公开(公告)号：US06552052B2

公开(公告)日：2003-04-22

申请号：US09818297

申请日：2001-03-26

申请人： Donald W. Hansen, Jr. ,  R. Keith Webber ,  E. Ann Hallinan ,  Mihaly V. Toth ,  Barnett S. Pitzele ,  Alok K. Awasthi ,  Alan E. Moormann ,  Suzanne Metz ,  Jeffery S. Snyder ,  William M. Moore ,  Jeffrey A. Scholten

发明人： Donald W. Hansen, Jr. ,  R. Keith Webber ,  E. Ann Hallinan ,  Mihaly V. Toth ,  Barnett S. Pitzele ,  Alok K. Awasthi ,  Alan E. Moormann ,  Suzanne Metz ,  Jeffery S. Snyder ,  William M. Moore ,  Jeffrey A. Scholten

IPC分类号： C07D27112

CPC分类号： C07D487/04 ,  C07D513/04 ,  C07D515/04 ,  C07F9/6561

摘要： Pyrrolo[2,1-c][1,2,4]thiadiazole or pyrollo[2,1-c][1,2,4]oxadiazoles having the formula: or pharmaceutically acceptable salts thereof, useful as nitric oxide synthase inhibitors wherein each substituent is defined herein.

摘要翻译： 具有下式的吡咯并[2,1-c] [1,2,4]噻二唑或pyrollo [2,1-c] [1,2,4]恶二唑或其药学上可接受的盐，其可用作一氧化氮合酶抑制剂，其中 每个取代基在本文中定义。

公开(公告)号：US06248895B1

公开(公告)日：2001-06-19

申请号：US09565917

申请日：2000-05-05

申请人： Alangudi Sankaranarayanan

发明人： Alangudi Sankaranarayanan

IPC分类号： C07D27112

CPC分类号： A61K31/4245 ,  C07D271/12

摘要： The invention discloses a novel compound of the benzofuroxan series used for cardiovascular disorders represented by the general formula (I) and pharmaceutically acceptable salts thereof wherein: R is —O—(CH2)n-X-R′; n=1 to 6; X is —NHC(O)—, or oxygen; R′ is lower alkyl (C1-C8), aromatic, heteroaromatic, substituted or unsubstituted saturated heterocyclic ring with one or two hetero atoms such as nitrogen or oxygen wherein substitution is with lower alkyl; or R is selected from wherein R″ is hydrogen, nitro, lower alkyl or—C(O)—R′″ wherein R′″ is hydrogen, lower alkyl or aryl. The invention also discloses process for the preparation of compounds of general formula I. The invention also discloses the use of the compounds of general formula I as defined above, as NO donors and/or in coronary heart diseases, and pharmaceutical compositions containing compounds of general formula I as active ingredients. The invention also discloses a method of treatment of mammal, including man, of coronary heart disease by administration of an effective amount of a compound of formula I as defined above.

摘要翻译： 本发明公开了一种用于由通式（I）表示的心血管疾病的苯并呋喃系列的新化合物及其药学上可接受的盐，其中R为-O-（CH 2）n X-R'; n = 1-6; X为 - NHC（O） - 或氧; R'是具有一个或两个杂原子如氮或氧的芳族，杂芳族，取代或未取代的饱和杂环，其中用低级烷基取代;或R 选自R“是氢，硝基，低级烷基或-C（O）-R”，其中R“'是氢，低级烷基或芳基。本发明还公开了制备通式 本发明还公开了如上定义的通式I化合物作为NO供体和/或冠心病的用途，以及含有通式I化合物作为活性成分的药物组合物。本发明还公开了一种 治疗哺乳动物，包括男性，冠心病 通过施用有效量的如上定义的式I化合物的疾病。