Xuanzhu Pharma Co., Ltd.

Ji Lin Hui Sheng Bio-Pharmaceutical Co., Ltd.

Beijing Huizhiheng Biotechnology Co., Ltd.

Chutian Shu

Zhenhua Wang

Jinyuan Wang

Frank Wu

Yuzhen Feng

Yongqian Wu

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. 

Crystal form of sodium-glucose cotransporter 2 inhibitor

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&#x3b8; positions of 6.7&#xb1;0.2&#xb0;, 7.9&#xb1;0.2&#xb0;, 8.6&#xb1;0.2&#xb0;, 12.0&#xb1;0.2&#xb0;, 13.9&#xb1;0.2&#xb0;, 15.9&#xb1;0.2&#xb0;, 17.3&#xb1;0.2&#xb0;, 18.3&#xb1;0.2&#xb0;, 18.7&#xb1;0.2&#xb0;, 21.0&#xb1;0.2&#xb0;, and 23.0&#xb1;0.2&#xb0;, as determined by using Cu-K&#x3b1; radiation; the Crystal form II has an X-ray powder diffraction pattern having characteristic peaks at the 2&#x3b8; positions of 6.9&#xb1;0.2&#xb0;, 8.5&#xb1;0.2&#xb0;, 14.8&#xb1;0.2&#xb0;, 15.6&#xb1;0.2&#xb0;, 16.7&#xb1;0.2&#xb0;, 17.1&#xb1;0.2&#xb0;, 17.9&#xb1;0.2&#xb0;, 18.7&#xb1;0.2&#xb0;, 19.1&#xb1;0.2&#xb0;, 21.5&#xb1;0.2&#xb0;, 23.5&#xb1;0.2&#xb0;, and 25.7&#xb1;0.2&#xb0;, as determined by using Cu-K&#x3b1; radiation; and the Crystal form III has an X-ray powder diffraction pattern having characteristic peaks at the 2&#x3b8; positions of 4.9&#xb1;0.2&#xb0;, 6.1&#xb1;0.2&#xb0;, 7.4&#xb1;0.2&#xb0;, 11.4&#xb1;0.2&#xb0;, 12.2&#xb1;0.2&#xb0;, 16.6&#xb1;0.2&#xb0;, and 18.4&#xb1;0.2&#xb0;, as determined by using Cu-K&#x3b1; radiation. 

Crystals of quinazoline derivative and preparation method therefor

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&#x3b8; positions of 6.0&#xb1;0.2&#xb0;, 7.3&#xb1;0.2&#xb0;, 11.7&#xb1;0.2&#xb0;, 12.9&#xb1;0.2&#xb0;, 18.4&#xb1;0.2&#xb0;, 24.7&#xb1;0.2&#xb0;, and 26.3&#xb1;0.2&#xb0;, as determined by using Cu-K&#x3b1; radiation, and the Crystal form II has an X-ray powder diffraction pattern having characteristic peaks at the 2&#x3b8; positions of 5.0&#xb1;0.2&#xb0;, 7.0&#xb1;0.2&#xb0;, 10.1&#xb1;0.2&#xb0;, 17.0&#xb1;0.2&#xb0;, 26.0&#xb1;0.2&#xb0;, and 26.5&#xb1;0.2&#xb0;, as determined by using Cu-K&#x3b1; radiation. 

Provided are prodrugs of a bicyclic substituted pyrimidine type PDE-5 inhibitors, pharmaceutically acceptable salts or stereoisomers thereof. Also provided are methods for preparing these prodrug compounds, pharmaceutical preparations, and pharmaceutical compositions, as well as a use of these compounds, pharmaceutical preparations and pharmaceutical compositions in the manufacture of medicaments for treatment and/or prophylaxis of sexual dysfunction and lower urinary tract symptoms.

Prodrugs of bicyclic substituted pyrimidine type PDE-5 inhibitors

The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, a stereoisomer or a solvate thereof, wherein R, R, R, R, X, Y, A and B are as defined in the specification. The present invention further relates to a method for preparing these compounds, a pharmaceutical composition containing these compounds, and a use of these compounds in manufacture of a medicament for treating and/or preventing proliferative diseases. 

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Jinan, China

Chutian Shu