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1. 发明申请

US20080227974A1 Novel Substituted Azetidinones 审中-公开
标题翻译：新型取代的氮杂环丁酮
公开(公告)号：US20080227974A1
公开(公告)日：2008-09-18
申请号：US11997391
申请日：2006-07-20
申请人： Jeffrey A. Pfefferkorn , Bharat K. Trivedi
发明人： Jeffrey A. Pfefferkorn , Bharat K. Trivedi
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。

2. 发明授权

US6001866A Method for treating and preventing inflammation and atherosclerosis 失效
标题翻译：治疗和预防炎症和动脉粥样硬化的方法
公开(公告)号：US6001866A
公开(公告)日：1999-12-14
申请号：US51002
申请日：1998-03-20
申请人： Joseph A. Cornicelli , Bradley D. Tait , Bharat K. Trivedi
发明人： Joseph A. Cornicelli , Bradley D. Tait , Bharat K. Trivedi
IPC分类号： A61K31/40 , A61K31/454 , A61K31/38 , A61K31/535 , A61K31/54
CPC分类号： A61K31/454 , A61K31/40
摘要： This invention provides a method for treating or preventing inflammation or atherosclerosis in mammals comprising administering an effective amount of a 15-LO inhibitor of Formula I: ##STR1## wherein: R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently are hydrogen, C.sub.1 -C.sub.6 alkyl, nitro, halo, CN, OR.sup.6, NR.sup.6 R.sup.7, --CO.sub.2 R.sup.6, CONR.sup.6 R.sup.7, CH.sub.2 OR.sup.6, or CH.sub.2 NR.sup.6 R.sup.7, and R.sup.2 and R.sup.3, and R.sup.4 and R.sup.5, when attached to adjacent ring atoms, can be --(CH.sub.2).sub.3 or 4 --;in which R.sup.6 and R.sup.7 independently are hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or benzyl, and when taken together with the nitrogen to which they are attached, R.sup.6 and R.sup.7 can complete a cyclic ring having from 3 to 7 carbon atoms; ##STR2## in which R.sup.8, R.sup.8', R.sup.9, and R.sup.9' independently are hydrogen or C.sub.1 -C.sub.6 alkyl, n is 0, 1, or 2, and Z.sup..crclbar. is an anion, and pharmaceutically acceptable salts thereof.
摘要翻译： PCT No.PCT / US96 / 14242 Sec。 371日期：1998年3月20日 102（e）1998年3月20日PCT PCT 1996年9月5日PCT公布。公开号WO97 / 12613 日本1997年4月10日本发明提供了治疗或预防哺乳动物炎症或动脉粥样硬化的方法，其包括给予有效量的式I的15-LO抑制剂：其中：R1是氢或C1-C6烷基; R2，R3，R4和R5独立地是氢，C1-C6烷基，硝基，卤素，CN，OR6，NR6R7，-CO2R6，CONR6R7，CH2OR6或CH2NR6R7，R2和R3，R4和R5连接到相邻的环原子可以是 - （CH 2）3或4-; 其中R6和R7独立地是氢，C1-C6烷基，苯基或苄基，当与它们所连接的氮一起时，R6和R7可以完成具有3至7个碳原子的环; 其中R8，R8'，R9和R9'独立地是氢或C1-C6烷基，n是0,1或2，并且Z（ - ）是一个阴离子，及其药学上可接受的盐。

3. 发明授权

US5620997A Isothiazolones 失效
标题翻译：异噻唑啉酮
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。

4. 发明授权

US5593967A Cholecystokinin antagonists, their preparation and therapeutic use 失效
标题翻译：缩胆囊素拮抗剂，其制备和治疗用途
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。

5. 发明授权

US4948806A Antihyperlipidemic and antiatherosclerotic compounds and compositions 失效
标题翻译：抗高脂血症和抗动脉粥样硬化的化合物和组合物
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。

6. 发明授权

US07244763B2 Compounds that modulate PPAR activity and methods of preparation 失效
标题翻译：调节PPAR活性的化合物和制备方法
公开(公告)号：US07244763B2
公开(公告)日：2007-07-17
申请号：US10774260
申请日：2004-02-06
申请人： Larry D. Bratton , Xue-Min Cheng , Noe Erasga , Gary F. Filzen , Andrew G. Geyer , Chitase Lee , Bharat K. Trivedi , Paul C. Unangst
发明人： Larry D. Bratton , Xue-Min Cheng , Noe Erasga , Gary F. Filzen , Andrew G. Geyer , Chitase Lee , Bharat K. Trivedi , Paul C. Unangst
IPC分类号： A61K31/235 , A61K31/38 , A61K31/35 , C07D405/00 , C07D261/06
CPC分类号： C07D213/74 , C07C59/72 , C07C62/34 , C07C323/20 , C07C323/21 , C07C323/22 , C07C323/25 , C07C323/62 , C07C2601/02 , C07C2602/08 , C07C2602/10 , C07C2603/18 , C07D213/34 , C07D215/36 , C07D261/08 , C07D263/57 , C07D263/58 , C07D307/79 , C07D311/58 , C07D333/22 , C07D333/60 , C07D405/12 , C07D413/12 , C07D417/12
摘要： This invention relates to compounds that alter PPAR activity. The invention also relates to pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing dyslipidemia, hypercholesterolemia, obesity, hyperglycemia, atherosclerosis, hypertriglyceridemia and hyperinsulinemia in a mammal. The present invention also relates to methods for making the disclosed compounds.
摘要翻译：本发明涉及改变PPAR活性的化合物。本发明还涉及化合物的药学上可接受的盐，包含该化合物或其盐的药学上可接受的组合物，以及使用它们作为治疗或预防哺乳动物血脂异常，高胆固醇血症，肥胖症，高血糖症，动脉粥样硬化，高甘油三酯血症和高胰岛素血症的治疗剂的方法。本发明还涉及制备所公开的化合物的方法。

7. 发明授权

US5331006A Amino acid analogs as CCK antagonists 失效
标题翻译：氨基酸类似物作为CCK拮抗剂
公开(公告)号：US5331006A
公开(公告)日：1994-07-19
申请号：US726656
申请日：1991-07-12
申请人： David C. Horwell , Julian Aranda , Corinne Augelli-Szafran , Hans-Jurgen Betche , Ann Holmes , Michael D. Mullican , Martyn C. Pritchard , Reginald S. Richardson , Edward Roberts , Bruce D. Roth , Bradley D. Tait , Bharat K. Trivedi , Uwe Trostmann , Paul C. Unangst
发明人： David C. Horwell , Julian Aranda , Corinne Augelli-Szafran , Hans-Jurgen Betche , Ann Holmes , Michael D. Mullican , Martyn C. Pritchard , Reginald S. Richardson , Edward Roberts , Bruce D. Roth , Bradley D. Tait , Bharat K. Trivedi , Uwe Trostmann , Paul C. Unangst
IPC分类号： C07C271/34 , C07D207/32 , C07D207/327 , C07D213/56 , C07D213/89 , C07D215/12 , C07D231/56 , C07D233/26 , C07D235/16 , C07D243/16 , C07D243/24 , C07D249/18 , C07D261/08 , C07D277/46 , C07D285/06 , C07D307/79 , C07D307/81 , C07D307/82 , C07D333/60 , C07D403/12 , C07D471/04 , A61K31/27 , C07C271/10
CPC分类号： C07D403/12 , C07C271/34 , C07D207/327 , C07D213/56 , C07D213/89 , C07D215/12 , C07D231/56 , C07D233/26 , C07D235/16 , C07D243/16 , C07D243/24 , C07D249/18 , C07D261/08 , C07D277/46 , C07D285/06 , C07D307/79 , C07D307/81 , C07D307/82 , C07D333/60 , C07D471/04 , C07C2103/74
摘要： Novel unnatural dipeptoids 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. The compounds are agents useful for preventing the response to withdrawal from chronic treatment or use of nicotine, diazepam, alcohol, cocaine, caffeine, and opioids. The compounds are also useful in treating and/or preventing panic attacks. Also disclosed are pharmaceutical compositions and methods of treatment using the dipeptoids 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 to prepare diagnostic compositions.
摘要翻译：公开了用作治疗肥胖症，胃肠胃分泌过多，胃泌素依赖性肿瘤或抗精神病药物的新型非天然罂粟脂。此外，化合物是抗焦虑剂和抗溃疡剂。这些化合物是可用于预防慢性治疗或使用尼古丁，地西泮，酒精，可卡因，咖啡因和阿片样物质的戒断反应的药剂。这些化合物也可用于治疗和/或预防恐慌发作。还公开了药物组合物和使用二趾甲的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用于制备诊断组合物的用途。

8. 发明授权

US5208224A Phosphorus containing compounds as antihypercholesterolemic and antiatherosclerotic agents 失效
标题翻译：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
申请人： Gary L. Bolton , Janak K. Padia , Bharat K. Trivedi
发明人： Gary L. Bolton , Janak K. Padia , Bharat K. Trivedi
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。

9. 发明授权

US5155127A N-(substituted aryl)-N'-(substituted alkoxy)-ureas and thioureas as antihypercholesterolemic and antiatherosclerotic agents 失效
标题翻译： 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.

10. 发明授权

US4923896A N-(substituted aryl)-N'-(substituted alkoxy)-ureas and thioureas as antihypercholesterolemic and antiatherosclerotic agents 失效
标题翻译： 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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