利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

53 条记录 (耗时 0.036 秒)

    Compounds
    2.
    发明授权
    Compounds 失效
    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。

    Process for Preparing Pyrido[2,3-d]pyrimidin-7-one and 3,4-Dihydropyrimido[4,5-d]pyrimidin-2(1H)-one Derivatives
    3.
    发明申请
    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
    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。

    Process for preparing pyrido[2,3-d]pyrimidin-7-one and 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one derivatives
    4.
    发明授权
    Process for preparing pyrido[2,3-d]pyrimidin-7-one and 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one derivatives 失效
    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。

    Compounds
    10.
    发明授权
    Compounds 失效
    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。