Invention Grant
- Patent Title: Preparation and use of 3-pyridyl substituted-6,6-difluoro bicyclic himbacine derivatives as par-1 receptor antagonists
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Application No.: US14912315Application Date: 2014-08-18
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Publication No.: US09808473B2Publication Date: 2017-11-07
- Inventor: James Francis Dropinski , Milana Maletic , Jae-Hun Kim , Deyou Sha
- 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/US2014/051404 WO 20140818
- International Announcement: WO2015/026686 WO 20150226
- Main IPC: A61K31/34
- IPC: A61K31/34 ; A61K31/60 ; A61K45/06 ; A61K31/4365 ; A61K31/444 ; C07D405/14 ; C07D409/14 ; C07D409/04 ; A61K31/343

Abstract:
The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof wherein: R1 is halo; —CN; alkyl; cycloalkyl; alkoxy; phenyl, which is optionally substituted one or twice independently by alkyl, halo, or —CN; or a thiophene ring, which is optionally substituted once or twice independently by alkyl. 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 ASC, secondary prevention of myocardial infarction or stroke, or PAD.
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