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    • 9. 发明授权
      US07902193B2 Phthalazinone derivatives 失效
    • Phthalazinone derivatives
    • 酞嗪衍生物
    • US07902193B2
    • 2011-03-08
    • US12271308
    • 2008-11-14
    • Muhammad Hashim Javaid , Keith Allan Menear , Sylvie Gomez , Marc Geoffrey Hummersone , Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Xiao-Ling Fan Cockcroft , Frank Kerrigan
    • Muhammad Hashim Javaid , Keith Allan Menear , Sylvie Gomez , Marc Geoffrey Hummersone , Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Xiao-Ling Fan Cockcroft , Frank Kerrigan
    • C07D237/32 , A61K31/502 , A61P35/00
    • C07D403/10 , C07D403/14 , C07D411/14 , C07D413/14 , C07D487/04
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 10. 发明申请
      US20080194546A1 Pyrido-, Pyrazo- and Pyrimido-Pyrimidine Derivatives as mTOR Inhibitors 审中-公开
    • Pyrido-, Pyrazo- and Pyrimido-Pyrimidine Derivatives as mTOR Inhibitors
    • US20080194546A1
    • 2008-08-14
    • US11842927
    • 2007-08-21
    • Marc Geoffrey Hummersone , Gomez Sylvie , Keith Allan Menear , Graeme Cameron Murray Smith , Karine Malagu , Heather Mary Ellen Duggan , Niall Morrison Barr Martin , Frederic Georges Marie Leroux , Gesine Johanna Hermann , Xiao-Ling Fan Cockcroft
    • Marc Geoffrey Hummersone , Gomez Sylvie , Keith Allan Menear , Graeme Cameron Murray Smith , Karine Malagu , Heather Mary Ellen Duggan , Niall Morrison Barr Martin , Frederic Georges Marie Leroux , Gesine Johanna Hermann , Xiao-Ling Fan Cockcroft
    • A61K31/5377 , C07D413/14 , A61K31/5513 , A61P35/00 , C07D243/14
    • C07D475/08 , C07D475/06 , C07D487/04
    • There is provided a compound of formula I: wherein: one or two of X5, X6 and X8 is N, and the others are CH; R7 is selected from halo, ORO1, SRS1, NRN1RN2, NRN7aC(═O)RC1, NRN7bSO2RS2a, an optionally substituted C5-20 heteroaryl group, or an optionally substituted C5-20 aryl group, where RO1 and RS1 are selected from H, an optionally substituted C5-20 aryl group, an optionally substituted C5-20 heteroaryl group, or an optionally substituted C1-7 alkyl group; RN1 and RN2 are independently selected from H, an optionally substituted C1-7 alkyl group, an optionally substituted C5-20 heteroaryl group, an optionally substituted C5-20 aryl group or RN1 and RN2 together with the nitrogen to which they are bound form a heterocyclic ring containing between 3 and 8 ring atoms; RC1 is selected from H, an optionally substituted C5-20 aryl group, an optionally substituted C5-20 heteroaryl group, an optionally substituted C1-7 alkyl group or NRN8RN9, where RN8 and RN9 are independently selected from H, an optionally substituted C1-7 alkyl group, an optionally substituted C5-20 heteroaryl group, an optionally substituted C5-20 aryl group or RN8 and RN9 together with the nitrogen to which they are bound form a heterocyclic ring containing between 3 and 8 ring atoms; RS2a is selected from H, an optionally substituted C5-20 aryl group, an optionally substituted C5-20 heteroaryl group, or an optionally substituted C1-7 alkyl group; RN7a and RN7b are selected from H and a C1-4 alkyl group; RN3 and RN4, together with the nitrogen to which they are bound, form a heterocyclic ring containing between 3 and 8 ring atoms; R2 is selected from H, halo, ORO2, SRS2b, NRN5RN6, an optionally substituted C5-20 heteroaryl group, and an optionally substituted C5-20 aryl group, wherein RO2 and RS2b are selected from H, an optionally substituted C5-20 aryl group, an optionally substituted C5-20 heteroaryl group, or an optionally substituted C1-7 alkyl group; RN5 and RN6 are independently selected from H, an optionally substituted C1-7 alkyl group, an optionally substituted C5-20 heteroaryl group, and an optionally substituted C5-20 aryl group, or RN5 and RN6 together with the nitrogen to which they are bound form a heterocyclic ring containing between 3 and 8 ring atoms, or a pharmaceutically acceptable salt thereof, with the proviso that when R2 is unsubstituted morpholino. RN3 and RN4 together with the nitrogen atom to which they are attached form an unsubstituted morpholino and R7 is unsubstituted phenyl, and X5 is CH, then X6 is not N and X8 is not CH, or X6 is not CH and X8 is not N, and when R2 is unsubstituted piperidinyl, RN3 and RN4 together with the nitrogen atom to which they are attached form an unsubstituted piperidinyl and R7 is unsubstituted phenyl, and X5 is CH, then X6 is not CH and X is not N. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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