HYDROBROMATE OF BENZODIAZEPINE DERIVATIVE, PREPARATION METHOD AND USE THEREOF

WIPO Patent Application WO/2018/103119

A1

The present invention provides a hydrobromate of methyl 3-[(4S)-8-bromo-1-methyl-6-(2-pyridyl)-4H-imidazole[1,2-a][1,4]benzodiazepine-4-yl]propionate and related crystal forms and preparation method and use thereof. The hydrobromate has an excellent solubility (greater than 100 mg/ml), which is significantly superior to other currently commercially available or developed salt products of the compound, and the hydrobromate is particularly suitable for the preparation of injections, has relatively good stability under various crystal forms, and has good practical value and market prospects.

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HUANG HAOXI (CN)
ZHUO GUOQING (CN)
SHANG GUONING (CN)
LIANG ZHEN (CN)
CHU TING (CN)
CHEN CUICUI (CN)
LUO MING (CN)
LI YINGFU (CN)
SU ZHONGHAI (CN)

PCT/CN2016/109564

June 14, 2018

December 13, 2016

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CHENGDU BRILLIANT PHARMACEUTICAL CO LTD (CN)

C07D487/04; A61K9/08; A61K9/19; A61K31/5517; A61P21/02; A61P23/00; A61P25/08; A61P25/20; A61P25/22

WO2008007081A1

2008-01-17

CN104768557A	2015-07-08
CN104968348A	2015-10-07
CN106380470A	2017-02-08
CN101501019A	2009-08-05
CN101501019A	2009-08-05
CN104968348A	2015-10-07
CN103221414A	2013-07-24
CN201380036582A	2013-05-22
US20070093475A1	2007-04-26
CN200780028964A	2007-07-10
CN201310166860A	2007-07-10

PROGRESS IN PHARMACEUTICAL SCIENCES, vol. 36, no. 4,151, 2012
See also references of EP 3553059A4

CHENGDU HUAFENG PATENT OFFICE (CN)

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