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    PHARMACEUTICAL COMBINATIONS
    2.
    发明公开
    PHARMACEUTICAL COMBINATIONS 审中-公开
    药物组合

    公开(公告)号：EP2049106A2

    公开(公告)日：2009-04-22

    申请号：EP07766218.7

    申请日：2007-07-13

    申请人： Astex Therapeutics Limited

    发明人： LYONS, John, Francis ,  SQUIRES, Matthew, Simon ,  THOMPSON, Neil, Thomas ,  GALLAGHER, Neil, James ,  CURRY, Jayne, Elizabeth

    IPC分类号： A61K31/415 ,  A61K31/4453 ,  A61P35/00 ,  A61P43/00

    CPC分类号： A61K31/4453 ,  A61K31/415 ,  A61K2300/00

    摘要： The invention provides a combination comprising an ancillary compound and a compound having the formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein 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 C1-4 hydrocarbyl 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, hydroxy, C1-4 hydrocarbyloxy, 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; 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.

    摘要翻译： 本发明提供包含辅助化合物和具有式（0）的化合物的组合：或其盐或互变异构体或N-氧化物或溶剂合物; 其中X是基团R1-A-NR4-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C 1-4烃基; 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，羟基，C 1-4烃氧基，氨基，单或二-C 1-4烃基氨基和具有3至12个环成员的碳环或杂环基团的取代基取代的C 1-8烃基， 并且其中烃基的1或2个碳原子可以任选地被选自O，S，NH，SO，SO 2的原子或基团替代; R2是氢; 卤素; C1-4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; R3选自氢和具有3至12个环成员的碳环和杂环基团; 并且R 4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。

    PHARMACEUTICAL COMBINATIONS
    3.
    发明公开
    PHARMACEUTICAL COMBINATIONS 审中-公开
    药物组合

    公开(公告)号：EP2046330A2

    公开(公告)日：2009-04-15

    申请号：EP07733530.5

    申请日：2007-07-13

    申请人： Astex Therapeutics Limited

    发明人： LYONS, John, Francis ,  SQUIRES, Matthew, Simon ,  THOMPSON, Neil, Thomas ,  GALLAGHER, Neil, James

    IPC分类号： A61K31/454 ,  A61P35/00

    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（0）化合物或其盐或互变异构体或N-氧化物或溶剂化物的组合; 其中X是R1-A-NR4-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C 1-4烃基; Y是1至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，其中烃基的1或2个碳原子可任选地被选自O，S，NH，SO，SO 2的原子或基团替代; R2是氢; 卤素; C1-4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; R3选自氢和具有3至12个环成员的碳环和杂环基团; 并且R 4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“）化合物或其盐，互变异构体，溶剂合物和N-氧化物：其中R1是2,6-二氯苯基; R2a和R2b都是氢; 和R3是基团：式（A）其中R4是C1-4烷基。

    PHARMACEUTICAL COMPOUNDS
    4.
    发明公开
    PHARMACEUTICAL COMPOUNDS 审中-公开
    药物化合物

    公开(公告)号：EP1968579A1

    公开(公告)日：2008-09-17

    申请号：EP06831505.0

    申请日：2006-12-29

    申请人： Astex Therapeutics Limited

    发明人： BERDINI, Valerio ,  CURRY, Jayne, Elizabeth ,  GALLAGHER, Neil, James ,  GILL, Adrian, Liam ,  LYONS, John, Francis

    IPC分类号： A61K31/4155 ,  A61K31/4184 ,  C07D403/04 ,  A61P35/00

    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, PDKl , Chk (e.g. Cbkl 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 (ErbBl), 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.

    PHARMACEUTICAL COMBINATIONS
    5.
    发明授权
    PHARMACEUTICAL COMBINATIONS 有权

    公开(公告)号：EP2073803B1

    公开(公告)日：2018-09-19

    申请号：EP07824133.8

    申请日：2007-10-12

    申请人： Astex Therapeutics Limited

    发明人： GALLAGHER, Neil, James ,  LYONS, John, Francis ,  THOMPSON, Neil, Thomas ,  YULE, Stephen, Murray ,  MURRAY, Christopher, William

    IPC分类号： A61K31/403

    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.