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    • 10. 发明授权
    • Phthalazinone derivatives
    • 酞嗪衍生物
    • US07902193B2
    • 2011-03-08
    • US12271308
    • 2008-11-14
    • Muhammad Hashim JavaidKeith Allan MenearSylvie GomezMarc Geoffrey HummersoneNiall Morrison Barr MartinGraeme Cameron Murray SmithXiao-Ling Fan CockcroftFrank Kerrigan
    • Muhammad Hashim JavaidKeith Allan MenearSylvie GomezMarc Geoffrey HummersoneNiall Morrison Barr MartinGraeme Cameron Murray SmithXiao-Ling Fan CockcroftFrank Kerrigan
    • C07D237/32A61K31/502A61P35/00
    • C07D403/10C07D403/14C07D411/14C07D413/14C07D487/04
    • A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; D is selected from: (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 (ii) where Q is O or S; RD is: 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, such that there is a double bond between the atoms substituted by RC1 and RC3.
    • 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:(i)其中Y1选自CH和N,Y2选自CH和N,Y3选自CH,CF和N; 和(ii)其中Q为O或S; RD是:其中RN1选自H和任选取代的C 1-10烷基; X选自单键NRN2,CRC3RC4和C = O; RN2选自H和任选取代的C 1-10烷基; RC3和RC4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。 RC1和RC2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; RC1和RC2与它们所连接的碳原子一起可以形成任选取代的螺 - 稠合的C 5-7碳环或杂环; 当X是单键时,RN1和RC2可以与它们所结合的N和C原子一起形成任选被取代的C5-7杂环; 并且当X是CRC3RC4时,RC2和RC4可以一起形成附加键,使得在被RC1和RC3取代的原子之间存在双键。