Abstract: The present invention relates to the technical field of pharmaceuticals, and in particular to a ketohexokinase inhibitor compound, a pharmaceutically acceptable salt, an ester or a stereoisomer thereof, a pharmaceutical composition and formulation containing the compound, the pharmaceutically acceptable salt, the ester or the stereoisomer thereof; a method for preparing the compound, the pharmaceutically acceptable salt, the ester or the stereoisomer thereof; and use of the compound, the pharmaceutically acceptable salt, the ester or the stereoisomer thereof in the manufacture of a medicament for treating and/or preventing KHK-mediated diseases and related conditions.

Abstract: Provided are a maleate of a quinazoline derivative-like tyrosine kinase inhibitor represented by Formula (1), and a crystal form thereof and a preparation method therefor, a pharmaceutical composition comprising the maleate and the crystal form thereof, as well as use of the maleate and the crystal form thereof in the manufacture of a medicament for treating and/or preventing a hyperproliferative disease and a chronic obstructive pulmonary disease.

Abstract: The present invention relates to biaryloxy derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channel is involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.

Abstract: Provided are a maleate of a quinazoline derivative-like tyrosine kinase inhibitor represented by Formula (1), and a crystal form thereof and a preparation method therefor, a pharmaceutical composition comprising the maleate and the crystal form thereof, as well as use of the maleate and the crystal form thereof in the manufacture of a medicament for treating and/or preventing a hyperproliferative disease and a chronic obstructive pulmonary disease.

Abstract: The present invention relates to biaryloxy derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channel is involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.

Abstract: The invention relates to Crystal form I, Crystal form II and Crystal form III of N-(4-((3-chloro-4-fluorophenyl)amino)-7-((7-methyl-7-azaspiro[3.5]nonan-2-yl)methoxy)quinazolin-6-yl)acrylamide represented by the following Formula (I), and preparation methods thereof, wherein the Crystal form I has an X-ray powder diffraction pattern having characteristic peaks at the 2? positions of 6.7±0.2°, 7.9±0.2°, 8.6±0.2°, 12.0±0.2°, 13.9±0.2°, 15.9±0.2°, 17.3±0.2°, 18.3±0.2°, 18.7±0.2°, 21.0±0.2°, and 23.0±0.2°, as determined by using Cu-K? radiation; the Crystal form II has an X-ray powder diffraction pattern having characteristic peaks at the 2? positions of 6.9±0.2°, 8.5±0.2°, 14.8±0.2°, 15.6±0.2°, 16.7±0.2°, 17.1±0.2°, 17.9±0.2°, 18.7±0.2°, 19.1±0.2°, 21.5±0.2°, 23.5±0.2°, and 25.7±0.2°, as determined by using Cu-K? radiation; and the Crystal form III has an X-ray powder diffraction pattern having characteristic peaks at the 2? positions of 4.9±0.2°, 6.1±0.2°, 7.4±0.2°, 11.4±0.2°, 12.2±0.2°, 16.6±0.2°, and 18.4±0.

Abstract: The present invention relates to a crystalline form of a co-crystal of an inhibitor against sodium-glucose cotransporter 2 with L-proline, a method for preparing the same, a pharmaceutical composition comprising the same, and use thereof. Specifically, the present invention relates to a crystalline form of a co-crystal of an inhibitor against sodium-glucose cotransporter 2 represented by formula (1), i.e., (2S,3R,4R,5S,6R)-2-(3-(4-(((1R,3s,5S)-bicyclo[3.1.0]hexan-3-yl)oxy)benzyl)-4-chlorophenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol, with L-proline, a method for preparing the same, a pharmaceutical composition comprising the same, and use thereof.

Abstract: The invention relates to Crystal form I and Crystal form II of dihydrochloride of N-(4-((3-chloro-4-fluorophenyl)amino)-7-((7-methyl-7-azaspiro[3.5]nonan-2-yl)methoxy)quinazolin-6-yl)acrylamide represented by the following Formula (I), and preparation methods therefor, wherein the Crystal form I has an X-ray powder diffraction pattern having characteristic peaks at the 2? positions of 6.0±0.2°, 7.3±0.2°, 11.7±0.2°, 12.9±0.2°, 18.4±0.2°, 24.7±0.2°, and 26.3±0.2°, as determined by using Cu-K? radiation, and the Crystal form II has an X-ray powder diffraction pattern having characteristic peaks at the 2? positions of 5.0±0.2°, 7.0±0.2°, 10.1±0.2°, 17.0±0.2°, 26.0±0.2°, and 26.5±0.2°, as determined by using Cu-K? radiation.

Abstract: The invention relates to quinazoline derivatives substituted by aniline which are represented by the below formula (I), pharmaceutical acceptable salts and stereoisomer thereof, wherein these groups of R1, R2, R3, R4, R5, R6, L and n have the meanings given in the specification. The invention also relates to preparation methods, pharmaceutical compositions, pharmaceutical preparation and the use for preparation of medicine of treating excessive hyperplasia and chronic obstructive pulmonary disease and uses for treating excessive hyperplasia and chronic obstructive pulmonary disease thereof.

Abstract: Disclosed is a compound of Formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof, or their stereoisomers, which can be used as tyrosine kinase inhibitor. Also disclosed is a method for preparing the compound, a pharmaceutical composition and a kit comprising the compound, and uses of the compound. The compound can be used as tyrosine kinase inhibitor, or can be used to reduce or inhibit activity of EGFR or mutant thereof, such as EGFR mutant comprising T790M mutation, in a cell, or to treat and/or prevent a disease associated with overactivity of EGFR, such as cancer.

Abstract: The invention relates to Crystal form I and Crystal form II of dihydrochloride of N-(4-((3-chloro-4-fluorophenyl)amino)-7-((7-methyl-7-azaspiro[3.5]nonan-2-yl)methoxy)quinazoli n-6-yl)acrylamide represented by the following Formula (I), and preparation methods therefor, wherein the Crystal form I has an X-ray powder diffraction pattern having characteristic peaks at the 2? positions of 6.0±0.2°, 7.3±0.2°, 11.7±0.2°, 12.9±0.2°, 18.4±0.2°, 24.7±0.2°, and 26.3±0.2°, as determined by using Cu-K? radiation, and the Crystal form II has an X-ray powder diffraction pattern having characteristic peaks at the 2? positions of 5.0±0.2°, 7.0±0.2°, 10.1±0.2°, 17.0±0.2°, 26.0±0.2°, and 26.5±0.2°, as determined by using Cu-K? radiation.

Abstract: The invention relates to Crystal form I, Crystal form II and Crystal form III of N-(4-((3-chloro-4-fluorophenyl)amino)-7-((7-methyl-7-azaspiro[3.5]nonan-2-yl)methoxy)quinazolin-6-yl)acrylamide represented by the following Formula (I), and preparation methods thereof, wherein the Crystal form I has an X-ray powder diffraction pattern having characteristic peaks at the 20 positions of 6.7±0.2°, 7.9±0.2°, 8.6±0.2°, 12.0±0.2°, 13.9±0.2°, 15.9±0.2°, 17.3±0.2°, 18.3±0.2°, 18.7±0.2°, 21.0±0.2°, and 23.0±0.2°, as determined by using Cu-K? radiation; the Crystal form II has an X-ray powder diffraction pattern having characteristic peaks at the 20 positions of 6.9±0.2°, 8.5±0.2°, 14.8±0.2°, 15.6±0.2°, 16.7±0.2°, 17.1±0.2°, 17.9±0.2°, 18.7±0.2°, 19.1±0.2°, 21.5±0.2°, 23.5±0.2°, and 25.7±0.2°, as determined by using Cu-K? radiation; and the Crystal form III has an X-ray powder diffraction pattern having characteristic peaks at the 20 positions of 4.9±0.2°, 6.1±0.2°, 7.4±0.2°, 11.4±0.2°, 12.2±0.2°, 16.6±0.2°, and 18.4±0.

Abstract: Disclosed is a polycyclic inhibitor of anaplastic lymphoma kinase as represented by Formula (I), or a pharmaceutically acceptable salt or stereoisomer thereof. Also disclosed is a method for preparing the compound, a pharmaceutical preparation and a pharmaceutical composition comprising the compound, and use of the compound, the pharmaceutically acceptable salt or stereoisomer thereof in manufacture of a medicament for the treatment and/or prevention of, for example, an anaplastic lymphoma kinase-mediated cancer or non-cancer related diseases.

Abstract: The present invention relates to a compound of Formula (I)-(IV) useful as ?-lactamase inhibitor, a pharmaceutically acceptable salt, ester, solvate or stereoisomer thereof, wherein R1, R2, M and ring A have definitions as those in the specification. The present invention further relates to methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and uses of these compounds. For example, the compounds of the present invention can be used as ?-lactamase inhibitors, for treatment and/or prophylaxis of diseases caused by bacterial infections, solving drug-resistance problems caused by ?-lactamases, especially bacterial drug-resistant diseases caused by type B metallo-?-lactamases.

Abstract: The invention relates to a quinazoline derivative represented by the general formula (I), a pharmaceutical acceptable salt and a stereoisomer thereof as tyrosine kinase inhibitor, wherein R1, R2, R3, R3?, R4, R5, R6, X, L, T, Z and q are as defined in the specification. The invention also relates to a process for preparing the same, a pharmaceutical composition and a pharmaceutical formulation containing the derivative, use of the derivative for treating excessive proliferative diseases and chronic obstructive pulmonary disease and use of the derivative in the manufacture of a medicament for treating excessive proliferative diseases and chronic obstructive pulmonary disease.

Abstract: The invention relates to a CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers; a pharmaceutical formulation, pharmaceutical composition and kit comprising said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers, and use of said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers. For example, the compounds of the invention are useful for reducing or inhibiting the activity of CDK4/6 kinase in a cell, and/or treating and/or preventing a cancer-related disease mediated by CDK4/6 kinase.

Abstract: The present invention belongs to the field of pharmaceutical technology, more specifically relates to optically pure benzyl-4-chlorophenyl-C-glucoside derivatives represented by formulae (II) and (III), a process for preparing these compounds and intermediates thereof, a pharmaceutical formulation and a pharmaceutical composition containing these compounds, and the use of the optically pure benzyl-4-chlorophenyl-C-glucoside derivative as a sodium glucose co-transporter (SGLT) inhibitor in manufacture of a medicament for treating and/or preventing diabetes mellitus (including insulin-dependent diabetes mellitus and non-insulin-dependent diabetes mellitus) or diabetes-associated diseases (including insulin resistance disease and obesity)

Abstract: The invention relates to a CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers; a pharmaceutical formulation, pharmaceutical composition and kit comprising said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers, and use of said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers. For example, the compounds of the invention are useful for reducing or inhibiting the activity of CDK4/6 kinase in a cell, and/or treating and/or preventing a cancer-related disease mediated by CDK4/6 kinase.

Abstract: The invention relates to quinazoline derivatives substituted by aniline which are represented by the below formula (I), pharmaceutical acceptable salts and stereoisomer thereof, wherein these groups of R1, R2, R3, R4, R5, R6, L and n have the meanings given in the specification. The invention also relates to preparation methods, pharmaceutical compositions, pharmaceutical preparation and the use for preparation of medicine of treating excessive hyperplasia and chronic obstructive pulmonary disease and uses for treating excessive hyperplasia and chronic obstructive pulmonary disease thereof.

Abstract: The invention relates to a quinazoline derivative represented by the general formula (I), a pharmaceutical acceptable salt and a stereoisomer thereof as tyrosine kinase inhibitor, wherein R1, R2, R3, R3?, R4, R5, R6, X, L, T, Z and q are as defined in the specification. The invention also relates to a process for preparing the same, a pharmaceutical composition and a pharmaceutical formulation containing the derivative, use of the derivative for treating excessive proliferative diseases and chronic obstructive pulmonary disease and use of the derivative in the manufacture of a medicament for treating excessive proliferative diseases and chronic obstructive pulmonary disease.