Cyanopyrrole containing cyclic carbamate and thiocarbamate biaryls and methods for preparing the same
    4.
    发明授权
    Cyanopyrrole containing cyclic carbamate and thiocarbamate biaryls and methods for preparing the same 失效
    含有环状氨基甲酸酯和硫代氨基甲酸酯联芳基的氰基吡咯及其制备方法

    公开(公告)号:US08129524B2

    公开(公告)日:2012-03-06

    申请号:US13179730

    申请日:2011-07-11

    IPC分类号: C07D265/12 C07D207/30

    CPC分类号: C07D413/04 C07D207/34

    摘要: Methods for preparing cyclic carbamates and thiocarbamates containing cyanopyrrole moieties and of the formula are provided: Z are the same or different and are H, optionally substituted C1 to C6 alkyl, or CORA; RA is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl; Q are the same or different and are H, OH, NH2, CN, halogen, optionally substituted C1 to C6 alkyl, optionally substituted C2 to C6 alkenyl, optionally substituted C1 to C6 alkynyl, optionally substituted C1 to C6 alkoxy, optionally substituted C1 to C6 aminoalkyl, or CORB; and RB is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl. Compounds including 2-amino-5-(5-cyano-1-methyl-1H-pyrrol-2-yl) benzoicacid methyl ester, 5-[4-amino-3-(1-hydroxy-1-methyl-ethyl)-phenyl]-1-methyl-1H-pyrrole-2-carbonitrile, and 2-amino-5-(5-cyano-1-methyl-1H-pyrrol-2-yl)-phenyl-ethanone, or pharmaceutically acceptable salts thereof, and the uses thereof are also provided.

    摘要翻译: 提供了含有氰基吡咯部分和下式的环状氨基甲酸酯和硫代氨基甲酸酯的方法:Z相同或不同,为H,任选取代的C 1 -C 6烷基或CORA; RA为H,任选取代的C 1至C 6烷基,任选取代的C 1至C 6烷氧基,或任选取代的C 1至C 6氨基烷基; Q相同或不同,为H,OH,NH 2,CN,卤素,任选取代的C 1至C 6烷基,任选取代的C 2至C 6烯基,任选取代的C 1至C 6炔基,任选取代的C 1至C 6烷氧基,任选取代的C 1至 C6氨基烷基或CORB; 且R B为H,任选取代的C 1至C 6烷基,任选取代的C 1至C 6烷氧基或任选取代的C 1至C 6氨基烷基。 包括2-氨基-5-(5-氰基-1-甲基-1H-吡咯-2-基)苯甲酸甲酯,5- [4-氨基-3-(1-羟基-1-甲基 - 乙基) - 苯基] -1-甲基-1H-吡咯-2-甲腈和2-氨基-5-(5-氰基-1-甲基-1H-吡咯-2-基) - 苯基 - 乙酮或其药学上可接受的盐, 并提供其用途。

    Thioamide derivatives as progesterone receptor modulators
    6.
    发明授权
    Thioamide derivatives as progesterone receptor modulators 失效
    硫代酰胺衍生物作为孕酮受体调节剂

    公开(公告)号:US07358246B2

    公开(公告)日:2008-04-15

    申请号:US11100860

    申请日:2005-04-07

    CPC分类号: C07D413/04 C07D403/04

    摘要: Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.

    摘要翻译: 提供了硫酰胺化合物,特别是硫代酰胺吡咯化合物及其制备方法。 这些硫代酰胺化合物可用作孕激素受体调节剂,避孕和治疗孕激素相关性疾病。

    CYANOPYRROLE CONTAINING CYCLIC CARBAMATE AND THIOCARBAMATE BIARYLS AND METHODS FOR PREPARING THE SAME
    8.
    发明申请
    CYANOPYRROLE CONTAINING CYCLIC CARBAMATE AND THIOCARBAMATE BIARYLS AND METHODS FOR PREPARING THE SAME 失效
    含有环状碳酸酯和硫代氨基甲酸酯的CYANOPYRROLE及其制备方法

    公开(公告)号:US20090306371A1

    公开(公告)日:2009-12-10

    申请号:US12508679

    申请日:2009-07-24

    CPC分类号: C07D413/04 C07D207/34

    摘要: Methods for preparing cyclic carbamates and thiocarbamates containing cyanopyrrole moieties and of the formula are provided. Z are the same or different and are H, optionally substituted C1 to C6 alkyl, or CORA; RA is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl; Q are the same or different and are H, OH, NH2, CN, halogen, optionally substituted C1 to C6 alkyl, optionally substituted C2 to C6 alkenyl, optionally substituted C1 to C6 alkynyl, optionally substituted C1 to C6 alkoxy, optionally substituted C1 to C6 aminoalkyl, or CORB; and RB is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl. Compounds including 2-amino-5-(5-cyano-1-methyl-1H-pyrrol-2-yl)benzoic acid methyl ester, 5-[4-amino-3-(1-hydroxy-1-methyl-ethyl)-phenyl]-1-methyl-1H-pyrrole-2-carbonitrile, and 2-amino-5-(5-cyano-1-methyl-1H-pyrrol-2-yl)-phenyl-ethanone, or pharmaceutically acceptable salts thereof, and the uses thereof are also provided.

    摘要翻译: 提供了制备含有氰基吡咯部分和下式的环状氨基甲酸酯和硫代氨基甲酸酯的方法。 Z相同或不同,为H,任选取代的C 1 -C 6烷基或CORA; RA为H,任选取代的C 1至C 6烷基,任选取代的C 1至C 6烷氧基,或任选取代的C 1至C 6氨基烷基; Q相同或不同,为H,OH,NH 2,CN,卤素,任选取代的C 1至C 6烷基,任选取代的C 2至C 6烯基,任选取代的C 1至C 6炔基,任选取代的C 1至C 6烷氧基,任选取代的C 1至 C6氨基烷基或CORB; 且R B为H,任选取代的C 1至C 6烷基,任选取代的C 1至C 6烷氧基或任选取代的C 1至C 6氨基烷基。 包括2-氨基-5-(5-氰基-1-甲基-1H-吡咯-2-基)苯甲酸甲酯,5- [4-氨基-3-(1-羟基-1-甲基 - 乙基) - 苯基] -1-甲基-1H-吡咯-2-甲腈和2-氨基-5-(5-氰基-1-甲基-1H-吡咯-2-基) - 苯基 - 乙酮或其药学上可接受的盐 ,并提供其用途。

    Thioamide derivatives as progesterone receptor modulators
    9.
    发明授权
    Thioamide derivatives as progesterone receptor modulators 失效
    硫代酰胺衍生物作为孕酮受体调节剂

    公开(公告)号:US07511071B2

    公开(公告)日:2009-03-31

    申请号:US12044287

    申请日:2008-03-07

    CPC分类号: C07D413/04 C07D403/04

    摘要: Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.

    摘要翻译: 提供了硫酰胺化合物,特别是硫代酰胺吡咯化合物及其制备方法。 这些硫代酰胺化合物可用作孕激素受体调节剂,避孕和治疗孕激素相关性疾病。

    Thioamide derivatives as progesterone receptor modulators
    10.
    发明授权
    Thioamide derivatives as progesterone receptor modulators 失效
    硫代酰胺衍生物作为孕酮受体调节剂

    公开(公告)号:US08168672B2

    公开(公告)日:2012-05-01

    申请号:US12698472

    申请日:2010-02-02

    IPC分类号: A61K31/40 C07D411/00

    CPC分类号: C07D413/04 C07D403/04

    摘要: Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.

    摘要翻译: 提供了硫酰胺化合物,特别是硫代酰胺吡咯化合物及其制备方法。 这些硫代酰胺化合物可用作孕激素受体调节剂,避孕和治疗孕激素相关性疾病。