Xuanzhu Pharma Co., Ltd.

Kbp Biosciences Co., Ltd.

Jinyuan Wang

Zhenhua Wang

Zhenhua Huang

Chutian Shu

Yuzhen Feng

Dedong Zhang

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.

Salt of a quinazoline derivative-like tyrosine kinase inhibitor and crystal form thereof

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. 

The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of X, Y, Y, Y, R, R, R, R, R, R, Cy and n are as presented in the description. 

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Jinan, China

Jinyuan Wang