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    Pharmaceutical Compounds
    7.
    发明申请
    Pharmaceutical Compounds 失效
    药物化合物

    公开(公告)号：US20100004232A1

    公开(公告)日：2010-01-07

    申请号：US12159054

    申请日：2006-12-29

    申请人： Valerio Berdini ,  Jayne Elizabeth Curry ,  Neil James Gallagher ,  Adrian Liam Gill ,  John Francis Lyons

    发明人： Valerio Berdini ,  Jayne Elizabeth Curry ,  Neil James Gallagher ,  Adrian Liam Gill ,  John Francis Lyons

    IPC分类号： A61K31/541 ,  A61K31/5377

    CPC分类号： C07D403/04 ,  A61K31/4155 ,  A61K31/4184 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/04 ,  C07D491/056 ,  C07D513/04

    摘要： The use of a compound for the manufacture of a medicament for the prophylaxis or treatment of: A. a disease state or condition mediated by a kinase which is BCR-abl, VEGFR, PDGFR, EGFR, Flt3, JAK (e.g. JAK2 or JAK3), C-abl, PDK1, Chk (e.g. Cbk1 or Chk2), FGFR (e.g. FGFR3), Ret, Eph (e.g. EphB2 or EphB4), or Src (e.g. cSrc); or B. a cancer in which the cancer cells thereof contain a drug resistant kinase mutation which is: (a) a threonine gatekeeper mutation; or (b) a drug-resistant gatekeeper mutation; or (c) an imatinib resistant mutation; or (d) a nilotinib resistant mutation; or (e) a dasatinib resistant mutation; or (f) a T670I mutation in KIT; or (g) a T674I mutation in PDGFR; or (h) T790M mutation in EGFR; or (i) a T315I mutation in abl; or C. a cancer which expresses a mutated molecular target which is a mutated form of BCRabl, c-kit, PDGF, EGF receptor or ErbB2; or D. a disease mediated by a kinase containing a mutation in a region of the protein that binds to or interacts with other cancer agents but does not bind to or interact with the compounds of formula (I) or (I′), for example a mutated kinase selected from c-abl, c-kit, PDGFR including PDGFR-beta and PDGFR-alpha, and ErbB family members such as EGFR (ErbB1), HER2 (ErbB2), ErbB3, and ErbB4, members of the Ephrin receptor family including EphA1, EphA2, EphA3, EphA4, EphA5, EphA8, EphA10, EphB1, EphB2, EphB3, EphB5, EphB6, c-Src and kinases of the JAK family such as TYK2; wherein the compound is a compound of the formula (I or I′): or a salt, solvate, tautomer or N-oxide thereof wherein R0′, R1, R1′, R2′, R3′, R4′, A′, X′, E, A and M are as defined in the claims.

    摘要翻译： 化合物用于制备用于预防或治疗以下药物的用途：A.由BCR-abl，VEGFR，PDGFR，EGFR，Flt3，JAK（例如JAK2或JAK3）的激酶介导的疾病状态或病症， ，C-abl，PDK1，Chk（例如Cbk1或Chk2），FGFR（例如FGFR3），Ret，Eph（例如EphB2或EphB4）或Src（例如cSrc）; 或B.一种其癌细胞含有耐药性激酶突变的癌症，其为：（a）苏氨酸关守突变; 或（b）耐药性守门人突变; 或（c）伊马替尼耐药突变; 或（d）尼洛替尼耐药突变; 或（e）达沙替尼抗性突变; 或（f）KIT中的T670I突变; 或（g）PDGFR中的T674I突变; 或（h）EGFR中的T790M突变; 或（i）abl中的T315I突变; 或C.表达突变形式的BCRab1，c-kit，PDGF，EGF受体或ErbB2的突变分子靶的癌症; 或D.由包含与其它癌症药物结合或与其它癌症药剂相互作用而不与式（I）或（I'）化合物结合或相互作用的蛋白质区域中的突变的激酶介导的疾病，例如 选自c-abl，c-kit，PDGFR（包括PDGFR-β和PDGFR-α）的突变激酶和ErbB家族成员如EGFR（ErbB1），HER2（ErbB2），ErbB3和ErbB4，Ephrin受体家族成员 包括EK1A1，EphA2，EphA3，EphA4，EphA5，EphA8，EphA10，EphB1，EphB2，EphB3，EphB5，EphB6，c-Src和JAK家族的激酶如TYK2; 其中所述化合物是式（I或I'）的化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中R 0'，R 1，R 1'，R 2'，R 3'，R 4'，A'，X '，E，A和M如权利要求中所定义。

    3,4-Disubstituted Pyrazoles as Cyclin Dependent Kinases (Cdk) or Aurora Kinase or Glycogen Synthase 3 (Gsk-3) Inhibitors
    9.
    发明申请
    3,4-Disubstituted Pyrazoles as Cyclin Dependent Kinases (Cdk) or Aurora Kinase or Glycogen Synthase 3 (Gsk-3) Inhibitors 审中-公开
    作为细胞周期蛋白依赖性激酶（Cdk）或极光激酶或糖原合酶3（Gsk-3）抑制剂的3,4-二取代吡唑类

    公开(公告)号：US20080004270A1

    公开(公告)日：2008-01-03

    申请号：US11571713

    申请日：2005-07-05

    申请人： Adrian Gill ,  Maria Carr ,  Michael O'Brien ,  Paul Wyatt ,  Valerio Berdini

    发明人： Adrian Gill ,  Maria Carr ,  Michael O'Brien ,  Paul Wyatt ,  Valerio Berdini

    IPC分类号： A61K31/5377 ,  A61K31/4188 ,  A61P25/28 ,  A61P35/00 ,  C07D235/02 ,  C07D471/02 ,  C07D265/34 ,  A61P37/00 ,  A61P31/12 ,  A61K31/47

    CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D495/04

    摘要： The invention provides compounds of the formula (I); or salts or solvates or N-oxides thereof; wherein: Rq is selected from groups (a), (b) and (c); the asterisk denoting the point of attachment to the pyrazole ring; X is N or CR5; X″ is NR4; O, S or S(O); A is a bond or —(CH2)m—(B)n—; B is C═O, NRg(C═O) or O(C═O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R0 is hydrogen or, together with NRg when present, forms a group —(CH2)p— wherein p is 2 to 4; and R1 to R6b are as defined in the description. Compounds of the formula (I) have activity as inhibitors of CDK, aurora and GSK-3 kinases are useful in treating or preventing diseases such as cancers that are mediated by the said kinases.

    摘要翻译： 本发明提供式（I）化合物; 或其盐或溶剂合物或N-氧化物; 其中：R q选自（a），（b）和（c）组; 星号表示与吡唑环的连接点; X是N或CR 5; X“是NR 4; O，S或S（O）; A是键或 - （CH 2）m - （B）n - B为CO，NR（CO）或O（CO），其中R为氢或任选被羟基取代的C 1-4烷基烃基 或C 1-4烷氧基; m为0,1或2; n为0或1; 当存在时，R 0是氢或与NR a一起形成基团 - （CH 2 CH 2）n - - 其中p为2至4; 和R 1至R 6b如说明书中所定义。 式（I）化合物具有作为CDK抑制剂的活性，极光和GSK-3激酶可用于治疗或预防诸如由所述激酶介导的癌症的疾病。