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Title:
BICYCLIC COMPOUND USED AS AN LP-PLA2 INHIBITOR, AND PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2016/180247
Kind Code:
A1
Abstract:
The present invention relates to a bicyclic compound used as an Lp-PLA2 inhibitor, a preparation method and pharmaceutical use thereof, and a pharmaceutical composition containing the compound. The structure of the bicyclic compound is shown in general formula I. The definitions of R1, R2, R3, X, Y, Z, Ar and n are shown in the description and claims. The compound shown in general formula I of the present invention can be used as an Lp-PLA2 inhibitor for preventing and/or treating and/or improving diseases related to the enzymatic activity of Lp-PLA2.

Inventors:
SHEN JIANHUA (CN)
WANG YIPING (CN)
CHEN XINDE (CN)
XU WENWEI (CN)
Application Number:
PCT/CN2016/080725
Publication Date:
November 17, 2016
Filing Date:
April 29, 2016
Export Citation:
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Assignee:
SHANGHAI INST MATERIA MEDICA CAS (CN)
International Classes:
C07D487/04; A61K31/519; A61P9/10; A61P17/06; A61P25/28; A61P27/02; A61P27/06; A61P29/00
Domestic Patent References:
WO2014114249A12014-07-31
WO2013013503A12013-01-31
WO2012076435A12012-06-14
WO2004021984A22004-03-18
WO2013014185A12013-01-31
Other References:
CHEN, XINDE ET AL.: "Discovery of a Novel Series of Imidazo[1, 2-a]pyrimidine Derivatives as Potent and Orally Bioavailable Lipoprotein-Associated Phospholipase A2 Inhibitors", JOURNAL OF MEDICINAL CHEMISTRY, vol. 58, no. 21, 19 October 2015 (2015-10-19), pages 8529 - 8541, XP055328252
KOPPEL, H.C. ET AL.: "Pyrimidines.I.Synthesis of Pyrimidinethiols", JOURNAL OF ORGANIC CHEMISTRY, vol. 26, 31 December 1961 (1961-12-31), pages 792 - 803, XP000929327
DARRELL, E.O.B. ET AL.: "Pyrimidines.VII.2-Amino-4-(substituted anilino) Pyrimidines", JOURNAL OF ORGANIC CHEMISTRY, vol. 27, no. 3, 31 December 1962 (1962-12-31), pages 1104 - 1107, XP055052599
Attorney, Agent or Firm:
KINGSOUND & PARTNERS (CN)
北京金信知识产权代理有限公司 (CN)
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