Related to macrocyclic compounds and therapeutic uses thereof. Discloses a compound of formula (I), or a pharmaceutically acceptable salt thereof, a solvate thereof or a solvate of the pharmaceutically acceptable salt, and their use for the preparation of a medicament of treatment of cancer.
C07D 487/12 - Composés hétérocycliques contenant des atomes d'azote comme uniques hétéro-atomes dans le système condensé, non prévus par les groupes dans lesquels le système condensé contient trois hétérocycles
C07D 471/22 - Composés hétérocycliques contenant des atomes d'azote comme uniques hétéro-atomes du système condensé, au moins un cycle étant un cycle à six chaînons avec un atome d'azote, non prévus dans les groupes dans lesquels le système condensé contient au moins quatre hétérocycles
A61K 31/504 - PyridazinesPyridazines hydrogénées formant une partie de systèmes cycliques pontés
The present application relates to the field of pharmaceutical chemistry. Specifically, the present application relates to a triaromatic ring derivative, specifically a salt of (6-((5-(3-(4-(trifluoromethyl)phenyl)-1,2,4-oxadiazole-5-yl)pyrazine-2-yl)oxy)-1-methyl-1H-indol-2-yl)(4-(4-(2,2,2-trifluoroethoxy)benzyl)piperazin-1-yl)methanone, a crystal form thereof, a pharmaceutical composition thereof, a preparation method therefor, and a use thereof. The salt and the crystal form thereof provided in the present application have good stability, high solubility, high bioavailability, good efficacy, good tablet dissolution, good tablet compressibility, good fluidity, good crystal morphology, good crystal particle size distribution, can be stably stored, and have a simple and reliable preparation method and great development value.
C07D 413/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
A61K 31/497 - Pyrazines non condensées contenant d'autres hétérocycles
The present invention relates to a novel boron containing compounds and a pharmaceutical acceptable salt thereof, and their use for the preparation of a medicament of treatment of cancer. The compounds in the present disclosure have specifically ability to kill ERa positive cancer cells and show dramatically therapeutical potential.
Provided are a polymorph of an EP4 receptor antagonist, a preparation method therefor and a use thereof, relating in particular to a polymorph of an EP4 receptor antagonist (S)-4-(1-(2-(4-fluorobenzyl)-4, 7-dihydro-5H-thieno [2,3-c]pyran-3-carboxamido) ethyl) benzoic acid, a preparation method therefor and a use thereof. Compared with an amorphous form of a compound represented by formula I, the polymorph of the present invention has higher stability and better processing performance and is very suitable for being prepared into a medicine
Provided are a polymorph of an EP4 receptor antagonist, a preparation method therefor and a use thereof, relating in particular to a polymorph of an EP4 receptor antagonist ( S)-4-(1-(2-( 4-fluorobenzyl)-4, 7-dihydro-SH-thieno [2,3-c ] pyran-3- carboxamido) ethyl) benzoicacid,a preparation method therefor and a use thereof. Compared with an amorphous form of a compound represented by formula I, the polymorph of the present invention has higher stability and better processing performance and is very suitable for being prepared into a medicine.
Provided are a polymorph of an EP4 receptor antagonist, a preparation method therefor and a use thereof, relating in particular to a polymorph of an EP4 receptor antagonist (S)-4-(1-(2-(4-fluorobenzyl) )-4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxamido)ethyl)benzoic acid, a preparation method therefor and a use thereof. Compared with an amorphous form of a compound represented by formula I, the polymorph of the present invention has higher stability and better processing performance and is very suitable for being prepared into a medicine.
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
A61P 19/00 - Médicaments pour le traitement des troubles du squelette
Disclosed by the present invention are a thienocyclic compound represented by formula (I), a pharmaceutically acceptable salt or a hydrate thereof, a composition containing the thienocyclic compound, and a preparation method therefor. Further disclosed by the present invention is an application of the thienocyclic compound as a prostaglandin EP4 receptor antagonist that is used for preventing and treating prostaglandin PGE2-mediated diseases, comprising malignant tumors, autoimmune diseases, inflammation, pain and osteoarthritis
Disclosed by the present invention are a thienocyclic compound represented by formula (I), a pharmaceutically acceptable salt or a hydrate thereof, a composition containing the thienocyclic compound, and a preparation method therefor. Further disclosed by the present invention is an application of the thienocyclic compound as a prostaglandin EP4 receptor antagonist that is used for preventing and treating prostaglandin PGE2-mediated diseases, comprising malignant tumors, autoimmune diseases, inflammation, pain and osteoarthritis
C07D 333/78 - Composés hétérocycliques contenant des cycles à cinq chaînons comportant un atome de soufre comme unique hétéro-atome du cycle condensés avec des carbocycles ou avec des systèmes carbocycliques condensés avec des cycles autres que des cycles à six chaînons ou avec des systèmes cycliques contenant de tels cycles
C07D 333/68 - Atomes de carbone comportant trois liaisons à des hétéro-atomes avec au plus une liaison à un halogène
Provided is a combination of an EP4 receptor antagonist and a PD-1 inhibitor for treating cancer. Specifically, provided is a product combination comprising: (i) a first pharmaceutical composition comprising (a) a first active ingredient, where the first active ingredient comprises an EP4 receptor antagonist and a pharmaceutically acceptable carrier; and (ii) a second pharmaceutical composition comprising (b) a second active ingredient, where the second active ingredient comprises a PD-1 inhibitor and a pharmaceutically acceptable carrier. The first pharmaceutical composition and the second pharmaceutical composition are different pharmaceutical compositions or the same pharmaceutical composition. The product combination of the present invention can synergistically treat malignant tumors.
C07D 333/78 - Composés hétérocycliques contenant des cycles à cinq chaînons comportant un atome de soufre comme unique hétéro-atome du cycle condensés avec des carbocycles ou avec des systèmes carbocycliques condensés avec des cycles autres que des cycles à six chaînons ou avec des systèmes cycliques contenant de tels cycles
C07D 333/68 - Atomes de carbone comportant trois liaisons à des hétéro-atomes avec au plus une liaison à un halogène
A61K 31/381 - Composés hétérocycliques ayant le soufre comme hétéro-atome d'un cycle ayant des cycles à cinq chaînons
A61K 31/4436 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle
A61K 31/4365 - 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 ayant le soufre comme hétéro-atome du cycle, p. ex. ticlopidine
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
Disclosed are a class of triaromatic compounds targeting a bifunctional phosphorylation site of STAT3, such as compounds represented by formulas (I) to (V), or pharmaceutically acceptable salts, hydrates, solvates, metabolites or prodrugs thereof. Further proposed are pharmaceutical compositions comprising the compounds represented by formulas (I) to (V). Further proposed are applications of the triaromatic compounds in the preparation of drugs for preventing and/or treating diseases caused or regulated by activation of the bifunctional phosphorylation site of STAT3.
C07D 413/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
10.
CLASS OF TRIAROMATIC COMPOUNDS TARGETING BIFUNCTIONAL PHOSPHORYLATION SITE OF STAT3 AND APPLICATIONS THEREOF
Disclosed are a class of triaromatic compounds targeting a bifunctional phosphorylation site of STAT3, such as compounds represented by formulas (I) to (V), or pharmaceutically acceptable salts, hydrates, solvates, metabolites or prodrugs thereof. Further proposed are pharmaceutical compositions comprising the compounds represented by formulas (I) to (V). Further proposed are applications of the triaromatic compounds in the preparation of drugs for preventing and/or treating diseases caused or regulated by activation of the bifunctional phosphorylation site of STAT3.
C07D 413/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
A61K 31/497 - Pyrazines non condensées contenant d'autres hétérocycles
brevets
