Spirocyclic derivatives as histone deacetylase inhibitors
    1.
    发明授权
    Spirocyclic derivatives as histone deacetylase inhibitors 有权
    螺环衍生物作为组蛋白脱乙酰酶抑制剂

    公开(公告)号:US08592444B2

    公开(公告)日:2013-11-26

    申请号:US12988197

    申请日:2009-04-14

    IPC分类号: C07D401/04 A61K31/438

    摘要: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C═R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.

    摘要翻译: 本发明涉及根据通式(I)的新的组蛋白脱乙酰酶抑制剂,其中:虚线是任选的附加键; n为0或1至4的整数; R1是氢; 任选被环烷基,芳基或杂芳基取代的C 1 -C 6烷基; (CO)R3; (SO2)R4; 环烷基 芳基; 或杂芳基; R2是任选被芳基或杂芳基取代的C 1 -C 6烷基; 芳基; 杂芳基; 或(CO)R5; X是CH 2,氧或NR 6; Y是一个键,CHR7或NR8; Z是氧,CR9R10或C = R11; R3,R4,R5,R6,R7,R8,R9,R10和R11在说明书中进一步定义; 及其药学上可接受的盐。

    SPIROCYCLIC DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
    9.
    发明申请
    SPIROCYCLIC DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 有权
    螺旋体脱乙酰酶抑制剂的螺环衍生物

    公开(公告)号:US20140080823A1

    公开(公告)日:2014-03-20

    申请号:US14088061

    申请日:2013-11-22

    摘要: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C═R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.

    摘要翻译: 本发明涉及根据通式(I)的新的组蛋白脱乙酰酶抑制剂,其中:虚线是任选的附加键; n为0或1至4的整数; R1是氢; 任选被环烷基,芳基或杂芳基取代的C 1 -C 6烷基; (CO)R3; (SO2)R4; 环烷基 芳基; 或杂芳基; R2是任选被芳基或杂芳基取代的C 1 -C 6烷基; 芳基; 杂芳基; 或(CO)R5; X是CH 2,氧或NR 6; Y是一个键,CHR7或NR8; Z是氧,CR9R10或C = R11; R3,R4,R5,R6,R7,R8,R9,R10和R11在说明书中进一步定义; 及其药学上可接受的盐。

    Combinations comprising a CDK inhibitor and a growth factor antibody or anti-mitotic
    10.
    发明授权
    Combinations comprising a CDK inhibitor and a growth factor antibody or anti-mitotic 有权
    包含CDK抑制剂和生长因子抗体或抗有丝分裂的组合

    公开(公告)号:US08084027B2

    公开(公告)日:2011-12-27

    申请号:US12278530

    申请日:2007-02-02

    IPC分类号: A61K39/395

    摘要: The present invention provides a combination comprising a compound A of formula (I) as set forth in the specification or a pharmaceutically acceptable salt thereof, and an antibody inhibiting a growth factor or its receptor and/or an antimitotic agent or a derivative or prodrug thereof, useful in the treatment of tumors. The chemical name of compound A is 8-[4-(4-methyl-piperazin-1-yl)-phenylamino]-1,4,4-trimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylic acid methylamide.

    摘要翻译: 本发明提供了包含本说明书中阐述的式(I)化合物A或其药学上可接受的盐和抑制生长因子或其受体的抗体和/或抗有丝分裂剂或其衍生物或前药的组合 ,可用于治疗肿瘤。 化合物A的化学名称是8- [4-(4-甲基 - 哌嗪-1-基) - 苯基氨基] -1,4,4-三甲基-4,5-二氢-1H-吡唑并[4,3-h ]喹唑啉-3-甲酸甲基酰胺。