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44 条记录 (耗时 0.057 秒)

    PHTHALAZINONE DERIVATIVES
    12.
    发明申请
    PHTHALAZINONE DERIVATIVES 审中-公开
    邻苯二酚衍生物

    公开(公告)号：US20090023727A1

    公开(公告)日：2009-01-22

    申请号：US12167567

    申请日：2008-07-03

    申请人： Muhammad Hashim Javaid ,  Keith Allan Menear ,  Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  David Alan Rudge ,  Craig Anthony Roberts

    发明人： Muhammad Hashim Javaid ,  Keith Allan Menear ,  Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  David Alan Rudge ,  Craig Anthony Roberts

    IPC分类号： A61K31/5377 ,  A61K31/502 ,  C07D403/08 ,  A61K31/53 ,  A61P35/00 ,  C07D403/14 ,  C07D413/14

    CPC分类号： C07D237/32 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12

    摘要： 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.

    摘要翻译： 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。

    Pyrido-, Pyrazo- and Pyrimido-Pyrimidine Derivatives as mTOR Inhibitors
    20.
    发明申请
    Pyrido-, Pyrazo- and Pyrimido-Pyrimidine Derivatives as mTOR Inhibitors 审中-公开

    公开(公告)号：US20080194546A1

    公开(公告)日：2008-08-14

    申请号：US11842927

    申请日：2007-08-21

    申请人： 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

    发明人： 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

    IPC分类号： A61K31/5377 ,  C07D413/14 ,  A61K31/5513 ,  A61P35/00 ,  C07D243/14

    CPC分类号： C07D475/08 ,  C07D475/06 ,  C07D487/04

    摘要： 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.