6-Amino-1,4-dihydro-benzo[d][1,3]oxazin-2-ones and analogs useful as progesterone receptor modulators
    56.
    发明申请
    6-Amino-1,4-dihydro-benzo[d][1,3]oxazin-2-ones and analogs useful as progesterone receptor modulators 失效
    6-氨基-1,4-二氢 - 苯并[d] [1,3]恶嗪-2-酮和可用作孕酮受体调节剂的类似物

    公开(公告)号:US20070225281A1

    公开(公告)日:2007-09-27

    申请号:US11804831

    申请日:2007-05-21

    IPC分类号: A61K31/535 C07D265/18

    摘要: Compounds having the structure of formula I are provided. In formula I, R1 is H, OH, substituted or unsubstituted C1 to C3 alkyl, C1 to C3 perfluoroalkyl, or COR6; R6 is H, substituted or unsubstituted C1 to C4 alkyl, aryl, substituted or unsubstituted C1 to C4 alkoxy, substituted or unsubstituted C1 to C3 aminoalkyl; R2 and R3 are H, substituted or unsubstituted C1 to C6 alkyl, C1 to C6 perfluoroalkyl, substituted or unsubstituted C2 to C6 alkenyl, substituted or unsubstituted C2 to C6 alkynyl, substituted or unsubstituted C3 to C6 cycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic; or R2 and R3 are fused to form spirocyclic rings; R4 is NHR7, OR7, NHSO2R7, or OSO2R7; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt, ester, or prodrug thereof. Such compounds are useful as progesterone receptor modulators and for treating progesterone receptor related conditions.

    摘要翻译: 提供具有式I结构的化合物。 在式I中,R 1是H,OH,取代或未取代的C 1至C 3烷基,C 1或N 2 C 3至C 3全氟烷基或COR 6; R 6是H,取代或未取代的C 1至C 4烷基,芳基,取代或未取代的C 1〜 至C 4烷氧基,取代或未取代的C 1至C 3氨基烷基; R 2和R 3均为H,取代或未取代的C 1至C 6烷基,C 1至C 6烷基, C 6至C 6全氟烷基,取代或未取代的C 2至C 6链烯基,取代或未取代的C 2, 取代或未取代的C 3至C 6环烷基,取代或未取代的芳基或取代或未取代的杂环基; 或R 2和R 3 3稠合形成螺环; R 4是NHR 7,OR 7,NHSO 2 R 7,或 OSO 2 R 7; Q是O,S,NR 8或CR 9 R 10; 或其药学上可接受的盐,酯或前药。 这些化合物可用作孕酮受体调节剂和用于治疗孕酮受体相关病症。

    Benzothiadiazolylphenylalkylamine derivatives and methods of their use
    57.
    发明申请
    Benzothiadiazolylphenylalkylamine derivatives and methods of their use 失效
    苯并噻二唑基苯基烷基胺衍生物及其使用方法

    公开(公告)号:US20070072918A1

    公开(公告)日:2007-03-29

    申请号:US11528792

    申请日:2006-09-27

    CPC分类号: C07D285/14

    摘要: The present invention is directed to benzothiadiazolylphenylalkylamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

    摘要翻译: 本发明涉及式I的苯并噻二唑基苯基烷基胺衍生物:或其药学上可接受的盐,含有这些衍生物的组合物及其用于预防和治疗由单胺再摄取改善的病症的方法,所述方法尤其包括血管舒缩症状(VMS) 特别是选自重度抑郁障碍,血管舒缩症状,压力和急迫性尿失禁,纤维肌痛,疼痛等的那些情况,特别是选自以下的那些病症:血管紧张素转换酶,抑制性功能障碍,性功能障碍,胃肠道和泌尿生殖系统疾病,慢性疲劳综合征,纤维瘤病综合征,神经系统疾病及其组合, 糖尿病性神经病变及其组合。

    Benzothiadiazolylphenylalkylamine derivatives and methods of their use
    59.
    发明授权
    Benzothiadiazolylphenylalkylamine derivatives and methods of their use 失效
    苯并噻二唑基苯基烷基胺衍生物及其使用方法

    公开(公告)号:US07601744B2

    公开(公告)日:2009-10-13

    申请号:US11528792

    申请日:2006-09-27

    IPC分类号: A61K31/41 C07D285/06

    CPC分类号: C07D285/14

    摘要: The present invention is directed to benzothiadiazolylphenylalkylamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

    摘要翻译: 本发明涉及式I的苯并噻二唑基苯基烷基胺衍生物:或其药学上可接受的盐,含有这些衍生物的组合物及其用于预防和治疗由单胺再摄取改善的病症的方法,所述方法尤其包括血管舒缩症状(VMS) 特别是选自重症抑郁障碍,血管舒缩症状,压力和急迫性尿失禁,纤维肌痛,疼痛等的那些病症,其中,所述疾病,性功能障碍,胃肠道和泌尿生殖系统疾病,慢性疲劳综合征,纤维肌痛综合征,神经系统疾病及其组合, 糖尿病性神经病变及其组合。