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438 条记录 (耗时 0.112 秒)

    Pyrrolopyridineamino derivatives as MPS1 inhibitors
    44.
    发明授权
    Pyrrolopyridineamino derivatives as MPS1 inhibitors 有权
    吡咯并吡啶氨基衍生物作为MPS1抑制剂

    公开(公告)号：US09371319B2

    公开(公告)日：2016-06-21

    申请号：US14004515

    申请日：2012-03-14

    申请人： Vassilios Bavetsias ,  Butrus Atrash ,  Sebastien Gaston Andre Naud ,  Peter William Sheldrake ,  Julian Blagg

    发明人： Vassilios Bavetsias ,  Butrus Atrash ,  Sebastien Gaston Andre Naud ,  Peter William Sheldrake ,  Julian Blagg

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04

    摘要： The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as “PPA derivatives”), particularly 1H-pyrrolo[3,2-c]pyridine-6-amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them. Formula (I)

    摘要翻译： 本发明涉及某些吡咯并吡啶氨基衍生物（以下称为“PPA衍生物”），特别是1H-吡咯并[3,2-c]吡啶-6-氨基衍生物用于抑制单轴1的主轴检查点功能 Mps1 - 也称为TTK）激酶直接或间接通过与Mps激酶本身的相互作用。 特别地，本发明涉及用作治疗和/或预防增殖性疾病如癌症的治疗剂的PPA衍生物。 本发明还涉及制备PPA衍生物的方法和包含它们的药物组合物。 式（I）

    ORTHO-CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E.G., PURINES) AS PROTEIN KINASES INHIBITORS
    49.
    发明申请
    ORTHO-CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E.G., PURINES) AS PROTEIN KINASES INHIBITORS 有权
    作为蛋白激酶抑制剂的ORTHO凝聚的吡啶和吡嗪衍生物（E.G.，PURINES）

    公开(公告)号：US20140303177A1

    公开(公告)日：2014-10-09

    申请号：US14310475

    申请日：2014-06-20

    申请人： ASTEX THERAPEUTICS LIMITED ,  THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL ,  CANCER RESEARCH TECHNOLOGY LIMITED

    发明人： Valerio BERDINI ,  Robert George BOYLE ,  Gordon SAXTY ,  David Winter WALKER ,  Steven John WOODHEAD ,  Paul Graham WYATT ,  Alastair DONALD ,  John CALDWELL ,  Ian COLLINS ,  Tatiana Faria DA FONSECA

    IPC分类号： C07D471/04 ,  A61K31/52 ,  A61K31/4545 ,  C07D487/04 ,  A61K31/519 ,  C07D473/34 ,  A61K31/522

    CPC分类号： C07D471/04 ,  A61K31/4545 ,  A61K31/519 ,  A61K31/52 ,  A61K31/522 ,  C07D473/34 ,  C07D487/04

    摘要： The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N═C(R6), (R7)C═N, (R8)N—C(O), (R8)2C—C(O), N═N or (R7)C═C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the G group; and provided that when E is aryl or heteroaryl, then Q2 is other than a bond; G is hydrogen, NR2R3, OH or SH provided that when E is aryl or heteroaryl and Q2 is a bond, then G is hydrogen; R1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R is hydrogen and G is NR2R3, then Q is a bond; and R2, R3, R4, R6 and R8 are as defined in the claims.

    摘要翻译： 本发明提供用作蛋白激酶B抑制剂的化合物，该化合物为式（I）化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中T为N或CR 5; J1-J2是N = C（R6），（R7）C = N，（R8）N-C（O），（R8）2C-C（O），N = N或（R7）C = C ）; E是5或6个环成员的单环碳环或杂环基，杂环基含有至多3个选自O，N和S的杂原子; Q1是键或饱和的C 1-3烃连接基团，连接基团中的一个碳原子任选被氧或氮原子代替，或者相邻的一对碳原子可被CONRq或NRqCO代替，其中Rq 是氢或甲基，或Rq是与R或Q1的碳原子连接的C 1-4亚烷基链，以形成环状部分; 并且其中所述连接基团Q1的碳原子可任选地具有一个或多个选自氟和羟基的取代基; Q2是含有1至3个碳原子的键或饱和烃连接基团，其中连接基团中的一个碳原子可任选被氧或氮原子取代; 并且其中所述连接基团的碳原子可以任选地具有一个或多个选自氟和羟基的取代基，条件是当存在的羟基不相对于G基团位于碳原子a时; 并且条件是当E是芳基或杂芳基时，则Q2不是键; G为氢，NR2R3，OH或SH，条件是当E为芳基或杂芳基且Q2为键时，则G为氢; R 1是氢或芳基或杂芳基，条件是当R是氢且G是NR 2 R 3时，则Q是一个键; 并且R 2，R 3，R 4，R 6和R 8如权利要求中所定义。

    Purine derivatives
    50.
    发明授权
    Purine derivatives 有权
    嘌呤衍生物

    公开(公告)号：US08846696B2

    公开(公告)日：2014-09-30

    申请号：US12489663

    申请日：2009-06-23

    申请人： Peter Martin Fischer ,  Michael Jarman ,  Edward McDonald ,  Bernard Nutley ,  Florence Raynaud ,  Stuart Wilson ,  Paul Workman

    发明人： Peter Martin Fischer ,  Michael Jarman ,  Edward McDonald ,  Bernard Nutley ,  Florence Raynaud ,  Stuart Wilson ,  Paul Workman

    IPC分类号： A61K31/52 ,  C07D473/16

    CPC分类号： C07D473/16 ,  A61K31/52 ,  Y02A50/411

    摘要： The present invention relates to compounds of formula 1 or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is methyl, ethyl or isopropyl, and the other is H; R3 and R4 are each independently H, branched or unbranched C1-C6 alkyl, or aryl, and wherein at least one of R3 and R4 is other than H; R5 is a branched or unbranched C1-C5 alkyl group or a C1-C6 cycloalkyl group, each of which may be optionally substituted with one or more OH groups; R6, R7, R8 and R9 are each independently H, halogen, NO2, OH, OMe, CN, NH2, COOH, CONH2, or SO2NH2. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.

    摘要翻译： 本发明涉及式1化合物或其药学上可接受的盐，其中R 1和R 2之一是甲基，乙基或异丙基，另一个是H; R 3和R 4各自独立地为H，支链或非支链的C 1 -C 6烷基或芳基，并且其中R 3和R 4中的至少一个不是H; R5是支链或非支链C 1 -C 5烷基或C 1 -C 6环烷基，其各自可以任选被一个或多个OH基取代; R6，R7，R8和R9各自独立地为H，卤素，NO2，OH，OMe，CN，NH2，COOH，CONH2或SO2NH2。 本发明的另一方面涉及包含式1化合物的药物组合物，以及所述化合物在治疗增殖性疾病，病毒性疾病，中风，脱发，中枢神经系统疾病，神经变性疾病或糖尿病中的用途。