Abrégé

A method for treating cholangiocarcinoma having PTEN gene mutation and/or deletion, which method specifically comprises administering, to a patient with cholangiocarcinoma, a therapeutically effective amount of a proteasome inhibitor as shown in formula (I) or formula (II) or a pharmaceutically acceptable salt thereof. Preferably, the cholangiocarcinoma is cholangiocarcinoma having PTEN gene mutation and/or deletion. The method overcomes the problem of an existing protease inhibitor having no therapeutic effect in the treatment of solid tumors due to drug distribution issues, and shows good efficacy in patients with cholangiocarcinoma, especially, cholangiocarcinoma caused by PTEN gene mutation and/or deletion.

Classes IPC  ?

• A61K 31/69 - Composés du bore
• A61P 35/00 - Agents anticancéreux

Abrégé

Disclosed in the present invention is a compound for regulating the activity of microRNA-124. The compound has a structure as represented by formula (I), and the compound can be used for preventing or treating inflammatory diseases including, but not limited to, inflammatory bowel disease, rheumatoid arthritis, Crohn's disease, ulcerative colitis, multiple sclerosis, Alzheimer's disease, Parkinson's disease, osteoarthritis, atherosclerosis, ankylosing spondylitis, psoriasis, dermatitis, Sjogren's syndrome, bronchitis, asthma, and inflammation associated with colon cancer, and in particular, inflammatory bowel disease, rheumatoid arthritis, Crohn's disease, ulcerative colitis, multiple sclerosis, osteoarthritis, ankylosing spondylitis, psoriasis, Sjogren's syndrome, bronchitis, and inflammation associated with colon cancer.

Classes IPC  ?

• 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 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
• 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 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 31/4545 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un cycle à six chaînons avec l'azote comme hétéro-atome du cycle, p. ex. pipampérone, anabasine
• A61K 31/496 - Pipérazines non condensées contenant d'autres hétérocycles, p. ex. rifampine, thiothixène ou sparfloxacine
• A61K 31/501 - PyridazinesPyridazines hydrogénées non condensées et contenant d'autres hétérocycles
• A61P 15/00 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs

Abrégé

A compound for treating diseases related to cerebral ischemic injury. The structure of the compound is as represented by formula (II) below. The compound exhibits higher bioavailability and higher distribution concentrations in rat plasma and brain tissues, and shows a good efficacy in the treatment of ischemic brain injury. A compound for treating diseases related to cerebral ischemic injury. The structure of the compound is as represented by formula (II) below. The compound exhibits higher bioavailability and higher distribution concentrations in rat plasma and brain tissues, and shows a good efficacy in the treatment of ischemic brain injury.

Classes IPC  ?

• C07D 307/83 - Atomes d'oxygène
• A61K 31/365 - Lactones
• A61P 9/10 - Médicaments pour le traitement des troubles du système cardiovasculaire des maladies ischémiques ou athéroscléreuses, p. ex. médicaments antiangineux, vasodilatateurs coronariens, médicaments pour le traitement de l'infarctus du myocarde, de la rétinopathie, de l'insuffisance cérébro-vasculaire, de l'artériosclérose rénale
• A61P 25/00 - Médicaments pour le traitement des troubles du système nerveux

Abrégé

The present invention provides a heteroaromatic ring compound serving as a CDK7 kinase inhibitor, preparation thereof, and a use thereof. The heteroaromatic ring compound is a compound having the structure of formula (I) or a pharmaceutically acceptable salt, ester, stereoisomer, solvent compound or prodrug thereof. The present invention also provides a pharmaceutical composition comprising the compound having the structure of formula (I) or the pharmaceutically acceptable salt, ester, stereoisomer, solvent compound or prodrug thereof. The present invention further provides a use of the compound having the structure of formula (I) or the pharmaceutical composition in the preparation of a CDK7 kinase inhibitor and in the preparation of a drug for treating and/or inhibiting CDK-related diseases. The CDK7 kinase inhibitor compound of the present invention has an enzyme and cell level biological activity superior to that of disclosed similar target compounds and lower cardiotoxicity. The compound of the present invention provides more options for novel antitumor drugs, and has good prospects of application in drugs.

Classes IPC  ?

• C07D 487/04 - Systèmes condensés en ortho
• A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
• A61P 35/00 - Agents anticancéreux

Abrégé

Pharmaceutical formulations include N-(5-((4-(5,6-dihydro-4H-pyrrolo [3,2,1-ij]quinolin-1-yl)piperidin-2-yl)amino)-4-methoxy-2-(methyl(2-(methyl-d3)amino)ethyl)phenyl)acetamide or a pharmaceutically acceptable salt thereof as active ingredient, along with at least one pharmaceutically acceptable excipient, formulated as an orally administrable capsule dosage.

Classes IPC  ?

• 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 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat

Abrégé

A base addition salt of a compound represented by formula (I) and a salt crystal form thereof, a preparation method therefor and a use thereof, as well as a pharmaceutical composition containing a therapeutically effective amount of the salt or crystal form and a use thereof in the treatment of ischemic brain injury-related diseases, spinal cord injuries, and neurodegenerative diseases.

Classes IPC  ?

• C07D 307/83 - Atomes d'oxygène
• A61K 31/343 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à cinq chaînons avec un oxygène comme seul hétéro-atome d'un cycle, p. ex. isosorbide condensés avec un carbocycle, p. ex. coumarane, bufaralol, béfunolol, clobenfurol, amiodarone
• A61P 9/10 - Médicaments pour le traitement des troubles du système cardiovasculaire des maladies ischémiques ou athéroscléreuses, p. ex. médicaments antiangineux, vasodilatateurs coronariens, médicaments pour le traitement de l'infarctus du myocarde, de la rétinopathie, de l'insuffisance cérébro-vasculaire, de l'artériosclérose rénale
• A61P 25/00 - Médicaments pour le traitement des troubles du système nerveux

Abrégé

A heteroaromatic ring compound as a RET kinase inhibitor, and the preparation and the use thereof, wherein the compound is a compound having the structure of formula (I) or a pharmaceutically acceptable salt thereof. The compound or a salt thereof can be used for treating or preventing diseases or conditions by targeting receptors of fused and mutated forms of the RET gene, can effectively inhibit the growth of multiple tumor cells, produces an inhibitory effect on a RET gene fusion mutation and other proteases, and can be used for preparing an anti-tumor drug. A heteroaromatic ring compound as a RET kinase inhibitor, and the preparation and the use thereof, wherein the compound is a compound having the structure of formula (I) or a pharmaceutically acceptable salt thereof. The compound or a salt thereof can be used for treating or preventing diseases or conditions by targeting receptors of fused and mutated forms of the RET gene, can effectively inhibit the growth of multiple tumor cells, produces an inhibitory effect on a RET gene fusion mutation and other proteases, and can be used for preparing an anti-tumor drug.

Classes IPC  ?

• C07D 471/04 - Systèmes condensés en ortho
• 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
• A61P 35/00 - Agents anticancéreux

Abrégé

Disclosed are novel crystal forms of a peptide boric acid compound, and in particular, disclosed are three crystal forms: crystal form A, crystal form B and crystal form D, and preparation methods therefor. The three crystal forms are stable in appearance state and stable in storage, and are suitable for preparing pharmaceutical preparations; moreover, the preparation methods are simple, avoid the use of concentration operations, and are high in product clarity; therefore, the process is simple and efficient, large-scale production can be achieved, and the present invention is environmentally-friendly.

Classes IPC  ?

• C07F 5/02 - Composés du bore
• A61K 31/69 - Composés du bore
• A61P 35/00 - Agents anticancéreux

Abrégé

A compound for treating an ischemic brain injury-related disease. The structure of the compound is as represented by formula (II) below. The compound is high in bioavailability and high in distribution concentration in rat plasma and brain tissues, and has a good effect on ischemic brain injury.

Classes IPC  ?

• C07D 307/83 - Atomes d'oxygène
• A61K 31/343 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à cinq chaînons avec un oxygène comme seul hétéro-atome d'un cycle, p. ex. isosorbide condensés avec un carbocycle, p. ex. coumarane, bufaralol, béfunolol, clobenfurol, amiodarone
• A61P 9/10 - Médicaments pour le traitement des troubles du système cardiovasculaire des maladies ischémiques ou athéroscléreuses, p. ex. médicaments antiangineux, vasodilatateurs coronariens, médicaments pour le traitement de l'infarctus du myocarde, de la rétinopathie, de l'insuffisance cérébro-vasculaire, de l'artériosclérose rénale
• A61P 25/00 - Médicaments pour le traitement des troubles du système nerveux

Abrégé

33)amino)ethyl)amino)phenyl)acetamide or a pharmaceutically acceptable salt thereof as an active ingredient, and at least one pharmaceutically acceptable excipient, and is prepared into a clinically acceptable oral formulation. The formulation can ensure that the active ingredient have good stability and dissolution effect, the produced samples have good dissolution uniformity in different dissolution mediums, the production process steps are simple, and the yield is higher.

Classes IPC  ?

• A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
• A61K 9/20 - Pilules, pastilles ou comprimés
• C07D 471/06 - Systèmes condensés en péri
• C07B 59/00 - Introduction d'isotopes d'éléments dans les composés organiques
• A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
• A61P 35/00 - Agents anticancéreux
• A61P 35/02 - Agents anticancéreux spécifiques pour le traitement de la leucémie

Abrégé

Disclosed are a heteroaromatic ring compound as a RET kinase inhibitor, and the preparation and the use thereof, wherein the compound is a compound having the structure of formula (I) or a pharmaceutically acceptable salt thereof. The compound or a salt thereof can be used for treating or preventing diseases or conditions by targeting receptors of fused and mutated forms of the RET gene, can effectively inhibit the growth of multiple tumor cells, produces an inhibitory effect on a RET gene fusion mutation and other proteases, and can be used for preparing an anti-tumor drug.

Classes IPC  ?

• C07D 471/04 - Systèmes condensés en ortho
• 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
• A61P 35/00 - Agents anticancéreux

Abrégé

A peptide borate ester compound or a pharmaceutical salt thereof, a preparation method for same, and pharmaceutical applications thereof. The structure of the peptide borate ester compound or of the pharmaceutical salt thereof is as represented by formula (I). The compound is applicable in preparing a proteasome inhibitor, applicable in treating a solid tumor and hematoma.

Classes IPC  ?

• C07F 5/04 - Esters des acides boriques
• A61K 31/69 - Composés du bore
• A61P 35/00 - Agents anticancéreux

Abrégé

Disclosed in the present invention are deuterated 3-(4,5-substituted pyrimidinamine) phenyl derivatives and applications thereof. The deuterated 3-(4,5-substituted pyrimidinamine) phenyl derivatives are compounds of a structure of formula (I) or pharmacologically acceptable salts thereof. The compounds or the salts thereof can be used for treating or preventing diseases or states of illnesses by means of certain mutant forms of epidermal growth factor receptors (EGFRs), can effectively inhibit the growth of multiple kinds of tumor cells, have an inhibiting effect on other proteases of the EGFRs and Her families, and can be used in the preparation of antitumor drugs.

Classes IPC  ?

• C07D 471/06 - Systèmes condensés en péri
• A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
• A61P 35/00 - Agents anticancéreux
• A61P 35/02 - Agents anticancéreux spécifiques pour le traitement de la leucémie