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Title:
CHOLIC ACID DERIVATIVE, AND PREPARATION METHOD AND MEDICAL USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2016/173397
Kind Code:
A1
Abstract:
The present invention relates to a cholic acid derivative, and a preparation method and a medical use thereof. In particular, the present invention relates to a cholic acid derivative with the structure of formula (I), a stereoisomer, or a pharmaceutically acceptable salt thereof. The series of compounds can be used to treat FXR mediated diseases, comprising cardiovascular disease, atherosclerosis, arteriosclerosis, hypercholesterolemia, hyperlipidemia and chronic hepatitis diseases, chronic liver diseases, gastrointestinal diseases, nephrosis, heart vascular diseases, metabolic diseases, cancer (for example colorectal cancer) or neurological signs, such as strokes and other diseases, with a wide range of medical applications, and are expected to develop into a new generation of FXR agonist.

Inventors:
YANG FEI (CN)
TONG ZHAOLONG (CN)
LI CHENGHAI (CN)
BAO RUDI (CN)
YU HONGPING (CN)
XU YAOCHANG (CN)
LU AIFENG (CN)
ZHONG HUIJUAN (CN)
Application Number:
PCT/CN2016/079167
Publication Date:
November 03, 2016
Filing Date:
April 13, 2016
Export Citation:
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Assignee:
SHANGHAI HANSOH BIOMEDICAL CO LTD (CN)
JIANGSU HANSOH PHARMACEUTICAL GROUP CO LTD (CN)
International Classes:
C07J9/00; A61K31/575; A61K31/58; A61P1/00; A61P1/16; A61P3/06; A61P9/00; C07J31/00; C07J41/00; C07J43/00; C07J51/00; C07J75/00
Domestic Patent References:
WO2015017813A22015-02-05
Foreign References:
US5466815A1995-11-14
US20140206657A12014-07-24
CN104672290A2015-06-03
Other References:
NGUYEN, T.T.H. ET AL.: "Synthesis of 24-(piperidin-1-yl, morpholin-4-yl and 4-methylpiperazin-1-yl)-5beta-cholan-3alpha-ols and four hydroxylated 23-(4,5-dihydroimidazol-2-yl)-24-nof--5beta-cholanes", COLLECTION OF CZECHOSLOVAK CHEMICAL COMMUNICATIONS, vol. 62, no. 3, 31 December 1997 (1997-12-31), pages 471 - 478, XP055326306
D'AMORE, C. ET AL.: "Design, Synthesis, and Biological Evaluation of Potent Dual Agonists of Nuclear and Membrane Bile Acid Receptors", JOURNAL OF MEDICINAL CHEMISTRY, vol. 57, no. 3, 4 January 2014 (2014-01-04), pages 937 - 954, XP055165457
HONORIO, K.M. ET AL.: "Hologram QSAR studies on farnesoid X receptor activators", LETTERS IN DRUG DESIGN & DISCOVERY, vol. 3, no. 4, 31 December 2006 (2006-12-31), pages 261 - 267, XP008082458, DOI: doi:10.2174/157018006776743206
Attorney, Agent or Firm:
GE CHENG & CO.,LTD. (CN)
北京戈程知识产权代理有限公司 (CN)
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