Chengdu Di'ao Pharmaceutical Group Co., Ltd.

Chengdu Di'ao Jiuhong Pharmaceutical Factor

Jianxin Ji

Tao N Zhang

Tao Zhang

Na Guo

Ting Xue

Xin Chen

Bogang Li

Bingqiang Kang

Xinfa Ye

Qiang Zhang

Yu Huang

Guangxin Dong

Xiangyang Peng

Xiaoxia Gong

Zhen Huang

Fengtian Du

Meirong Zhou

Wei Zhan

Yi Jin

Jufang Yan

Xiaowei Yan

Dongguang Qin

Yongrongn Yang

Bing Guang

Junjian Liu

Disclosed are a phthalic hydrazide (phthalazine ketone) compound, and a pharmaceutical composition comprising the same. As a DNA repair enzyme poly (ADP-ribozyme) polymerase inhibitor, the compound and the pharmaceutical composition can effectively treat diseases involving PARP enzymatic activity, including cancer, neural degenerative diseases, inflammation and the like.

Poly (ADP-ribose) polymerase inhibitor

Disclosed is a synthesis method of a compound of formula 1,5-[[2(R)-[1(R)-[3,5-bis(trifluoromethyl)phenyl]ethoxyl]-3(S)-4-fluorophenyl-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazole-3-one (i.e. aprepitant), which comprises cyclizing a compound of formula 4 in a solvent, wherein R is C-Calkyl. The intermediate for preparing aprepitant is also disclosed. The present method is especially suitable for industrial production of aprepitant.

Preparation method of 5-[[2(R)-[1(R)-[3,5-bis(trifluoromethyl) phenyl]ethoxy]-3(S)-4-fluorophenyl-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazole-3-one

The invention provides the use of ursolic acid saponin and oleanolic acid saponin of formula (I) in preparing medicaments for increasing leucocytes and/or platelets. The invention also provides a pharmaceutical composition containing the same compound. The invention utilizes the cheap and accessible ursolic acid and oleanolic acid which are widely present in natural plants as raw materials, introduces monosaccharyls or oligosaccharyls by structural modification. It is proved by pharmacological tests that the compound of formula (I) have an activity of obviously increasing leucocytes and/or platelets. 

Use of ursolic acid saponin,oleanolic acid saponin in preparation of increasing leucocytes and/or platelet medicine

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Sichuan, China

Jianxin Ji