Invention Grant
- Patent Title: Factor IXa inhibitors
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Application No.: US14652237Application Date: 2013-12-16
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Publication No.: US09708308B2Publication Date: 2017-07-18
- Inventor: Cameron James Smith , John Qiang Tan , Ting Zhang , James Balkovec , William John Greenlee , Liangqin Guo , Yi-Heng Chen , Yili Chen , Jiayi Xu , Samuel Chackalamannil , Tomokazu Hirabayashi , Hiroshi Nagasue , Kouki Ogawa
- Applicant: Merck Sharp & Dohme Corp. , Mochida Pharmaceutical Co., Ltd.
- Applicant Address: US NJ Rahway JP Tokyo
- Assignee: Merck Sharp Dohme Corp.,Mochida Pharmacuetical Co., Ltd.
- Current Assignee: Merck Sharp Dohme Corp.,Mochida Pharmacuetical Co., Ltd.
- Current Assignee Address: US NJ Rahway JP Tokyo
- Agent Nicole M. Beeler; Catherine D. Fitch
- International Application: PCT/US2013/075233 WO 20131216
- International Announcement: WO2014/120346 WO 20140807
- Main IPC: C07D471/04
- IPC: C07D471/04 ; C07D413/14 ; C07D417/14 ; C07D487/04 ; C07D498/04

Abstract:
The present invention provides a compound of Formula (I) wherein R1 is H or C1-6 alkyl, R2, is H or C1-6 alkyl or CH2OH, R3 is H or C1-6 alkyl, and R4 is H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, then R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl or —CH2OH, and when R2, R3, and R4 are H, then R1 is C1-6 alkyl; A is 1) a 9-10 membered bicyclic heterocycle having 1-3 heteroatoms independently selected from N, S and O, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with R5 and unsubstituted or substituted with R6 and unsubstituted or substituted with NH2, or 2) a 6-9 membered monocyclic or bicyclic carbocyclic ring system unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with —CH2NH2; and B is 1) a 5- or 6-membered monocyclic heterocycle having 1 or 2 heteroatoms independently selected from N, S or O, which is unsubstituted or substituted on a carbon or nitrogen atom with R7, unsubstituted or substituted on a carbon or nitrogen atom with R8, and unsubstituted or substituted on a carbon or nitrogen atom with R9, or 2) an 8- or 9-membered fused bicyclic heterocycle having 1, 2 or 3 nitrogen atoms which is unsubstituted or substituted on a carbon or nitrogen atom with R7, and unsubstituted or substituted on a carbon or nitrogen atom with R8; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses.
Public/Granted literature
- US20150322056A1 Factor IXa Inhibitors Public/Granted day:2015-11-12
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