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1. 发明授权

US09150593B2 Fluoroergoline analogs 有权
标题翻译：氟麦角灵类似物
公开(公告)号：US09150593B2
公开(公告)日：2015-10-06
申请号：US14568598
申请日：2014-12-12
申请人： MAP Pharmaceuticals, Inc.
发明人： Robert O. Cook , Jian Zhang , Thomas A. Armer
IPC分类号： A61K31/495 , C07D519/00 , C07D519/02 , C07D498/14 , A61K9/00 , A61K31/4985 , C07D457/04 , C07D498/04
CPC分类号： C07D519/02 , A61K9/0075 , A61K9/0078 , A61K31/495 , A61K31/4985 , C07D457/04 , C07D498/04 , C07D498/14 , C07D519/00
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-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.
摘要翻译：本文提供新的氟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。

2. 发明申请

US20150038525A1 NOVEL METHYSERGIDE DERIVATIVES 审中-公开
标题翻译：新型甲基衍生物
公开(公告)号：US20150038525A1
公开(公告)日：2015-02-05
申请号：US14520522
申请日：2014-10-22
申请人： MAP Pharmaceuticals, Inc.
发明人： Libo WU , Jian ZHANG
IPC分类号： C07D471/06
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-HT2B receptor without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein such as, for example, are methods of agonizing the 5-HT1A receptor using the compounds and compositions disclosed herein.
摘要翻译：本文提供了新颖的甲基麦芽糖衍生物及其组合物。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或其症状（例如偏头痛和帕金森病）的方法。在本文提供的其它实施方案中，例如，是使用本文公开的化合物和组合物来拮抗5-HT 2B受体而不激发5-HT 2B受体的方法。在其它实施方案中，本文提供的例如是使用本文公开的化合物和组合物来激发5-HT 1A受体的方法。

3. 发明授权

US08841448B2 Fluoroergoline analogs 有权
标题翻译：氟麦角灵类似物
公开(公告)号：US08841448B2
公开(公告)日：2014-09-23
申请号：US14047815
申请日：2013-10-07
申请人： Map Pharmaceuticals, Inc.
发明人： Robert O. Cook , Jian Zhang , Thomas A. Armer
IPC分类号： C07D471/00 , C07D487/00 , C07D491/00 , C07D495/00 , C07D497/00 , C07D519/02 , C07D498/14
CPC分类号： C07D519/02 , A61K9/0075 , A61K9/0078 , A61K31/495 , A61K31/4985 , C07D457/04 , C07D498/04 , C07D498/14 , C07D519/00
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-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.
摘要翻译：本文提供新的氟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。

4. 发明申请

US20140179707A1 NOVEL ERGOLINE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译：新颖的胆固醇衍生物及其用途
公开(公告)号：US20140179707A1
公开(公告)日：2014-06-26
申请号：US14134127
申请日：2013-12-19
申请人： MAP PHARMACEUTICALS, INC.
发明人： Thomas Armer , Shashidhar Kori , Libo Wu
IPC分类号： A61K31/4985 , A61M15/00
CPC分类号： A61K31/4985
摘要： Provided herein are 8′-Hydroxy-2-CF3-dihydroergotamine (8′OH-2-CF3-DHE) compounds, compositions, and dosage forms containing such compositions. Also 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-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.
摘要翻译：本文提供了含有这种组合物的8'-羟基-2- CF 3 - 二氢麦角胺（8'OH-2-CF3-DHE）化合物，组合物和剂型。本文还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。

5. 发明申请

US20140073647A1 NOVEL FLUOROERGOLINE ANALOGS 有权
公开(公告)号：US20140073647A1
公开(公告)日：2014-03-13
申请号：US14047839
申请日：2013-10-07
申请人： MAP PHARMACEUTICALS, INC.
发明人： Robert O. Cook , Jian Zhang , Thomas A. Armer
IPC分类号： C07D498/14
CPC分类号： C07D519/02 , A61K9/0075 , A61K9/0078 , A61K31/495 , A61K31/4985 , C07D457/04 , C07D498/04 , C07D498/14 , C07D519/00
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-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.

6. 发明申请

US20140039188A1 NOVEL ISO-ERGOLINE DERIVATIVES 有权
标题翻译：新型的ISO-ERGOLINE衍生物
公开(公告)号：US20140039188A1
公开(公告)日：2014-02-06
申请号：US14045767
申请日：2013-10-03
申请人： MAP PHARMACEUTICALS, INC.
发明人： Jian Zhang , Robert O. Cook
IPC分类号： C07D457/12 , C07D519/02
CPC分类号： C07D457/12 , C07D519/00 , C07D519/02
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-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.
摘要翻译：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。

7. 发明授权

US08517009B2 Methods and apparatus for delivering aerosolized medication 有权
公开(公告)号：US08517009B2
公开(公告)日：2013-08-27
申请号：US12460119
申请日：2009-07-13
申请人： Prashant Kakade
发明人： Prashant Kakade
IPC分类号： B05B1/26 , A61M15/00
CPC分类号： A61M15/009 , A61M11/04 , A61M15/0005 , A61M15/0021 , A61M15/0065 , A61M2206/16 , B05B1/26
摘要： A pulmonary drug delivery device having one or more vortexing elements which impart beneficial flow characteristics to an inspiratory air flow carrying a medicament into the patient's lungs.

8. 发明授权

US08475845B2 Method of particle formation 有权
标题翻译：颗粒形成方法
公开(公告)号：US08475845B2
公开(公告)日：2013-07-02
申请号：US11995676
申请日：2006-07-14
申请人： Linda Sze Tu , Hubert Leonardus Regtop , Neil Russell Foster , Pascal Hickey
发明人： Linda Sze Tu , Hubert Leonardus Regtop , Neil Russell Foster , Pascal Hickey
IPC分类号： B01J2/06 , A61K31/567 , A61K31/167 , A61K31/58 , A61K31/137
CPC分类号： B01J2/06 , A61K9/0075 , A61K9/14 , A61K9/145 , A61K31/137 , A61K31/167 , A61K31/567 , A61K31/58 , A61K45/06 , A61K2300/00
摘要： A method of co-formulating two or more pharmaceutically active compounds into a particulate product including contacting a dense, supercritical or near-critical fluid With a suspension of a first active compound in a medium that is miscible with the dense fluid and a solution of a second active compound in a solvent that is miscible with the dense fluid. The product may be the first active agent coated with the second active agent. The method may use coaxial nozzles for the fluid, media or solvents. The method may be applied to production of dry powders for inhalation including beta-agonists and corticosteroids. Apparatus for use in the method comprising means for streams of solvents, media and dense fluids to enter a precipitation chamber at substantially the same point and means for collection of particles under gravity in one or more collection chambers.
摘要翻译：将两种或更多种药物活性化合物共配制成颗粒产物的方法，包括将稠密，超临界或近临界流体与第一活性化合物的悬浮液接触在与稠密流体混合的介质中，在与稠密流体混溶的溶剂中的第二活性化合物。该产品可以是涂覆有第二活性剂的第一活性剂。该方法可以使用用于流体，介质或溶剂的同轴喷嘴。该方法可用于生产用于吸入的干粉，包括β-激动剂和皮质类固醇。用于该方法的装置包括用于在基本上相同点处进入沉淀室的溶剂流，介质和致密流体的装置以及用于在一个或多个收集室中在重力下收集颗粒的装置。

9. 发明申请

US20110152280A1 NOVEL ERGOLINE ANALOGS 有权
标题翻译：新的胆固醇类似物
公开(公告)号：US20110152280A1
公开(公告)日：2011-06-23
申请号：US12978314
申请日：2010-12-23
申请人： ROBERT O. COOK , Thomas A. Armer , Sergey Alexandrovich Kosarev , Dejian Xie
发明人： ROBERT O. COOK , Thomas A. Armer , Sergey Alexandrovich Kosarev , Dejian Xie
IPC分类号： A61K31/4985 , C07D519/02 , A61P25/06 , A61P25/16 , A61P25/24 , A61P25/00 , A61P1/08 , A61P3/00
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-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.
摘要翻译：本文提供了新的麦角灵衍生物及其药物组合物。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。

10. 发明申请

US20100247655A1 Synthesis of Small Particles 有权
标题翻译：小颗粒的合成
公开(公告)号：US20100247655A1
公开(公告)日：2010-09-30
申请号：US12646767
申请日：2009-12-23
申请人： Neil Russell Foster , Hubert Leonardus Regtop , Fariba Dehghani
发明人： Neil Russell Foster , Hubert Leonardus Regtop , Fariba Dehghani
IPC分类号： A61K9/14 , B29B9/00 , A61K38/28 , A61P3/10
CPC分类号： A61K9/0073 , A61K9/0075 , A61K9/14 , A61K9/1688 , A61K9/51 , A61K38/28 , B01J2/02
摘要： The invention provides an apparatus for forming fine particles of a substance in a precipitation chamber, in which the apparatus has means to convey the fine particles from the precipitation chamber to at least one particle collection chamber, downstream of the precipitation chamber, the particle collection chamber having an inlet and an outlet separate from the inlet. The invention also provides a method of forming fine particles of a substance, the method comprising contacting a non-gaseous fluid containing the substance with a dense fluid to expand the non-gaseous fluid in a precipitation chamber, conveying a resulting mixture of fluid and the fine particles from the precipitation chamber to a collection chamber, the collection chamber having an inlet and an outlet separate from the inlet.
摘要翻译：本发明提供了一种用于在沉淀室中形成物质的细颗粒的装置，其中该装置具有将沉淀室中的细颗粒输送到沉淀室下游的至少一个颗粒收集室，颗粒收集室具有与入口分离的入口和出口。本发明还提供了一种形成物质细颗粒的方法，该方法包括将含有该物质的非气态流体与致密流体接触以在沉淀室中膨胀非气态流体，将所得到的流体混合物和从沉淀室到收集室的细颗粒，收集室具有与入口分离的入口和出口。

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