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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

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。

3. 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。

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

US20090048444A1 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） - 酮衍生物的方法
公开(公告)号：US20090048444A1
公开(公告)日：2009-02-19
申请号：US12253327
申请日：2008-10-17
申请人： James F. Callahan , Jeffrey C. Boehm , Zehong Wan , Hongxing Yan , Xichen Lin
发明人： James F. Callahan , Jeffrey C. Boehm , Zehong Wan , Hongxing Yan , Xichen Lin
IPC分类号： C07D487/04 , C07D471/04
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; G2 is CH; Rx is chloro, bromo, iodo, or O—S(O)2CF3; Rg is a C1-10 alkyl; 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-酮药代动力学的新方法，其中G1是CH2; G2是CH; R x是氯，溴，碘或O-S（O）2 C 3 F 3; Rg为C1-10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 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，并且其中部分可以任选被取代。其包括使下式化合物：其中R y是氯，溴，碘，O-S（O）2 C 3 F 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. 发明授权

US07479558B2 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：US07479558B2
公开(公告)日：2009-01-20
申请号：US11388375
申请日：2006-03-24
申请人： James F. Callahan , Jeffrey C. Boehm , Zehong Wan , Hongxing Yan , Xichen Lin
发明人： James F. Callahan , Jeffrey C. Boehm , Zehong Wan , Hongxing Yan , Xichen Lin
IPC分类号： C07D487/04 , C07D239/30 , C07D413/04 , C07D471/04
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：本发明涉及一种制备式（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CH2或NH：G2 是CH或氮; R x是氯，溴，碘或O-S（O）2 C 3 F 3; Rg为C1-10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 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，并且其中部分可以任选被取代。其包括使下式化合物：其中R y是氯，溴，碘，O-S（O）2 C 3 F 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。

8. 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。

9. 发明申请

US20090239846A1 Novel Compounds 审中-公开
标题翻译：新型化合物
公开(公告)号：US20090239846A1
公开(公告)日：2009-09-24
申请号：US11908435
申请日：2006-03-24
申请人： James F. Callahan , Zehong Wan , Hongxing Yan , Xichen Lin
发明人： James F. Callahan , Zehong Wan , Hongxing Yan , Xichen Lin
IPC分类号： A61K31/551 , A61K31/5377 , A61K31/519 , C07D243/08 , C07D413/00 , C07D487/04
CPC分类号： C07D487/04
摘要： Novel substituted 1,5,7-trisubstituted-3,4-dihydro-pyrimido[4,5-d]pyrimidin-2-(1H)-one compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.
摘要翻译：新型取代的1,5,7-三取代-3,4-二氢嘧啶并[4,5-d]嘧啶-2-（1H） - 酮化合物及其组合物及其在CSBP / RK / p38激酶抑制剂治疗中的用途。

10. 发明授权

US07674789B2 Compounds 失效
标题翻译：化合物
公开(公告)号：US07674789B2
公开(公告)日：2010-03-09
申请号：US11389112
申请日：2006-03-24
申请人： James F. Callahan , Zehong Wan , Hongxing Yan , Xichen Lin
发明人： James F. Callahan , Zehong Wan , Hongxing Yan , Xichen Lin
IPC分类号： A61K31/5355 , A61K31/519 , C07D487/04 , A61P29/00 , C07D239/30 , C07D239/38
CPC分类号： C07D487/04
摘要： The present invention is directed to compounds of formula (I), (Ia),(Ic) and (Id), compositions, and uses thereof as an inhibitor of the p38 kinase, and wherein, inter alia 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; R3 is C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroarylC1-10 alkyl, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may 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′)—Rh—NH—C(═N—CN)NRqRq′; and R2 is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及作为p38激酶抑制剂的式（I），（Ia），（Ic）和（Id），其组合物和用途的化合物，其中除了其中R 1是C（Z）N （R10'）（CR10R20）vRb，C（Z）O（CR10R20）vRb，N（R10'）C（Z）（CR10R20）vRb; N（R 10'）C（Z）N（R 10'）（CR 10 R 20）v R b; 或N（R 10'）OC（Z）（CR 10 R 20）v R b; 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C 1-10烷基或杂环基C 1-10烷基部分，并且其中这些部分中的每一个可以是任选的取代 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'） - Rh-NH-C（= N-CN）NRqRq' 和R 2是氢，C 1-10烷基，C 3-7环烷基，C 3-7环烷基烷基，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，，不包括氢，可以任选被取代; 或其药学上可接受的盐。

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