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    • 1. 发明公开
    • 4-HETEROARYMETHYL SUBSTITUTED PHTHALAZINONE DERIVATIVES
    • 4-杂芳基取代的酞嗪酮衍生物
    • EP1948642A1
    • 2008-07-30
    • EP06794830.7
    • 2006-10-19
    • Kudos Pharmaceuticals LtdMaybridge Limited
    • JAVAID, Muhammad, HashimMENEAR, Keith, AllanGOMEZ, SylvieHUMMERSONE, Marc, GeoffreyMARTIN, Niall, Morrisson, BarrSMITH, Graeme, Cameron, MurrayCOCKCROFT, Xiao-Ling, FanKERRIGAN, Frank
    • C07D403/14C07D411/14A61K31/502A61P31/20
    • C07D403/10C07D403/14C07D411/14C07D413/14C07D487/04
    • 1.A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; D is selected from formula (i), where Y1 is selected from CH and N , Y2 is selected from CH and N, Y3 is selected from CH, CF and N; and formulae (ii), (A) and (B) where Q is O or S; RD is formula (C) wherein RN1 is selected from H and optionally substituted C1-10 alkyl; X is selected from a single bond, NRN2, CRC3RC4 and C=O; RN2 is selected from H and optionally substituted C1-10 alkyl; Rc3 and Rc4 are independently selected from H, R, C(=O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; Y is selected from NRN3 and CRc1Rc2; RC1 and RC2 are independently selected from H, R, C(=O)OR, where R is optionally substituted C1 -10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; RC1 and RC2 together with the carbon atom to which they are attached may form an optionally substituted spiro-fused C5-7 carbocylic or heterocyclic ring; and when X is a single bond RN1 and RC2 may together with the N and C atoms to which they are bound, form an optionally substituted C5-7 heterocylic ring; and when X is CRC3RC4, RC2 and RC4 may together form an additional bond, s uch that there is a double bond between the atoms substituted by RC1 and RC3.
    • 1.式(I)的化合物:其中:A和B一起表示任选取代的稠合芳环; D选自式(i),其中Y 1选自CH和N,Y 2选自CH和N,Y 3选自CH,CF和N; 和其中Q是O或S的式(ii),(A)和(B) RD是式(C),其中RN1选自H和任选取代的C1-10烷基; X选自单键NRN2,CRC3RC4和C = O; RN2选自H和任选取代的C1-10烷基; R c3和R c4独立地选自H,R,C(= O)OR,其中R是任选取代的C 1-10烷基,任选取代的C 5-20芳基或任选取代的C 3-20杂环基; Y选自NRN3和CRc1Rc2; RC 1和RC 2独立地选自H,R,C(= O)OR,其中R为任选取代的C 1-10烷基,任选取代的C 5-20芳基或任选取代的C 3-20杂环基; RC1和RC2与它们所连接的碳原子一起可形成任选取代的螺稠合的C5-7碳环或杂环; 并且当X是单键时,RN1和RC2可以与它们所键合的N和C原子一起形成任选取代的C5-7杂环; 并且当X是CRC3RC4时,RC2和RC4可以一起形成额外的键,例如RC1和RC3取代的原子之间存在双键。