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    Phthalazinone derivatives
    13.
    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
    15.
    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。

    Pyrido-, Pyrazo- and Pyrimido-Pyrimidine Derivatives as mTOR Inhibitors
    16.
    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
    17.
    发明授权
    Phthalazinone derivatives 有权
    酞嗪衍生物

    公开(公告)号：US07750006B2

    公开(公告)日：2010-07-06

    申请号：US11352178

    申请日：2006-02-10

    申请人： Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  Charles Richard White ,  Roger Frank Newton ,  Diane Gillian Douglas ,  Penny Jane Eversley ,  Julia Vile

    发明人： Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  Charles Richard White ,  Roger Frank Newton ,  Diane Gillian Douglas ,  Penny Jane Eversley ,  Julia Vile

    IPC分类号： A01N43/58 ,  A61K31/50 ,  C07D237/26

    CPC分类号： C07D401/12 ,  A61K31/50 ,  A61K31/502 ,  C07D237/32 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： A method of treatment of a disease of the human or animal body mediated by PARP comprising administering to such a subject a therapeutically effective amount of a compound of formula: or an isomer, salt, solvate, chemically protected form, and prodrug thereof, wherein: A and B together represent an optionally substituted, fused aromatic ring; RC is represented by -L-RL, where L is of formula: —(CH2)n1-Qn2-(CH2)n3— wherein n1, n2 and n3 are each selected from 0, 1, 2 and 3, the sum of n1, n2 and n3 is 1, 2 or 3 and Q is selected from O, S, NH, C(═O) or —CR1R2—, where R1 and R2 are independently selected from hydrogen, halogen or optionally substituted C1-7 alkyl, or may together with the carbon atom to which they are attached form a C3-7 cyclic alkyl group, which may be saturated (a C3-7 cycloalkyl group) or unsaturated (a C3-7 cycloalkenyl group), or one of R1 and R2 may be attached to an atom in RL to form an unsaturated C3-7 cycloalkenyl group which comprises the carbon atoms to which R1 and R2 are attached in Q, —(CH2)n3— (if present) and part of RL; and RL is optionally substituted C5-20 aryl; and RN is selected from hydrogen, optionally substituted C1-7 alkyl, C3-20 heterocyclyl, and C5-20 aryl, hydroxy, ether, nitro, amino, amido, thiol, thioether, sulfoxide and sulfone.

    摘要翻译： 一种治疗由PARP介导的人体或动物体的疾病的方法，包括向所述受试者施用治疗有效量的式：或其异构体，盐，溶剂化物，化学保护形式及其前药的化合物，其中： A和B一起表示任选取代的稠合芳环; RC由-L-RL表示，其中L为下式： - （CH2）n1-Qn2-（CH2）n3-，其中n1，n2和n3各自选自0,1,2和3，n1 ，n2和n3是1,2或3，Q选自O，S，NH，C（= O）或-CR1R2-，其中R1和R2独立地选自氢，卤素或任选取代的C 1-7烷基， 或者可以与它们所连接的碳原子一起形成可以是饱和的（C 3-7环烷基）或不饱和的（C 3-7环烯基）或R 1和R 2中的一个的C 3-7环烷基 可以连接到RL中的原子以形成不饱和的C 3-7环烯基，其包含在Q， - （CH 2）n 3-（如果存在）和部分RL中R 1和R 2连接的碳原子; 并且RL是任选取代的C 5-20芳基; 并且RN选自氢，任选取代的C 1-7烷基，C 3-20杂环基和C 5-20芳基，羟基，醚，硝基，氨基，酰胺基，硫醇，硫醚，亚砜和砜。

    PHTHALAZINONE DERIVATIVES
    19.
    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。