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1. 发明授权

US08575204B2 Nicotinamide derivates useful as P38 inhibitors 有权
标题翻译：可用作P38抑制剂的烟酰胺衍生物
公开(公告)号：US08575204B2
公开(公告)日：2013-11-05
申请号：US12713448
申请日：2010-02-26
申请人： Nicola Mary Aston , Paul Bamborough , Ann Louise Walker
发明人： Nicola Mary Aston , Paul Bamborough , Ann Louise Walker
IPC分类号： C07D213/02 , A61K31/44
CPC分类号： C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.
摘要翻译：式（I）化合物：p38激酶的抑制剂，可用于治疗由p38激酶活性介导的或由p38活性产生的细胞因子介导的病状或疾病状态。

2. 发明申请

US20080176891A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：US20080176891A1
公开(公告)日：2008-07-24
申请号：US11858144
申请日：2007-09-20
申请人： Paul Bamborough , Michael David Barker , Sebastien Andre Campos , Richard Peter Charles Cousins , Paul Faulder , Heather Hobbs , Duncan Stuart Holmes , Michael John Johnston , John Liddle , Jeremy John Payne , John Martin Pritchard , Caroline Whitworth
发明人： Paul Bamborough , Michael David Barker , Sebastien Andre Campos , Richard Peter Charles Cousins , Paul Faulder , Heather Hobbs , Duncan Stuart Holmes , Michael John Johnston , John Liddle , Jeremy John Payne , John Martin Pritchard , Caroline Whitworth
IPC分类号： A61K31/437 , C07D221/04 , A61P29/00 , A61P19/02 , A61P11/06
CPC分类号： C07D471/04
摘要： The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds according to formula (I): and salts thereof.The compounds of the invention are inhibitors of kinase activity, in particular IKK2 activity.
摘要翻译：本发明涉及某些新化合物。具体地，本发明涉及根据式（I）的化合物及其盐。本发明的化合物是激酶活性的抑制剂，特别是IKK2活性。

3. 发明申请

US20070129354A1 Biphenyl carboxylic amide p38 kinase inhibitors 失效
标题翻译：联苯羧酰胺p38激酶抑制剂
公开(公告)号：US20070129354A1
公开(公告)日：2007-06-07
申请号：US10551502
申请日：2004-04-07
申请人： Nicola Aston , Paul Bamborough , Katherine Jones , Vipulkumar Patel , Stephen Swanson , Ann Walker
发明人： Nicola Aston , Paul Bamborough , Katherine Jones , Vipulkumar Patel , Stephen Swanson , Ann Walker
IPC分类号： A61K31/54 , A61K31/5377 , A61K31/495 , A61K31/445 , A61K31/426 , A61K31/421 , A61K31/4164 , A61K31/40 , A61K31/165
CPC分类号： C07D271/06 , C07C235/42 , C07C235/46 , C07C237/30 , C07C237/42 , C07C275/42 , C07C311/04 , C07C311/15 , C07C2601/02 , C07D295/088 , C07D295/185
摘要： Compound of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
摘要翻译：式（I）化合物或其药学上可接受的衍生物及其作为药物的用途，特别是作为p38激酶抑制剂。

4. 发明申请

US20060276516A1 Nicotinamide Derivatives Useful as p38 Inhibitors 有权
标题翻译：适用于p38抑制剂的烟酰胺衍生物
公开(公告)号：US20060276516A1
公开(公告)日：2006-12-07
申请号：US11462858
申请日：2006-08-07
申请人： Nicola Aston , Paul Bamborough , Ann Walker
发明人： Nicola Aston , Paul Bamborough , Ann Walker
IPC分类号： A61K31/455 , C07D213/46
CPC分类号： C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.
摘要翻译：式（I）化合物：p38激酶的抑制剂，可用于治疗由p38激酶活性介导的或由p38活性产生的细胞因子介导的病状或疾病状态。

5. 发明授权

US07125898B2 Nicotinamide derivatives useful as p38 inhibitors. 有权
标题翻译：可用作p38抑制剂的烟酰胺衍生物。
公开(公告)号：US07125898B2
公开(公告)日：2006-10-24
申请号：US10503968
申请日：2003-02-10
申请人： Nicola Mary Aston , Paul Bamborough , Ann Louise Walker
发明人： Nicola Mary Aston , Paul Bamborough , Ann Louise Walker
IPC分类号： C07D213/02 , A61K31/44
CPC分类号： C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.
摘要翻译：式（I）化合物：p38激酶的抑制剂，可用于治疗由p38激酶活性介导的或由p38活性产生的细胞因子介导的病状或疾病状态。

6. 发明申请

US20120184553A1 NOVEL COMPOUNDS 有权
标题翻译：新型化合物
公开(公告)号：US20120184553A1
公开(公告)日：2012-07-19
申请号：US13498975
申请日：2010-09-27
申请人： Paula Louise Nichols , Andrew John Eatherton , Paul Bamborough , Karamjit Singh Jandu , Oliver James Philps , Daniele Andreotti
发明人： Paula Louise Nichols , Andrew John Eatherton , Paul Bamborough , Karamjit Singh Jandu , Oliver James Philps , Daniele Andreotti
IPC分类号： A61K31/5377 , A61K31/4406 , C07C235/56 , A61K31/167 , C07D237/20 , A61K31/50 , A61K31/4402 , C07D239/42 , A61K31/505 , C07D401/12 , A61K31/4545 , A61K31/496 , C07D413/12 , A61P25/16 , C07D213/75
CPC分类号： C07C235/64 , C07D213/75 , C07D231/40 , C07D237/20 , C07D261/14 , C07D263/48 , C07D401/12 , C07D403/12 , C07D413/12
摘要： The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.
摘要翻译：本发明涉及抑制LRRK2激酶活性的新化合物，其制备方法，含有它们的组合物及其用于治疗特征为LRRK2激酶活性，特别是帕金森病和阿尔茨海默病的疾病的用途。

7. 发明授权

US08207176B2 Compounds 失效
标题翻译：化合物
公开(公告)号：US08207176B2
公开(公告)日：2012-06-26
申请号：US11908440
申请日：2006-03-24
申请人： James F. Callahan , Jeffrey C. Boehm , Anthony William James Cooper , Stefano Livia , Paul Bamborough , Neysa Nevins , Zehong Wan , Beth A. Norton , Xichen Lin
发明人： James F. Callahan , Jeffrey C. Boehm , Anthony William James Cooper , Stefano Livia , Paul Bamborough , Neysa Nevins , Zehong Wan , Beth A. Norton , Xichen Lin
IPC分类号： C07D471/04 , A61K31/519 , A61P29/00 , C07D409/06
CPC分类号： C07D487/04
摘要： The present invention is directed to novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds, compositions, and use in therapy as CSBP/RK/p38 kinase inhibitors of Formulas (V) and (Va) wherein inter alia, G5 and G6 are nitrogen and CH, provided that only one of G5 or G6 is nitrogen and the other is CH; R1 is C(Z)N(R10′)(CR10R20)vRb, C(Z)O(CR10R20)vRb, N(R10′)C(Z)(CR10R20)vRb, N(R10′)C(Z)N(R10′)(CR10R20)vRb, or N(R10′)OC(Z)(CR10R20)vRb; R1′ is independently selected at each occurrence from halogen, C1-4 alkyl, halo-substituted-C1-4 alkyl, cyano, nitro, (CR10R20)v′NRdRd′, (CR10R20)v′C(O)R12, SR5, S(O)R5, S(O)2R5, or (CR10R20)v′OR13; Rb is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or heterocyclylC1-10 alkyl moiety, which moieties, excluding hydrogen, may all be optionally substituted; X is R2, OR2′, S(O)mR2′, (CH2)n′N(R10′)S(O)mR2′, (CH2)n′N(R10′)C(O)R2′, (CH2)n′NR4R14, (CH2)n′N(R2′)(R2″), or N(R10′)RhNH—C(═N—CN)NRqRq′; and R3 is a C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted.
摘要翻译：本发明涉及新型取代的2,4,8-三取代8H-吡啶并[2,3-d]嘧啶-7-酮，其含有化合物，组合物和用于治疗作为CSBP / RK / p38激酶抑制剂的式 V）和（Va）其中G5和G6特别是氮和CH，条件是G5或G6中只有一个是氮，另一个是CH; R1是C（Z）N（R10'）（CR10R20）vRb，C（Z）O（CR10R20）vRb，N（R10'）C（Z）（CR10R20）vRb，N（R10'）C（Z）（R10'）（CR10R20）vRb或N（R10'）OC（Z）（CR10R20）vRb; 卤素，C 1-4烷基，卤素取代的C 1-4烷基，氰基，硝基，（CR 10 R 20）v'NR d R d'，（CR 10 R 20）v'C（O）R 12，SR 5， S（O）R 5，S（O）2 R 5或（CR 10 R 20）v'OR 13; R b是氢，C 1-10烷基，C 3-7环烷基，C 3-7环烷基C 1-10烷基，芳基，芳基C 1-10烷基，杂芳基，杂芳基C 1-10烷基，杂环基或杂环基C 1-10烷基部分，可以任选地被取代; X是R2，OR2'，S（O）mR2'，（CH2）n'N（R10'）S（O）mR2'，（CH2）n'N（R10'）C（O）R2' ）n'NR4R14，（CH2）n'N（R2'）（R2“）或N（R10'）RhNH-C（= N-CN）NRqRq' 并且R 3是C 1-10烷基，C 3-7环烷基，C 3-7环烷基C 1-10烷基，芳基，芳基C 1-10烷基，杂芳基，杂芳基C 1-10烷基，杂环基或杂环基C 1-10烷基部分，这些部分可以任选被取代。

8. 发明申请

US20100215652A1 NICOTINAMIDE DERIVATES USEFUL AS P38 INHIBITORS 有权
公开(公告)号：US20100215652A1
公开(公告)日：2010-08-26
申请号：US12713433
申请日：2010-02-26
申请人： Nicola Mary ASTON , Paul Bamborough , Ann Louise Walker
发明人： Nicola Mary ASTON , Paul Bamborough , Ann Louise Walker
IPC分类号： A61K39/395 , A61K31/444 , A61K31/44 , A61K31/4439 , A61K31/496 , A61K38/13 , A61K31/7028 , A61P11/00 , A61P9/00 , A61P17/06 , A61P17/00 , A61P9/10 , A61P1/00 , A61P37/06 , A61P3/10 , A61P19/10
CPC分类号： C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.

9. 发明授权

US07709506B2 Nicotinamide derivatives useful as p38 inhibitors 有权
标题翻译：可用作p38抑制剂的烟酰胺衍生物
公开(公告)号：US07709506B2
公开(公告)日：2010-05-04
申请号：US11462851
申请日：2006-08-07
申请人： Nicola Mary Aston , Paul Bamborough , Ann Louise Walker
发明人： Nicola Mary Aston , Paul Bamborough , Ann Louise Walker
IPC分类号： A61K31/44 , C07D213/02
CPC分类号： C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.
摘要翻译：式（I）化合物：p38激酶的抑制剂，可用于治疗由p38激酶活性介导的或由p38活性产生的细胞因子介导的病状或疾病状态。

10. 发明授权

US07572790B2 Biphenyl carboxylic amide p38 kinase inhibitors 失效
标题翻译：联苯羧酰胺p38激酶抑制剂
公开(公告)号：US07572790B2
公开(公告)日：2009-08-11
申请号：US10551502
申请日：2004-04-07
申请人： Nicola Mary Aston , Paul Bamborough , Katherine Louise Jones , Vipulkumar Kantibhai Patel , Stephen Swanson , Ann Louise Walker
发明人： Nicola Mary Aston , Paul Bamborough , Katherine Louise Jones , Vipulkumar Kantibhai Patel , Stephen Swanson , Ann Louise Walker
IPC分类号： A61K31/54 , A61K31/5377 , A61K31/495 , A61K31/445 , A61K31/426 , A61K31/421 , A61K31/4164 , A61K31/40 , A61K31/165
CPC分类号： C07D271/06 , C07C235/42 , C07C235/46 , C07C237/30 , C07C237/42 , C07C275/42 , C07C311/04 , C07C311/15 , C07C2601/02 , C07D295/088 , C07D295/185
摘要： Compound of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
摘要翻译：式（I）化合物或其药学上可接受的衍生物及其作为药物的用途，特别是作为p38激酶抑制剂。

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