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    Substituted benzothiadiazinedioxide derivatives and methods of their use
    2.
    发明授权
    Substituted benzothiadiazinedioxide derivatives and methods of their use 失效
    取代的苯并噻二嗪二氧化物衍生物及其使用方法

    公开(公告)号：US07718652B2

    公开(公告)日：2010-05-18

    申请号：US11955004

    申请日：2007-12-12

    Applicant: Joel Adam Goldberg ,  Andrew Fensome ,  Casey Cameron McComas ,  Puwen Zhang

    Inventor： Joel Adam Goldberg ,  Andrew Fensome ,  Casey Cameron McComas ,  Puwen Zhang

    IPC: C07D285/16 ,  A61K31/5415

    CPC classification number: C07D285/16

    Abstract: The present invention is directed to substituted benzothiadiazinedioxide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.

    Abstract translation: 本发明涉及式I的取代苯并噻二嗪二
    醇衍生物：或其药学上可接受的盐，立体异构体或互变异构体，其是单胺再摄取抑制剂，含有这些衍生物的组合物，及其用于预防和治疗病症的方法， 尤其是血管舒缩症状，性功能障碍，胃肠道疾病和泌尿生殖器疾病，抑郁症，内源性行为障碍，认知障碍，糖尿病性神经病，疼痛和其它疾病或病症。

    Combination regimens using progesterone receptor modulators
    10.
    发明授权
    Combination regimens using progesterone receptor modulators 失效
    使用孕酮受体调节剂的联合治疗方案

    公开(公告)号：US06759408B2

    公开(公告)日：2004-07-06

    申请号：US10141792

    申请日：2002-05-09

    Applicant: Gary S. Grubb ,  Puwen Zhang ,  Eugene A. Terefenko ,  Andrew Fensome ,  Jay E. Wrobel ,  Horace Fletcher, III ,  James P. Edwards ,  Todd K. Jones ,  Christopher M. Tegley ,  Lin Zhi

    Inventor： Gary S. Grubb ,  Puwen Zhang ,  Eugene A. Terefenko ,  Andrew Fensome ,  Jay E. Wrobel ,  Horace Fletcher, III ,  James P. Edwards ,  Todd K. Jones ,  Christopher M. Tegley ,  Lin Zhi

    IPC: A61K31535

    CPC classification number: A61K31/535 ,  A61K31/56 ,  Y10S514/843 ,  A61K2300/00

    Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1 and R2 may be single substituents or fused; R3 is H, OH, NH2, C1 to C6 alkyl, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl; RC is H, or optionally substituted C1 to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, alkynyl, C1 to C6 alkoxy, amino, or C1 to C6 aminoalkyl; and R5 is a benzene ring, a five or six membered heterocyclic ring; or pharmaceutically acceptable salt thereof. Methods of treatment include contraception, secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas, adenocarcinomas minimization of side effects, or food intake stimulation.

    Abstract translation: 本发明涉及使用具有通式结构的孕酮受体的拮抗剂的取代的二氢吲哚衍生物化合物的环状组合疗法和方案：其中R 1和R 2可以是单个取代基或稠合的; R 3是H，OH，NH 2，C 1 -C 6烷基，COR C或任选取代的C 1 -C 6烷基，C 3至C 6烯基或炔基; R C是H或任选取代的C 1至C 3烷基，芳基，C 1至C 3烷氧基或C 1至C 3氨基烷基; R 4是H，卤素，CN，NO 2或任选取代的C 1至C 6烷基，炔基，C 1至C 6烷氧基，氨基或C 1至C 6氨基烷基; 和R 5为苯环，五或六元杂环; 或其药学上可接受的盐。 治疗方法包括避孕，继发性闭经，功能障碍性出血，子宫平滑肌瘤，子宫内膜异位症，多囊卵巢综合征，癌，腺癌最小化副作用或食物摄取刺激。

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