公开(公告)号：EP2224928A1

公开(公告)日：2010-09-08

申请号：EP08858138.4

申请日：2008-12-04

申请人： GlaxoSmithKline LLC

发明人： LONDREGAN, Allyn, T. ,  MARINO, Joseph, Paul ,  MCATEE, John, Jeffrey

IPC分类号： A61K31/535

CPC分类号： C07D403/04

摘要： The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula (I): wherein R1, R2a, R2b, R5a, R6a, A, B, K, L, M, Y, Z, I, and m are defined herein, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are sEH inhibitors and can be used in the treatment of diseases mediated by the sEH enzyme, such as hypertension. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting sEH and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

摘要翻译： 本发明涉及新型sEH抑制剂及其在治疗由sEH酶介导的疾病中的用途。 具体而言，本发明涉及根据式（I）的化合物：其中R1，R2a，R2b，R5a，R6a，A，B，K，L，M，Y，Z，I和m如本文所定义， 其药学上可接受的盐。 本发明的化合物是sEH抑制剂并且可以用于治疗由sEH酶介导的疾病，例如高血压。 因此，本发明还涉及包含本发明化合物的药物组合物。 本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物抑制sEH和治疗与之相关的病症的方法。

公开(公告)号：EP2240021A1

公开(公告)日：2010-10-20

申请号：EP09705999.2

申请日：2009-01-30

申请人： GlaxoSmithKline LLC

发明人： MARINO, Joseph, Paul ,  MCATEE, John, Jeffrey

IPC分类号： A01N43/40 ,  A61K31/445 ,  A61K31/16

CPC分类号： C07D401/04

摘要： The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula (I): wherein R1, R2, R3, R5a, R6a, A, B, K, L, M, Y, Z, x, and m are defined herein, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are sEH inhibitors and can be used in the treatment of diseases mediated by the sEH enzyme, such as hypertension. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting sEH and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

摘要翻译： 本发明涉及新型sEH抑制剂及其在治疗由sEH酶介导的疾病中的用途。 具体而言，本发明涉及根据式（I）的化合物：其中R1，R2，R3，R5a，R6a，A，B，K，L，M，Y，Z，x和m如本文所定义， 其药学上可接受的盐。 本发明的化合物是sEH抑制剂并且可以用于治疗由sEH酶介导的疾病，例如高血压。 因此，本发明还涉及包含本发明化合物的药物组合物。 本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物抑制sEH和治疗与之相关的病症的方法。