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51. 发明授权

US5389661A Imidazole and 1,2,4-triazole derivatives with angiotensin II antagonist properties 失效
标题翻译：咪唑和1,2,4-三唑衍生物与血管紧张素II拮抗剂的性质
公开(公告)号：US5389661A
公开(公告)日：1995-02-14
申请号：US194535
申请日：1994-02-10
申请人： Ila Sircar , Jagadish C. Sircar
发明人： Ila Sircar , Jagadish C. Sircar
IPC分类号： C07D401/06 , C07D403/06 , C07D403/14 , A61K31/41 , A61K31/415 , C07D257/04
CPC分类号： C07D401/06 , C07D403/06 , C07D403/14
摘要： This invention relates to novel substituted imidazole and triazole derivatives which antagonize the binding of angiotensin II to its receptors. The compounds are useful in the treatment of hypertension, heart failure, glaucoma, and hyperaldosteronism. Methods of making the compounds, novel intermediates useful in the preparation of the compounds, pharmaceutical compositions containing the compounds, and methods of using them are also covered.
摘要翻译：本发明涉及拮抗血管紧张素II与其受体的结合的新型取代的咪唑和三唑衍生物。该化合物可用于治疗高血压，心力衰竭，青光眼和醛固酮增多症。制备化合物的方法，可用于制备化合物的新中间体，含有该化合物的药物组合物，以及使用它们的方法也被覆盖。

52. 发明授权

US5322950A Imidazole with angiotensin II antagonist properties 失效
标题翻译：咪唑与血管紧张素II拮抗剂的性质
公开(公告)号：US5322950A
公开(公告)日：1994-06-21
申请号：US985395
申请日：1992-12-04
申请人： Ila Sircar , Jagadish C. Sircar
发明人： Ila Sircar , Jagadish C. Sircar
IPC分类号： C07D401/06 , C07D403/06 , C07D403/14
CPC分类号： C07D401/06 , C07D403/06 , C07D403/14
摘要： This invention relates to novel substituted imidazole and triazole derivatives which antagonize the binding of angiotensin II to its receptors. The compounds are useful in the treatment of hypertension, heart failure, glaucoma, and hyperaldosteronism. Methods of making the compounds, novel intermediates useful in the preparation of the compounds, pharmaceutical compositions containing the compounds, and methods of using them are also covered.
摘要翻译：本发明涉及拮抗血管紧张素II与其受体的结合的新型取代的咪唑和三唑衍生物。该化合物可用于治疗高血压，心力衰竭，青光眼和醛固酮增多症。制备化合物的方法，可用于制备化合物的新中间体，含有该化合物的药物组合物，以及使用它们的方法也被覆盖。

53. 发明授权

US5260278A Diol-containing renin inhibitors 失效
标题翻译：含二醇的肾素抑制剂
公开(公告)号：US5260278A
公开(公告)日：1993-11-09
申请号：US678469
申请日：1991-04-01
申请人： Richard Himmelsbach , John C. Hodges , James S. Kaltenbronn , William C. Patt , Joseph T. Repine , Ila Sircar
发明人： Richard Himmelsbach , John C. Hodges , James S. Kaltenbronn , William C. Patt , Joseph T. Repine , Ila Sircar
IPC分类号： A61K38/00 , C07D233/54 , C07K5/065 , A61K37/02 , C07D265/30 , C07D295/26 , C07K5/06
CPC分类号： C07D233/64 , C07K5/06078 , A61K38/00 , Y10S530/86
摘要： The invention concerns novel renin-inhibitory peptides which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism, and diseases caused by retroviruses including HTLV-I and -III. Processes for preparing the peptides, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, or hyperaldosteronism.
摘要翻译：本发明涉及可用于治疗肾素相关性高血压，充血性心力衰竭，醛固酮增多症和由逆转录病毒（包括HTLV-1和-III）引起的疾病的新型肾素抑制肽。包括肽的制备方法，含有它们的组合物和使用它们的方法。还包括使用该化合物来确定肾素相关性高血压或醛固酮增多症的存在的诊断方法。

54. 发明授权

US4980351A 3-aminopropoxyaryl derivatives having cardiotonic and antihypertensive use and compositions thereof 失效
标题翻译：具有强心剂和抗高血压用途的3-氨基丙氧基芳基衍生物及其组合物
公开(公告)号：US4980351A
公开(公告)日：1990-12-25
申请号：US117252
申请日：1987-11-04
申请人： Hubert G. K. Barth , Ila Sircar
发明人： Hubert G. K. Barth , Ila Sircar
IPC分类号： C07D215/22 , C07D215/233 , C07D401/12
CPC分类号： C07D215/233 , C07D401/12
摘要： The present invention are novel 3-aminopropoxyaryl derivatives, compositions and methods of use thereof for treating congestive heart failure, coronary heart disease, or myocardial ischemia.
摘要翻译：本发明是新型3-氨基丙氧基芳基衍生物，其用于治疗充血性心力衰竭，冠心病或心肌缺血的组合物和用途。

55. 发明授权

US4734415A Substituted 4,5-dihydro-6-(substituted)-phenyl-3(2H)-pyridazinones and 6-(substituted) phenyl-3(2H)-pyridazinones 失效
标题翻译：取代的4,5-二氢-6-（取代的） - 苯基-3（2H） - 哒嗪酮和6-（取代的）苯基-3（2H） - 哒嗪酮
公开(公告)号：US4734415A
公开(公告)日：1988-03-29
申请号：US477695
申请日：1983-03-22
申请人： Ila Sircar , James A. Bristol
发明人： Ila Sircar , James A. Bristol
IPC分类号： C07D403/10 , C07D521/00 , C07D237/04 , A61K31/50
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D403/10
摘要： Substituted 4,5-dihydro-6-(substituted)phenyl-3(2H)-pyridazinone compounds and 6-(substituted)phenyl-3(2H)-pyridazinone compounds and pharmaceutically acceptable salts thereof are useful as cardiotonic and antihypertensive agents.Said compounds cause a significant increase in myocardial contractility in the dog. Said compounds also cause a decrease in blood pressure in the spontaneously hypertensive rat. Said compounds are produced by reacting substituted .gamma.-oxobenzenebutanoic acids with suitably substituted hydrazines to provide 4,5-dihydro-6-(substituted)phenyl-3(2H)-pyridazinones which are dehydrogenated to 6-(substituted)phenyl-3(2H)-pyridazinones.Both the intermediate 4,5-dihydro-6-(substituted)phenyl-3(2H)-pyridazinones and the 6-(substituted)phenyl-3(2H)-pyridazinones are useful as cardiotonic and antihypertensive agents.
摘要翻译：取代的4,5-二氢-6-（取代的）苯基-3（2H） - 哒嗪酮化合物和6-（取代的）苯基-3（2H） - 哒嗪酮化合物及其药学上可接受的盐可用作强心剂和抗高血压剂。所述化合物引起狗中心肌收缩力的显着增加。所述化合物还引起自发性高血压大鼠血压降低。所述化合物通过使取代的γ-氧代苯丁酸与适当取代的肼反应制得，得到4,5-二氢-6-（取代的）苯基-3（2H） - 哒嗪酮，将其脱氢为6-（取代的）苯基-3（2H ） - 哒嗪酮。中间体4,5-二氢-6-（取代的）苯基-3（2H） - 哒嗪酮和6-（取代的）苯基-3（2H） - 哒嗪酮均可用作强心剂和抗高血压剂。

56. 发明授权

US4607037A Cardiotonic 2(1H)-pyridinones 失效
标题翻译：强心2（1-H） - 吡啶酮
公开(公告)号：US4607037A
公开(公告)日：1986-08-19
申请号：US681737
申请日：1984-12-14
申请人： James A. Bristol , Ila Sircar
发明人： James A. Bristol , Ila Sircar
IPC分类号： C07D211/14 , C07D211/18 , C07D211/22 , C07D213/85 , C07D235/06 , C07D401/10 , C07D521/00 , A61K31/445
CPC分类号： C07D235/06 , C07D211/14 , C07D211/18 , C07D211/22 , C07D213/85 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/10
摘要： Certain 2(1H)-pyridinones are cardiotonic agents. Methods for their preparation and use are disclosed.
摘要翻译：某些2（1-H） - 吡啶酮是强心剂。公开了其制备和使用方法。

57. 发明授权

US4599332A 4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]-ethenyl]-3(2H)- pyridazinones and related compounds 失效
标题翻译： -4,5-二氢-6- [2- [4-（1H-咪唑-1-基）苯基] - 乙烯基] -3（2H） - 哒嗪酮和相关化合物
公开(公告)号：US4599332A
公开(公告)日：1986-07-08
申请号：US669323
申请日：1984-11-09
申请人： Ila Sircar
发明人： Ila Sircar
IPC分类号： C07D403/10 , C07D521/00 , A61K31/50
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D403/10
摘要： 4,5-Dihydro-6-[2-[4-(1H -imidazol-1-yl)phenyl]alkylenyl or alkylene-3(2H)-pyridazinones and related compounds and pharmaceutically acceptable acid addition salts thereof are useful as cardiotonic and antihypertensive agents.The above compounds cause a significant increase in myocardial contractility in the dog and also cause a decrease in blood pressure in the spontaneously hypertensive rat. The compounds are produced by reacting the appropriate .gamma.-oxobutanoic acid with a suitably substituted hydrazine to provide 4,5-dihydro-6-[4-[imidazolylphenyl]-alkenylene or alkylene-3(2H)-pyridazinones which may be oxidized to 6-[4-[imidazolylphenyl]alkenylene or alkylene-3(2H)-pyridazinones.
摘要翻译： 4,5-二氢-6- [2- [4-（1H-咪唑-1-基）苯基]亚烷基或亚烷基-3（2H） - 哒嗪酮及其相关化合物及其药学上可接受的酸加成盐可用作强心剂和抗高血压药。上述化合物引起狗中心肌收缩力的显着增加，并引起自发性高血压大鼠血压降低。通过使合适的γ-氧代丁酸与适当取代的肼反应制得化合物，得到4,5-二氢-6- [4- [咪唑基苯基] - 亚烯基或亚烷基-3（2H） - 哒嗪酮，其可被氧化成6 - [4- [咪唑基苯基]亚烯基或亚烷基-3（2H） - 哒嗪酮。

58. 发明授权

US4503061A Substituted phenyl-pyridinones as cardiotonic agents 失效
标题翻译：取代的苯基 - 吡啶酮作为强心剂
公开(公告)号：US4503061A
公开(公告)日：1985-03-05
申请号：US515799
申请日：1983-07-22
申请人： James A. Bristol , Ila Sircar
发明人： James A. Bristol , Ila Sircar
IPC分类号： C07D211/14 , C07D211/18 , C07D211/22 , C07D213/85 , C07D235/06 , C07D401/10 , C07D521/00 , C07D401/02 , A61K31/44
CPC分类号： C07D235/06 , C07D211/14 , C07D211/18 , C07D211/22 , C07D213/85 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/10
摘要： Certain 2(1H)-pyridinones are cardiotonic agents. Methods for their preparation and use are disclosed.
摘要翻译：某些2（1H） - 吡啶酮是强心剂。公开了其制备和使用方法。

59. 发明授权

US4413011A Substituted 2,2-dimethyl-5-phenoxypentanoic acid benzamides as anti-arteriosclerotic agents and method 失效
公开(公告)号：US4413011A
公开(公告)日：1983-11-01
申请号：US238398
申请日：1981-02-26
申请人： Ila Sircar , Ann Holmes
发明人： Ila Sircar , Ann Holmes
IPC分类号： A61K31/165 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/44 , A61K31/4406 , A61K31/4418 , A61P3/06 , A61P9/10 , C07C67/00 , C07C235/24 , C07C301/00 , C07C303/40 , C07C311/35 , C07D213/34 , C07D213/42 , A61K31/24 , C07C63/52 , C07C69/76
CPC分类号： C07D213/42 , Y10S514/824
摘要： New substituted 2,2-dimethyl-5-phenoxypentanoic acid benzamides which are useful as anti-arteriosclerotic agents are disclosed. These compounds elevate the high density lipoprotein fraction of cholesterol, and also lower the low density lipoprotein fraction of cholesterol.

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