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公开(公告)号:US07629363B2
公开(公告)日:2009-12-08
申请号:US11226556
申请日:2005-09-14
申请人: Balekudru Devadas , John Walker , Shaun R. Selness , Terri L. Boehm , Richard C. Durley , Rajesh Devraj , Brian S. Hickory , Paul V. Rucker , Kevin D. Jerome , Heather M. Madsen , Edgardo Alvira , Michele A. Promo , Radhika M. Blevis-Bal , Laura D. Marruto , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey S. Shieh , Aruna Sambandam , Shuang Liu , Ian L. Scott , Kevin F. McGee
发明人: Balekudru Devadas , John Walker , Shaun R. Selness , Terri L. Boehm , Richard C. Durley , Rajesh Devraj , Brian S. Hickory , Paul V. Rucker , Kevin D. Jerome , Heather M. Madsen , Edgardo Alvira , Michele A. Promo , Radhika M. Blevis-Bal , Laura D. Marruto , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey S. Shieh , Aruna Sambandam , Shuang Liu , Ian L. Scott , Kevin F. McGee
IPC分类号: A61K31/44 , C07D211/02
CPC分类号: C07D213/64 , C07D213/69 , C07D213/70 , C07D213/74 , C07D213/75 , C07D213/79 , C07D213/84 , C07D213/85 , C07D215/22 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/10
摘要: Disclosed are compounds Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R3/R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
摘要翻译: 公开了式I化合物及其药学上可接受的盐,其中R 1,R 2,R 3 / R 4和R 5在本文中定义。 这些化合物可用于治疗由不受调节的p38 MAP激酶和/或TNF活性引起或加重的疾病和病症。 还公开了含有化合物的药物组合物,制备化合物的方法和使用该化合物的治疗方法。
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52.
公开(公告)号:US20090270350A1
公开(公告)日:2009-10-29
申请号:US12162048
申请日:2007-02-05
申请人: Balekudru Devadas , Susan J. Hartmann , Richard F. Heier , Kevin D. Jerome , Steve A. Kolodziej , John Mathias , Monica B. Norton , Michele A. Promo , Paul V. Rucker , Shaun Selness
发明人: Balekudru Devadas , Susan J. Hartmann , Richard F. Heier , Kevin D. Jerome , Steve A. Kolodziej , John Mathias , Monica B. Norton , Michele A. Promo , Paul V. Rucker , Shaun Selness
IPC分类号: A61K31/695 , C07F7/18 , A61K31/4439 , C07D401/12
CPC分类号: C07D401/12 , C07D403/12
摘要: This invention is directed generally to substituted pyridinone and pyrimidinone compounds that generally inhibit p38 kinase, TNF, and/or cyclooxygeπase activity. Such substituted pyridinone and pyrimidinone compounds include compounds generally corresponding in structure to the following formula: wherein Z, n, R1, R2a, R2b, R2c, R2d, R2e, R3a, R3b, R3c, R3d, R4, R5, R6, R7a, R7b, R7c, R7d and R7e are as defined in this specification. This invention also is directed to compositions of such substituted pyridinones and pyrimidinones (particularly pharmaceutical compositions), and methods for treating disorders (typically pathological disorders) associated with p38 kinase activity, TNF activity, and/or cyclooxygenase-2 activity.
摘要翻译: 本发明通常涉及通常抑制p38激酶,TNF和/或环氧糖蛋白酶活性的取代的吡啶酮和嘧啶酮化合物。 这种取代的吡啶酮和嘧啶酮化合物包括通式在下列结构相应的化合物:其中Z,n,R1,R2a,R2b,R2c,R2d,R2e,R3a,R3b,R3c,R3d,R4,R5,R6,R7a, R7b,R7c,R7d和R7e如本说明书中所定义。 本发明还涉及这种取代的吡啶酮和嘧啶酮(特别是药物组合物)的组合物,以及用于治疗与p38激酶活性,TNF活性和/或环氧合酶-2活性相关的疾病(通常为病理学障碍)的方法。
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53.
公开(公告)号:US07138411B2
公开(公告)日:2006-11-21
申请号:US10303150
申请日:2002-11-22
申请人: Jeffery S Carter , Mark G Obukowicz , Balekudru Devadas , John J Talley , David L Brown , Matthew J Graneto , Stephen R Bertenshaw , Donald J Rogier, Jr. , Srinivasan Raj Nagarajan , Cathleen E Hanau , Susan J Hartmann , Cindy L Ludwig , Suzanne Metz , Donald E Korte
发明人: Jeffery S Carter , Mark G Obukowicz , Balekudru Devadas , John J Talley , David L Brown , Matthew J Graneto , Stephen R Bertenshaw , Donald J Rogier, Jr. , Srinivasan Raj Nagarajan , Cathleen E Hanau , Susan J Hartmann , Cindy L Ludwig , Suzanne Metz , Donald E Korte
IPC分类号: A61K31/47 , A61K31/38 , A61K31/35 , C07D307/77 , C07D335/04
CPC分类号: C07D215/54 , C07D311/22 , C07D311/58 , C07D311/92 , C07D335/06 , C07D401/12 , C07D405/04 , C07D407/04 , C07D407/12 , C07D409/04 , C07D471/04 , C07D491/04 , C07D493/04
摘要: A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I′ wherein X, A1, A2, A3, A4, R, R″, R1 and R2 are as described in the specification.
摘要翻译: 描述了一类苯并吡喃,苯并噻喃,二氢喹啉,二氢萘及其类似物,用于治疗环氧合酶-2介导的病症。 特别感兴趣的化合物由式I'定义,其中X,A 1,A 2,A 3,A 4, SUP>,R,R“,R”1“和”R“2如说明书中所述。
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公开(公告)号:US06933304B2
公开(公告)日:2005-08-23
申请号:US09881913
申请日:2001-06-15
申请人: Srinivasan Raj Nagarajan , Ish Kumar Khanna , Michael B. Tollefson , Scott B. Mohler , Barbara Chen , Mark Russell , Balekudru Devadas , Thomas D. Penning , Lori A. Schretzman , Dale P. Spangler , Mark Laurence Boys , Nizal Samuel Chandrakumar , Hung-Fun Lu
发明人: Srinivasan Raj Nagarajan , Ish Kumar Khanna , Michael B. Tollefson , Scott B. Mohler , Barbara Chen , Mark Russell , Balekudru Devadas , Thomas D. Penning , Lori A. Schretzman , Dale P. Spangler , Mark Laurence Boys , Nizal Samuel Chandrakumar , Hung-Fun Lu
IPC分类号: A61K31/4245 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/5383 , A61P3/14 , A61P9/00 , A61P9/08 , A61P9/10 , A61P19/02 , A61P19/10 , A61P21/00 , A61P27/02 , A61P35/00 , A61P43/00 , C07D213/74 , C07D231/38 , C07D233/60 , C07D233/88 , C07D405/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D498/04
CPC分类号: C07D213/74 , C07D231/38 , C07D233/88 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively antagonizing the αVβ3 and/or the αVβ5 integrin without significantly antagonizing the IIb/IIIa or αVβ6 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拮抗α-β3 和/或α5AT55整联蛋白,而不显着拮抗IIb / IIIa或α5β6 / SUB>整合素。
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公开(公告)号:US08563558B2
公开(公告)日:2013-10-22
申请号:US13312768
申请日:2011-12-06
申请人: Shaun R. Selness , Joseph B. Monahan , John F. Schindler , Balekudru Devadas , Susan L. Hockerman
发明人: Shaun R. Selness , Joseph B. Monahan , John F. Schindler , Balekudru Devadas , Susan L. Hockerman
IPC分类号: C07D401/12 , C07D239/42 , A61P35/00
CPC分类号: A61K45/06 , A61K31/506 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14 , A61K2300/00
摘要: The present disclosure provides pyridine urea compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): wherein R1, R2, R3, R4, R5, V and W are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.
摘要翻译: 本公开提供了吡啶脲化合物,其可用于治疗p38激酶介导的疾病,例如淋巴瘤和自身炎性疾病,其具有式(I)的结构:其中R1,R2,R3,R4,R5,V和W为 如详细描述中所定义; 包含至少一种化合物的药物组合物; 以及使用该化合物治疗p38激酶介导的疾病的方法。
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公开(公告)号:US08507499B2
公开(公告)日:2013-08-13
申请号:US13312720
申请日:2011-12-06
IPC分类号: A61K31/506 , C07D403/14
CPC分类号: A61K31/506 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14
摘要: The present disclosure provides indole/indazole-pyrimidinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): wherein W, X, R1, R2, R3, R4, R5 and R6 are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.
摘要翻译: 本公开提供了可用于治疗p38激酶介导的疾病(例如淋巴瘤和自身炎性疾病)的吲哚/吲唑 - 嘧啶基化合物,其具有式(I)的结构:其中W,X,R 1,R 2,R 3,R 4 R5和R6如详细说明中所定义; 包含至少一种化合物的药物组合物; 以及使用该化合物治疗p38激酶介导的疾病的方法。
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公开(公告)号:US20120142696A1
公开(公告)日:2012-06-07
申请号:US13312720
申请日:2011-12-06
IPC分类号: A61K31/506 , C07D417/14 , C07D401/14 , A61P29/00 , A61P9/10 , A61P37/06 , A61P37/02 , A61P37/00 , A61P3/10 , A61P3/00 , A61P35/00 , A61P35/02 , C07D403/14 , A61P43/00 , C07D413/14
CPC分类号: A61K31/506 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14
摘要: The present disclosure provides indole/indazole-pyrimidinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): wherein W, X, R1, R2, R3, R4, R5 and R6 are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.
摘要翻译: 本公开提供了可用于治疗p38激酶介导的疾病(例如淋巴瘤和自身炎性疾病)的吲哚/吲唑 - 嘧啶基化合物,其具有式(I)的结构:其中W,X,R 1,R 2,R 3,R 4 R5和R6如详细说明中所定义; 包含至少一种化合物的药物组合物; 以及使用该化合物治疗p38激酶介导的疾病的方法。
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公开(公告)号:US07119098B2
公开(公告)日:2006-10-10
申请号:US10311385
申请日:2001-06-15
申请人: Srinivasan Raj Nagarajan , Ish Kumar Khanna , Michael B. Tollefson , Scott B. Mohler , Barbara B. Chen , Mark Russell , Balekudru Devadas , Thomas D. Penning , Lori A. Schretzman , Dale P. Spangler , Mark L. Boys , Nizal S. Chandrakumar , Hwang-Fun Lu
发明人: Srinivasan Raj Nagarajan , Ish Kumar Khanna , Michael B. Tollefson , Scott B. Mohler , Barbara B. Chen , Mark Russell , Balekudru Devadas , Thomas D. Penning , Lori A. Schretzman , Dale P. Spangler , Mark L. Boys , Nizal S. Chandrakumar , Hwang-Fun Lu
IPC分类号: C07D403/12 , C07D403/14 , C07D401/12 , A61K31/443 , A61K31/4375
CPC分类号: C07D213/74 , C07D231/38 , C07D233/88 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要: The present invention relates to a class of compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of Formula (I), and methods of selectively antagonizing the ανβ3 and/or the ανβ5 integrin without significantly antagonizing the IIb/IIIa 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,和选择性拮抗化合物3和/或 在不显着拮抗IIb / IIIa整联蛋白的情况下,所述的5'-整联蛋白。
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59.
公开(公告)号:US07109211B2
公开(公告)日:2006-09-19
申请号:US10922036
申请日:2004-08-19
申请人: Jeffery S Carter , Mark G Obukowicz , Balekudru Devadas , John J Talley , David L Brown , Matthew J Graneto , Stephen R Bertenshaw , Donald J. Rogier, Jr. , Srinivasan Raj Nagarajan , Cathleen E Hanau , Susan J Hartmann , Cindy L Ludwig , Suzanne Metz , Donald E Korte
发明人: Jeffery S Carter , Mark G Obukowicz , Balekudru Devadas , John J Talley , David L Brown , Matthew J Graneto , Stephen R Bertenshaw , Donald J. Rogier, Jr. , Srinivasan Raj Nagarajan , Cathleen E Hanau , Susan J Hartmann , Cindy L Ludwig , Suzanne Metz , Donald E Korte
IPC分类号: A61K31/47 , C07D211/30
CPC分类号: C07D335/06 , C07D215/54 , C07D311/22 , C07D311/58 , C07D311/92 , C07D401/12 , C07D405/04 , C07D407/04 , C07D407/12 , C07D409/04 , C07D471/04 , C07D491/04 , C07D493/04
摘要: A class of benzopyran, derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I′ wherein X, A1, A2, A3, A4, R, R″, R1 and R2 are as described in the specification.
摘要翻译: 描述了一类苯并吡喃衍生物用于治疗环氧合酶-2介导的病症。 特别感兴趣的化合物由式I'定义,其中X,A 1,A 2,A 3,A 4, SUP>,R,R“,R”1“和”R“2如说明书中所述。
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公开(公告)号:US06906051B2
公开(公告)日:2005-06-14
申请号:US10717238
申请日:2003-11-19
申请人: Peter Ruminiski , Thomas D. Penning , Lan Jiang , Balekudru Devadas , Thomas Rogers , Jennifer VanCamp , Chester Yuan
发明人: Peter Ruminiski , Thomas D. Penning , Lan Jiang , Balekudru Devadas , Thomas Rogers , Jennifer VanCamp , Chester Yuan
IPC分类号: C07D307/33 , A61K31/365 , A61K31/506 , A61P1/02 , A61P3/14 , A61P9/00 , A61P9/10 , A61P19/02 , A61P19/10 , A61P21/00 , A61P27/02 , A61P31/12 , A61P35/00 , A61P35/04 , A61P43/00 , C07D309/30 , C07D405/12 , C07D405/14 , A61K31/33 , A61K31/505 , C07D239/00 , C07D305/00 , C07D407/00
CPC分类号: C07D405/12 , C07D309/30 , C07D405/14
摘要: The present invention relates to a class of compounds represented by the Formula I: or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the αVβ3 and/or the αVβ5 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,以及选择性抑制或拮抗α SUB> 3和/或α5AT55整联蛋白。
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