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1. 发明授权

US07420061B2 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。

2. 发明授权

US5760068A Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation 失效
标题翻译：用于治疗炎症的取代的吡唑基苯磺酰胺
公开(公告)号：US5760068A
公开(公告)日：1998-06-02
申请号：US648113
申请日：1996-09-06
申请人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter , Stephen H. Docter , Stella S. Yu
发明人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter , Stephen H. Docter , Stella S. Yu
IPC分类号： A61K31/415 , A61K31/4155 , A61K31/416 , A61K31/4178 , A61K31/4245 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/505 , A61K31/506 , A61P5/14 , A61P9/00 , A61P19/02 , A61P25/04 , A61P25/06 , A61P29/00 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/18 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D495/04
CPC分类号： C07D495/04 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
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: ##STR1## or a pharmaceutically-acceptable salt thereof.
摘要翻译： PCT No.PCT / US94 / 12720 Sec。 371日期1996年9月6日 102（e）日期1996年9月6日PCT 1994年11月14日PCT PCT。 WO95 / 15316 PCT出版物日期：1995年6月8日描述了一类吡唑基苯磺酰胺化合物用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由式II定义：其中R 1，R 2，

3. 发明授权

US5466823A Substituted pyrazolyl benzenesulfonamides 失效
标题翻译：取代的吡唑基苯磺酰胺
公开(公告)号：US5466823A
公开(公告)日：1995-11-14
申请号：US160594
申请日：1993-11-30
申请人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter
发明人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter
IPC分类号： A61K31/415 , A61P11/06 , A61P17/06 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D495/04 , C07D413/10
CPC分类号： C07D405/04 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D409/04 , 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 I: ##STR1## or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类吡唑基苯磺酰胺化合物用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由式I定义：其中（I）或其药学上可接受的盐。

4. 发明授权

US5563165A Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation 失效
标题翻译：用于治疗炎症的取代的吡唑基苯磺酰胺
公开(公告)号：US5563165A
公开(公告)日：1996-10-08
申请号：US457059
申请日：1995-06-01
申请人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter
发明人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter
IPC分类号： A61K31/415 , A61P11/06 , A61P17/06 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D495/04 , A61K31/535
CPC分类号： C07D405/04 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D409/04 , 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 I: ##STR1##
摘要翻译：描述了一类吡唑基苯磺酰胺化合物用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由式I定义：（I）

5. 发明授权

US5504215A Substituted pyrazolyl benzenesulfonamide compounds for the treatment of inflammation 失效
公开(公告)号：US5504215A
公开(公告)日：1996-04-02
申请号：US458079
申请日：1995-06-01
申请人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter
发明人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter
IPC分类号： A61K31/415 , A61P11/06 , A61P17/06 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D495/04
CPC分类号： C07D405/04 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D409/04 , 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 I: ##STR1## or a pharmaceutically-acceptable salt thereof.

6. 发明授权

US5508426A Substituted pyrazolyl benzenesulfonamide compounds for the treatment of inflammation 失效
标题翻译：用于治疗炎症的取代的吡唑基苯磺酰胺化合物
公开(公告)号：US5508426A
公开(公告)日：1996-04-16
申请号：US457185
申请日：1995-06-01
申请人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter
发明人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter
IPC分类号： A61K31/415 , A61P11/06 , A61P17/06 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D495/04
CPC分类号： C07D405/04 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D409/04 , 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 I: ##STR1## or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类吡唑基苯磺酰胺化合物用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由式I定义：其中（I）或其药学上可接受的盐。

7. 发明授权

US5753688A Substituted pyrazolyl benzenesulfonamides for the treatment of gastrointestinal conditions 失效
标题翻译：取代的吡唑基苯磺酰胺用于治疗胃肠道疾病
公开(公告)号：US5753688A
公开(公告)日：1998-05-19
申请号：US534757
申请日：1995-09-27
申请人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter
发明人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter
IPC分类号： A61K31/415 , A61K31/4155 , A61K31/416 , A61K31/4178 , A61K31/4245 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/505 , A61K31/506 , A61P5/14 , A61P9/00 , A61P19/02 , A61P25/04 , A61P25/06 , A61P29/00 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/18 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D495/04 , A61K31/63
CPC分类号： C07D495/04 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
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 I: ##STR1## or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类吡唑基苯磺酰胺化合物用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由式I定义：其中（I）或其药学上可接受的盐。

8. 发明授权

US5668161A Substituted thiazoles for the treatment of inflammation 失效
标题翻译：用于治疗炎症的取代的噻唑
公开(公告)号：US5668161A
公开(公告)日：1997-09-16
申请号：US679462
申请日：1996-07-09
申请人： John J. Talley , Jeffery S. Carter , Paul W. Collins , Steven W. Kramer , Thomas D. Penning , Donald J. Rogier, Jr. , Roland S. Rogers
发明人： John J. Talley , Jeffery S. Carter , Paul W. Collins , Steven W. Kramer , Thomas D. Penning , Donald J. Rogier, Jr. , Roland S. Rogers
IPC分类号： C07D277/24 , A61K31/425 , A61K31/426 , A61K31/44 , A61P3/00 , A61P29/00 , C07D277/20 , C07D277/26 , C07D277/28 , C07D277/30 , C07D277/32 , C07D277/34 , C07D277/40 , C07D277/42 , C07D277/50 , C07D277/52 , C07D277/56 , C07D417/04 , C07D417/12
CPC分类号： C07D417/04 , C07D277/26 , C07D277/30 , C07D277/42 , C07D277/56 , C07D417/12
摘要： A class of substituted thiazolyl compounds is described for use in treating inflammation disorders. Compounds are defined by Formula II ##STR1## wherein R.sup.1 is selected from hydrido, alkyl, haloalkyl, cyanoalkyl, alkylamino, aralkyl, arylamino, heteroarylsulfonylalkyl, heteroarylsulfonylhaloalkyl, aralkylamino, aryloxyalkyl, alkoxycarbonyl, aryl optionally substituted at a substitutable position with one or more radicals selected from halo and alkoxy, and heterocyclic optionally substituted at a substitutable position with one or more radicals selected from halo and alkyl; wherein R.sup.4 is selected from alkyl and amino; and wherein R.sup.5 is selected from aryl and heteroaryl; wherein R.sup.5 is optionally substituted at a substitutable position with one or more radicals selected from halo, alkyl and alkoxy; provided R.sup.5 is not phenyl at position 4 when R.sup.1 is .alpha.,.alpha.-bis(trifluoromethyl)methanol and R.sup.4 is methyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类用于治疗炎症的取代的噻唑基化合物。化合物由式II其中R 1选自氢，烷基，卤代烷基，氰基烷基，烷基氨基，芳烷基，芳基氨基，杂芳基磺酰基烷基，杂芳基磺酰基卤代烷基，芳烷基氨基，芳氧基烷基，烷氧基羰基，任选地在可取代的位置被取代的芳基与一个或多个选自卤素和烷氧基的基团和任选地在可取代的位置被一个或多个选自卤素和烷基的基团取代的杂环; 其中R 4选自烷基和氨基; 并且其中R 5选自芳基和杂芳基; 其中R 5任选在可取代的位置被一个或多个选自卤素，烷基和烷氧基的基团取代; 条件是当R 1为α时，R 5不在第4位为苯基，α-双（三氟甲基）甲醇，且R 4为甲基; 或其药学上可接受的盐。

9. 发明授权

US5510496A Substituted pyrazolyl benzenesulfonamides 失效
标题翻译：取代的吡唑基苯磺酰胺
公开(公告)号：US5510496A
公开(公告)日：1996-04-23
申请号：US456441
申请日：1995-06-01
申请人： John J. Talley , Thomas D. Penning , Paul W. Collins , James W. Malecha , Stephen R. Bertenshaw , Matthew J. Graneto
发明人： John J. Talley , Thomas D. Penning , Paul W. Collins , James W. Malecha , Stephen R. Bertenshaw , Matthew J. Graneto
IPC分类号： A61K31/415 , A61P11/06 , A61P17/06 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D495/04
CPC分类号： C07D405/04 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D409/04 , 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 I: ##STR1## wherein R.sup.1 is selected from sulfamyl, fluoro, chloro, methyl, hydroxyl, methoxy and trifluoromethyl: wherein R.sup.2 is selected from hydrido, difiuoromethyl, trifluoromethyl, amido, dichloromethyl, trichloromethyl, pentafluoroethyl, cyano, heptatluoropropyl, difluorochloromethyl, methoxycarbonyl, dichlorofluoromethyl, N-phenylamido, N-3-fluorophenyl) amido, 2-pyridylamido, N-(4-methylphenyl)amido, hydroxypropyl, N-(3-chlorophenyl)amido, N-(4-methoxyphenyl)amido, hydroxymethyl, hydroxyethyl, carboxylpropyl, carboxymethyl and carboxyethyl; wherein R.sup.3 is selected from hydrido, methyl, triflouromethyl, fluoro, chloro and bromo; wherein R.sup.4 is selected from phenyl, biphenyl, pyrazinyl, cyclohexyl, cyclohexenyl and thienyl; and wherein R.sup.4 is optionally substituted at a substitutable position with one or more radicals selected from chloro, bromo, fluoro, methylthio, methylsulfonyl, morpholinyl, amino, methyl, ethyl, propyl, isopropyl, butyl, ethoxy, nitro, chloromethyl, trifluoromethoxy, trifluoroenhoxy, fluoromethyl, methoxy, difluoromethyl, trifluoromethyl, dichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, and difluoropropyl; or wherein R.sup.3 and R.sup.4 together form ##STR2## provided R.sup.2 and R.sup.3 are not both hydrido; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类吡唑基苯磺酰胺化合物用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由式I定义：其中R 1选自氨磺酰基，氟，氯，甲基，羟基，甲氧基和三氟甲基：其中R 2选自氢，二氟甲基，三氟甲基，酰氨基，二氯甲基，三氯甲基，五氟乙基，氰基，七氟丙基，二氟氯甲基，甲氧基羰基，二氯氟甲基，N-苯基酰氨基，N-3-氟苯基）酰氨基，2-吡啶基酰氨基，N-（4-甲基苯基）酰氨基，羟丙基，N-（3-氯苯基） N-（4-甲氧基苯基）酰氨基，羟甲基，羟乙基，羧基丙基，羧甲基和羧乙基; 其中R 3选自氢，甲基，三氟甲基，氟，氯和溴; 其中R 4选自苯基，联苯基，吡嗪基，环己基，环己烯基和噻吩基; 并且其中R 4在可取代位置任选被一个或多个选自氯，溴，氟，甲硫基，甲基磺酰基，吗啉基，氨基，甲基，乙基，丙基，异丙基，丁基，乙氧基，硝基，氯甲基，三氟甲氧基，三氟甲氧基氟甲基，甲氧基，二氟甲基，三氟甲基，二氯甲基，五氟乙基，七氟丙基，二氟氯甲基，二氯氟甲基，二氟乙基和二氟丙基; 或者其中R3和R4一起形成“IMAGE”，其中R2和R3不都是氢的; 或其药学上可接受的盐。

10. 发明授权

US5908852A 1,3,5 trisubstituted pyrazole compounds for treatment of inflammation 失效
标题翻译：用于治疗炎症的1,3,5三取代吡唑化合物
公开(公告)号：US5908852A
公开(公告)日：1999-06-01
申请号：US647911
申请日：1996-05-30
申请人： John J Talley , Donald J Rogier, Jr. , Thomas D. Penning , Stella S Yu
发明人： John J Talley , Donald J Rogier, Jr. , Thomas D. Penning , Stella S Yu
IPC分类号： C07D231/12 , C07D231/16 , A61K31/415 , C07D405/04 , C07D405/09
CPC分类号： C07D231/12 , C07D231/16
摘要： A class of 1,3,5-substituted pyrazoles is described for the treatment of inflammation, including treatment of pain and disorders such as arthritis. Compounds of particular interest are of Formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as described herein; or a pharmaceutically-acceptable salt thereof.
摘要翻译： PCT No.PCT / US94 / 12722 Sec。 371日期：1996年5月30日 102（e）日期1996年5月30日PCT 1994年11月14日PCT PCT。 WO95 / 15318 PCT公开号日期：1995年6月8日描述了一类1,3,5-取代的吡唑用于治疗炎症，包括治疗疼痛和疾病如关节炎。特别感兴趣的化合物是式I，其中R 1，R 2，R 3和R 4如本文所述; 或其药学上可接受的盐。

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