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21. 发明授权

US06875785B2 Heterocyclo substituted hydroxamic acid derivatives as cyclooxygenase-2 and 5-lipoxygenase inhibitors 失效
标题翻译：杂环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：US06875785B2
公开(公告)日：2005-04-05
申请号：US10254701
申请日：2002-09-25
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： A61P29/00 , C07D231/12 , C07D263/32 , A61K31/421 , C07D413/00
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。

22. 发明授权

US06753344B2 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。

23. 发明授权

US06696477B2 Heterocyclo substituted hydroxamic acid derivatives as cyclooxygenase-2 and 5-lipoxygenase inhibitors 失效
标题翻译：杂环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：US06696477B2
公开(公告)日：2004-02-24
申请号：US09997633
申请日：2001-11-29
申请人： John J. Talley , James A. Sikorski , Matthew J. Graneto , Jeffery S. Carter , Bryan H. Norman , Balekudru Devadas
发明人： John J. Talley , James A. Sikorski , Matthew J. Graneto , Jeffery S. Carter , Bryan H. Norman , Balekudru Devadas
IPC分类号： C07D23110
CPC分类号： C07D231/12 , B60G17/018 , B60G2400/102 , B60G2400/206 , B60G2400/25 , B60G2400/60 , B60G2400/91 , B64C27/001 , B64C2027/004 , 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. Compounds of particular interest are defined by Formula I wherein A, Y, R1, R2, R3, R4 and R5 are as defined in the specification.
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。特别感兴趣的化合物由式I定义，其中A，Y，R 1，R 2，R 3，R 4和R 5如说明书中所定义。

24. 发明授权

US5696143A Benz �G! indazolyl derivatives for the treatment of inflammation 失效
标题翻译： Benz [G]吲唑基衍生物用于治疗炎症
公开(公告)号：US5696143A
公开(公告)日：1997-12-09
申请号：US309294
申请日：1994-09-20
申请人： John J. Talley , Stephen R. Bertenshaw , Roland S. Rogers
发明人： John J. Talley , Stephen R. Bertenshaw , Roland S. Rogers
IPC分类号： C07D231/54 , A61K31/415
CPC分类号： C07D231/54
摘要： A class of benz�g!indazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein A is --CH.dbd.CH--; wherein R.sup.1 is selected from lower haloalkyl, cyano, lower alkoxycarbonyl, lower N-alkylaminocarbonyl, N-phenylaminocarbonyl, lower N,N-dialkylaminocarbonyl and lower N-alkyl-N-phenylaminocarbonyl; wherein R.sup.2 is phenyl substituted at a substitutable position with a radical selected from lower alkylsulfonyl and sulfamyl; and wherein R.sup.3 is one or more radicals selected from halo, lower alkylthio, lower alkylsulfinyl, lower alkyl, cyano, lower alkoxycarbonyl, aminocarbonyl, lower N-alkylaminocarbonyl, lower haloalkyl, hydroxyl, lower alkoxy, lower hydroxyalkyl, lower haloalkoxy, amino, lower N,N-dialkylamino and nitro; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类苯并[g]吲唑基衍生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（I）定义，其中A为-CH = CH-; 其中R 1选自低级卤代烷基，氰基，低级烷氧基羰基，低级N-烷基氨基羰基，N-苯基氨基羰基，低级N，N-二烷基氨基羰基和低级N-烷基-N-苯基氨基羰基。其中R2是在可取代的位置被选自低级烷基磺酰基和氨磺酰基的基团取代的苯基; 并且其中R 3是一个或多个选自卤素，低级烷硫基，低级烷基亚磺酰基，低级烷基，氰基，低级烷氧基羰基，氨基羰基，低级N-烷基氨基羰基，低级卤代烷基，羟基，低级烷氧基，低级羟烷基，低级卤代烷氧基，氨基，低级 N，N-二烷基氨基和硝基; 或其药学上可接受的盐。

25. 发明授权

US07119203B2 Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors 失效
标题翻译：哌啶基和哌嗪基 - 磺酰基甲基异羟肟酸及其作为蛋白酶抑制剂的用途
公开(公告)号：US07119203B2
公开(公告)日：2006-10-10
申请号：US10618288
申请日：2003-04-25
申请人： Thomas E. Barta , Daniel P. Becker , Louis J. Bedell , Terri L. Boehm , David L. Brown , Jeffery N. Carroll , Yiyuan Chen , Yvette M. Fobian , John N. Freskos , Alan F. Gasiecki , Margaret L. Grapperhaus , Robert M. Heintz , Susan L. Hockerman , Darren J. Kassab , Ish K. Khanna , Stephen A. Kolodziej , Mark A. Massa , Joseph J. McDonald , Brent V. Mischke , Deborah A. Mischke , Patrick B. Mullins , Mark A. Nagy , Monica B. Norton , Joseph G. Rico , Michelle A. Schmidt , Nathan W. Stehle , John J. Talley , William F. Vernier , Clara I. Villamil , Lijuan J. Wang , Thomas A. Wynn
发明人： Thomas E. Barta , Daniel P. Becker , Louis J. Bedell , Terri L. Boehm , David L. Brown , Jeffery N. Carroll , Yiyuan Chen , Yvette M. Fobian , John N. Freskos , Alan F. Gasiecki , Margaret L. Grapperhaus , Robert M. Heintz , Susan L. Hockerman , Darren J. Kassab , Ish K. Khanna , Stephen A. Kolodziej , Mark A. Massa , Joseph J. McDonald , Brent V. Mischke , Deborah A. Mischke , Patrick B. Mullins , Mark A. Nagy , Monica B. Norton , Joseph G. Rico , Michelle A. Schmidt , Nathan W. Stehle , John J. Talley , William F. Vernier , Clara I. Villamil , Lijuan J. Wang , Thomas A. Wynn
IPC分类号： C07D405/14 , C07D405/12 , A61K31/496
CPC分类号： C07D213/74 , C07D211/66 , C07D211/96 , C07D309/08 , C07D335/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D411/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04
摘要： This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.
摘要翻译：本发明一般涉及蛋白酶（也称为“蛋白酶”）抑制剂，尤其涉及哌啶基和哌嗪基 - 磺酰基甲基异羟肟酸，其特别是抑制基质金属蛋白酶（也称为“基质金属蛋白酶”或“MMP “）活性和/或蛋白聚糖蛋白聚糖酶活性。这样的异羟肟酸通常在结构上对应于下式：（其中A 1，A 2，Y，E 1， 2，E 3和R x如本说明书中所定义），并且还包括这些化合物的盐。本发明还涉及这种异羟肟酸的组合物，用于合成这种异羟肟酸的中间体，制备这种异羟肟酸的方法，以及用于治疗与MMP活性和/或蛋白聚糖蛋白聚糖酶活性相关的病症（特别是病理状态）的方法。

27. 发明授权

US5475027A Retroviral protease inhibitors 失效
标题翻译：逆转录病毒蛋白酶抑制剂
公开(公告)号：US5475027A
公开(公告)日：1995-12-12
申请号：US148817
申请日：1993-11-08
申请人： John J. Talley , Daniel P. Getman , Ko-Chung Lin , Gary A. DeCrescenzo , Donald J. Rogier, Jr. , John N. Freskos
发明人： John J. Talley , Daniel P. Getman , Ko-Chung Lin , Gary A. DeCrescenzo , Donald J. Rogier, Jr. , John N. Freskos
IPC分类号： A61K31/17 , A61K31/195 , A61K31/197 , A61K31/27 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K38/00 , C07C213/02 , C07C271/20 , C07C271/22 , C07C275/14 , C07C275/18 , C07C275/22 , C07C275/24 , C07C275/28 , C07C311/47 , C07C317/44 , C07C317/50 , C07C323/60 , C07C329/06 , C07C335/08 , C07C335/12 , C07D213/81 , C07D215/48 , C07D215/50 , C07D215/54 , C07D215/56 , C07D217/26 , C07D235/06 , C07D235/24 , C07D239/38 , C07D241/44 , C07D295/13 , C07D295/15 , C07D307/85 , C07D401/12 , C07K5/02 , C07K5/06 , C07K5/078
CPC分类号： C07K5/06191 , A61K31/17 , A61K31/195 , A61K31/197 , A61K31/27 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , C07C213/02 , C07C271/20 , C07C271/22 , C07C275/14 , C07C275/18 , C07C275/22 , C07C275/24 , C07C275/28 , C07C311/47 , C07C317/44 , C07C317/50 , C07C323/60 , C07C329/06 , C07C335/08 , C07C335/12 , C07D213/81 , C07D215/48 , C07D215/50 , C07D215/54 , C07D215/56 , C07D217/26 , C07D235/06 , C07D235/24 , C07D239/38 , C07D241/44 , C07D295/13 , C07D295/15 , C07D307/85 , C07D401/12 , C07K5/0207 , C07K5/021 , C07K5/06026 , C07K5/06139 , A61K38/00 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译：含尿素的羟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。

28. 发明授权

US5434178A 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：US5434178A
公开(公告)日：1995-07-18
申请号：US160517
申请日：1993-11-30
申请人： John J. Talley , Donald J. Rogier, Jr.
发明人： John J. Talley , Donald J. Rogier, Jr.
IPC分类号： A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P25/04 , A61P29/00 , C07D231/12 , C07D231/16 , C07D401/04 , C07D405/04 , C07D409/04 , C07D231/14
CPC分类号： C07D231/12 , C07D231/16 , C07D405/04 , C07D409/04
摘要： A class of 1,3,5-triaryl or heteroaryl 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 is lower alkylsulfonyl or sulfamyl; wherein R.sup.2 is aryl or heteroaryl; wherein R.sup.2 is optionally substituted at substitutable positions with one or more radicals selected from halo, lower alkoxy, lower alkyl, nitro, lower alkylthio, amino, lower haloalkyl, hydroxyl, carboxyl, N-monoalkylamino, N,N-dialkylamino, cyano, alkoxycarbonyl and acylamino; wherein R.sup.3 is selected from hydrido, lower alkyl, lower haloalkyl, cyano, carboxyl, alkoxycarbonyl, amino, acyl, acylamino, halo and alkylsulfonylamino; wherein R.sup.4 is aryl or heteroaryl; wherein R.sup.4 is optionally substituted at a substitutable position with one or more radicals selected from halo, lower alkoxy, lower alkyl, nitro, lower alkylthio, amino, lower haloalkyl, hydroxyl, carboxyl, N-monoalkylamino, N,N-dialkylamino, cyano, alkoxycarbonyl and acylamino; provided R.sup.2 and R.sup.4 cannot be phenyl or substituted triazole, when R.sup.1 is sulfamyl; further provided R.sup.2 cannot be 4-methoxyphenyl or 4-methylphenyl when R.sup.4 is 4-methoxyphenyl or 4-methylphenyl and when R.sup.1 is sulfamyl; and further provided that R.sup.2 cannot be tetrazole when R.sup.4 is fluorophenyl, and when R.sup.1 is methylsulfonyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类1,3,5-三芳基或杂芳基吡唑用于治疗炎症，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的化合物，其中R 1是低级烷基磺酰基或亚磺酰基; 其中R2是芳基或杂芳基; 其中R2任选在可取代的位置被一个或多个选自卤素，低级烷氧基，低级烷基，硝基，低级烷硫基，氨基，低级卤代烷基，羟基，羧基，N-单烷基氨基，N，N-二烷基氨基，氰基，烷氧羰基和酰氨基; 其中R 3选自氢，低级烷基，低级卤代烷基，氰基，羧基，烷氧基羰基，氨基，酰基，酰氨基，卤素和烷基磺酰基氨基; 其中R4是芳基或杂芳基; 其中R 4在可取代位置任选被一个或多个选自卤素，低级烷氧基，低级烷基，硝基，低级烷硫基，氨基，低级卤代烷基，羟基，羧基，N-单烷基氨基，N，N-二烷基氨基，氰基，烷氧基羰基和酰氨基; 当R1是亚磺酰基时，R2和R4不能是苯基或取代的三唑; 进一步提供当R 4是4-甲氧基苯基或4-甲基苯基时，当R 1是亚磺酰基时，R 2不能是4-甲氧基苯基或4-甲基苯基; 并且进一步提供当R 4为氟苯基时，R 2不能为四唑，并且当R 1为甲基磺酰基时; 或其药学上可接受的盐。

29. 发明授权

US5516907A Heterocyclic-substituted pyrazolyl benzenesulfonamides for the treatment of inflammation 失效
标题翻译：用于治疗炎症的杂环取代的吡唑基苯磺酰胺
公开(公告)号：US5516907A
公开(公告)日：1996-05-14
申请号：US457654
申请日：1995-06-01
申请人： John J. Talley , Donald J. Rogier, Jr.
发明人： John J. Talley , Donald J. Rogier, Jr.
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 benzenesulfonamido 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。

30. 发明授权

US5475013A Retroviral protease inhibitors 失效
标题翻译：逆转录病毒蛋白酶抑制剂
公开(公告)号：US5475013A
公开(公告)日：1995-12-12
申请号：US886531
申请日：1992-05-20
申请人： John J. Talley , Daniel P. Getman , John N. Freskos , Ko-Chung Lin , Robert M. Heintz , Donald J. Rogier, Jr. , Deborah E. Bertenshaw
发明人： John J. Talley , Daniel P. Getman , John N. Freskos , Ko-Chung Lin , Robert M. Heintz , Donald J. Rogier, Jr. , Deborah E. Bertenshaw
IPC分类号： A61K31/17 , A61K31/195 , A61K31/197 , A61K31/27 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K38/00 , C07C213/02 , C07C271/20 , C07C271/22 , C07C275/14 , C07C275/18 , C07C275/22 , C07C275/24 , C07C275/28 , C07C311/47 , C07C317/44 , C07C317/50 , C07C323/60 , C07C329/06 , C07C335/08 , C07C335/12 , C07D213/81 , C07D215/48 , C07D215/50 , C07D215/54 , C07D217/26 , C07D235/06 , C07D235/24 , C07D239/38 , C07D241/44 , C07D295/13 , C07D295/15 , C07D307/85 , C07D401/12 , C07K5/02 , C07K5/06 , C07K5/078
CPC分类号： C07K5/06191 , A61K31/17 , A61K31/195 , A61K31/197 , A61K31/27 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , C07C213/02 , C07C271/20 , C07C271/22 , C07C275/14 , C07C275/18 , C07C275/22 , C07C275/24 , C07C275/28 , C07C311/47 , C07C317/44 , C07C317/50 , C07C323/60 , C07C329/06 , C07C335/08 , C07C335/12 , C07D213/81 , C07D215/48 , C07D215/50 , C07D215/54 , C07D217/26 , C07D235/06 , C07D235/24 , C07D239/38 , C07D241/44 , C07D295/13 , C07D295/15 , C07D307/85 , C07D401/12 , C07K5/0207 , C07K5/021 , C07K5/06026 , C07K5/06139 , A61K38/00 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译：含尿素的羟胺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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