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1. 发明申请

US20090156597A1 Novel Compounds 失效
标题翻译：新型化合物
公开(公告)号：US20090156597A1
公开(公告)日：2009-06-18
申请号：US12132793
申请日：2008-06-04
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： A61K31/519 , A61K31/5377 , A61P3/00 , A61P27/00 , A61P11/00 , A61P9/00 , A61P25/00 , C07D471/04
CPC分类号： C07D487/04
摘要： Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.
摘要翻译：新型取代的2,4,8-三取代8H-吡啶并[2,3-d]嘧啶-7-酮的化合物和组合物，以及它们在CSBP / RK / p38激酶抑制剂治疗中的用途。

2. 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。

3. 发明授权

US08354416B2 7,8-dihydropyrido[2,3-d]pyrimidin-4-yl substituted compounds as inhibitors of p38 kinase 失效
标题翻译： 7,8-二氢吡啶并[2,3-d]嘧啶-4-基取代的化合物作为p38激酶的抑制剂
公开(公告)号：US08354416B2
公开(公告)日：2013-01-15
申请号：US12132793
申请日：2008-06-04
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 , A61P9/10
CPC分类号： C07D487/04
摘要： Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.
摘要翻译：新型取代的2,4,8-三取代8H-吡啶并[2,3-d]嘧啶-7-酮的化合物和组合物，以及它们在CSBP / RK / p38激酶抑制剂治疗中的用途。

4. 发明授权

US07678801B2 Compounds 失效
标题翻译：化合物
公开(公告)号：US07678801B2
公开(公告)日：2010-03-16
申请号：US11388968
申请日：2006-03-24
申请人： James F. Callahan , Jeffrey C. Boehm , Anthony William James Cooper , Stefano Livia , Neysa Nevins , Zehong Wan , Beth A. Norton , Paul Bamborough , Xichen Lin
发明人： James F. Callahan , Jeffrey C. Boehm , Anthony William James Cooper , Stefano Livia , Neysa Nevins , Zehong Wan , Beth A. Norton , Paul Bamborough , Xichen Lin
IPC分类号： A61K31/519 , A61K31/4545 , A61P29/00 , C07D413/14 , C07D471/04 , C07D487/04
CPC分类号： C07D487/04
摘要： Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use use in therapy as CSBP/RK/p38 kinase inhibitors.
摘要翻译：新型取代的2,4,8-三取代8H-吡啶并[2,3-d]嘧啶-7-酮含有化合物和组合物，及其在CSBP / RK / p38激酶抑制剂治疗中的用途。

5. 发明申请

US20090069318A1 Novel Compounds 失效
公开(公告)号：US20090069318A1
公开(公告)日：2009-03-12
申请号：US11908440
申请日：2006-03-24
申请人： James Francis Callahan , Jeffrey C. Boehm , Anthony William James Cooper , Stefano Livia , Neysa Nevins , Zehong Wan , Beth A. Norton , Xichen Lin
发明人： James Francis Callahan , Jeffrey C. Boehm , Anthony William James Cooper , Stefano Livia , Neysa Nevins , Zehong Wan , Beth A. Norton , Xichen Lin
IPC分类号： A61K31/5377 , C07D471/04 , A61K31/519
CPC分类号： C07D487/04
摘要： Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.

6. 发明申请

US20060235029A1 Novel compounds 失效
标题翻译：新型化合物
公开(公告)号：US20060235029A1
公开(公告)日：2006-10-19
申请号：US11388968
申请日：2006-03-24
申请人： James Callahan , Jeffrey Boehm , Anthony Cooper , Stefano Livia , Neysa Nevins , Zehong Wan , Beth Norton
发明人： James Callahan , Jeffrey Boehm , Anthony Cooper , Stefano Livia , Neysa Nevins , Zehong Wan , Beth Norton
IPC分类号： A61K31/519 , A61K31/4745 , C07D471/02 , C07D487/02
CPC分类号： C07D487/04
摘要： Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use use in therapy as CSBP/RK/p38 kinase inhibitors.
摘要翻译：新型取代的2,4,8-三取代8H-吡啶并[2,3-d]嘧啶-7-酮含有化合物和组合物，及其在CSBP / RK / p38激酶抑制剂治疗中的用途。

7. 发明申请

US20120142668A1 CATHEPSIN C INHIBITORS 审中-公开
标题翻译： CATHEPSIN C抑制剂
公开(公告)号：US20120142668A1
公开(公告)日：2012-06-07
申请号：US13389631
申请日：2010-08-11
申请人： Niall Anderson , Ann M. Bullion , Neysa Nevins , Michael R. Palovich , Steven L. Sollis , Michael D. Wall , Jakob Busch-Petersen , Brian Evans , Huijie Li
发明人： Niall Anderson , Ann M. Bullion , Neysa Nevins , Michael R. Palovich , Steven L. Sollis , Michael D. Wall , Jakob Busch-Petersen , Brian Evans , Huijie Li
IPC分类号： A61K31/397 , C07D211/60 , C07C229/38 , C07D277/46 , C07D209/08 , C07D213/75 , C07D231/40 , C07D401/12 , C07D417/12 , A61K31/165 , A61K31/4453 , A61K31/24 , A61K31/404 , A61K31/4406 , A61K31/415 , A61K31/4468 , A61P11/00 , A61K31/426 , A61K31/454 , C07C237/20
CPC分类号： C07C237/22 , C07B2200/07 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07D205/04 , C07D209/14 , C07D209/44 , C07D211/56 , C07D211/58 , C07D213/75 , C07D231/40 , C07D277/46 , C07D285/135 , C07D295/185 , C07D307/22 , C07D309/14 , C07D333/24 , C07D333/36 , C07D401/12 , C07D403/12 , C07D417/12
摘要： Disclosed are 4-amino-2-butenamides of Formula (I) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin C enzyme such as chronic obstructive pulmonary disease.
摘要翻译：公开了具有药理活性的式（I）的4-氨基-2-丁烯酰胺，含有它们的药物组合物和用于治疗组织蛋白酶C酶介导的疾病如慢性阻塞性肺病的方法。

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