NOVEL FLUOROERGOLINE ANALOGS
    1.
    发明公开
    NOVEL FLUOROERGOLINE ANALOGS 审中-公开
    新FLUORERGOLIN类似物

    公开(公告)号:EP2723735A1

    公开(公告)日:2014-04-30

    申请号:EP12803230.7

    申请日:2012-06-22

    IPC分类号: C07D457/00

    摘要: Provided herein are novel fluoroergoline 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-HTiD and/or the 5-HT1B receptor, without agonizing the 5-HT2B receptor using the compounds and composittons 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.

    CORTICOSTEROID PARTICLES AND METHOD OF PRODUCTION
    2.
    发明公开
    CORTICOSTEROID PARTICLES AND METHOD OF PRODUCTION 审中-公开
    CORTICOSTEROIDPARTIKEL及其制造方法

    公开(公告)号:EP2618818A1

    公开(公告)日:2013-07-31

    申请号:EP11827373.9

    申请日:2011-09-20

    IPC分类号: A61K9/14 A01N37/18 A61K31/16

    摘要: A new particle morphology of glucocorticosteroids is described. The forms have a particle morphology that is particularly well suited for use in an inhaled corticosteroid drug suspension formulation for delivery from a next generation nebulizer device. Use of the new glucocorticosteroid particles enables enhanced drug delivery efficiency and increased residence time of the delivered drug in the lungs. New methods for producing glucocorticosteroid particles having these specific particle morphologies are also described. The methods provide a simplified, reproducible and scalable particle formation process that can produce glucocorticosteroid particles having a narrow particle size and shape distribution, a low surface energy, a low aspect ratio, uniform particle morphology and a reduced specific surface area.

    NOVEL CABERGOLINE DERIVATIVES
    3.
    发明公开
    NOVEL CABERGOLINE DERIVATIVES 审中-公开
    新的卡比醇衍生物

    公开(公告)号:EP2863747A1

    公开(公告)日:2015-04-29

    申请号:EP12879191.0

    申请日:2012-06-22

    IPC分类号: A01N43/42 A61K31/44

    CPC分类号: C07D457/06 C07D457/04

    摘要: Provided herein are novel cabergoline analogs 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 dopaminergic D
    2 receptors and/or antagonizing or inhibiting activity of receptors such as the 5-HT
    2 serotonin receptors using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT
    ID and/or the 5-HT
    IB receptor, without agonizing (or very weakly agonising) the 5-HT
    2B receptor using the compounds and compositions disclosed herein.

    摘要翻译: 本文提供了新的卡麦角林类似物及其组合物。 在其他实施方案中,本文提供了使用本文公开的化合物和组合物治疗,预防或改善多种医学病症例如偏头痛和帕金森病的方法。 在其他实施方案中,本文提供使用本文公开的化合物和组合物激动多巴胺能D2受体和/或拮抗或抑制受体如5-HT2 5-羟色胺受体的活性的方法。 在其他实施方案中,本文提供了激动受体如5-HT1D和/或5-HT1B受体而不激动(或非常弱地激动)使用化合物的5-HT2B受体的方法 和本文公开的组合物。

    NOVEL NEUROMODULATORY COMPOUNDS
    4.
    发明公开
    NOVEL NEUROMODULATORY COMPOUNDS 审中-公开
    新型化合物神经调节

    公开(公告)号:EP2793583A1

    公开(公告)日:2014-10-29

    申请号:EP12860106.9

    申请日:2012-06-22

    CPC分类号: C07D457/12 A61K31/48

    摘要: 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-HT
    lD and/or the 5-HT
    1B receptor, without agonizing the 5-HT
    2B 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 alpha
    2A and/or the aIpha2B receptors using the compounds and compositions disclosed herein. In other embodiments, provided herein are methods of agonizing dopaminergic D
    2 receptors and/or antagonizing or inhibiting activity of receptors such as the 5-HT
    2 receptors using the compounds and compositions disclosed herein.

    NOVEL METHYSERGIDE DERIVATIVES
    6.
    发明公开
    NOVEL METHYSERGIDE DERIVATIVES 审中-公开
    新颖的美甲碳酸酯衍生物

    公开(公告)号:EP2934143A1

    公开(公告)日:2015-10-28

    申请号:EP13864398.6

    申请日:2013-12-19

    发明人: WU, Libo ZHANG, Jian

    CPC分类号: C07D471/06 C07D457/06

    摘要: Provided herein are novel methysergide derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders or symptoms thereof, such as, migraine and Parkinson's disease using the compounds and compositions disclosed herein. In still other embodiments, provided herein, such as, for example, are methods for antagonizing the 5-HT
    2B receptor without agonizing the 5-HT
    2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein such as, for example, are methods of agonizing the 5-HT
    1A receptor using the compounds and compositions disclosed herein.

    摘要翻译: 本文提供了新颖的二甲麦角新碱衍生物及其组合物。 在其他实施方案中,本文提供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或其症状,例如偏头痛和帕金森病的方法。 在其他实施方案中,本文提供了例如用于使用本文公开的化合物和组合物拮抗5-HT 2B受体而不激动5-HT 2B受体的方法。 在其他实施方案中,本文提供的例如是使用本文公开的化合物和组合物激动5-HT 1A受体的方法。

    NOVEL ISO-ERGOLINE DERIVATIVES
    7.
    发明公开
    NOVEL ISO-ERGOLINE DERIVATIVES 审中-公开
    新的ISO-ERGOLINE衍生物

    公开(公告)号:EP2793580A1

    公开(公告)日:2014-10-29

    申请号:EP12860451.9

    申请日:2012-06-22

    IPC分类号: A01N43/42 A61K31/44

    摘要: 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-HT
    ID and/or the 5-HT
    1B receptor, without agonizing the 5-HT
    2B 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 alpha
    2A and/or the alpha
    2B receptors using the compounds and compositions disclosed herein.

    摘要翻译: 本文提供了新颖的异麦角碱衍生物及其组合物。 在其他实施方案中,本文提供使用本文公开的化合物和组合物治疗,预防或改善多种医学病症例如偏头痛的方法。 在其他实施方案中,本文提供了使用本文公开的化合物和组合物激动受体例如5-HT ID和/或5-HT 1B受体而不激动5-HT 2B受体的方法。 在其他实施方案中,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受体活性的方法。

    NOVEL ERGOLINE ANALOGS
    8.
    发明公开
    NOVEL ERGOLINE ANALOGS 审中-公开
    新的ERGOLINE类似物

    公开(公告)号:EP2515654A1

    公开(公告)日:2012-10-31

    申请号:EP10840201.7

    申请日:2010-12-23

    IPC分类号: A01N43/42 A61K31/44

    CPC分类号: C07D519/02 C07D457/04

    摘要: Provided herein are novel ergoline derivatives and pharmaceutical 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-HT
    1D and or 5-HT
    1B 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-HT
    2B 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.

    摘要翻译: 本文提供了新颖的麦角灵衍生物及其药物组合物。 在其他实施方案中,本文提供使用本文公开的化合物和组合物治疗,预防或改善多种医学病症例如偏头痛的方法。 在其他实施方案中,本文提供使用本文公开的化合物和组合物激动受体例如5-HT 1D和/或5-HT 1B受体的方法。 在其他实施方案中,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。 在其他实施方案中,本文提供了使用本文公开的化合物和组合物调节血清素转运的方法。