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1.发明授权
公开(公告)号：US5504104A
公开(公告)日：1996-04-02
申请号：US155412
申请日：1993-11-19
IPC分类号： C07D311/92 , C07D311/94 , A61K31/35 , C07D311/78
CPC分类号： C07D311/94 , C07D311/92 , Y10S514/885
摘要： The present invention relates to novel substituted tricyclic pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The tricyclic pyrone derivatives are useful in the development of therapies for the treatment of vital infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized tricyclic pyrones and of related structures.
摘要翻译： 本发明涉及新型取代的三环pyrones和有效抑制HIV天冬氨酰蛋白酶阻断HIV感染性的相关结构。 三环吡喃酮衍生物可用于开发用于治疗重要感染和疾病（包括AIDS）的治疗。 本发明还涉及合成多功能三环pyrones和相关结构的方法。
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公开(公告)号：US5389682A
公开(公告)日：1995-02-14
申请号：US118374
申请日：1993-09-13
申请人： Bradley D. Tait , Michael W. Wilson
发明人： Bradley D. Tait , Michael W. Wilson
IPC分类号： C07C275/26 , C07C275/30 , C07C275/34 , C07C275/42 , C07C311/16 , C07C311/58 , C07C317/42 , C07C323/44 , C07C335/12 , C07D209/18 , A61K31/17 , A61K31/18 , C07C275/28
CPC分类号： C07C275/26 , C07C275/30 , C07C275/34 , C07C275/42 , C07C311/16 , C07C311/58 , C07C317/42 , C07C323/44 , C07C335/12 , C07D209/18 , C07C2101/14 , C07C2103/74
摘要： The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.
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公开(公告)号：US6001866A
公开(公告)日：1999-12-14
申请号：US51002
申请日：1998-03-20
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。
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公开(公告)号：US5510375A
公开(公告)日：1996-04-23
申请号：US155728
申请日：1993-11-19
IPC分类号： C07D311/56 , A61K31/35
CPC分类号： C07D311/56
摘要： The present invention relates to novel coumarin derivatives and related compounds which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The coumarin derivatives are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized coumarins and of related structures.
摘要翻译： 本发明涉及有效抑制HIV天冬氨酰蛋白酶阻断HIV感染性的新型香豆素衍生物和相关化合物。 香豆素衍生物可用于开发用于治疗病毒感染和疾病（包括AIDS）的治疗。 本发明还涉及多功能香豆素的合成方法和相关结构。
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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。
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