公开(公告)号：US5104891A

公开(公告)日：1992-04-14

申请号：US449700

申请日：1989-12-11

申请人： Philippe R. Bovy ,  Joan M. O'Neal ,  Timothy S. Chamberlain ,  Joe T. Collins

发明人： Philippe R. Bovy ,  Joan M. O'Neal ,  Timothy S. Chamberlain ,  Joe T. Collins

IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61K31/675 ,  A61P9/00 ,  A61P9/04 ,  A61P9/12 ,  A61P43/00 ,  C07D235/02 ,  C07D403/10 ,  C07F9/6558

CPC分类号： C07D235/02 ,  C07D403/10

摘要： A class of cycloheptimidazolone compounds is described as angiotensin II antagonists for use in control of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, alkyl, halo, alkanoyl, carboxyl, alkoxycarbonyl, phenyl, haloalkyl, alkoxyalkyl, formyl, cyano, alkoxy, phenoxy, phenylthio, alkylthio; wherein R.sup.3 is alkyl, alkenyl, alkynyl, hydroxyalkyl and alkoxyalkyl; wherein each of R.sup.5 through R.sup.13 is independently selected from hydrido, alkyl, haloalkyl, halo, nitro, cyano, hydroxy, alkoxy, alkylthio, aryl, aryloxy, arythio, and acidic groups such as carboxylic acid, with the proviso that at least one of R.sup.9 through R.sup.13 substituents is an acidic group; or a pharmaceutically-acceptable ester, amide or salt thereof.

公开(公告)号：US5281615A

公开(公告)日：1994-01-25

申请号：US840471

申请日：1992-02-24

申请人： Philippe R. Bovy ,  Joan M. O'Neal ,  Timothy S. Chamberlain ,  Joe T. Collins

发明人： Philippe R. Bovy ,  Joan M. O'Neal ,  Timothy S. Chamberlain ,  Joe T. Collins

IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61K31/675 ,  A61P9/00 ,  A61P9/04 ,  A61P9/12 ,  A61P43/00 ,  C07D235/02 ,  C07D403/10 ,  C07F9/6558 ,  C07D257/04

CPC分类号： C07D235/02 ,  C07D403/10

摘要： A class of cycloheptimidazolone compounds is described as angiotensin II antagonists for use in control of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, alkyl, halo, alkanoyl, carboxyl, alkoxycarbonyl, phenyl, haloalkyl, alkoxyalkyl, formyl, cyano, alkoxy, phenoxy, phenylthio, alkylthio; wherein R.sup.3 is alkyl, alkenyl, alkynyl, hydroxyalkyl and alkoxyalkyl; wherein each of R.sup.5 through R.sup.13 is independently selected from hydrido, alkyl, haloalkyl, halo, nitro, cyano, hydroxy, alkoxy, alkylthio, aryl, aryloxy, arythio, and acidic groups such as carboxylic acid, with the proviso that at least one of R.sup.9 through R.sup.13 substituents is an acidic group; or a pharmaceutically-acceptable ester, amide or salt thereof.

摘要翻译： 一类环庚咪唑酮化合物被描述为用于控制高血压的血管紧张素II拮抗剂。 特别感兴趣的化合物是式（*化学结构*）的化合物，其中R 1和R 2各自独立地选自氢，烷基，卤素，烷酰基，羧基，烷氧基羰基，苯基，卤代烷基，烷氧基烷基，甲酰基，氰基，烷氧基，苯氧基 ，苯硫基，烷硫基; 其中R3是烷基，烯基，炔基，羟基烷基和烷氧基烷基; 其中R 5至R 13中的每一个独立地选自氢，烷基，卤代烷基，卤素，硝基，氰基，羟基，烷氧基，烷硫基，芳基，芳氧基，仲氨基和酸性基团如羧酸，条件是至少一个 R9至R13取代基是酸性基团; 或其药学上可接受的酯，酰胺或其盐。

公开(公告)号：US06130333A

公开(公告)日：2000-10-10

申请号：US200863

申请日：1998-11-27

申请人： Horng-Chih Huang ,  Timothy S. Chamberlain ,  Steven Lynn Settle ,  William Dean Joy ,  Ned R. Siegel ,  Leslie D. Bell

发明人： Horng-Chih Huang ,  Timothy S. Chamberlain ,  Steven Lynn Settle ,  William Dean Joy ,  Ned R. Siegel ,  Leslie D. Bell

IPC分类号： A61K31/4184 ,  C07D405/04 ,  C07D405/14 ,  C07D471/04 ,  C07D235/04 ,  A61K31/443 ,  C07D401/06 ,  C07D471/02 ,  A61K81/437 ,  A61N27/06

CPC分类号： C07D405/04 ,  A61K31/4184 ,  C07D405/14 ,  C07D471/04

摘要： The present invention provides for compounds having the following Formulae I-III, ##STR1## and ##STR2## The compounds of the present invention are useful in the treatment of a variety of disease such as glaucoma, sexual dysfunction, asthma and cardiovascular disorders such as stable-, unstable- and variant-angina, hypertension, pulmonary hypertension, congestive heart failure, atherosclerosis, and thrombosis.

摘要翻译： 本发明提供具有以下式I-III的化合物，本发明化合物可用于治疗各种疾病，如青光眼，性功能障碍，哮喘和心血管疾病如稳定，不稳定和 变异型心绞痛，高血压，肺动脉高压，充血性心力衰竭，动脉粥样硬化和血栓形成。