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1. 发明授权

US06677364B2 Substituted sulfonylphenylheterocycles as cyclooxygenase-2 and 5-lipoxygenase inhibitors 失效
标题翻译：取代的磺酰基苯基杂环作为环加氧酶-2和5-脂氧合酶抑制剂
公开(公告)号：US06677364B2
公开(公告)日：2004-01-13
申请号：US10004960
申请日：2001-12-04
申请人： John J. Talley , James A. Sikorski , Balekudru Devadas , Matthew J. Graneto , Jeffery S. Carter , Bryan H. Norman , Roland S. Rogers , Hwang-Fun Lu , David L. Brown
发明人： John J. Talley , James A. Sikorski , Balekudru Devadas , Matthew J. Graneto , Jeffery S. Carter , Bryan H. Norman , Roland S. Rogers , Hwang-Fun Lu , David L. Brown
IPC分类号： A61K314178
CPC分类号： A61K31/44 , A61K31/15 , A61K31/277 , A61K31/4015
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。

2. 发明授权

US06274590B1 Method of treating skin related conditions 失效
标题翻译：治疗皮肤相关病症的方法
公开(公告)号：US06274590B1
公开(公告)日：2001-08-14
申请号：US09661719
申请日：2000-09-14
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： A61K31381
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, 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 S; wherein X is one or two substituents 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 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，其衍生物和类似物，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是S; 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R2和R3独立地是芳基或杂芳基; 并且其中R2和R3任选地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的基团取代; 或其药学上可接受的盐。

3. 发明授权

US5985902A Substituted isoxazole for the treatment of inflammation 失效
标题翻译：取代的异恶唑用于治疗炎症
公开(公告)号：US5985902A
公开(公告)日：1999-11-16
申请号：US801768
申请日：1997-02-18
申请人： John J Talley , Srinivasan Nagarajan , Roland S Rogers
发明人： John J Talley , Srinivasan Nagarajan , Roland S Rogers
IPC分类号： A61K31/42 , A61K31/4439 , A61P1/00 , A61P1/02 , A61P1/04 , A61P3/10 , A61P7/00 , A61P7/06 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/12 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/06 , A61P19/08 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/12 , A61P35/00 , A61P37/00 , A61P43/00 , C07D261/08 , C07D261/10 , C07D261/12 , C07D261/18 , C07D413/04 , A61K31/44 , C07D413/06 , C07D413/12
CPC分类号： C07D261/10 , C07D261/08 , C07D261/12 , C07D261/18 , C07D413/04
摘要： A class of substituted isoxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1## wherein R.sup.1 is selected from hydroxyl, lower alkyl, carboxyl, lower carboxyalkyl, lower aminocarbonylalkyl, lower alkoxycarbonylalkyl, lower aralkyl, lower alkoxyalkyl, lower aralkoxyalkyl, lower alkylthioalkyl, lower aralkylthioalkyl, lower alkylaminoalkyl, lower aryloxyalkyl, lower arylthioalkyl, lower haloalkyl, lower hydroxylalkyl, cycloalkyl, cycloalkylalkyl, and aralkyl; wherein R.sup.3 is selected from cycloalkyl, cycloalkenyl, aryl, and heteroaryl; wherein R.sup.3 is optionally substituted at a substitutable position with one or more radicals independently selected from lower alkylsulfinyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower hydroxyalkyl, lower haloalkoxy, amino, lower alkylamino, lower arylamino, lower aminoalkyl, nitro, halo, lower alkoxy, aminosulfonyl, and lower alkylthio; and wherein R.sup.4 is selected from lower alkyl, hydroxyl and amino; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类用于治疗炎症和炎症相关疾病的取代的异恶唑基化合物。特别感兴趣的化合物由式II定义，其中R1选自羟基，低级烷基，羧基，低级羧基烷基，低级氨基羰基烷基，低级烷氧基羰基烷基，低级芳烷基，低级烷氧基烷基，低级芳烷氧基烷基，低级烷硫基烷基，低级芳烷硫基烷基，低级烷基氨基烷基，低级芳氧基烷基低级芳基硫代烷基，低级卤代烷基，低级羟基烷基，环烷基，环烷基烷基和芳烷基; 其中R 3选自环烷基，环烯基，芳基和杂芳基; 其中R 3在可取代的位置任选被一个或多个独立地选自低级烷基亚磺酰基，低级烷基，氰基，羧基，低级烷氧基羰基，低级卤代烷基，羟基，低级羟烷基，低级卤代烷氧基，氨基，低级烷基氨基，低级芳基氨基，低级氨基烷基，硝基，卤素，低级烷氧基，氨基磺酰基和低级烷硫基; 并且其中R 4选自低级烷基，羟基和氨基; 或其药学上可接受的盐。

4. 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，

5. 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。

6. 发明授权

US07030153B2 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。

7. 发明授权

US06492413B2 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：US06492413B2
公开(公告)日：2002-12-10
申请号：US09528934
申请日：2000-03-20
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： A61K314025
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NR1; 其中R1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R2和R3独立地是芳基或杂芳基; 并且其中R2和R3任选在可取代的位置被一个或多个选自磺酰胺基，烷基磺酰基，卤素，低级烷氧基和低级烷基的基团取代; 或其药学上可接受的盐。

8. 发明授权

US06413960B1 Substituted pyrazolyl benzenesulfonamides for the treatment of asthma 失效
标题翻译：用于治疗哮喘的取代的吡唑基苯磺酰胺
公开(公告)号：US06413960B1
公开(公告)日：2002-07-02
申请号：US09609011
申请日：2000-05-30
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 , 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： A61P1106
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 II: wherein R2 is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, 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 aralkenyl 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.
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II定义：其中R2选自氢化，烷基，卤代烷基，烷氧基羰基，氰基，氰基烷基，羧基，氨基羰基，烷基氨基羰基，环烷基氨基羰基，芳基氨基羰基，羧基烷基氨基羰基，羧基烷基，芳烷氧基羰基烷基氨基羰基，氨基羰基烷基，烷氧基羰基氰基烯基和羟烷基。其中R 3选自氢，烷基，氰基，羟基烷基，环烷基，烷基磺酰基和卤素; 并且其中R 4选自芳烯基，芳基，环烷基，环烯基和杂环; 其中R 4在可取代位置任选被一个或多个选自卤素，烷硫基，烷基磺酰基，氰基，硝基，卤代烷基，烷基，羟基，烯基，羟基烷基，羧基，环烷基，烷基氨基，二烷基氨基，烷氧基羰基，氨基羰基，烷氧基，卤代烷氧基，氨磺酰基，杂环和氨基; 只要R2和R3都不是氢的; 进一步提供当R 3是氢的时，当R 4是苯基时，R 2不是羧基或甲基; 进一步提供当R 2是甲基时，R 4不是三唑基; 进一步提供当R 2是羧基时，R 4不是芳烯基，氨基羰基或乙氧基羰基; 进一步提供，当R 2是甲基且R 3是羧基时，R 4不是苯基; 并且进一步提供当R 2是三氟甲基时，R 4不是未取代的噻吩基; 或其药学上可接受的盐。

9. 发明授权

US6156781A Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation 有权
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：US6156781A
公开(公告)日：2000-12-05
申请号：US449076
申请日：1999-11-24
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 , A61P11/06 , A61P17/06 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D495/04 , A61P17/07
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 II: ##STR1## wherein R.sup.2 is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R.sup.3 is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R.sup.4 is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R.sup.4 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 R.sup.2 and R.sup.3 are not both hydrido; further provided that R.sup.2 is not carboxyl or methyl when R.sup.3 is hydrido and when R.sup.4 is phenyl; further provided that R.sup.4 is not triazolyl when R.sup.2 is methyl; further provided that R.sup.4 is not aralkenyl when R.sup.2 is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R.sup.4 is not phenyl when R.sup.2 is methyl and R.sup.3 is carboxyl; and further provided that R.sup.4 is not unsubstituted thienyl when R.sup.2 is trifluoromethyl; 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II定义：其中R2选自氢化，烷基，卤代烷基，烷氧基羰基，氰基，氰基烷基，羧基，氨基羰基，烷基氨基羰基，环烷基氨基羰基，芳基氨基羰基，羧基烷基氨基羰基，羧基烷基，芳烷氧基羰基烷基氨基羰基，氨基羰基烷基，烷氧基羰基氰基烯基和羟烷基。其中R 3选自氢，烷基，氰基，羟基烷基，环烷基，烷基磺酰基和卤素; 并且其中R 4选自芳烯基，芳基，环烷基，环烯基和杂环; 其中R 4在可取代位置任选被一个或多个选自卤素，烷硫基，烷基磺酰基，氰基，硝基，卤代烷基，烷基，羟基，烯基，羟基烷基，羧基，环烷基，烷基氨基，二烷基氨基，烷氧基羰基，氨基羰基，烷氧基，卤代烷氧基，氨磺酰基，杂环和氨基; 只要R2和R3都不是氢的; 进一步提供当R 3是氢的时，当R 4是苯基时，R 2不是羧基或甲基; 进一步提供当R 2是甲基时，R 4不是三唑基; 进一步提供当R 2是羧基时，R 4不是芳烯基，氨基羰基或乙氧基羰基; 进一步提供，当R 2是甲基且R 3是羧基时，R 4不是苯基; 并且进一步提供当R 2是三氟甲基时，R 4不是未取代的噻吩基; 或其药学上可接受的盐。

10. 发明授权

US5633272A Substituted isoxazoles for the treatment of inflammation 失效
标题翻译：用于治疗炎症的取代的异恶唑
公开(公告)号：US5633272A
公开(公告)日：1997-05-27
申请号：US473884
申请日：1995-06-07
申请人： John J. Talley , David L. Brown , Srinivasan Nagarajan , Jeffery S. Carter , Richard M. Weier , Michael A. Stealey , Paul W. Collins , Roland S. Rogers, deceased , Karen Seibert
发明人： John J. Talley , David L. Brown , Srinivasan Nagarajan , Jeffery S. Carter , Richard M. Weier , Michael A. Stealey , Paul W. Collins , Roland S. Rogers, deceased , Karen Seibert
IPC分类号： A61P29/00 , C07D261/08 , C07D261/10 , C07D261/12 , C07D261/18 , C07D413/04 , C07D261/06 , A61K31/42 , C07D261/14
CPC分类号： C07D261/10 , C07D261/08 , C07D261/12 , C07D261/18 , C07D413/04
摘要： A class of substituted isoxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1## wherein R.sup.1 is selected from hydroxyl, lower alkyl, carboxyl, lower carboxyalkyl, lower aminocarbonylalkyl, lower alkoxycarbonylalkyl, lower aralkyl, lower alkoxyalkyl, lower aralkoxyalkyl, lower alkylthioalkyl, lower aralkylthioalkyl, lower alkylaminoalkyl, lower aryloxyalkyl, lower arylthioalkyl, lower haloalkyl, lower hydroxylalkyl, cycloalkyl, cycloalkylalkyl, and aralkyl; wherein R.sup.3 is selected from cycloalkyl, cycloalkenyl, aryl, and heteroaryl; wherein R.sup.3 is optionally substituted at a substitutable position with one or more radicals independently selected from lower alkylsulfinyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower hydroxyalkyl, lower haloalkoxy, amino, lower alkylamino, lower arylamino, lower aminoalkyl, nitro, halo, lower alkoxy, aminosulfonyl, and lower alkylthio; and wherein R.sup.4 is selected from lower alkyl, hydroxyl and amino; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类用于治疗炎症和炎症相关疾病的取代的异恶唑基化合物。特别感兴趣的化合物由式II其中R1选自羟基，低级烷基，羧基，低级羧基烷基，低级氨基羰基烷基，低级烷氧基羰基烷基，低级芳烷基，低级烷氧基烷基，低级芳烷氧基烷基，低级烷硫基烷基，低级芳烷硫基烷基，低级低级芳氧基烷基，低级芳基硫代烷基，低级卤代烷基，低级羟基烷基，环烷基，环烷基烷基和芳烷基; 其中R 3选自环烷基，环烯基，芳基和杂芳基; 其中R 3在可取代的位置任选被一个或多个独立地选自低级烷基亚磺酰基，低级烷基，氰基，羧基，低级烷氧基羰基，低级卤代烷基，羟基，低级羟烷基，低级卤代烷氧基，氨基，低级烷基氨基，低级芳基氨基，低级氨基烷基，硝基，卤素，低级烷氧基，氨基磺酰基和低级烷硫基; 并且其中R 4选自低级烷基，羟基和氨基; 或其药学上可接受的盐。

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