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    • 2. 发明授权
    • Compounds
    • 化合物
    • US08207176B2
    • 2012-06-26
    • US11908440
    • 2006-03-24
    • James F. CallahanJeffrey C. BoehmAnthony William James CooperStefano LiviaPaul BamboroughNeysa NevinsZehong WanBeth A. NortonXichen Lin
    • James F. CallahanJeffrey C. BoehmAnthony William James CooperStefano LiviaPaul BamboroughNeysa NevinsZehong WanBeth A. NortonXichen Lin
    • C07D471/04A61K31/519A61P29/00C07D409/06
    • C07D487/04
    • 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.
    • 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。