发明名称 |
Thrombin inhibitors |
摘要 |
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure:;or a pharmaceutically acceptable salt thereof, whereinQ is CH2, NR4, O, S, S(O) or S(O2), wherein R4 is H, C1-6 alkyl, aryl, or C3-8 cycloalkyl;R1 is a heterocycle or —(CR5R6)1-2NH2, wherein R5 and R6, each time in which they occur, are independently H, C1-6 alkyl, —CH2F, —CHF2, CF3 or —CH2OH;R2 is OH, NH2 or NHSO2CH3;R3 is C1-6 alkyl. |
申请公布号 |
US9133147(B2) |
申请公布日期 |
2015.09.15 |
申请号 |
US201314387977 |
申请日期 |
2013.03.22 |
申请人 |
Merck Sharp & Dohme Corp. |
发明人 |
Blizzard Timothy Allen;Biftu Tesfaye |
分类号 |
C07D295/18;C07D241/04;C07D265/30;C07D279/12;C07D211/60;A61K31/497;A61K9/00;A61K47/12;A61K9/20 |
主分类号 |
C07D295/18 |
代理机构 |
|
代理人 |
Beeler Nicole M.;Fitch Catherine D. |
主权项 |
1. A compound of the formula I or a pharmaceutically acceptable salt thereof, wherein Q is S, S(O) or S(O2); R1 is a heterocycle or —(CR5R6)1-2NH2, wherein R5 and R6, each time in which they occur, are independently H, C1-6 alkyl, —CH2F, —CHF2, CF3 or —CH2OH; R2 is OH, NH2 or NHSO2CH3; and R3 is C1-6 alkyl. |
地址 |
Rahway NJ US |