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    • 1. 发明申请
    • PHTHALAZINONE DERIVATIVES
    • 邻苯二酚衍生物
    • US20090023727A1
    • 2009-01-22
    • US12167567
    • 2008-07-03
    • Muhammad Hashim JavaidKeith Allan MenearNiall Morrison Barr MartinGraeme Cameron Murray SmithDavid Alan RudgeCraig Anthony Roberts
    • Muhammad Hashim JavaidKeith Allan MenearNiall Morrison Barr MartinGraeme Cameron Murray SmithDavid Alan RudgeCraig Anthony Roberts
    • A61K31/5377A61K31/502C07D403/08A61K31/53A61P35/00C07D403/14C07D413/14
    • C07D237/32C07D401/10C07D401/12C07D401/14C07D403/12C07D405/12
    • A compound of the formula (I): wherein: R represents one or more optional substituents on the fused cyclohexene ring; X can be NRX or CRXRY; if X=NRX then n is 1 or 2 and if X=CRXRY then n is 1; if X=NRX, then RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, optionally substituted C5-20 aryl, optionally substituted C3-20 heterocyclyl, optionally substituted amido, optionally substituted thioamido, optionally substituted ester, optionally substituted acyl, and optionally substituted sulfonyl groups; if X=CRXRY then RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, optionally substituted C5-20 aryl, optionally substituted C3-20 heterocyclyl, optionally substituted amido, optionally substituted thioamido, optionally substituted sulfonamino, optionally substituted ether, optionally substituted ester, optionally substituted acyl, optionally substituted acylamido, and optionally substituted sulfonyl groups and RY is selected from H, hydroxy, optionally substituted amino, or RX and RY may together form an optionally substituted spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.
    • 式(I)的化合物:其中:R表示稠合环己烯环上的一个或多个任选的取代基; X可以是NRX或CRXRY; 如果X = NRX,则n为1或2,如果X = CRXRY,则n为1; 如果X = NRX,则RX选自H,任选取代的C 1-20烷基,任选取代的C 5-20芳基,任选取代的C 3-20杂环基,任选取代的酰胺基,任选取代的硫代酰氨基,任选取代的酯,任选地 取代的酰基和任选取代的磺酰基; 如果X = CRXRY,则RX选自H,任选取代的C 1-20烷基,任选取代的C 5-20芳基,任选取代的C 3-20杂环基,任选取代的酰胺基,任选取代的硫代酰氨基,任选取代的磺酰氨基,任选取代的 醚,任选取代的酯,任选取代的酰基,任选取代的酰基酰氨基和任选取代的磺酰基,RY选自H,羟基,任选取代的氨基,或RX和RY可以一起形成任选取代的螺C 3-7环烷基或杂环基 组; RC1和RC2均为氢,或当X为CRXRY时,RC1,RC2,RX和RY与它们所连接的碳原子一起形成任选取代的稠合芳环; 并且R 1选自H和卤素。
    • 6. 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。