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1.
公开(公告)号:US20050049252A1
公开(公告)日:2005-03-03
申请号:US10922036
申请日:2004-08-19
申请人: Jeffery Carter , Mark Obukowicz , Balekudru Devadas , John Talley , David Brown , Matthew Graneto , Stephen Bertenshaw , Donald Rogier , Srinivasan Nagarajan , Cathleen Hanau , Susan Hartmann , Cindy Ludwig , Suzanne Metz , Donald Korte
发明人: Jeffery Carter , Mark Obukowicz , Balekudru Devadas , John Talley , David Brown , Matthew Graneto , Stephen Bertenshaw , Donald Rogier , Srinivasan Nagarajan , Cathleen Hanau , Susan Hartmann , Cindy Ludwig , Suzanne Metz , Donald Korte
IPC分类号: A61K31/35 , A61K31/352 , A61K31/36 , A61K31/382 , A61K31/4184 , A61K31/436 , A61K31/4375 , A61K31/47 , A61P29/00 , A61P43/00 , C07D215/54 , C07D311/22 , C07D311/58 , C07D311/92 , C07D335/06 , C07D401/12 , C07D405/04 , C07D407/04 , C07D407/12 , C07D409/04 , C07D471/04 , C07D491/04 , C07D491/052 , C07D493/04 , C07D471/02 , A61K31/519 , C07D491/02 , C07D498/02
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,R,R“,R 1和R 2如 在说明书中描述。
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2.Process for preparing prodrugs of benzenesulfonamide-containing COX-2 inhibitors 有权
标题翻译: 制备含苯磺酰胺的COX-2抑制剂前药的方法公开(公告)号:US07420061B2
公开(公告)日:2008-09-02
申请号:US10939852
申请日:2004-09-13
申请人: John J. Talley , James W. Malecha , Stephen Bertenshaw , Matthew J. Graneto , Jeffery S. Carter , Jinglin Li , Srinivasan R. Nagarajan , David L. Brown , Donald J. Rogier, Jr. , Thomas D. Penning , Ish K. Khanna , Xiangdong Xu , Richard M. Weier
发明人: John J. Talley , James W. Malecha , Stephen Bertenshaw , Matthew J. Graneto , Jeffery S. Carter , Jinglin Li , Srinivasan R. Nagarajan , David L. Brown , Donald J. Rogier, Jr. , Thomas D. Penning , Ish K. Khanna , Xiangdong Xu , Richard M. Weier
IPC分类号: C07D263/04
CPC分类号: C07D207/33 , A61K31/18 , A61K31/415 , A61K31/42 , A61K31/635 , C07C311/16 , C07C311/51 , C07C2601/10 , C07D231/12 , C07D233/64 , C07D261/08 , C07D263/32 , C07D307/58 , C07D401/04 , C07D417/04 , C07D495/04
摘要: Prodrugs of COX-2 inhibitors are described as being useful in treating inflammation and inflammation-related disorders.
摘要翻译: 描述了COX-2抑制剂的前药用于治疗炎症和炎症相关疾病。
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3.Process for preparing prodrugs of benzenesulfonamide-containing cox-2 inhibitors 有权
标题翻译: 制备含苯磺酰胺的cox-2抑制剂的前药的方法公开(公告)号:US06436967B1
公开(公告)日:2002-08-20
申请号:US09661859
申请日:2000-09-14
申请人: John J Talley , James W Malecha , Stephen Bertenshaw , Matthew J Graneto , Jeffery Carter , Jinglin Li , Srinivasan Nagarajan , David L Brown , Donald J Rogier, Jr. , Thomas D Penning , Ish K Khanna , Xiangdong Xu , Richard M Weier
发明人: John J Talley , James W Malecha , Stephen Bertenshaw , Matthew J Graneto , Jeffery Carter , Jinglin Li , Srinivasan Nagarajan , David L Brown , Donald J Rogier, Jr. , Thomas D Penning , Ish K Khanna , Xiangdong Xu , Richard M Weier
IPC分类号: A61K3144
CPC分类号: C07D207/33 , A61K31/18 , A61K31/415 , A61K31/42 , A61K31/635 , C07C311/16 , C07C311/51 , C07C2601/10 , C07D231/12 , C07D233/64 , C07D261/08 , C07D263/32 , C07D307/58 , C07D401/04 , C07D417/04 , C07D495/04
摘要: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to prodrugs of compounds which selectively inhibit cyclooxygenase-2. The use of non-steroidal antiinflammatory drugs (NSAIDs) in treating pain and the swelling associated with inflammation also produce severe side effects, including life threatening ulcers. The recent discovery of an inducible enzyme associated with inflammation (“prostaglandin G/H synthase II” or “cyclooxygenase-2 (COX-2)”) provides a viable target of inhibition which more effectively reduces inflammation and produces fewer and less drastic side effects.
摘要翻译: 本发明涉及抗炎药物领域,具体涉及选择性抑制环加氧酶-2的化合物的前药。非甾体抗炎药(NSAID)在治疗疼痛和与炎症有关的肿胀中的应用也产生严重的副作用, 包括危及生命的溃疡。 最近发现与炎症相关的可诱导酶(“前列腺素G / H合酶II”或“环加氧酶-2(COX-2)”)提供了可行的抑制靶标,其更有效地减少炎症并产生越来越少的副作用 。
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4.Process for preparing prodrugs of benzenesulfonamide-containing cox-2 inhibitors 失效
标题翻译: 制备含苯磺酰胺的cox-2抑制剂的前药的方法公开(公告)号:US06815460B2
公开(公告)日:2004-11-09
申请号:US10178697
申请日:2002-06-24
申请人: John J Talley , James W Malecha , Stephen Bertenshaw , Matthew J Graneto , Jeffery Carter , Jinglin Li , Srinivasan Nagarajan , David L Brown , Donald J Rogier, Jr. , Thomas D Penning , Ish K Khanna , Xiangdong Xu , Richard M Weier
发明人: John J Talley , James W Malecha , Stephen Bertenshaw , Matthew J Graneto , Jeffery Carter , Jinglin Li , Srinivasan Nagarajan , David L Brown , Donald J Rogier, Jr. , Thomas D Penning , Ish K Khanna , Xiangdong Xu , Richard M Weier
IPC分类号: A61K3142
CPC分类号: C07D207/33 , A61K31/18 , A61K31/415 , A61K31/42 , A61K31/635 , C07C311/16 , C07C311/51 , C07C2601/10 , C07D231/12 , C07D233/64 , C07D261/08 , C07D263/32 , C07D307/58 , C07D401/04 , C07D417/04 , C07D495/04
摘要: Prodrugs of COX-2 inhibitors and methods of their preparation are described. The prodrugs of COX-2 inhibitors are described as being useful in treating inflammation and inflammation-related disorders.
摘要翻译: 描述了COX-2抑制剂的前体药物及其制备方法。 COX-2抑制剂的前药被描述为可用于治疗炎症和炎症相关疾病。
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公开(公告)号:US5932598A
公开(公告)日:1999-08-03
申请号:US5610
申请日:1998-01-12
申请人: John J Talley , James W Malecha , Stephen Bertenshaw , Matthew J Graneto , Jeffery Carter , Jinglin Li , Srinivasan Nagarajan , David L Brown , Donald J Rogier, Jr. , Thomas D Penning , Ish K Khanna , Xiangdong Xu , Richard M Weier
发明人: John J Talley , James W Malecha , Stephen Bertenshaw , Matthew J Graneto , Jeffery Carter , Jinglin Li , Srinivasan Nagarajan , David L Brown , Donald J Rogier, Jr. , Thomas D Penning , Ish K Khanna , Xiangdong Xu , Richard M Weier
IPC分类号: C07D233/64 , A61K31/00 , A61K31/18 , A61K31/34 , A61K31/341 , A61K31/365 , A61K31/40 , A61K31/415 , A61K31/4162 , A61K31/4164 , A61K31/42 , A61K31/421 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/635 , A61P1/02 , A61P1/04 , A61P3/10 , A61P5/16 , A61P7/06 , A61P9/10 , A61P11/02 , A61P11/06 , A61P11/08 , A61P13/12 , A61P15/06 , A61P17/02 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/08 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/28 , A61P27/02 , A61P27/12 , A61P29/00 , A61P29/02 , A61P31/12 , A61P35/00 , A61P37/00 , A61P43/00 , C07C311/16 , C07C311/39 , C07C311/51 , C07D20060101 , C07D207/32 , C07D207/327 , C07D207/33 , C07D231/12 , C07D233/54 , C07D233/62 , C07D261/08 , C07D263/32 , C07D307/46 , C07D307/58 , C07D401/04 , C07D417/04 , C07D495/04 , A61K31/16 , C07D207/00 , C07D207/12 , C07D211/72 , C07D211/84 , C07D223/04 , C07D231/10 , C07D403/02
CPC分类号: C07D207/33 , A61K31/18 , A61K31/415 , A61K31/42 , A61K31/635 , C07C311/16 , C07C311/51 , C07D231/12 , C07D233/64 , C07D261/08 , C07D263/32 , C07D307/58 , C07D401/04 , C07D417/04 , C07D495/04 , C07C2101/10
摘要: Prodrugs of COX-2 inhibitors are described as being useful in treating inflammation and inflammation-related disorders.
摘要翻译: 描述了COX-2抑制剂的前药用于治疗炎症和炎症相关疾病。
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公开(公告)号:US20050131050A1
公开(公告)日:2005-06-16
申请号:US11048037
申请日:2005-01-31
申请人: John Talley , Thomas Penning , Paul Collins , Donald Rogier , James Malecha , Julie Miyashiro , Stephen Bertenshaw , Ish Khanna , Matthew Graneto , Roland Rogers , Jeffery Carter , Stephen Docter , Stella Yu
发明人: John Talley , Thomas Penning , Paul Collins , Donald Rogier , James Malecha , Julie Miyashiro , Stephen Bertenshaw , Ish Khanna , Matthew Graneto , Roland Rogers , Jeffery Carter , Stephen Docter , Stella Yu
IPC分类号: C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D495/04 , A61K31/416 , A61K31/4152 , C07D231/10 , C07D45/02
CPC分类号: C07D409/04 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D495/04
摘要: A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: wherein R2 is selected from hydrido, alkyl, haloalkyl, alkoxycaronyl, cyano, cyanoalkyl, carboxyl, aminocaronyl, alkylaminocarbonyl, cycloalklaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, amioncarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R3 is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R4 is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R4 is optionally substituted at a substitutable position with one or more radicals selected from halo alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R2 and R3 are not both hydrido; further provided that R2 is not carboxyl or methyl when R3 is hydrido and when R4 is phenyl; further provided that R4 is not triazolyl when R2 is methyl; further provided that R4 is not arakenyl when R2 is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R4 is not phenyl when R2 is methyl and R3 is carboxyl; and further provided that R4 is not unsubstituted thienyl when R2 is trifluoromethyl; or a pharmaceutically-acceptable salt thereof.
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7.Process for preparing prodrugs of benzenesulfonamide-containing COX-2 inhibitors 有权
标题翻译: 制备含苯磺酰胺的COX-2抑制剂前药的方法公开(公告)号:US20050032851A1
公开(公告)日:2005-02-10
申请号:US10939852
申请日:2004-09-13
申请人: John Talley , James Malecha , Stephen Bertenshaw , Matthew Graneto , Jeffery Carter , Jinglin Li , Srinivasan Nagarajan , David Brown , Donald Rogier , Thomas Penning , Ish Khanna , Xiangdong Xu , Richard Weier
发明人: John Talley , James Malecha , Stephen Bertenshaw , Matthew Graneto , Jeffery Carter , Jinglin Li , Srinivasan Nagarajan , David Brown , Donald Rogier , Thomas Penning , Ish Khanna , Xiangdong Xu , Richard Weier
IPC分类号: C07D233/64 , A61K31/00 , A61K31/18 , A61K31/34 , A61K31/341 , A61K31/365 , A61K31/40 , A61K31/415 , A61K31/4162 , A61K31/4164 , A61K31/42 , A61K31/421 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/635 , A61P1/02 , A61P1/04 , A61P3/10 , A61P5/16 , A61P7/06 , A61P9/10 , A61P11/02 , A61P11/06 , A61P11/08 , A61P13/12 , A61P15/06 , A61P17/02 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/08 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/28 , A61P27/02 , A61P27/12 , A61P29/00 , A61P29/02 , A61P31/12 , A61P35/00 , A61P37/00 , A61P43/00 , C07C311/16 , C07C311/39 , C07C311/51 , C07D20060101 , C07D207/32 , C07D207/327 , C07D207/33 , C07D231/12 , C07D233/54 , C07D233/62 , C07D261/08 , C07D263/32 , C07D307/46 , C07D307/58 , C07D401/04 , C07D417/04 , C07D495/04 , A61K31/425
CPC分类号: C07D207/33 , A61K31/18 , A61K31/415 , A61K31/42 , A61K31/635 , C07C311/16 , C07C311/51 , C07C2601/10 , C07D231/12 , C07D233/64 , C07D261/08 , C07D263/32 , C07D307/58 , C07D401/04 , C07D417/04 , C07D495/04
摘要: Prodrugs of COX-2 inhibitors are described as being useful in treating inflammation and inflammation-related disorders.
摘要翻译: 描述了COX-2抑制剂的前药用于治疗炎症和炎症相关疾病。
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