公开(公告)号：US20140206706A1

公开(公告)日：2014-07-24

申请号：US14219311

申请日：2014-03-19

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Jon J. Hangeland ,  Mimi L. Quan ,  Joanne M. Smallheer ,  Gregory S. Bisacchi ,  James R. Corte ,  Todd J. Friends ,  Zhong Sun ,  Karen A. Rossi ,  Cullen L. Cavallaro

IPC: C07D417/04 ,  C07D263/32 ,  C07D231/12 ,  C07D403/04 ,  C07D235/08 ,  C07D233/64 ,  C07D401/12 ,  C07D249/08

CPC classification number: C07D417/14 ,  C07D231/12 ,  C07D233/64 ,  C07D233/68 ,  C07D233/90 ,  C07D235/08 ,  C07D235/14 ,  C07D235/16 ,  C07D249/08 ,  C07D249/12 ,  C07D263/12 ,  C07D263/14 ,  C07D263/32 ,  C07D277/30 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06

Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.

Abstract translation: 本发明提供了治疗有需要的患者治疗有效量的至少一种式（I）或式（V）化合物或其立体异构体或药学上可接受的盐或溶剂化物的血栓形成或炎性病症的方法： 其中变量A，L，Z，R3，R4，R6，R11，X1，X2和X3如本文所定义。 式（I）的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。 特别地，它涉及作为选择性因子XIa抑制剂的化合物。 本发明还提供了式I范围内的化合物，涉及包含这些化合物的药物组合物。

公开(公告)号：US20130131074A1

公开(公告)日：2013-05-23

申请号：US13744604

申请日：2013-01-18

Applicant: Bristol-Myers Squibb Company

Inventor： Dean A. Wacker ,  Karen A. Rossi ,  Ying Wang ,  Gang Wu

IPC: C07D403/14 ,  A61K31/4545 ,  A61K45/06 ,  C07D403/12 ,  A61K31/501 ,  C07D401/12 ,  A61K31/506

CPC classification number: C07D403/14 ,  A61K31/4545 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/14

Abstract: Novel compounds of structure Formula I: or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein Z, R1, R2, R21, T1, T2, T3 and T4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.

Abstract translation: 提供结构式I的新型化合物或其对映体，非对映异构体或其药学上可接受的盐，其中Z，R 1，R 2，R 21，T 1，T 2，T 3和T 4在本文中定义，其是GPR119G蛋白偶联 受体调节剂。 GPR119 G蛋白偶联受体调节剂可用于治疗，预防或减缓需要GPR119 G蛋白偶联受体调节剂治疗的疾病进展。 因此，本公开还涉及包含这些新化合物的组合物以及通过使用任何这些新化合物或包含任何这些新化合物的组合物来治疗与GPR119G蛋白偶联受体的活性有关的疾病或病症的方法。