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1. 发明申请

US20060211727A1 Novel compounds 失效
标题翻译：新型化合物
公开(公告)号：US20060211727A1
公开(公告)日：2006-09-21
申请号：US10545565
申请日：2004-02-13
申请人： Jeffrey Boehm , James Callahan , Ralph Hall , Xichen Lin , Katherine Widdowson
发明人： Jeffrey Boehm , James Callahan , Ralph Hall , Xichen Lin , Katherine Widdowson
IPC分类号： C07D471/02 , A61K31/4745
CPC分类号： C07D215/227 , C07D215/38 , C07D471/04
摘要： Novel substituted 1,5,7-trisubstituted-1,8-napthyridin-2(1H)-one compounds; 1,5,7 trisubstituted-1,6-napthyridine-2-(1H)-one compounds and 1,5,7-trisubstituted quinoline-2(1H)-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and pharmaceutical compositions for use in such therapy.
摘要翻译：新的取代的1,5,7-三取代-1,8-萘啶-2（1H） - 酮化合物; 1,5,7-三取代-1,6-萘啶-2-（1H） - 酮化合物和1,5,7-三取代喹啉-2（1H） - 酮化合物，其制备方法，其用于治疗 CSBP / p38激酶介导的疾病和用于这种治疗的药物组合物。

2. 发明申请

US20060293348A1 Novel compounds 失效
标题翻译：新型化合物
公开(公告)号：US20060293348A1
公开(公告)日：2006-12-28
申请号：US10511770
申请日：2003-04-18
申请人： Jeffrey Boehm , Katherine Widdowson , James Callahan , Zehong Wan
发明人： Jeffrey Boehm , Katherine Widdowson , James Callahan , Zehong Wan
IPC分类号： A61K31/519 , C07D487/02
CPC分类号： C07D471/04
摘要： Novel substituted 2, 4, 8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/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-酮化合物和用作CSBP / p38激酶抑制剂治疗的组合物。

3. 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。

4. 发明申请

US20080096905A1 Process For Preparing Pyrido[2,3-D]Pyrimidin-7-One And 3,4-Dihydropyrimido{4,5-D}Pyrimidin-2(1H)-One Derivatives 审中-公开
标题翻译：制备吡啶并[2,3-D]嘧啶-7-酮和3,4-二氢嘧啶并[4,5-D]嘧啶-2（1H） - 衍生物的方法
公开(公告)号：US20080096905A1
公开(公告)日：2008-04-24
申请号：US11908839
申请日：2006-03-24
申请人： James Callahan , Jeffrey Boehm , Zehong Wan , Hohgxing Yan
发明人： James Callahan , Jeffrey Boehm , Zehong Wan , Hohgxing Yan
IPC分类号： A61K31/519 , C07D487/02
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention is directed to a novel method of preparing of 2,4,8-trisubstituted pyrido[2,3-d]pyrimidin-7-one pharmacophores of Formula (II) wherein G1 is CH2 or NH: G2 is CH or nitrogen; Rx is chloro, bromo, iodo, or O—S(O)2CF3; Rg is a C1-10alkyl; m is 0, or an integer having a value of 1, or 2; R3 is a C1-10alkyl, C3-7cycloalkyl, C3-7cycloalkyl C1-10alkyl, aryl, arylC1-10alkyl, heteroaryl, heteroarylC1-10alkyl, heterocyclic or a heterocyclylC1-10alkyl moiety, and wherein each of these moieties may be optionally substituted. which comprises reacting a compound of the formula: wherein Ry is chloro, bromo, iodo, O—S(O)2CF3; and Rg is a C1-10alkyl; with a olefin forming reagent in a suitable base to yield a compound of Formula (II), wherein m=0 and oxidizing the sulphur as necessary or desired.
摘要翻译：本发明涉及一种制备式（II）的2,4,8-三取代吡啶并[2,3-d]嘧啶-7-酮药效团的新方法，其中G1是CH 2 或NH：G2为CH或氮; Rx是氯，溴，碘或O-S（O）2 CF 3。 R 1是C 1-10烷基; m为0，或值为1或2的整数; R 3是C 1-10烷基，C 3-7环烷基，C 3-7环烷基C 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个烷基部分，并且其中这些部分中的每一个可以是任选取代的。其包括使下式化合物：其中R y是氯，溴，碘，O-S（O）2 CF 3 3; 且R g为C 1-10烷基; 与合适的碱中的烯烃形成试剂反应，得到式（II）的化合物，其中m = 0并根据需要氧化硫。

5. 发明申请

US20080051416A1 Novel Compounds 审中-公开
标题翻译：新型化合物
公开(公告)号：US20080051416A1
公开(公告)日：2008-02-28
申请号：US11576748
申请日：2005-10-05
申请人： Jeffrey Boehm , James Callahan , Zehong Wan , Hongxing Yan
发明人： Jeffrey Boehm , James Callahan , Zehong Wan , Hongxing Yan
IPC分类号： A61K31/495 , A61K31/164 , A61K31/195 , A61K31/215 , A61K31/40 , A61P43/00 , C07C233/00 , C07D207/00 , C07D221/00 , C07D295/00 , C07D277/02 , C07D233/54 , C07D213/02 , C07C311/01 , C07C229/00 , A61K31/4164 , A61K31/426 , A61K31/44 , A61K31/445
CPC分类号： C07C311/37 , C07C233/65 , C07C233/66 , C07C233/69 , C07C233/78 , C07C255/24 , C07C275/42 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/14 , C07D211/58 , C07D213/75 , C07D231/40 , C07D233/61 , C07D277/46 , C07D285/08 , C07D295/13 , C07D417/12
摘要： The present invention is directed to novel compounds of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
摘要翻译：本发明涉及新的式（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。

6. 发明申请

US20060258687A1 Process for preparing pyrido[2,3-d]pyrimidin-7-one and 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one derivatives 失效
标题翻译：制备吡啶并[2,3-d]嘧啶-7-酮和3,4-二氢嘧啶并[4,5-d]嘧啶-2（1H） - 酮衍生物的方法
公开(公告)号：US20060258687A1
公开(公告)日：2006-11-16
申请号：US11388375
申请日：2006-03-24
申请人： Jeffrey Boehm , James Callahan , Zehong Wan , Hongxing Yan
发明人： Jeffrey Boehm , James Callahan , Zehong Wan , Hongxing Yan
IPC分类号： A61K31/519 , C07D487/02
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention is directed to a novel method of preparing of 2,4,8-trisubstituted pyrido[2,3-d]pyrimidin-7-one pharmacophores of Formula (II) or (IIa) wherein G1 is CH2 or NH: G2 is CH or nitrogen; Rx is chloro, bromo, iodo, or O—S(O)2CF3; Rg is a C1-10alkyl; m is 0, or an integer having a value of 1, or 2; 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. which comprises reacting a compound of the formula: wherein Ry is chloro, bromo, iodo, O—S(O)2CF3; and Rg is a C1-10 alkyl; with a olefin forming reagent in a suitable base to yield a compound of Formula (II), or (IIa) wherein m=0 and oxidizing the sulphur as necessary or desired.
摘要翻译：本发明涉及制备式（II）或（IIa）的2,4,8-三取代吡啶并[2,3-d]嘧啶-7-酮药效团的新方法，其中G1是CH 2 或NH：G2是CH或氮; Rx是氯，溴，碘或O-S（O）2 CF 3。 R 1是C 1-10烷基; m为0，或值为1或2的整数; R 3是C 1-10烷基，C 3-7环烷基，C 3-7环烷基C 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个烷基部分，并且其中这些部分中的每一个可以是任选取代的。其包括使下式化合物：其中R y是氯，溴，碘，O-S（O）2 CF 3 3; 且R g为C 1-10烷基; 在合适的碱中加入烯烃形成试剂，得到式（II）化合物或其中m = 0的（IIa），并根据需要氧化硫。

7. 发明申请

US20060106058A1 Chemical compounds 失效
公开(公告)号：US20060106058A1
公开(公告)日：2006-05-18
申请号：US10530986
申请日：2003-10-15
申请人： Joelle Burgess , James Callahan , Toshihiro Hamajima , Satoru Ida , Ichiro Mori , Jun Tang
发明人： Joelle Burgess , James Callahan , Toshihiro Hamajima , Satoru Ida , Ichiro Mori , Jun Tang
IPC分类号： A61K31/4709 , C07D215/38 , A61K31/47 , C07D405/02 , C07D403/02
CPC分类号： C07D401/12 , C07D215/54 , C07D405/12
摘要： 3-carboxy quinoline derivatives, which are useful as YAK3 inhibitors are described herein. The described invention also includes methods of making such 3-carboxy quinoline derivatives as well as methods of using the same in the treatment of diseases mediated by inappropriate YAK3 activity.

8. 发明申请

US20060058391A1 Calcilytic compounds 有权
公开(公告)号：US20060058391A1
公开(公告)日：2006-03-16
申请号：US10536416
申请日：2003-11-25
申请人： Robert Marquis , Linda Casillas , Joshi Ramanjulu , James Callahan
发明人： Robert Marquis , Linda Casillas , Joshi Ramanjulu , James Callahan
IPC分类号： A61K31/195 , C07C229/64
CPC分类号： C07C217/54 , C07C217/30 , C07C217/32 , C07C217/34 , C07C229/34 , C07C2602/08
摘要： Novel Calcilytic compounds and methods of using them are provided.

9. 发明申请

US20050165086A1 Nf-kb inhibitors 失效
公开(公告)号：US20050165086A1
公开(公告)日：2005-07-28
申请号：US10510841
申请日：2003-04-11
申请人： James Callahan , Yue Li
发明人： James Callahan , Yue Li
IPC分类号： C07D333/50 , A61K31/381 , A61P1/00 , A61P3/10 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/04 , A61P19/10 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/18 , A61P35/00 , A61P37/02 , A61P43/00 , C07D333/74 , C07D333/78 , C07D333/76
CPC分类号： C07D333/74 , C07D333/78
摘要： The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-β phosphorylation of IκB. In so doing these aminothiophene inhibitors block pathological activation of transcription factor NF-κB in which diseases excessive activation of NF-κB is implicated.

10. 发明申请

US20050043352A1 Quinoline inhibitors of hyaki and hyak3 kinases 失效
标题翻译：喹喔啉和hyak3激酶的喹啉抑制剂
公开(公告)号：US20050043352A1
公开(公告)日：2005-02-24
申请号：US10474084
申请日：2002-04-04
申请人： Deborah Bryan , Joelle Burgess , James Callahan
发明人： Deborah Bryan , Joelle Burgess , James Callahan
IPC分类号： A61K31/47 , A61K31/4709 , A61K31/5377 , A61P7/00 , A61P7/06 , A61P13/12 , A61P15/16 , A61P19/00 , A61P25/28 , A61P31/00 , A61P31/10 , A61P31/12 , A61P31/18 , A61P33/00 , A61P35/00 , A61P35/02 , A61P37/00 , A61P39/00 , A61P43/00 , C07D215/54 , C07D401/12
CPC分类号： C07D401/12 , A61K31/47 , A61K31/4709 , C07D215/54
摘要： This invention relates to novel quinoline inhibitors of hYAK1 and hYAK3 kinases and pharmaceutically acceptable salts, hydrates or solvates thereof, pharmaceutical compositions thereof, and methods of treatment of diseases in which an excessive amount of either such kinase is a factor.
摘要翻译：本发明涉及hYAK1和hYAK3激酶的新型喹啉抑制剂及其药学上可接受的盐，水合物或溶剂化物，其药物组合物和治疗其中过量的这种激酶是因子的疾病的方法。

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