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    Phthalazinone derivatives
    4.
    发明授权
    Phthalazinone derivatives 失效
    酞嗪衍生物

    公开(公告)号：US07470688B2

    公开(公告)日：2008-12-30

    申请号：US11550004

    申请日：2006-10-17

    申请人： 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

    发明人： 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

    IPC分类号： A61K31/502 ,  A61K31/5355 ,  A61K31/53 ,  C07D487/00 ,  C07D413/10 ,  C07D253/04 ,  C07D253/06 ,  C07D251/10 ,  A61P9/10

    CPC分类号： C07D403/10 ,  C07D403/14 ,  C07D411/14 ,  C07D413/14 ,  C07D487/04

    摘要： 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 heterocyclic 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.

    摘要翻译： 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原子一起形成任选取代的C 5-7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。

    Phthalazinone derivatives
    5.
    发明授权
    Phthalazinone derivatives 失效
    酞嗪衍生物

    公开(公告)号：US07902193B2

    公开(公告)日：2011-03-08

    申请号：US12271308

    申请日：2008-11-14

    申请人： 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

    发明人： 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

    IPC分类号： C07D237/32 ,  A61K31/502 ,  A61P35/00

    CPC分类号： C07D403/10 ,  C07D403/14 ,  C07D411/14 ,  C07D413/14 ,  C07D487/04

    摘要： 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.

    摘要翻译： 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。

    PHTHALAZINONE DERIVATIVES
    6.
    发明申请
    PHTHALAZINONE DERIVATIVES 失效
    邻苯二酚衍生物

    公开(公告)号：US20090069303A1

    公开(公告)日：2009-03-12

    申请号：US12271308

    申请日：2008-11-14

    申请人： 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

    发明人： 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

    IPC分类号： A61K31/551 ,  C07D237/30 ,  A61K31/502 ,  C07D253/06 ,  A61K31/53 ,  A61P9/00 ,  A61P29/00 ,  A61P3/10 ,  A61P25/00 ,  A61P35/00 ,  C07D413/14 ,  A61K31/5377 ,  C07D243/08

    CPC分类号： C07D403/10 ,  C07D403/14 ,  C07D411/14 ,  C07D413/14 ,  C07D487/04

    摘要： 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.

    摘要翻译： 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。

    2 -OXYHETEROARYLAMIDE DERIVATIVES AS PARP INHIBITORS
    10.
    发明申请
    2 -OXYHETEROARYLAMIDE DERIVATIVES AS PARP INHIBITORS 审中-公开
    作为PARP抑制剂的2-异烟酰胺衍生物

    公开(公告)号：US20090281086A1

    公开(公告)日：2009-11-12

    申请号：US12304835

    申请日：2007-06-15

    申请人： Muhammad Hashim Javaid ,  Xiao-Ling Fan Cockcroft ,  Keith Allan Menear ,  Niall Morrison Barr Martin

    发明人： Muhammad Hashim Javaid ,  Xiao-Ling Fan Cockcroft ,  Keith Allan Menear ,  Niall Morrison Barr Martin

    IPC分类号： A61K31/496 ,  C07D409/12 ,  C07D409/14 ,  A61K31/498 ,  A61K31/551 ,  A61P7/00 ,  A61P29/00 ,  A61P9/00 ,  A61P25/00 ,  A61P35/00

    CPC分类号： C07D333/38 ,  C07D409/12

    摘要： A compound of the formula (I): and pharmaceutically acceptable salts thereof, wherein: HetA is a C5 arylene group, wherein the two substituent groups are on adjacent ring atoms, and where the group is further optionally substituted by one halo, amino or C1-7 alkoxy group; Y is —CRC1RC2—(CH2)m—, where m is 0 or 1, RC1 is selected from H, CH3 and CF3, and RC2 is selected from H and CH3, or RC1 and RC2 together with the carbon atom to which they are attached form the 1,1-cyclopropylene group formula (A): RN1 and RN2 are independently selected from H and R, where R is optionally substituted C1-10 alkyl, C3-20 heterocyclyl and C5-20 aryl; or RN1 and RN2, together with the nitrogen atom to which they are attached form an optionally substituted 5-7 membered, nitrogen containing, heterocylic ring; HetB is selected from: (i), where Y1 and Y3 are independently selected from CH and N, Y2 is selected from CX and N and X is H, Cl or F; and (ii), (aa), (bb) Q is O or S.

    摘要翻译： 式（I）的化合物及其药学上可接受的盐，其中：HetA是C5亚芳基，其中两个取代基在相邻的环原子上，并且其中该基团进一步任选地被一个卤素，氨基或C 1 -7烷氧基 Y是-CRC1RC2-（CH2）m-，其中m是0或1，RC1选自H，CH3和CF3，RC2选自H和CH3，或RC1和RC2与它们所在的碳原子一起 连接形成1,1-亚环丙基基团（A）：RN1和RN2独立地选自H和R，其中R是任选取代的C 1-10烷基，C 3-20杂环基和C 5-20芳基; 或RN1和RN2与它们所连接的氮原子一起形成任选取代的5-7元含氮杂环; HetB选自：（i）其中Y1和Y3独立地选自CH和N，Y2选自CX和N，X是H，Cl或F; 和（ii），（aa），（bb）Q是O或S.