Shanghai Hengrui Pharmaceutical Co., Ltd.

Jiangsu Hengrui Medicine Company Ltd.

Hadasit Medical Research Services and Development Ltd.

Northwestern University

Jiangsu Hansoh Pharmaceutical Co., Ltd.

Hejun Lu

Qing Dong

Piaoyang Sun

Bin Gui

Richard B Silverman

Yaron Ilan

Hongjian Jiang

Hongbo Fei

Haowei Wang

Ehud Zigmond

Takuya Matsumoto

Wei Zhang

Peng Cho Tang

Fanglong Yang

Guangyuan Shen

Fuqiang Zhao

Zhigang Lin

Dongliang Guan

Jianghong Fu

Pyrazolopyrimidone derivatives and methods of use thereof are described. Specifically, pharmaceutical uses of pyrazolopyrimidone derivatives represented by the general formula (II) and pharmaceutically acceptable salts thereof are described, wherein the definitions of substituents in the general formula (II) are the same as the definitions in the specification. The pyrazolopyrimidone derivatives are useful as gonadotropin releasing hormone (GnRH) antagonists, such as for therapeutic agents for endometriosis. 

Pyrazolopyrimidone derivatives and methods of use thereof

Methods of preparation and pharmaceutical uses of pyrazolopyrimidone derivatives are described. Specifically, methods of preparation and pharmaceutical uses of pyrazolopyrimidone derivatives represented by the general formula (II) and pharmaceutically acceptable salts thereof are described, wherein the definitions of substituents in the general formula (II) are the same as the definitions in the specification. The pyrazolopyrimidone derivatives are useful as gonadotropin releasing hormone (GnRH) antagonists, such as for therapeutic agents for endometriosis. 

Pyrazolopyrimidone or Pyrrolotriazone derivatives, method of preparing same, and pharmaceutical applications thereof

Pyrazolopyrimidone and pyrrolotriazone derivatives, methods of preparation thereof, and pharmaceutical uses thereof are described. Specifically, pyrazolopyrimidone and pyrrolotriazone derivatives represented by the general formula (I) and pharmaceutically acceptable salts thereof are described. The pyrazolopyrimidone and pyrrolotriazone derivatives are useful as gonadotropin releasing hormone (GnRH) antagonists, such as for therapeutic agents for endometriosis. The definitions of the substituents in the general formula (I) are the same as the definitions in the specification. 

Pyrazolopyrimidone or pyrrolotriazone derivatives, method of preparing same, and pharmaceutical applications thereof

Methods for treating androgen receptor-mediated diseases, such as breast cancer, with imidazoline derivatives of formula (I) are provided: 

Methods of treating androgen receptor-mediated disorders with imidazoline derivatives

New imidazoline derivatives represented by formula (I): preparation methods thereof, pharmaceutical compositions comprising such derivatives, and applications of such derivatives in preparing androgen receptor antagonists and medicaments for treating diseases such as prostate cancer are described.

Imidazoline derivatives, preparation methods thereof, and their applications in medicine

The invention relates to inhibition of ornithine aminotransferase (OAT) for suppression of tumor cells proliferation. More particularly, the invention relates to methods of treatment of proliferative disorders by the selective inhibition of OAT, and further provides the use of OAT inhibitors, specifically, 5-amino-1,3-hexadienyl-carboxylic acid (Gabaculine), and Gabaculine analogue 8, for compositions and methods for the treatment of proliferative disorders such as hepatocellular carcinoma. The invention further provides methods and kits for the diagnosis of a pathologic proliferative disorder in a mammalian subject, based on determining the level of OAT expressed in a biological sample obtained from a subject.

Inhibition of ornithine aminotransferase for the treatment of proliferative disorders

Disclosed are new dicycloazaalkane derivates represented by general formula (I), preparation processes and pharmaceutical compositions containing them, and the uses for treatment especially for dipeptidyl peptidase inhibitor (DPP-IV), in which each substitute group of general formula (I) is as defined in specification. 

Dicycloazaalkane derivates, preparation processes and medical uses thereof

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Shanghai, China

Hejun Lu