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1. 发明授权

US07834004B2 Sulfonyl-substituted bicyclic compounds as modulators of PPAR 有权
标题翻译：磺酰基取代的双环化合物作为PPAR的调节剂
公开(公告)号：US07834004B2
公开(公告)日：2010-11-16
申请号：US12204489
申请日：2008-09-04
申请人： Stewart A. Noble , Guy Oshiro , James W. Malecha , Cunxiang Zhao , Carmen Robinson , Sergio G. Duron , Michael Sertic , Andrew K. Lindstrom , Andrew K. Shiau , Christopher D Bayne , Mehmet Kahraman , Boliang Lou , Steven P. Govek
发明人： Stewart A. Noble , Guy Oshiro , James W. Malecha , Cunxiang Zhao , Carmen Robinson , Sergio G. Duron , Michael Sertic , Andrew K. Lindstrom , Andrew K. Shiau , Christopher D Bayne , Mehmet Kahraman , Boliang Lou , Steven P. Govek
IPC分类号： A61K31/496 , A61K31/343 , A61K31/404 , A61K31/551 , A61K31/495 , C07D333/52 , C07D403/02 , C07D209/04 , C07D405/02 , C07D307/78
CPC分类号： C07D213/74 , C07D209/08 , C07D211/96 , C07D257/04 , C07D295/26 , C07D333/60 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/12 , C07D487/08
摘要： Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
摘要翻译：公开了作为过氧化物酶体增殖物激活受体的调节剂的化合物，包含其的药物组合物和使用其的治疗疾病的方法。

2. 发明申请

US20080287477A1 Novel Compounds as Modulators of Ppar 审中-公开
标题翻译：新型化合物作为Ppar的调节剂
公开(公告)号：US20080287477A1
公开(公告)日：2008-11-20
申请号：US12083426
申请日：2006-10-11
申请人： James W. Malecha , Andrew K. Lindstrom , Sergio G. Duron , Steven P. Govek
发明人： James W. Malecha , Andrew K. Lindstrom , Sergio G. Duron , Steven P. Govek
IPC分类号： A61K31/192 , C07D239/42 , C07C311/29 , A61P29/00 , A61P17/00 , A61P27/02 , A61P19/00 , A61K31/505 , A61P3/00
CPC分类号： C07C311/17 , C07C311/18 , C07C2602/08 , C07D239/42 , C07D261/20
摘要： Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
摘要翻译：公开了作为过氧化物酶体增殖物激活受体的调节剂的化合物，包含其的药物组合物和使用其的治疗疾病的方法。

3. 发明授权

US06720315B2 Dihydrostilbene alkanoic acid derivatives 失效
标题翻译：二氢芪链烷酸衍生物
公开(公告)号：US06720315B2
公开(公告)日：2004-04-13
申请号：US09882137
申请日：2001-06-15
申请人： Thomas Rogers , Michael Clare , Hwang-Fun Lu , Mark Russell , James W. Malecha , Ish Kumar Khanna , Thomas Penning , Srinivasan Raj Nagarajan , Heather Stenmark
发明人： Thomas Rogers , Michael Clare , Hwang-Fun Lu , Mark Russell , James W. Malecha , Ish Kumar Khanna , Thomas Penning , Srinivasan Raj Nagarajan , Heather Stenmark
IPC分类号： A61K3133
CPC分类号： C07D213/74 , C07D239/14 , C07D401/12
摘要： The present invention relates to a class of compounds represented by the Formula 1. or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula 1, and methods of selectively inhibiting or antagonizing the &agr;V&bgr;3 and/or the &agr;V&bgr;5 integrin.
摘要翻译：本发明涉及一类由式1表示的化合物或其药学上可接受的盐，包含式1化合物的药物组合物和选择性抑制或拮抗αVβ3和/或αVbeta5整联蛋白的方法。

4. 发明授权

US5852210A Cinnamic acid derivatives 失效
标题翻译：肉桂酸衍生物
公开(公告)号：US5852210A
公开(公告)日：1998-12-22
申请号：US825080
申请日：1997-03-27
申请人： Barbara B. Chen , Helen Y. Chen , Michael Clare , Stephen H. Docter , Ish Kumar Khanna , Francis Jan Koszyk , James W. Malecha , Julie Marion Miyashiro , Thomas D. Penning , Joseph G. Rico , Peter G. Ruminski , Mark A. Russell , Richard Mathias Weier , Xiangdong Xu , Stella S. Yu , Yi Yu
发明人： Barbara B. Chen , Helen Y. Chen , Michael Clare , Stephen H. Docter , Ish Kumar Khanna , Francis Jan Koszyk , James W. Malecha , Julie Marion Miyashiro , Thomas D. Penning , Joseph G. Rico , Peter G. Ruminski , Mark A. Russell , Richard Mathias Weier , Xiangdong Xu , Stella S. Yu , Yi Yu
IPC分类号： A61K31/00 , A61K31/195 , A61K31/215 , A61K31/216 , A61K31/275 , A61K31/277 , A61K31/415 , A61K31/4164 , A61K31/4178 , A61K31/42 , A61K31/421 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/505 , A61K31/506 , A61K31/54 , A61P3/00 , A61P3/14 , A61P9/00 , A61P9/14 , A61P19/00 , A61P19/10 , A61P35/00 , A61P35/04 , C07C205/34 , C07C205/35 , C07C205/37 , C07C205/44 , C07C205/45 , C07C205/56 , C07C205/57 , C07C275/42 , C07C279/18 , C07C279/22 , C07C279/24 , C07D231/06 , C07D233/50 , C07D233/54 , C07D233/64 , C07D239/14 , C07D239/42 , C07D263/32 , C07D279/06 , C07D401/12 , C07D403/12 , C07C241/00 , C07C205/00 , C07D233/44 , C07D239/02
CPC分类号： C07D231/06 , C07C205/34 , C07C205/35 , C07C205/37 , C07C205/44 , C07C205/45 , C07C205/56 , C07C205/57 , C07C275/42 , C07C279/18 , C07C279/22 , C07C279/24 , C07D233/50 , C07D233/64 , C07D239/14 , C07D239/42 , C07D263/32 , C07D279/06 , C07D401/12 , C07D403/12
摘要： The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.
摘要翻译：本发明涉及一类由式I表示的化合物或其药学上可接受的盐，包含式I化合物的药物组合物和选择性抑制或拮抗αvβ3整联蛋白的方法。

5. 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，

6. 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。

7. 发明申请

US20090264417A1 SULFONYL-SUBSTITUTED BICYCLIC COMPOUNDS AS MODULATORS OF PPAR 有权
公开(公告)号：US20090264417A1
公开(公告)日：2009-10-22
申请号：US12204489
申请日：2008-09-04
申请人： Stewart A. Noble , Guy Oshiro , James W. Malecha , Cunxiang Zhao , Carmen Robinson , Sergio G. Duron , Michael Sertic , Andrew K. Lindstrom , Andrew K. Shiau , Christopher D. Bayne , Mehmet Kahraman , Boliang Lou , Steven P. Govek
发明人： Stewart A. Noble , Guy Oshiro , James W. Malecha , Cunxiang Zhao , Carmen Robinson , Sergio G. Duron , Michael Sertic , Andrew K. Lindstrom , Andrew K. Shiau , Christopher D. Bayne , Mehmet Kahraman , Boliang Lou , Steven P. Govek
IPC分类号： A61K31/551 , C07D295/26 , A61K31/495 , A61K31/496 , C07K1/107 , C07D401/04 , C07D403/12
CPC分类号： C07D213/74 , C07D209/08 , C07D211/96 , C07D257/04 , C07D295/26 , C07D333/60 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/12 , C07D487/08
摘要： Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.

8. 发明申请

US20090029971A1 SULFONYL-SUBSTITUTED BICYCLIC COMPOUNDS AS MODULATORS OF PPAR 有权
标题翻译：作为PPAR的调节剂的磺基取代的双环化合物
公开(公告)号：US20090029971A1
公开(公告)日：2009-01-29
申请号：US12204459
申请日：2008-09-04
申请人： Stewart A. Noble , Guy Oshiro , James W. Malecha , Cunxiang Zhao , Carmen Robinson , Sergio G. Duron , Michael Sertic , Andrew K. Lindstrom , Andrew K. Shiau , Christopher D. Bayne , Mehmet Kahraman , Boliang Lou , Steve P. Govek
发明人： Stewart A. Noble , Guy Oshiro , James W. Malecha , Cunxiang Zhao , Carmen Robinson , Sergio G. Duron , Michael Sertic , Andrew K. Lindstrom , Andrew K. Shiau , Christopher D. Bayne , Mehmet Kahraman , Boliang Lou , Steve P. Govek
IPC分类号： A61K31/496 , C07D241/04 , C07D401/04 , C07D211/70 , A61K31/4418 , A61K31/551 , A61K31/495 , C07D401/12 , C07D409/14
CPC分类号： C07D213/74 , C07D209/08 , C07D211/96 , C07D257/04 , C07D295/26 , C07D333/60 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/12 , C07D487/08
摘要： Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
摘要翻译：公开了作为过氧化物酶体增殖物激活受体的调节剂的化合物，包含其的药物组合物和使用其的治疗疾病的方法。

9. 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。

10. 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。

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