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    Pyrido-, Pyrazo- and Pyrimido-Pyrimidine Derivatives as mTOR Inhibitors
    13.
    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.

    PHTHALAZINONE DERIVATIVES
    15.
    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。

    COMPOUNDS
    20.
    发明申请
    COMPOUNDS 审中-公开
    化合物

    公开(公告)号：US20100130473A1

    公开(公告)日：2010-05-27

    申请号：US11817134

    申请日：2006-02-24

    申请人： Marc Geoffrey Hummersone ,  Sylvie Gomez ,  Keith Allan Menear ,  Xiao-Ling Fan Cockcroft ,  Graeme Cameron Murray Smith

    发明人： Marc Geoffrey Hummersone ,  Sylvie Gomez ,  Keith Allan Menear ,  Xiao-Ling Fan Cockcroft ,  Graeme Cameron Murray Smith

    IPC分类号： A61K31/5377 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  A61P35/00 ,  A61K31/53 ,  A61K31/551 ,  A61K31/553 ,  A61K31/519

    CPC分类号： C07D251/70 ,  C07D239/48 ,  C07D239/50 ,  C07D239/94 ,  C07D295/135 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D413/12 ,  C07D417/04 ,  C07D471/04

    摘要： Compounds of formula (I): A-B—C and isomers, salts, solvates, chemically protected forms, and prodrugs thereof wherein: B is selected from the group consisting of formula (i) where RN is H or Me; or B is a divalent C5 heterocyclic residue containing one or two ring heteroatoms; A is formula (ii) RA3 and RA5 are independently selected from halo, ORO and RAC, where RO is H or Me, and RAC is H or C1-4 alkyl; XA is selected from N and CRA4, where RA4 is selected from H, ORO, CH2OH, CO2H, NHSO2Me and NHCOMe; RA2 and RA6 are independently selected from H, halo and ORO; or RA3 and RA4 together with the carbon atoms to which they are attached, or RA2 and RA3 together with the carbon atoms to which they are attached, may form a C5-6 heterocylic or heteroaromatic ring, containing at least one nitrogen ring atom; where if X is not N, 1, 2, or 3 of RA2 to RA6 are not H; C is formula (iii) where X is selected from N and CH, Y is selected from N and CH, and Z is selected from N and CRC6; RC3 is selected from H, halo and an optionally substituted N-containing C5-7 heterocyclic group; RC5 is a group selected from formula (iv) which group may be selected by one or two C1-4 alkyl groups or a carboxy group; RC6 is H; or, when X and Y are N, RC5 and RC6 (when Z is CRC6) together with the carbon atoms to which they are attached may form a fused C6 aromatic ring selected from the group consisting of formula (v).

    摘要翻译： 式（I）化合物：A-B-C及其异构体，盐，溶剂合物，化学保护形式及其前药。其中：B选自式（ⅰ），其中RN为H或Me; 或B是含有一个或两个环杂原子的二价C5杂环残基; A是式（ⅱ）RA 3和RA 5独立地选自卤素，ORO和RAC，其中RO是H或Me，RAC是H或C 1-4烷基; XA选自N和CRA4，其中RA4选自H，ORO，CH2OH，CO2H，NHSO2Me和NHCOMe; RA2和RA6独立地选自H，卤素和ORO; 或RA3和RA4与它们所连接的碳原子一起，或RA2和RA3与它们所连接的碳原子一起可以形成含有至少一个氮环原子的C 5-6杂环或杂芳环; 其中如果X不是RA，RA6的N，1,2或3不是H; C是式（ⅲ），其中X选自N和CH，Y选自N和CH，Z选自N和CRC 6; RC3选自H，卤素和任选取代的含N的C 5-7杂环基; RC5是选自式（iv）的基团，该基团可以被一个或两个C 1-4烷基或羧基选择; RC6为H; 或者当X和Y为N时，RC5和RC6（当Z为CRC6时）与它们所连接的碳原子一起形成选自式（v）的稠合C 6芳环。