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1.α- and β- amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors 有权
标题翻译: α-和β-二羧酸 - 氨基酸羟乙基氨基磺酰胺,可用作逆转录病毒蛋白酶抑制剂公开(公告)号:USRE42889E1
公开(公告)日:2011-11-01
申请号:US11788947
申请日:2007-04-23
申请人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Robert M. Heintz , Deborah E. Bertenshaw
发明人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Robert M. Heintz , Deborah E. Bertenshaw
IPC分类号: A61K31/36 , C07D317/50
CPC分类号: C07C311/05 , A61K38/00 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/18 , C07C311/20 , C07C311/24 , C07C311/29 , C07C311/32 , C07C311/41 , C07C311/46 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/28 , C07C317/44 , C07C323/49 , C07C323/67 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07D209/08 , C07D213/30 , C07D213/42 , C07D213/64 , C07D213/73 , C07D213/74 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D217/26 , C07D233/64 , C07D239/26 , C07D241/18 , C07D241/44 , C07D261/08 , C07D263/34 , C07D263/56 , C07D277/24 , C07D277/62 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/45 , C07D307/79 , C07D307/85 , C07D317/62 , C07D333/32 , C07D333/34 , C07D333/48 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D493/04 , C07K5/06026 , C07K5/06139
摘要: α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译: α-和β-氨基酸羟乙基氨基磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的,特别是作为HIV蛋白酶的抑制剂。
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2.
公开(公告)号:US20080176842A1
公开(公告)日:2008-07-24
申请号:US11940035
申请日:2007-11-14
IPC分类号: A61K31/18 , A61K31/495 , A61K31/445 , A61K31/496 , A61K31/5377 , C07D413/02 , C07D401/02 , C07D403/02 , C07D295/14 , C07C311/00 , A61P31/18
CPC分类号: C07C311/29 , C07D235/26 , C07D235/32 , C07D277/82 , C07D295/26 , C07D307/79 , C07D317/62 , C07D319/18 , C07D405/12
摘要: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.
摘要翻译: 双亚磺酰氨基羟乙基氨基化合物作为逆转录病毒蛋白酶抑制剂是有效的,特别是作为HIV蛋白酶的抑制剂。 本发明涉及下式的逆转录病毒蛋白酶抑制化合物:或其药学上可接受的盐,前药或酯,其中变量如本文所定义。
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公开(公告)号:US20080167255A1
公开(公告)日:2008-07-10
申请号:US11954170
申请日:2007-12-11
申请人: Eduardo J. Martinez , John J. Talley , Stephen Antonelli , Timothy C. Barden , Regina Lundrigan-Soucy , Wayne C. Schairer , Jing-Jing Yang , Daniel P. Zimmer , Brian Cali , Mark G. Currie , Peter S. Yorgey
发明人: Eduardo J. Martinez , John J. Talley , Stephen Antonelli , Timothy C. Barden , Regina Lundrigan-Soucy , Wayne C. Schairer , Jing-Jing Yang , Daniel P. Zimmer , Brian Cali , Mark G. Currie , Peter S. Yorgey
IPC分类号: A61K31/7052 , C07D205/04 , A61K31/397 , A61K31/69 , A61P9/00 , A61K31/66 , C07H15/00
CPC分类号: C07D205/08 , A61K31/337 , A61K31/397 , A61K45/06 , C07D263/20 , C07D401/04 , C07D405/10 , C07D409/04 , C07D453/02 , C07F7/1804 , C07F9/568 , C07H7/04 , C07H15/203 , A61K2300/00
摘要: 4-Biarylyl-1-phenylazetidin-2-ones useful for the treatment of hypercholesterolemia are disclosed. The compounds are of the general formula in which represents an aryl or heteroaryl residue; Ar represents an aryl residue; U is a two to six atom chain; and the R's represent substituents.
摘要翻译: 公开了可用于治疗高胆固醇血症的4-二苄基-1-苯基氮杂环丁-2-酮。 该化合物具有以下通式:其中表示芳基或杂芳基残基; Ar表示芳基残基; U是2至6个原子链; R代表取代基。
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4.α- and β-amino acid hydroxyethlamino sulfonyl urea derivatives useful as retroviral protease inhibitors 失效
标题翻译: 可用作逆转录病毒蛋白酶抑制剂的α-和β-氨基酸羟乙基氨基磺酰脲衍生物公开(公告)号:US07232817B2
公开(公告)日:2007-06-19
申请号:US11235524
申请日:2005-09-27
申请人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Eric T. Sun
发明人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Eric T. Sun
IPC分类号: A61K31/535 , A61K31/50 , C07D31/535 , C07D403/02 , C07D471/02
CPC分类号: C07D213/42 , C07C307/06 , C07D215/48 , C07D215/50 , C07D215/54 , C07D235/06 , C07D239/38 , C07D307/85 , C07K5/06026 , C07K5/06139 , C07K5/06191
摘要: α- and β-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译: α-和β-氨基酸羟乙基氨基磺酰脲衍生物化合物作为逆转录病毒蛋白酶抑制剂是有效的,特别是作为HIV蛋白酶的抑制剂。
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5.
公开(公告)号:US07115618B2
公开(公告)日:2006-10-03
申请号:US10812343
申请日:2004-03-30
申请人: Michael J. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Robert M. Heintz , Deborah E. Bertenshaw
发明人: Michael J. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Robert M. Heintz , Deborah E. Bertenshaw
IPC分类号: A61K31/36 , C07D317/50
CPC分类号: C07C311/05 , A61K38/00 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/18 , C07C311/20 , C07C311/24 , C07C311/29 , C07C311/32 , C07C311/41 , C07C311/46 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/28 , C07C317/44 , C07C323/49 , C07C323/67 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07D209/08 , C07D213/30 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D233/64 , C07D239/26 , C07D277/24 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/79 , C07D317/62 , C07D333/34 , C07D405/12 , C07D417/12 , C07K5/06026 , C07K5/06139
摘要: α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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6.
公开(公告)号:US07109211B2
公开(公告)日:2006-09-19
申请号:US10922036
申请日:2004-08-19
申请人: Jeffery S Carter , Mark G Obukowicz , Balekudru Devadas , John J Talley , David L Brown , Matthew J Graneto , Stephen R Bertenshaw , Donald J. Rogier, Jr. , Srinivasan Raj Nagarajan , Cathleen E Hanau , Susan J Hartmann , Cindy L Ludwig , Suzanne Metz , Donald E Korte
发明人: Jeffery S Carter , Mark G Obukowicz , Balekudru Devadas , John J Talley , David L Brown , Matthew J Graneto , Stephen R Bertenshaw , Donald J. Rogier, Jr. , Srinivasan Raj Nagarajan , Cathleen E Hanau , Susan J Hartmann , Cindy L Ludwig , Suzanne Metz , Donald E Korte
IPC分类号: A61K31/47 , C07D211/30
CPC分类号: C07D335/06 , C07D215/54 , C07D311/22 , C07D311/58 , C07D311/92 , C07D401/12 , C07D405/04 , C07D407/04 , C07D407/12 , C07D409/04 , C07D471/04 , C07D491/04 , C07D493/04
摘要: A class of benzopyran, derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I′ wherein X, A1, A2, A3, A4, R, R″, R1 and R2 are as described in the specification.
摘要翻译: 描述了一类苯并吡喃衍生物用于治疗环氧合酶-2介导的病症。 特别感兴趣的化合物由式I'定义,其中X,A 1,A 2,A 3,A 4, SUP>,R,R“,R”1“和”R“2如说明书中所述。
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7.3,4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents 失效
标题翻译: 具有用作抗炎剂的3,4-二芳基噻吩及其类似物公开(公告)号:US07030153B2
公开(公告)日:2006-04-18
申请号:US10329332
申请日:2002-12-27
申请人: John J. Talley , Stephen R. Bertenshaw , Paul W. Collins , Thomas D. Penning , David B. Reitz , Roland S. Rogers
发明人: John J. Talley , Stephen R. Bertenshaw , Paul W. Collins , Thomas D. Penning , David B. Reitz , Roland S. Rogers
IPC分类号: A61K31/38 , C07D333/16
CPC分类号: C07D307/38 , A61K31/341 , A61K31/365 , C07D307/58 , C07D333/16 , C07D333/18 , C07D333/28 , C07D333/38 , C07D409/04
摘要: A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: wherein Y is selected from O, S and NR1; wherein R1 is selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R2 and R3 are independently aryl or heteroaryl; and wherein R2 and R3 are optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译: 一类3,4-二芳基取代的噻吩,呋喃和吡咯衍生物及其类似物,含有它们的药物组合物和使用它们治疗炎症和炎症相关疾病的方法。 特别感兴趣的化合物由式I定义:其中Y选自O,S和NR 1; 其中R 1选自氢和低级烷基; 其中X是一个或两个选自氢,卤素,低级烷氧基羰基和羧基的取代基; 其中R 2和R 3独立地是芳基或杂芳基; 并且其中R 2和R 3在任选被一个或多个选自亚磺酰基,烷基磺酰基,卤素,低级烷氧基和低级烷基基团的基团任选取代; 或其药学上可接受的盐。
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公开(公告)号:US06762187B2
公开(公告)日:2004-07-13
申请号:US10245710
申请日:2002-09-18
申请人: John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Kathryn L. Reed , Ko-Chung Lin , John Nicholas Freskos , Michael Clare , Donald Joseph Rogier, Jr. , Robert M. Heintz , Michael L. Vazquez , Richard A. Mueller
发明人: John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Kathryn L. Reed , Ko-Chung Lin , John Nicholas Freskos , Michael Clare , Donald Joseph Rogier, Jr. , Robert M. Heintz , Michael L. Vazquez , Richard A. Mueller
IPC分类号: A61K314965
CPC分类号: C07D401/12 , C07D207/16 , C07D211/60 , C07D217/26
摘要: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译: 含有羟基胺化合物的N-杂环部分作为逆转录病毒蛋白酶抑制剂是有效的,特别是作为HIV蛋白酶抑制剂。
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9.Thiophene substituted hydroxamic acid derivatives as cyclooxygenase-2 and 5-lipoxygenase inhibitors 失效
标题翻译: 噻吩取代的异羟肟酸衍生物作为环加氧酶-2和5-脂氧合酶抑制剂公开(公告)号:US06753344B2
公开(公告)日:2004-06-22
申请号:US10317751
申请日:2002-12-12
申请人: John J. Talley , James A. Sikorski , Matthew J. Graneto , Jeffery S. Carter , Bryan H. Norman , Balekudru Devadas , Hwang-Fun Lu
发明人: John J. Talley , James A. Sikorski , Matthew J. Graneto , Jeffery S. Carter , Bryan H. Norman , Balekudru Devadas , Hwang-Fun Lu
IPC分类号: A61K3138
CPC分类号: C07D231/12 , C07D263/32
摘要: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.
摘要翻译: 本发明涉及抗炎药物领域,具体涉及用于治疗由环氧合酶-2或5-脂氧合酶如炎症介导的病症的化合物,组合物和方法。
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公开(公告)号:US06750338B2
公开(公告)日:2004-06-15
申请号:US10268818
申请日:2002-10-10
申请人: Matthew J. Graneto , Michael L. Vazquez , Susan J. Hartmann , Suzanne Metz , John J. Talley , David L. Brown , Richard M. Weier , Michael A. Stealey , Xiangdong Xu
发明人: Matthew J. Graneto , Michael L. Vazquez , Susan J. Hartmann , Suzanne Metz , John J. Talley , David L. Brown , Richard M. Weier , Michael A. Stealey , Xiangdong Xu
IPC分类号: C07D40104
CPC分类号: C07D401/14 , C07D231/18 , C07D339/00 , C07D401/04 , C07D405/14 , C07D409/06
摘要: This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.
摘要翻译: 本发明涉及制备用作p38激酶和COX-2抑制剂的选择的5-取代的吡唑的新方法。
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