Invention Grant
US09340530B2 Preparation and use of bicyclic himbacine derivatives as PAR-1 receptor antagonists
有权
双环him啶衍生物作为PAR-1受体拮抗剂的制备和应用
- Patent Title: Preparation and use of bicyclic himbacine derivatives as PAR-1 receptor antagonists
- Patent Title (中): 双环him啶衍生物作为PAR-1受体拮抗剂的制备和应用
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Application No.: US14383176Application Date: 2013-02-27
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Publication No.: US09340530B2Publication Date: 2016-05-17
- Inventor: Mihir Mandal , Timothy A. Blizzard , Helen Chen , Harry Chobanian , Yan Guo , Barbara Pio , Zhicai Wu , Tesfaye Biftu , William J. Greenlee , Johnny Zhaoning Zhu
- Applicant: Merck, Sharp & Dohme Corp.
- Applicant Address: US NJ Rahway
- Assignee: Merck Sharp & Dohme Corp.
- Current Assignee: Merck Sharp & Dohme Corp.
- Current Assignee Address: US NJ Rahway
- Agent Nicole M. Beeler; Catherine D. Fitch
- International Application: PCT/US2013/027838 WO 20130227
- International Announcement: WO2013/134012 WO 20130912
- Main IPC: A61K31/44
- IPC: A61K31/44 ; C07D401/06 ; C07D417/14 ; C07D405/06 ; A61K45/06 ; A61K31/365 ; A61K31/4365 ; A61K31/443 ; A61K31/4439 ; A61K31/616 ; C07D401/14 ; C07D405/14 ; C07D413/14 ; A61K31/444

Abstract:
The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: X is —O—, —N(R), —C(R8)(R9) or —C(O)—; and Y is —O—, —N(R), —C(R8)(R9) or —C(O)— and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ACS, secondary prevention of myocardial infarction or stroke, or PAD.
Public/Granted literature
- US20150025046A1 PREPARATION AND USE OF BICYCLIC HIMBACINE DERIVATIVES AS PAR-1 RECEPTOR ANTAGONISTS Public/Granted day:2015-01-22
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