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    • 1. 发明授权
    • Substituted indolo 4,3 FG quinolines useful for treating migraine
    • 取代吲哚4,3吡啶喹啉可用于治疗偏头痛
    • US08710092B2
    • 2014-04-29
    • US12978314
    • 2010-12-23
    • Jian ZhangRobert O. CookThomas A. ArmerSergey Alexandrovich KosarevDejian Xie
    • Jian ZhangRobert O. CookThomas A. ArmerSergey Alexandrovich KosarevDejian Xie
    • A61K31/40
    • C07D519/02C07D457/04
    • Provided herein are substituted indolo[4,3-fg]quinolines of Formula (I) and (II) where R1-R6 and R13 are as defined in the specification and pharmaceutical compositions thereof which are useful in treating, preventing, or ameliorating a variety of medical disorders such as, for example, migraine. In other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and or 5-HT1B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of regulating serotonin transport using the compounds and compositions disclosed herein.
    • 本文提供了式(I)和(II)的取代的吲哚并[4,3-f]喹啉,其中R 1 -R 6和R 13如说明书及其药物组合物中所定义,其可用于治疗,预防或改善品种 的医学病症,例如偏头痛。 在其它实施方案中,本文提供了使用本文公开的化合物和组合物来激发受体例如5-HT1D和/或5-HT1B受体的方法。 在其它实施方案中,本文提供了使用本文公开的化合物和组合物拮抗或抑制受体例如5-HT 2B受体的活性的方法。 在其它实施方案中,本文提供了使用本文公开的化合物和组合物调节5-羟色胺转运的方法。
    • 4. 发明授权
    • Neuromodulatory compounds
    • 神经调节化合物
    • US08946420B2
    • 2015-02-03
    • US13531427
    • 2012-06-22
    • Robert O. CookJian ZhangThomas A. Armer
    • Robert O. CookJian ZhangThomas A. Armer
    • A61K31/48C07D457/12
    • C07D457/12A61K31/48
    • Provided herein are novel neuromodulatory compounds and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine and Parkinson's disease, using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and/or the 5-HT1B receptor, without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the adrenergic alpha2A and/or the alpha2B receptors using the compounds and compositions disclosed herein. In other embodiments, provided herein are methods of agonizing dopaminergic D2 receptors and/or antagonizing or inhibiting activity of receptors such as the 5-HT2 receptors using the compounds and compositions disclosed herein.
    • 本文提供了新型神经调节化合物及其组合物。 在其它实施方案中,本文提供了使用本文公开的化合物和组合物治疗,预防或改善各种医学病症例如偏头痛和帕金森病的方法。 在其它实施方案中,本文提供的是使用本文公开的化合物和组合物来激发受体例如5-HT1D和/或5-HT1B受体而不激发5-HT 2B受体的方法。 在其它实施方案中,本文提供了使用本文公开的化合物和组合物来拮抗或抑制受体例如肾上腺素α2A和/或α2B受体的活性的方法。 在其它实施方案中,本文提供了使用本文公开的化合物和组合物来激发多巴胺能D2受体和/或拮抗或抑制受体(例如5-HT 2受体)的活性的方法。
    • 8. 发明授权
    • Iso-ergoline derivatives
    • 异麦角灵衍生物
    • US08592445B2
    • 2013-11-26
    • US13531416
    • 2012-06-22
    • Jian ZhangRobert O. Cook
    • Jian ZhangRobert O. Cook
    • A01N43/42A61K31/44
    • C07D457/12C07D519/00C07D519/02
    • Provided herein are novel iso-ergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and/or the 5-HT1Breceptor, without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the adrenergic alpha2A and/or the alpha2Breceptors using the compounds and compositions disclosed herein.
    • 本文提供新颖的异麦角灵衍生物及其组合物。 在其它实施方案中,本文提供了使用本文公开的化合物和组合物治疗,预防或改善各种医学病症例如偏头痛的方法。 在其它实施方案中,本文提供的是使用本文公开的化合物和组合物来激发受体例如5-HT1D和/或5-HT1B受体而不激发5-HT 2B受体的方法。 在其它实施方案中,本文提供了使用本文公开的化合物和组合物拮抗或抑制受体例如肾上腺素α2A和/或α2B受体的活性的方法。
    • 9. 发明申请
    • NOVEL ISO-ERGOLINE DERIVATIVES
    • 新型的ISO-ERGOLINE衍生物
    • US20130158064A1
    • 2013-06-20
    • US13531416
    • 2012-06-22
    • Jian ZhangRobert O. Cook
    • Jian ZhangRobert O. Cook
    • C07D457/12A61P25/06A61P25/16A61K31/48
    • C07D457/12C07D519/00C07D519/02
    • Provided herein are novel iso-ergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and/or the 5-HT1Breceptor, without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the adrenergic alpha2A and/or the alpha2Breceptors using the compounds and compositions disclosed herein.
    • 本文提供新颖的异麦角灵衍生物及其组合物。 在其它实施方案中,本文提供了使用本文公开的化合物和组合物治疗,预防或改善各种医学病症例如偏头痛的方法。 在其它实施方案中,本文提供的是使用本文公开的化合物和组合物来激发受体例如5-HT1D和/或5-HT1B受体而不激发5-HT 2B受体的方法。 在其它实施方案中,本文提供了使用本文公开的化合物和组合物拮抗或抑制受体例如肾上腺素α2A和/或α2B受体的活性的方法。