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1. 发明授权

US07153959B2 Substituted pyrazoles as p38 kinase inhibitors 失效
标题翻译：取代的吡唑作为p38激酶抑制剂
公开(公告)号：US07153959B2
公开(公告)日：2006-12-26
申请号：US10374781
申请日：2003-02-25
申请人： Ashok S. Naraian , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xu , Ish K. Khanna , Yi Yu , Win Naing , Syaulan Yang
发明人： Ashok S. Naraian , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xu , Ish K. Khanna , Yi Yu , Win Naing , Syaulan Yang
IPC分类号： C07D401/04 , C07D401/14 , C07D413/02
CPC分类号： C07D409/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D453/02 , C07D471/04 , C07D473/00 , C07D487/04
摘要： A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.
摘要翻译：描述了一类吡唑衍生物用于治疗p38激酶介导的病症。特别感兴趣的化合物由式IA定义，其中R 1，R 2，R 3和R 4是如说明书中所述。

2. 发明授权

US07112669B2 Processes for preparation of 9,11-epoxy steroids and intermediates useful therein 失效
标题翻译：制备9,11-环氧类固醇及其中有用的中间体的方法
公开(公告)号：US07112669B2
公开(公告)日：2006-09-26
申请号：US11052549
申请日：2005-02-07
申请人： John S. Ng , Chin Liu , Dennis K. Anderson , Jon P. Lawson , Joseph J. Wieczorek , Sastry A. Kunda , Leo J. Letendre , Mark J. Pozzo , Yuen-Lung L. Sing , Ping T. Wang , Edward E. Yonan , Richard M. Weier , Thomas R. Kowar , Julio A. Baez , Bernhard Erb
发明人： John S. Ng , Chin Liu , Dennis K. Anderson , Jon P. Lawson , Joseph J. Wieczorek , Sastry A. Kunda , Leo J. Letendre , Mark J. Pozzo , Yuen-Lung L. Sing , Ping T. Wang , Edward E. Yonan , Richard M. Weier , Thomas R. Kowar , Julio A. Baez , Bernhard Erb
IPC分类号： C07J21/00 , C07J71/00
CPC分类号： C07J71/00 , C07D301/12 , C07J1/0059 , C07J21/00 , C07J21/003 , C07J31/006 , C07J41/0094 , C07J53/002 , C07J71/0005 , C07J71/0015 , C07J75/00 , C12P33/005 , C12P33/10
摘要： Intermediates in the preparation of 9,11-epoxy steroids are disclosed. Particularly, disclosed are 11,12-epoxy steroid, 4,5-9,11-diepoxy steroid and 12-keto steroid intermediates.
摘要翻译：公开了制备9,11-环氧类固醇的中间体。特别公开的是11,12-环氧类固醇，4,5-9,11-二环氧类固醇和12-酮类固醇中间体。

4. 发明授权

US06815460B2 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。

5. 发明授权

US06613789B2 Heterocyclo-substituted imidazoles for the treatment of inflammation 失效
标题翻译：杂环取代的咪唑用于治疗炎症
公开(公告)号：US06613789B2
公开(公告)日：2003-09-02
申请号：US10004944
申请日：2001-12-05
申请人： Ish K. Khanna , Richard M. Weier , Paul W. Collins , Yi Yu , Xiangdong Xu , Richard A. Partis , Francis J. Koszyk , Renee M. Huff
发明人： Ish K. Khanna , Richard M. Weier , Paul W. Collins , Yi Yu , Xiangdong Xu , Richard A. Partis , Francis J. Koszyk , Renee M. Huff
IPC分类号： A61K3144
CPC分类号： C07D233/64 , C07D233/32 , C07D233/90 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D419/04
摘要： A class of imidazolyl compounds is described for use in treating inflammation. Compounds of particular interest are defined by Formula V: and pharmaceutically-acceptable salts thereof.
摘要翻译：描述了一类咪唑基化合物用于治疗炎症。特别感兴趣的化合物由式V定义：及其药学上可接受的盐。

6. 发明授权

US06426360B1 4,5-substituted imidazolyl compounds for the treatment of inflammation 失效
标题翻译：用于治疗炎症的4,5-取代的咪唑基化合物
公开(公告)号：US06426360B1
公开(公告)日：2002-07-30
申请号：US09571033
申请日：2000-05-15
申请人： Richard M Weier , Paul W Collins , Michael A Stealey , Thomas E Barta , Renee M Huff
发明人： Richard M Weier , Paul W Collins , Michael A Stealey , Thomas E Barta , Renee M Huff
IPC分类号： A01N4350
CPC分类号： C07D233/64 , C07D233/84 , C07D233/88 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04
摘要： A class of compounds is described for treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula wherein R1 is selected from lower alkyl, lower haloalkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower alkenyloxyalkyl, mercapto, lower alkylcarbonyl, lower haloalkylcarbonyl, phenylcarbonyl, lower aralkylcarbonyl, lower aralkenyl, lower aryloxyalkyl, lower aralkyloxyalkyl, lower arylsulfonyl, lower aralkylsulfonyl, lower arylthioalkyl, lower heteroarylalkylthioalkyl, and heteroaryl selected from 2-thienyl, 2-furyl, 3-furyl, 2-pyridyl, 4-pyridyl and 2-benzofuryl; wherein R2 and R3 are independently selected from heteroaryl, cycloalkyl and aryl, wherein the heteroaryl, cycloalkyl and aryl radicals are substituted at a substitutable position with one or more radicals selected from hydrido, halo, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, aminosulfonyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl, lower haloalkoxy, amino, lower alkylamino, phenylamino and nitro; and wherein R4 is selected from hydrido, lower alkyl and acyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类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通式Ⅵ所定义：R1选自低级烷基，低级卤代烷基，低级羟烷基，低级烷氧基烷基，低级烯氧基烷基，巯基，低级烷基羰基，低级卤代烷基羰基，苯基羰基，低级芳烷基羰基，低级芳烯基，低级芳氧基烷基，低级芳烷氧基烷基，芳基磺酰基，低级芳烷基磺酰基，低级芳基硫代烷基，低级杂芳基烷硫基烷基和选自2-噻吩基，2-呋喃基，3-呋喃基，2-吡啶基，4-吡啶基和2-苯并呋喃基的杂芳基。其中R2和R3独立地选自杂芳基，环烷基和芳基，其中杂芳基，环烷基和芳基在可取代的位置被一个或多个选自氢，卤代，低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基，氨基磺酰基，低级烷基，氰基，羧基，低级烷氧基羰基，低级卤代烷基，羟基，低级烷氧基，低级羟基烷基，低级烷氧基烷基，低级卤代烷氧基，氨基，低级烷基氨基，苯基氨基和硝基。并且其中R 4选自氢，低级烷基和酰基; 或其药学上可接受的盐。

7. 发明授权

US06423713B1 Substituted pyrazoles as p38 kinase inhibitors 失效
标题翻译：取代的吡唑作为p38激酶抑制剂
公开(公告)号：US06423713B1
公开(公告)日：2002-07-23
申请号：US09918481
申请日：2001-07-31
申请人： Ashok Anantanarayan , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xi , Ish K. Khanna , Yi Yu
发明人： Ashok Anantanarayan , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xi , Ish K. Khanna , Yi Yu
IPC分类号： A61K31496
CPC分类号： C07D409/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D453/02 , C07D471/04 , C07D473/00 , C07D487/04
摘要： A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.
摘要翻译：描述了一类吡唑衍生物用于治疗p38激酶介导的病症。特别感兴趣的化合物由式IA定义，其中R1，R2，R3和R4如说明书中所述。

8. 发明授权

US06335336B1 3(5)-Heteroaryl substituted pyrazoles as p38 kinase inhibitors 失效
标题翻译： 3（5） - 芳基取代的吡唑作为p38激酶抑制剂
公开(公告)号：US06335336B1
公开(公告)日：2002-01-01
申请号：US09561423
申请日：2000-04-28
申请人： Ashok Anantanarayan , Michael Clare , Lifeng Geng , Gunnar J. Hanson , Richard A. Partis , Michael A. Stealey , Richard M. Weier
发明人： Ashok Anantanarayan , Michael Clare , Lifeng Geng , Gunnar J. Hanson , Richard A. Partis , Michael A. Stealey , Richard M. Weier
IPC分类号： C07D40144
CPC分类号： C07D401/04 , C07D401/14
摘要： A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I
摘要翻译：描述了一类吡唑衍生物用于治疗p38激酶介导的病症。特别感兴趣的化合物由式I定义

10. 发明授权

US5916905A 2,3-substituted pyridines for the treatment of inflammation 失效
标题翻译： 2,3-取代的吡啶用于治疗炎症
公开(公告)号：US5916905A
公开(公告)日：1999-06-29
申请号：US894102
申请日：1997-08-08
申请人： Richard M Weier , Len F Lee , Richard A Partis , Francis J Koszyk
发明人： Richard M Weier , Len F Lee , Richard A Partis , Francis J Koszyk
IPC分类号： C07D213/61 , C07D213/64 , C07D213/70 , C07D213/76 , C07D213/82 , C07D213/85 , A61K31/44
CPC分类号： C07D213/64 , C07D213/61 , C07D213/70 , C07D213/76 , C07D213/82 , C07D213/85
摘要： A class of substituted pyridyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II wherein R.sup.1 is selected from hydrido, halo, alkoxy, haloalkoxy, aryl, alkylthio, alkylamino, aralkoxy, azido and alkenyloxy; wherein R.sup.2 is selected from hydrido, cyano, hydroxyalkyl, haloalkyl, aminoalkyl, alkylaminoalkyl, alkylcarbonyloxyalkyl, aminocarbonyl and alkylcarbonylaminoalkyl; and wherein R.sup.5 and R.sup.6 are one or more radicals independently selected from halo, alkylsulfonyl, aminosulfonyl, alkoxy and alkylthio; provided one of R.sup.5 and R.sup.6 is substituted with alkylsulfonyl, aminosulfonyl, or haloalkylsulfonyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译： PCT No.PCT / US96 / 01111 Sec。 371日期：1997年8月8日 102（e）日期1997年8月8日PCT提交1996年2月8日PCT公布。出版物WO96 / 24584 日期1996年8月15日描述了一类用于治疗炎症和炎症相关疾病的吡啶基化合物。特别感兴趣的化合物由式II定义，其中R 1选自氢，卤素，烷氧基，卤代烷氧基，芳基，烷硫基，烷基氨基，芳烷氧基，叠氮基和烯氧基; 氰基，羟基烷基，卤代烷基，氨基烷基，烷基氨基烷基，烷基羰氧基烷基，氨基羰基和烷基羰基氨基烷基;其中R2选自氢，氰基，并且其中R 5和R 6是一个或多个独立地选自卤素，烷基磺酰基，氨基磺酰基，烷氧基和烷硫基的基团; 其中R5和R6之一被烷基磺酰基，氨基磺酰基或卤代烷基磺酰基取代; 或其药学上可接受的盐。

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