Abstract: Disclosed is a trifluoromethyl-substituted sulfonamide BCL-2-selective inhibitor, in particular disclosed are a compound of formula I, a stereoisomer or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition thereof. Also disclosed are the uses of said compound and of a pharmaceutical composition comprising same for treating anti-apoptotic BCL-2-related diseases, such as cancer.

Abstract: The present application relates to a macrocycle containing aminopyrazole and pyrimidine, which is represented by formula (I), a pharmaceutical composition thereof, and a use thereof in inhibiting tropomyosin receptor kinase (Trk) activity and in treating diseases in mammals that are mediated by Trk.

Abstract: Disclosed are a crystal of a maleate of a compound of formula (I), a preparation method for the crystal, a crystallization composition of same, a pharmaceutical composition of same, and uses thereof in preventing and treating a tumor.

Abstract: The present application belongs to the field of medicinal chemistry, and relates to crystals of an aniline pyrimidine compound serving as an EGFR inhibitor. Specifically, the present application relates to crystal A, crystal B and crystal C of N-(2-((2-(dimethyl amino)ethyl)(methyl)amino)-4-methoxy-5-(4-(3-methyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazole-1-base)pyrimidine-2-base amino)phenyl)acrylamide (formula I) hydrochloride, and also relates to the method for preparing the crystal A, the crystal B and the crystal C, a crystal composition comprising the crystal A, the crystal B, and the crystal C, a pharmaceutical composition comprising the crystal A, the crystal B and the crystal C or the crystal composition thereof, and medical uses thereof. The crystal A, the crystal B and the crystal C in the present application has the advantages of high purity, high crystallization degree, good stability and the like.

Abstract: The present application relates to a macrocycle containing aminopyrazole and pyrimidine, which is represented by formula (1), a pharmaceutical composition thereof, and a use thereof in inhibiting tropornyosin receptor kinase (Trk) activity and in treating diseases in mammals that are mediated by Trk.

Abstract: Provided is a method for preparing an intermediate of 6-arylaminopyridonecarboxamide compound as an MEK inhibitor, comprising preparing a compound of formula (III) as an intermediate of 6-arylaminopyridonecarboxamide compound using a compound of formula V as a raw material.

Abstract: The present application belongs to the field of medicinal chemistry, and relates to crystals of an aniline pyrimidine compound serving as an EGFR inhibitor. Specifically, the present application relates to crystal A, crystal B and crystal C of N-(2-((2-(dimethyl amino)ethyl)(methyl)amino)-4-methoxy-5-(4-(3-methyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazole-1-base)pyrimidine-2-base amino)phenyl)acrylamide (formula I) hydrochloride, and also relates to the method for preparing the crystal A, the crystal B and the crystal C, a crystal composition comprising the crystal A, the crystal B, and the crystal C, a pharmaceutical composition comprising the crystal A, the crystal B and the crystal C or the crystal composition thereof, and medical uses thereof. The crystal A, the crystal B and the crystal C in the present application has the advantages of high purity, high crystallization degree, good stability and the like.

Abstract: The disclosure relates to a crystal of an aniline pyrimidine compound of trifluoroethyl substituted indole and a salt thereof as an EGFR inhibitor, specifically relates to a crystal of a compound represented by formula I, a crystal of monomethyl sulfonate of the compound represented by formula I or a crystal of dimethyl sulfonate of the compound represented by formula I, and further relates to a method for preparing the crystal, a crystalline composition comprising the crystal, or a pharmaceutical composition comprising the crystal or a crystalline composition thereof, and a medical use thereof.

Abstract: Disclosed are a crystal of a maleate of a compound of formula (I), a preparation method for the crystal, a crystallization composition of same, a pharmaceutical composition of same, and uses thereof in preventing and treating a tumor.

Abstract: Provided is a method for preparing an intermediate of 6-arylaminopyridonecarboxamide compound as an MEK inhibitor, comprising preparing a compound of formula (III) as an intermediate of 6-arylaminopyridonecarboxamide compound using a compound of formula V as a raw material.

Abstract: The present invention provides a crystal of 6-arylamino pyridone carboxamide compound and a preparation method thereof. The crystal is obtained by dissolving 6-(2-chloro-4-iodophenylamino)-N-(2-hydroxylethyoxyl)-5-methyl-4-oxo-4,5-dihydrofuro[3,2-c]pyridin-7-carboxamide in an aprotic polar solvent and adding a second solvent thereto. The crystallization method has the advantage of simple and convenient operations, and is beneficial to an industrial production. The resulting crystal has the advantage a high purity and good stability, and is benefit to the manufacture and storage of a medicament containing the same.

Abstract: The present invention provides a crystal of 6-arylamino pyridone carboxamide compound and a preparation method thereof. The crystal is obtained by dissolving 6-(2-chloro-4-iodophenylamino)-N-(2-hydroxylethyoxyl)-5-methyl-4-oxo-4,5-dihydrofuro[3,2-c]pyridin-7-carboxamide in an aprotic polar solvent and adding a second solvent thereto. The crystallization method has the advantage of simple and convenient operations, and is beneficial to an industrial production. The resulting crystal has the advantage a high purity and good stability, and is benefit to the manufacture and storage of a medicament containing the same.