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    Pharmaceutical Compounds
    21.
    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。

    PHARMACEUTICAL COMBINATIONS
    23.
    发明申请
    PHARMACEUTICAL COMBINATIONS 有权
    药物组合

    公开(公告)号：US20100179145A1

    公开(公告)日：2010-07-15

    申请号：US12445180

    申请日：2007-10-12

    申请人： Neil James Gallagher ,  John Francis Lyons ,  Neil Thomas Thompson ,  Stephen Murray Yule ,  Christopher William Murray

    发明人： Neil James Gallagher ,  John Francis Lyons ,  Neil Thomas Thompson ,  Stephen Murray Yule ,  Christopher William Murray

    IPC分类号： A61K31/4035 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/437 ,  A61K31/454 ,  A61K31/415 ,  C07D471/04 ,  C07D209/44 ,  A61P31/12 ,  A61P35/00

    CPC分类号： A61K31/403 ,  A61K31/4035 ,  A61K45/06 ,  A61K2300/00

    摘要： The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The combinations have activity as Hsp90 and/or glycogen synthase kinase-3 and/or cyclin dependent kinase inhibitors.

    摘要翻译： 本发明提供包含（或基本上由）一种或多种辅助化合物和式（I）化合物或其盐，互变异构体，溶剂合物和N-氧化物的组合; 其中R1是羟基或氢; R2是羟基; 甲氧基或氢; 条件是R 1和R 2中的至少一个是羟基; R3选自氢; 卤素; 氰基; 任选取代的C 1-5烃基和任选取代的C 1-5烃氧基; R4选自氢; 其中n为0或1，R7为任选取代的无环C 1-5烃基或具有3至7个环成员的单环碳环或杂环基团 - （O）n -R 7基团; 卤素; 氰基; 羟基; 氨基; 和任选取代的单或二-C 1-5烃基 - 氨基; 或R 3和R 4一起形成5至7个环成员的单环碳环或杂环; 并且NR 5 R 6形成具有8至12个环成员的任选取代的双环杂环基，其中多达5个环成员是选自氧，氮和硫的杂原子。 这些组合具有作为Hsp90和/或糖原合酶激酶-3和/或细胞周期蛋白依赖性激酶抑制剂的活性。

    COMBINATIONS OF PYRAZOLE DERIVATIVES FOR THE INHIBITION OF CDKS AND GSK'S
    24.
    发明申请
    COMBINATIONS OF PYRAZOLE DERIVATIVES FOR THE INHIBITION OF CDKS AND GSK'S 审中-公开
    用于抑制CDKS和GSK'S的吡唑衍生物的组合

    公开(公告)号：US20100021420A1

    公开(公告)日：2010-01-28

    申请号：US12373827

    申请日：2007-07-13

    申请人： John Francis Lyons ,  Matthew Simon Squires ,  Neil Thomas Thompson ,  Neil James Gallagher

    发明人： John Francis Lyons ,  Matthew Simon Squires ,  Neil Thomas Thompson ,  Neil James Gallagher

    IPC分类号： A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K39/395 ,  A61K38/21 ,  A61K38/20 ,  A61K33/24

    CPC分类号： A61K31/454 ,  A61K45/06 ,  A61K2300/00

    摘要： A combination comprising (a) a compound of formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein X is R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C═O, NR9(C═O) or 0(C═O) wherein R9 is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1 to 3 carbon atoms; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or an optionally substituted C1-8 hydrocarbyl group wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy; or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C1-4 alkoxy; R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C1-4 alkoxy; and (b) a compound of formula (I′″) or salts, tautomers, solvates and N-oxides thereof: wherein R1 is 2,6-dichlorophenyl; R2a and R2b are both hydrogen; and R3 is a group: formula (A) where R4 is C1-4 alkyl.

    摘要翻译： 包含（a）式（O）化合物或其盐或互变异构体或其N-氧化物或溶剂合物的组合; 其中X为R 1 -A-NR 4 - 或5或6元碳环或杂环; A为键，SO 2，C-O，NR 9（C-O）或O（C-O），其中R 9为氢或任选被羟基或C 1-4烷氧基取代的C 1-4烃基; Y是1〜3个碳原子的键或亚烷基链; R1是氢; 具有3至12个环成员的碳环或杂环基; 或任选取代的C 1-8烃基，其中烃基中的1或2个碳原子可以任选地被选自O，S，NH，SO，SO 2的原子或基团取代; R2是氢; 卤素; C 1-4烷氧基; 或任选被卤素，羟基或C 1-4烷氧基取代的C 1-4烃基; R 3选自具有3至12个环成员的氢和碳环和杂环基; R4是氢或任选被卤素，羟基或C 1-4烷氧基取代的C 1-4烃基; 和（b）式（I“）的化合物或其盐，互变异构体，溶剂化物和N-氧化物：其中R1是2,6-二氯苯基; R2a和R2b都是氢; 并且R 3是下式：其中R 4是C 1-4烷基的式（A）。

    Pharmaceutical Compounds
    25.
    发明申请
    Pharmaceutical Compounds 审中-公开
    药物化合物

    公开(公告)号：US20090036435A1

    公开(公告)日：2009-02-05

    申请号：US11814461

    申请日：2006-01-20

    申请人： Jayne Elizabeth Curry ,  John Francis Lyons ,  Matthew Simon Squires ,  Neil Thomas Thompson ,  Kyla Merriom Thompson ,  Paul Graham Wyatt

    发明人： Jayne Elizabeth Curry ,  John Francis Lyons ,  Matthew Simon Squires ,  Neil Thomas Thompson ,  Kyla Merriom Thompson ,  Paul Graham Wyatt

    IPC分类号： A61K31/541 ,  A61K31/415 ,  A61K31/41 ,  A61K31/4439 ,  A61K31/4196 ,  A61K31/454 ,  A61K31/496 ,  A61P35/00 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/5377 ,  A61K31/497 ,  A61K31/422 ,  A61K31/4545

    CPC分类号： A61K31/5685 ,  A61K31/135 ,  A61K31/138 ,  A61K31/195 ,  A61K31/255 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4188 ,  A61K31/4196 ,  A61K31/4535 ,  A61K31/565 ,  A61K31/675 ,  A61K39/395 ,  A61K45/06 ,  A61K2300/00

    摘要： The invention provides a combination of an ancillary agent and a compound having the formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein the ancillary agent is selected from: a monoclonal antibody, an alkylating agent, an anticancer agent, a further CDK inhibitor and a hormone, hormone agonist, hormone antagonist or hormone modulating agent; X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C═O, NR9(C═O) or 0(C═O) wherein R9 is hydrogen or Ĉhydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, Ĉhydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; Ĉalkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a Ĉhydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).

    摘要翻译： 本发明提供了辅助剂和具有式（O）的化合物或其盐或互变异构体或N-氧化物或溶剂合物的组合： 其中所述辅助剂选自：单克隆抗体，烷化剂，抗癌剂，另外的CDK抑制剂和激素，激素激动剂，激素拮抗剂或激素调节剂; X是R1-A-NR4-基团或5或6元碳环或杂环; A是键，SO 2，C-O，NR 9（C-O）或O（C-O），其中R 9是氢或任选被羟基或C 1-4烷氧基取代的羟基; Y是长度为1,2或3个碳原子的键或亚烷基链; R1是氢; 具有3至12个环成员的碳环或杂环基; 或任选被一个或多个选自卤素（例如氟），羟基，羟基氧基，氨基，单 - 或二-C 1-4烃基氨基的取代基取代的C 1-8烃基和具有3-12个环成员的碳环或杂环基 并且其中烃基中的1或2个碳原子可以任选地被选自O，S，NH，SO，SO 2的原子或基团取代; R2是氢; 卤素; Ĉ烷氧基（如甲氧基）; 或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烃基; R 3选自具有3至12个环成员的氢和碳环和杂环基; 和R 4是氢或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的烃基。