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公开(公告)号：US5620997A
公开(公告)日：1997-04-15
申请号：US456149
申请日：1995-05-31
申请人： Gary L. Bolton , John M. Domagala , Edward F. Elslager , Rocco D. Gogliotti , Terri S. Purchase , Joseph P. Sanchez , Bharat K. Trivedi
发明人： Gary L. Bolton , John M. Domagala , Edward F. Elslager , Rocco D. Gogliotti , Terri S. Purchase , Joseph P. Sanchez , Bharat K. Trivedi
IPC分类号： A61K31/428 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/519 , A61K31/5377 , A61P9/10 , A61P29/00 , A61P31/12 , A61P31/14 , C07D275/04 , C07D417/04 , C07D513/04 , C07D513/14 , C07D275/06 , A61K31/41
CPC分类号： C07D275/04 , C07D513/04 , C07D513/14
摘要： Isothiazolones having the general structure ##STR1## where A is a monocyclic or bicyclic ring which may contain up to 3 heteroatoms selected from O, S, and N; R.sup.1 and R.sup.2 are substituent groups such as alkyl, alkoxy, hydroxy, nitro, cyano, amino, and carboxy; and R.sup.5 is alkyl, cycloalkyl, phenyl, and Het. The isothiazolones are useful as anti-retroviral agents, anti-inflammatory agents, and anti-atherosclerotic agents.
摘要翻译： 具有一般结构
的异噻唑酮，其中A是可以含有至多3个选自O，S和N的杂原子的单环或双环; R1和R2是取代基，例如烷基，烷氧基，羟基，硝基，氰基，氨基和羧基; R5是烷基，环烷基，苯基和Het。 异噻唑酮可用作抗逆转录病毒剂，抗炎剂和抗动脉粥样硬化剂。 -
公开(公告)号：US5593967A
公开(公告)日：1997-01-14
申请号：US41647
申请日：1993-04-01
申请人： David C. Horwell , Edward Roberts , Ann Holmes , Janak K. Padia , William H. Roark , Bruce D. Roth , Bharat K. Trivedi , Jurgen Kleinschroth , David C. Rees , Reginald S. Richardson
发明人： David C. Horwell , Edward Roberts , Ann Holmes , Janak K. Padia , William H. Roark , Bruce D. Roth , Bharat K. Trivedi , Jurgen Kleinschroth , David C. Rees , Reginald S. Richardson
IPC分类号： A61K38/00 , C07D209/14 , C07D209/20 , C07K5/02 , C07K5/065 , C07K5/078 , C07K14/595 , C07D209/18 , C07D217/00
CPC分类号： C07K14/595 , C07D209/14 , C07D209/20 , C07K5/0202 , C07K5/06078 , C07K5/06156 , A61K38/00
摘要： Novel cholecystokinin antagonists useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further, the compounds are antianxiety agents and antiulcer agents. They are agents useful for preventing the response to the withdrawal from chronic treatment with use of nicotine, diazepam, alcohol, cocaine, coffee, or opioids. The compounds of the invention are also useful in treating and/or preventing panic. Also disclosed are pharmaceutical compositions and methods of treatment using the antagonists as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds in diagnostic compositions.
摘要翻译： 新颖的缩胆囊素拮抗剂可用作治疗肥胖的药物，胃肠胃分泌过多，胃泌素依赖性肿瘤或抗精神病药。 此外，化合物是抗焦虑剂和抗溃疡剂。 它们是用于防止使用尼古丁，地西泮，酒精，可卡因，咖啡或阿片样物质从慢性治疗中撤回的反应的药剂。 本发明的化合物也可用于治疗和/或预防恐慌。 还公开了使用拮抗剂的药物组合物和治疗方法以及制备它们的方法和可用于其制备的新型中间体。 本发明的另一个特征是本发明化合物在诊断组合物中的用途。
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13.发明授权
公开(公告)号：US4948806A
公开(公告)日：1990-08-14
申请号：US364349
申请日：1989-06-09
申请人： Bharat K. Trivedi
发明人： Bharat K. Trivedi
IPC分类号： C07C275/28 , C07D311/58 , C07D311/90 , C07D313/08
CPC分类号： C07D311/58 , C07C275/28 , C07D311/90 , C07D313/08 , C07C2102/08 , C07C2102/10 , C07C2103/18
摘要： Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.
摘要翻译： 某些N-2,6-二烷基 - 或N-2,6-二烷氧基苯基-N'-芳烷基脲化合物是酶酰基CoA：胆固醇酰基转移酶（ACAT）的有效抑制剂，因此是治疗高胆固醇血症或动脉粥样硬化的有用药物 。
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14.发明授权Phosphorus containing compounds as antihypercholesterolemic and antiatherosclerotic agents 失效含磷化合物作为抗高胆固醇血症和抗动脉粥样硬化剂
公开(公告)号：US5208224A
公开(公告)日：1993-05-04
申请号：US668534
申请日：1991-03-13
IPC分类号： C07F9/32 , C07F9/40 , C07F9/44 , C07F9/6584
CPC分类号： C07F9/65842 , C07F9/3211 , C07F9/4006 , C07F9/4407
摘要： Novel phosphorus containing compounds are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.
摘要翻译： 描述了新的含磷化合物，以及其制备方法及其药物组合物，其可用于预防肠内胆固醇吸收，因此可用于治疗高胆固醇血症和动脉粥样硬化。
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15.发明授权N-(substituted aryl)-N'-(substituted alkoxy)-ureas and thioureas as antihypercholesterolemic and antiatherosclerotic agents 失效N-（取代的芳基）-N' - （取代的烷氧基） - 硫脲和硫脲作为抗胆碱酯酶和抗菌药物
公开(公告)号：US5155127A
公开(公告)日：1992-10-13
申请号：US462563
申请日：1990-01-18
申请人： Bharat K. Trivedi
发明人： Bharat K. Trivedi
IPC分类号： A61K31/17 , A61K31/35 , A61K31/352 , A61K31/353 , A61K31/38 , A61K31/382 , A61P3/06 , A61P9/10 , C07C273/18 , C07C275/28 , C07C275/64 , C07C335/16 , C07C335/40 , C07D311/20 , C07D335/06
CPC分类号： C07C275/28 , C07C275/64 , C07C335/16
摘要： Novel N-[substituted aryl]-N'-(substituted alkoxy)-urea and thiourea derivatives are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.
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16.发明授权N-(substituted aryl)-N'-(substituted alkoxy)-ureas and thioureas as antihypercholesterolemic and antiatherosclerotic agents 失效N-（取代的芳基）-N' - （取代的烷氧基） - 脲和硫脲作为抗高胆固醇血症和抗动脉粥样硬化剂
公开(公告)号：US4923896A
公开(公告)日：1990-05-08
申请号：US308911
申请日：1989-02-09
申请人： Bharat K. Trivedi
发明人： Bharat K. Trivedi
IPC分类号： C07C275/28 , C07C275/64
CPC分类号： C07C275/28 , C07C275/64
摘要： Novel N-[substituted aryl]-N'-(substituted alkoxy)-urea and thiourea derivatives are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.
摘要翻译： 描述了新的N- [取代的芳基] -N' - （取代的烷氧基） - 脲和硫脲衍生物，以及其制备方法和药物组合物，其可用于预防胆固醇的肠道吸收，因此是有用的 在治疗高胆固醇血症和动脉粥样硬化。
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公开(公告)号：US20080227974A1
公开(公告)日：2008-09-18
申请号：US11997391
申请日：2006-07-20
IPC分类号： C07D205/04
CPC分类号： C07D205/08
摘要： Novel azetidinones and pharmaceutical compositions are described, as are the methods of using such compounds and compositions to treat subjects, including humans, suffering from hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis.
摘要翻译： 还描述了新的氮杂环丁酮和药物组合物，以及使用这些化合物和组合物来治疗患有高脂血症，高胆固醇血症，高甘油三酯血症和动脉粥样硬化的受试者（包括人）的方法。
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公开(公告)号：US4791103A
公开(公告)日：1988-12-13
申请号：US771590
申请日：1985-09-05
CPC分类号： C07H19/16
摘要： Novel N.sup.6 -substituted adenosines having desirable ratio of affinities at A1 or A2 receptors and highly desirable central nervous system and cardiovascular activities, such as analgesic, antipsychotic, sedative, or antihypertensive as well as immunoinflammatory activity.
摘要翻译： 新的N6-取代的腺苷在A1或A2受体和非常需要的中枢神经系统和心血管活动（例如止痛剂，抗精神病药，镇静剂或抗高血压药物）以及免疫炎症活性中具有合适的亲和力比例。
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19.发明授权
公开(公告)号：US4683223A
公开(公告)日：1987-07-28
申请号：US772984
申请日：1985-09-09
申请人： Bharat K. Trivedi
发明人： Bharat K. Trivedi
CPC分类号： C07H19/16
摘要： N.sup.6 -Benzopyrano- and benzothiopyranoadenosines and pharmaceutically acceptable acid addition salts having highly desirable central nervous system antiinflammatory and antihypertensive properties, processes for their manufacture and pharmaceutical compositions and methods for using said compounds and compositions are described.
摘要翻译： 描述了具有高度期望的中枢神经系统抗炎和抗高血压性质的N6-苯并吡喃并苯并噻喃并腺苷和其药学上可接受的酸加成盐，其制备方法和药物组合物以及使用所述化合物和组合物的方法。
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公开(公告)号：US4673670A
公开(公告)日：1987-06-16
申请号：US857891
申请日：1986-04-30
CPC分类号： C07H19/16
摘要： N.sup.6 -Acenaphthyl adenosines and analogs thereof and pharmaceutically acceptable acid addition salts having highly desirable blood pressure lowering properties, processes for their manufacture and pharmaceutical compositions and methods for using said compounds and compositions are described.
摘要翻译： 描述了N6-苊基腺苷及其类似物和具有高度期望的降血压性质的药学上可接受的酸加成盐，其制备方法和药物组合物以及使用所述化合物和组合物的方法。
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