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    Diaminopyrazoles
    5.
    发明授权
    Diaminopyrazoles 失效
    二氨基吡唑

    公开(公告)号：US06458823B1

    公开(公告)日：2002-10-01

    申请号：US09963254

    申请日：2001-09-25

    Applicant: Adam Matthew Gilbert ,  Zhen-jia Chen

    Inventor： Adam Matthew Gilbert ,  Zhen-jia Chen

    IPC: A61K314155

    CPC classification number: C07D231/38 ,  C07D401/12

    Abstract: This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula wherein: R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl; R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2; n is 0 or 1; R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons; and all crystalline forms and the pharmaceutically acceptable salts thereof.

    Abstract translation: 本发明涉及平滑肌痉挛状态或过度肌肉收缩的治疗，例如用糠醛的化合物促进尿失禁：R1和R2分别是1至6个碳原子的直链烷基，3至6个碳原子的支链烷基，或 3至6个碳原子的环烷基，其中R 2可以被F，Cl，Br，I，OH，NH 2，氰基，C 1 -C 6烷氧基，C 1 -C 6烷硫基，COOH或COOC 1 -C 6烷基取代; R 3是芳基或杂芳基 任选被0至4个独立地选自C 1 -C 6烷基，C 1 -C 6烷氧基，氰基，F，Cl，Br，C 1 -C 6烷硫基，CO 2 R 1，CONH 2，OH，NH 2和NO 2基团取代的基团取代; n为0 或1; R 4为碳原子数为1〜10的直链烷基，碳原子数为3〜10的支链烷基或碳原子数为3〜10的环烷基;以及所有结晶形式及其药学上可接受的盐。

    Diaminopyrazoles
    9.
    发明授权
    Diaminopyrazoles 失效
    二氨基吡唑

    公开(公告)号：US06319941B1

    公开(公告)日：2001-11-20

    申请号：US09655897

    申请日：2000-09-06

    Applicant: Adam Matthew Gilbert ,  Zhen-jia Chen

    Inventor： Adam Matthew Gilbert ,  Zhen-jia Chen

    IPC: A61K31415

    CPC classification number: C07D231/38 ,  C07D401/12

    Abstract: This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula wherein: R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R1 and R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl; R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2; n is 0 or 1; R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons; and all crystalline forms and the pharmaceutically acceptable salts thereof.

    Abstract translation: 本发明涉及平滑肌痉挛状态或过度肌肉收缩的治疗，例如用糠醛的化合物促进尿失禁：R1和R2分别是1至6个碳原子的直链烷基，3至6个碳原子的支链烷基，或 3至6个碳原子的环烷基，其中R 1和R 2可以被F，Cl，Br，I，OH，NH 2，氰基，C 1 -C 6烷氧基，C 1 -C 6烷硫基，COOH或COOC 1 -C 6烷基取代; R 3是芳基或 任选被0至4个独立地选自C 1 -C 6烷基，C 1 -C 6烷氧基，氰基，F，Cl，Br，C 1 -C 6烷硫基，CO 2 R 1，CONH 2，OH，NH 2和NO 2的基团取代的杂芳基; n 为0或1; R 4为碳原子数为1〜10的直链烷基，碳数为3〜10的支链烷基或碳原子数为3〜10的环烷基;以及所有结晶形式及其药学上可接受的盐。

    Diaminopyrazoles
    10.
    发明授权
    Diaminopyrazoles 失效
    二氨基吡唑

    公开(公告)号：US06313149B1

    公开(公告)日：2001-11-06

    申请号：US09655891

    申请日：2000-09-06

    Applicant: Adam Matthew Gilbert ,  Zhen-jia Chen

    Inventor： Adam Matthew Gilbert ,  Zhen-jia Chen

    IPC: A61K31415

    CPC classification number: C07D231/38 ,  C07D401/12

    Abstract: This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula wherein: R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R1 R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl; R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2; n is 0 or 1; R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons; and all crystalline forms and the pharmaceutically acceptable salts thereof

    Abstract translation: 本发明涉及平滑肌痉挛状态或过度肌肉收缩的治疗，例如用糠醛的化合物促进尿失禁：R1和R2分别是1至6个碳原子的直链烷基，3至6个碳原子的支链烷基，或 3至6个碳原子的环烷基，其中R 1可被F，Cl，Br，I，OH，NH 2，氰基，C 1 -C 6烷氧基，C 1 -C 6烷硫基，COOH或COOC 1 -C 6烷基取代; R 3是芳基或杂芳基 任选地被0至4个独立地选自C 1 -C 6烷基，C 1 -C 6烷氧基，氰基，F，Cl，Br，C 1 -C 6烷硫基，CO 2 R 1，CONH 2，OH，NH 2和NO 2基团取代的基团取代; n是 0或1; R 4是碳原子数1〜10的直链烷基，碳原子数3〜10的支链烷基或碳原子数3〜10的环烷基;全部结晶形式及其药学上可接受的盐

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