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12 条记录 (耗时 0.037 秒)

    PHARMACEUTICAL COMPOUNDS HAVING HSP90 INHIBITORY OR MODULATING ACTIVITY
    3.
    发明公开
    PHARMACEUTICAL COMPOUNDS HAVING HSP90 INHIBITORY OR MODULATING ACTIVITY 审中-公开
    药剂师VERBINDUNGEN MIT HSP90-HEMMENDER ODER MODULIERENDER WIRKUNG

    公开(公告)号：EP2081891A2

    公开(公告)日：2009-07-29

    申请号：EP07824114.8

    申请日：2007-10-12

    申请人： Astex Therapeutics Limited

    发明人： CONGREVE, Miles Stuart ,  FAZAL, Lyndsey Helen ,  FREDERICKSON, Martyn ,  MURRAY, Christopher William ,  O'BRIEN, Michael Alistair ,  WOODHEAD, Andrew James ,  LYONS, John Francis ,  THOMPSON, Neil Thomas

    IPC分类号： C07D209/08 ,  C07D209/44 ,  C07D215/08 ,  C07D401/04 ,  C07D401/12 ,  C07D419/10 ,  C07D471/04 ,  C07D471/10 ,  C07D491/08 ,  C07D491/10 ,  A61K31/438

    CPC分类号： C07D403/06 ,  C07D209/08 ,  C07D209/44 ,  C07D215/08 ,  C07D215/14 ,  C07D217/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D491/08 ,  C07D491/10 ,  C07D491/107 ,  C07D491/18

    摘要： The invention provides a compound for use in medicine, the compound being a compound of the formula (Vl0) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R 1 : is„ hydrogen, hydroxy, or O-Rz; R2a is hydroxy, methoxy or O-Rz; provided that at least one of R1 and R2a is O-Rz; Rz is Lp-Rp1; SO3H; a glucuronide residue; a mono-, di- or tripeptide residue; or; Lp is a bond, C=O, (C=O)O, (C=O)NRp1 or S(O)xNRp1; x is 1 or 2; Rp1 is hydrogen or a an optionally substituted C1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that Rp1 is not hydrogen when Lp is a bond, C=O or (C=O)O; and provided also that O-Rz does not contain an 0-0 moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group Rp1; and R3, R4a, R8 and R10 are defined in the claims. The compounds of formula (Vl0) are pro-drugs of parent compounds wherein R1 and/or R2a are hydroxy, wherein the parent compounds have Hsp90 inhibiting activity.

    摘要翻译： 本发明提供一种用于医药的化合物，该化合物为式（VI0）化合物或其盐，溶剂化物，互变异构体或N-氧化物：其中双环基团：选自结构式C1，C5和C6： 其中n为0,1,2或3; R1是氢，羟基或O-Rz; R2a是羟基，甲氧基或O-Rz; 条件是R1和R2a中的至少一个是O-Rz; Rz是Lp-Rp1; SO3H; 葡萄糖苷酸残基; 单，二或三肽残基; 或Lp为键，C = O，（C = O）O，（C = O）NRp1或S（O）xNRp1; x为1或2; Rp1是氢或任选取代的含有0,1或2个碳环和0,1,2,3,4,5或6碳 - 碳多重键的C1〜25烃基，条件是当Lp为 C = O或（C = O）O; 并且还提供O-Rz不含有O-O部分; 并且不包括其中R 1是羟基并且R 2a是甲氧基的化合物; Rp2和Rp3相同或不同，并且各自为基团Rp1; R3，R4a，R8和R10在权利要求中限定。 式（VI0）化合物是其中R 1和/或R 2a是羟基的母体化合物的前药，其中母体化合物具有Hsp90抑制活性。

    HYDROXYBENZAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF HSP90
    5.
    发明公开
    HYDROXYBENZAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF HSP90 审中-公开
    羟基苯甲酰胺衍生物及其作为HSP90抑制剂的用途

    公开(公告)号：EP1883402A2

    公开(公告)日：2008-02-06

    申请号：EP06726757.5

    申请日：2006-04-13

    申请人： Astex Therapeutics Limited

    发明人： CHESSARI, Gianni ,  CONGREVE, Miles Stuart ,  NAVARRO, Eva Figueroa ,  FREDERICKSON, Martyn ,  MURRAY, Christopher ,  WOOLFORD, Alison Jo-Anne ,  CARR, Maria Grazia ,  O'BRIEN,Michael Alistair ,  WOODHEAD, Andrew James

    IPC分类号： A61K31/401 ,  A61K31/445 ,  A61K31/5375 ,  A61K31/166 ,  C07C233/65 ,  C07C233/66 ,  C07D207/10 ,  C07D211/34 ,  C07D295/02 ,  C07D309/14 ,  C07D265/30 ,  C07D295/18 ,  C07D211/42 ,  C07D211/22 ,  C07D211/56

    CPC分类号： C07D401/12 ,  C07C65/21 ,  C07D209/08 ,  C07D209/44 ,  C07D215/08 ,  C07D217/06 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D471/10 ,  C07D491/08 ,  C07D491/10

    摘要： The invention provides a compound for use as an inhibitor of Hsp90, the compound having 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; C 1-5 hydrocarbyl and C 1-5 hydrocarbyloxy; wherein the C 1-5 hydrocarbyl and C 1-5 hydrocarbyloxy moieties are each optionally substituted by one or more substituents selected from hydroxy, halogen, C 1-2 alkoxy, amino, mono- and di-C 1-2 alkylamino, and aryl and heteroaryl groups of 5 to 12 ring members; R4 is selected from hydrogen; a group -(O)n-R7 where n is 0 or 1 and R7 is an acyclic C 1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and mono- or di-C 1-5 hydrocarbyl-amino, wherein the acyclic Ci-5 hydrocarbyl group and the mono and di-C 1-5 hydrocarbylamino moieties in each instance are optionally substituted by one or more substituents selected from hydroxy, halogen, C 1-2 alkoxy, amino, mono- and di-C 1-2 alkylamino, and aryl and heteroaryl groups of 5 to 12 ring members; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and R5 and R6 are as defined in the claims.

    摘要翻译： 本发明提供了用作Hsp90抑制剂的化合物，具有式（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是羟基或氢; R2是羟基; 甲氧基或氢; 条件是R1和R2中的至少一个是羟基; R3选自氢; 卤素; 氰基; C 1-5烃基和C 1-5烃氧基; 其中C 1-5烃基和C 1-5烃氧基部分各自任选被一个或多个选自以下的取代基取代：羟基，卤素，C 1-2烷氧基，氨基，单 - 和二-C 1-2烷基氨基和芳基 和5至12个环成员的杂芳基; R4选自氢; 基团 - （O）n -R 7，其中n是0或1并且R 7是无环C 1-5烃基或具有3-7个环成员的单环碳环或杂环基团; 卤素; 氰基; 羟基; 氨基; 和单-C 1 -C 5烃基 - 氨基，其中无环C 1-5烃基和单和二-C 1-5烃氨基部分在每种情况下任选被一个或多个选自以下的取代基取代：羟基，卤素 ，C 1-2烷氧基，氨基，单 - 和二-C 1-2烷基氨基和5-12个环成员的芳基和杂芳基; 或R3和R4一起形成5至7个环成员的单环碳环或杂环; R5和R6如权利要求中所定义。

    THIAZOLE AND ISOTHIAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS
    7.
    发明公开
    THIAZOLE AND ISOTHIAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS 审中-公开
    噻唑和异噻唑ALS蛋白激酶抑制剂

    公开(公告)号：EP1781647A2

    公开(公告)日：2007-05-09

    申请号：EP05762253.2

    申请日：2005-07-22

    申请人： Astex Therapeutics Limited

    发明人： BERDINI, Valerio ,  EARLY, Theresa Rachael ,  O'BRIEN, Michael Alistair ,  WOODHEAD, Andrew James ,  WYATT, Paul Graham

    IPC分类号： C07D417/12

    CPC分类号： C07D275/03 ,  C07D277/56 ,  C07D417/12 ,  C07D417/14

    摘要： The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by a cyclin dependent kinase, the compound having the formula (I): (I) and salts, tautomers, N-oxides or solvates thereof; wherein A is a bond, 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; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; Q is S or CR2; J is S or CH; provided that one of Q and J is S, and the other of Q and J is not S; when Q is S, there is a double bond between the ring carbon atoms “a” and “b” and a double bond between the ring nitrogen N and J; and when J is S, there is a double bond between Q and the ring carbon atom “a” and a double bond between the ring nitrogen N and the ring carbon atom “b”; and R1 to R4 are as defined in the claims.