainment services, namely, providing online, non-downloadable videos in the field of entertainment production featuring sounds, music, images, videos and textual information via communications networks; arranging, conducting and organization of educational conferences, congresses, colloquiums, training workshops, seminars and symposiums in the field of sports, arts, investment, finance, business development, artificial intelligence, biotechnology, pharmaceuticals, medical device, diagnostics, digital health, medical and scientific research, clinical trials, healthcare and cancer patient support, and providing educational information relating thereto; educational services, namely, conducting classes, seminars, and workshops in the field of human resource development and capacity development; educational services, namely, conducting classes, seminars, and workshops in the field of corporate business revitalization; educational services, namely, conducting classes, seminars and workshops in the field of financial management and business evaluations; education and training for managers, business owners and general employees, namely, conducting classes, seminars and workshops in the field of business marketing and management; educational services, namely, conducting classes, seminars and workshops in the field of financial, investment and retirement plans
84.
TREATMENT METHODS FOR SUBJECTS HAVING CANCER WITH A DYSREGULATED MAPK AND/OR PI3K PATHWAY
A method of treating a subject with cancer having a dysregulated MAPK and/or PI3K pathway, whereby the subject is administered an effective amount of 4-(4-(3-((2-(tert-butylamino)ethyl)amino)-6-(5-(trifluoromethyl)-l,3,4-oxadiazol-2-yl)pyridin-2-yl)piperidin-l-yl)-5,5-dimethyl-5H-pyrolo[2,3-d]pyrimidin-6(7H)-one or a pharmaceutically acceptable salt thereof.
The present disclosure relates to a juniper pollen protein selected from (a)-(c) below. (a) A protein comprising an amino acid sequence represented by SEQ ID NO: 2. (b) A protein comprising an amino acid sequence represented by SEQ ID NO: 2 with one or more amino acids substituted, deleted, or added, and having a juniper pollen allergen activity. (c) A protein having at least 90% amino acid identity with the amino acid sequence represented by SEQ ID NO: 2, and having a juniper pollen allergen activity.
The present disclosure relates to a juniper pollen protein selected from (a)-(c) below. (a) A protein comprising an amino acid sequence represented by SEQ ID NO: 2. (b) A protein comprising an amino acid sequence represented by SEQ ID NO: 2 with one or more amino acids substituted, deleted, or added, and having a juniper pollen allergen activity. (c) A protein having at least 90% amino acid identity with the amino acid sequence represented by SEQ ID NO: 2, and having a juniper pollen allergen activity.
The present invention relates to a process for producing 4-(2-fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide, including: coupling 4-(4-amino-2-fluorophenoxy)-7-methoxy-N-methylquinoline-6-carboxamide to 2-phenylacetyl isothiocyanate.
Provided is a novel cancer treatment method which exhibits a remarkably excellent antitumor effect with little side effects. An antitumor agent includes a biphenyl compound for use in a treatment of a subject having cancer. The treatment comprises administering an immune checkpoint molecule regulator to the subject.
A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
A61K 45/00 - Préparations médicinales contenant des ingrédients actifs non prévus dans les groupes
The present invention provides a compound represented by formula (I) or a pharmaceutically acceptable salt thereof which has the effect of antagonizing the LPA1 receptor.
C07C 275/16 - Dérivés d'urée, c.-à-d. composés contenant l'un des groupes les atomes d'azote ne faisant pas partie de groupes nitro ou nitroso ayant des atomes d'azote de groupes urée liés à des atomes de carbone acycliques d'un squelette carboné acyclique et saturé étant substitué de plus par des groupes carboxyle
C07C 275/26 - Dérivés d'urée, c.-à-d. composés contenant l'un des groupes les atomes d'azote ne faisant pas partie de groupes nitro ou nitroso ayant des atomes d'azote de groupes urée liés à des atomes de carbone de cycles autres que des cycles aromatiques à six chaînons
C07D 209/14 - Radicaux substitués par des atomes d'azote ne faisant pas partie d'un radical nitro
C07D 309/14 - Atomes d'azote ne faisant pas partie d'un radical nitro
C07D 319/18 - Éthylènedioxybenzènes, non substitués sur l'hétérocycle
C07D 307/79 - Benzo [b] furannesBenzo [b] furannes hydrogénés avec uniquement des atomes d'hydrogène, des radicaux hydrocarbonés ou des radicaux hydrocarbonés substitués, liés directement aux atomes de carbone de l'hétérocycle
C07D 333/54 - Benzo [b] thiophènesBenzo [b] thiophènes hydrogénés avec uniquement des atomes d'hydrogène, des radicaux hydrocarbonés ou des radicaux hydrocarbonés substitués, liés directement aux atomes de carbone de l'hétérocycle
C07D 335/02 - Composés hétérocycliques contenant des cycles à six chaînons comportant un atome de soufre comme unique hétéro-atome du cycle non condensés avec d'autres cycles
C07C 311/01 - Sulfonamides ayant des atomes de soufre de groupes sulfonamide liés à des atomes de carbone acycliques
C07D 271/113 - Oxadiazoles-1, 3, 4Oxadiazoles-1, 3, 4 hydrogénés avec des atomes d'oxygène, de soufre ou d'azote, liés directement aux atomes de carbone du cycle, les atomes d'azote ne faisant pas partie d'un radical nitro
A pharmaceutical composition for treating cartilage dysplasia, comprising 1-[(3S)-3-[4-amino-3-[2-(3,5-dimethoxyphenyl)ethynyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-pyrrolidinyl]-2-propen-1-one or a pharmaceutically acceptable salt thereof, and a treatment method using the pharmaceutical composition.
2 administered as a one hour (1 h) infusion. Also provided are methods of treatment using a solid oral dosage form according to an embodiment of the invention.
A61K 31/706 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
A61K 31/20 - Acides carboxyliques, p. ex. acide valproïque ayant un groupe carboxyle lié à une chaîne acyclique d'au moins sept atomes de carbone, p. ex. acides stéarique, palmitique ou arachidique
A61K 31/7016 - Disaccharides, p. ex. lactose, lactulose
In one embodiment, the present invention provides an antibody specifically binding to human GH, or an antigen-binding fragment thereof. In one embodiment, the present invention pertains to an antibody specifically binding to human GH, or an antigen-binding fragment thereof, the antibody or antigen-binding fragment thereof comprising a heavy chain variable region (VH) and a light chain variable region (VL), wherein: the VH includes the amino acid sequence of SEQ ID NO: 5 as a VH complementarity determining region (CDR) 1 (VHCDR1), the amino acid sequence of SEQ ID NO: 6 as a VHCDR2, and the amino acid sequence of SEQ ID NO: 7 as a VHCDR3; and the VL includes the amino acid sequence of SEQ ID NO: 8 as a VL complementarity determining region (CDR) 1 (VLCDR1), the amino acid sequence of SEQ ID NO: 9 as a VLCDR2, and the amino acid sequence of SEQ ID NO: 10 as a VLCDR3.
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
A61P 3/10 - Médicaments pour le traitement des troubles du métabolisme de l'homéostase du glucose de l'hyperglycémie, p. ex. antidiabétiques
A61P 5/08 - Médicaments pour le traitement des troubles du système endocrinien des hormones de l'hypophyse antérieure, p. ex. TSH, ACTH, FSH, LH, PRL, GH pour réduire, bloquer ou contrarier l'activité des hormones de l'hypophyse antérieure
A61P 11/00 - Médicaments pour le traitement des troubles du système respiratoire
A61P 13/12 - Médicaments pour le traitement des troubles du système urinaire des reins
A61P 19/02 - Médicaments pour le traitement des troubles du squelette des troubles articulaires, p. ex. arthrites, arthroses
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
[Problem] Provided is a novel therapeutic agent for chronic glomerulonephritis.
[Problem] Provided is a novel therapeutic agent for chronic glomerulonephritis.
[Solution] A therapeutic agent for chronic glomerulonephritis comprising, as an active ingredient, a compound represented by the following general formula (I) or a salt thereof:
[Problem] Provided is a novel therapeutic agent for chronic glomerulonephritis.
[Solution] A therapeutic agent for chronic glomerulonephritis comprising, as an active ingredient, a compound represented by the following general formula (I) or a salt thereof:
[Problem] Provided is a novel therapeutic agent for chronic glomerulonephritis.
[Solution] A therapeutic agent for chronic glomerulonephritis comprising, as an active ingredient, a compound represented by the following general formula (I) or a salt thereof:
[Selected Drawing] None
The present invention provides an agent for adjuvant therapy of tumors that exerts remarkable inhibitory effects on tumor metastasis and recurrence while developing few side effects. The agent for adjuvant therapy comprises, as an active ingredient, a peptide having 4 linked CTL epitopes.
A61K 39/39 - Préparations médicinales contenant des antigènes ou des anticorps caractérisées par les additifs immunostimulants, p. ex. par les adjuvants chimiques
A61K 38/16 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés
A61K 47/65 - Séquences de liaison, liants ou bras-espaceurs peptidiques, p. ex. séquences de liaison peptidiques vulnérable aux protéases
The invention provides new pyrazine derivatives of formula (I):
The invention provides new pyrazine derivatives of formula (I):
The invention provides new pyrazine derivatives of formula (I):
or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein. The invention also provides pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61K 9/19 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p. ex. poudres lyophilisées
C07D 519/00 - Composés hétérocycliques contenant plusieurs systèmes de plusieurs hétérocycles déterminants condensés entre eux ou condensés avec un système carbocyclique commun non prévus dans les groupes ou
The present invention provides a phenol compound represented by the following Formula (I) or a salt thereof:
The present invention provides a phenol compound represented by the following Formula (I) or a salt thereof:
The present invention provides a phenol compound represented by the following Formula (I) or a salt thereof:
wherein R1, R2, R5, L1, L2, L3, A, X, and m are as described in the specification.
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 205/04 - Composés hétérocycliques comportant des cycles à quatre chaînons ne contenant qu'un atome d'azote comme unique hétéro-atome du cycle non condensés avec d'autres cycles ne comportant pas de liaison double entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques
C07D 409/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07D 417/10 - 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 carbonée contenant des cycles aromatiques
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
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 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
97.
4-AMINOBUT-2-ENAMIDE DERIVATIVES AND SALTS THEREOF
The present invention provides an antitumor agent comprising a compound or a pharmaceutically acceptable salt thereof that covalently binds to GTP-bound KRASG12C as an active ingredient.
The invention relates to methods of synthesizing 2′-deoxy-2′,2′-difluorotetrahydrouridine with increased purity and uniform particle size distribution. In particular, methods of the invention include crystallization and isolation procedures rendering synthetic reaction intermediates. The invention further includes compositions comprising the final compound in highly pure form, including lower number of impurities and lower levels of individual and total impurities.
A benzoic acid salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile is provided. A sorbic acid salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile is also provided.
A method of treating an LSD1-related disease or disorder in a patient in need, the method comprising administering an effective amount of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile or a salt thereof to the patient on an administration schedule comprising daily dosing for one week or two weeks, followed by a resting period of one week.
A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
