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    • 6. 发明申请
    • Use of surface tension reducing agents in aerosol formulations
    • 在气溶胶配方中使用表面张力降低剂
    • US20090081297A1
    • 2009-03-26
    • US11412523
    • 2006-04-27
    • Robert O. CookThomas A. Armer
    • Robert O. CookThomas A. Armer
    • A61K9/14C07J5/00
    • C07J5/00A61K9/0073A61K9/10A61K9/12A61K47/24A61K47/26
    • The present disclosure describes aerosol formulations that are particularly effective for pulmonary aerosol delivery. The aerosol formulations comprise an aqueous dispersion of active agent particles, said aqueous dispersion having an excess of a surface tension reducing agent. As a result of the reduced surface tension of the aqueous dispersion, the resulting aerosol droplets formed have a particle size less in one embodiment of than 10 microns in size or in an alternate embodiment of less than 6 microns in size. The present disclosure also provides for a method for forming an aerosol from said aerosol formulation, a method of treating a mammal in need of said treatment using said aerosol formulation, and a method of diagnosing a mammal in need of such diagnosis using said aerosol formulation.
    • 本公开描述了对肺部气雾剂递送特别有效的气雾剂制剂。 气溶胶制剂包含活性剂颗粒的水分散体,所述水分散体具有过量的表面张力降低剂。 由于水性分散体的表面张力降低,所形成的所得气溶胶微滴的尺寸在一个实施方案中的尺寸小于10微米,或在尺寸小于6微米的替代实施方案中具有较小的粒度。 本公开还提供了用于从所述气溶胶制剂形成气溶胶的方法,使用所述气溶胶制剂治疗需要所述治疗的哺乳动物的方法,以及使用所述气溶胶制剂诊断需要进行诊断的哺乳动物的方法。
    • 10. 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。