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1. 发明授权

US08044207B2 Pyridinoylpiperidines as 5-HT1F agonists 有权
标题翻译：吡啶基哌啶作为5-HT1F激动剂
公开(公告)号：US08044207B2
公开(公告)日：2011-10-25
申请号：US12220225
申请日：2008-07-22
申请人： Vincent Mancuso
发明人： Vincent Mancuso
IPC分类号： C07D401/06
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where; R1 is C1-C6 alkyl, substituted C1-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C3 alkyl, substituted C3-C7 cycloalkyl-C1-C3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II; R3 is hydrogen or C1-C3 alkyl; R4 is hydrogen, halo, or C1-C3 alkyl; R5 is hydrogen or C1-C3 alkyl; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.
摘要翻译：本发明涉及式I化合物或其药学上可接受的酸加成盐，其中： R 1是C 1 -C 6烷基，取代的C 1 -C 6烷基，C 3 -C 7环烷基，取代的C 3 -C 7环烷基，C 3 -C 7环烷基-C 1 -C 3烷基，取代的C 3 -C 7环烷基-C 1 -C 3烷基，苯基，取代的苯基，杂环或取代的杂环; R 2是氢，C 1 -C 3烷基，C 3 -C 6环烷基-C 1 -C 3烷基或式II基团; R3是氢或C1-C3烷基; R4是氢，卤素或C1-C3烷基; R5是氢或C1-C3烷基; R6是氢或C1-C6烷基; n为1〜6的整数。本发明的化合物可用于激活5-HT1F受体，抑制神经元蛋白质外渗，以及治疗或预防哺乳动物偏头痛。本发明还涉及合成式I化合物中的中间体的方法。

2. 发明授权

US07630699B2 Systems and methods of scale model correction to account for antenna coupling loss 有权
标题翻译：规模模型校正的系统和方法来考虑天线耦合损耗
公开(公告)号：US07630699B2
公开(公告)日：2009-12-08
申请号：US11613038
申请日：2006-12-19
申请人： Vincent Mancuso
发明人： Vincent Mancuso
IPC分类号： H04B7/00
CPC分类号： G01R29/10
摘要： The invention relates to systems and methods which may allow the determination of a correction factor between full scale antennas and scale antennas in order to determine the coupling loss of the full scale antennas on full scale structures based on models of the full scale structures.
摘要翻译：本发明涉及可以允许确定全尺度天线和缩放天线之间的校正因子的系统和方法，以便基于满量程结构的模型来确定全尺度结构上的全尺寸天线的耦合损耗。

3. 发明授权

US07291619B2 Melanocortin receptor agonists 失效
标题翻译：黑皮质素受体激动剂
公开(公告)号：US07291619B2
公开(公告)日：2007-11-06
申请号：US10466121
申请日：2002-01-23
申请人： Christopher Kelly Biggers , Karin Briner , Christopher William Doecke , Matthew Joseph Fisher , Larry Wayne Hertel , Vincent Mancuso , Michael John Martinelli , John Philip Mayer , Paul Leslie Ornstein , Timothy Ivo Richardson , Jikesh Arvind Shah , Qing Shi , Zhipei Wu , Chaoyu Xie
发明人： Christopher Kelly Biggers , Karin Briner , Christopher William Doecke , Matthew Joseph Fisher , Larry Wayne Hertel , Vincent Mancuso , Michael John Martinelli , John Philip Mayer , Paul Leslie Ornstein , Timothy Ivo Richardson , Jikesh Arvind Shah , Qing Shi , Zhipei Wu , Chaoyu Xie
IPC分类号： A61K31/496 , C07D217/26 , C07D209/44
CPC分类号： A61K45/06 , C07D209/44 , C07D217/14 , C07D217/26 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to melanocortin receptor agonists of formula (I), which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction
摘要翻译：本发明涉及式（I）的黑皮质素受体激动剂，其可用于治疗肥胖症，糖尿病和男性和/或女性性功能障碍

4. 发明授权

US07169777B2 Melanocortin receptor agonists 失效
标题翻译：黑皮质素受体激动剂
公开(公告)号：US07169777B2
公开(公告)日：2007-01-30
申请号：US10466250
申请日：2002-01-23
申请人： Ryan Thomas Backer , Karin Briner , Ivan Collado Caño , Oscar De Frutos Garcia , Christopher William Doecke , Matthew Joseph Fisher , Cristina Garcia-Paredes , Steven Lee Kuklish , Vincent Mancuso , Michael John Martinelli , Ana Isabel Mateo Herranz , Jeffrey Thomas Mullaney , Paul Leslie Ornstein , Zhipei Wu , Chaoyu Xie
发明人： Ryan Thomas Backer , Karin Briner , Ivan Collado Caño , Oscar De Frutos Garcia , Christopher William Doecke , Matthew Joseph Fisher , Cristina Garcia-Paredes , Steven Lee Kuklish , Vincent Mancuso , Michael John Martinelli , Ana Isabel Mateo Herranz , Jeffrey Thomas Mullaney , Paul Leslie Ornstein , Zhipei Wu , Chaoyu Xie
IPC分类号： A61K31/496 , A61K31/5377 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/14 , A61K31/551
CPC分类号： C07D209/48 , A61K38/00 , C07D209/44 , C07D217/12 , C07D217/16 , C07D217/26 , C07K5/06191
摘要： The present invention relates to melanocortin receptor agonist of the formula I useful in the treatment of obesity, diabetes, and male and/or female sexual dysfunction
摘要翻译：本发明涉及式I的黑皮质素受体激动剂，其用于治疗肥胖症，糖尿病以及男性和/或女性性功能障碍

5. 发明申请

US20050075344A1 Melanocortin receptor agonists 失效
标题翻译：黑皮质素受体激动剂
公开(公告)号：US20050075344A1
公开(公告)日：2005-04-07
申请号：US10500476
申请日：2003-01-21
申请人： Ryan Backer , Ivan Collado Caño , Oscar De Furtos-Garcia , Christopher Doecke , Matthew Fisher , Steven Kuklish , Vincent Mancuso , Michael Martinelli , Jeffrey Mullaney , Paul Ornstein , Chaoyu Xie
发明人： Ryan Backer , Ivan Collado Caño , Oscar De Furtos-Garcia , Christopher Doecke , Matthew Fisher , Steven Kuklish , Vincent Mancuso , Michael Martinelli , Jeffrey Mullaney , Paul Ornstein , Chaoyu Xie
IPC分类号： A61K31/496 , A61K45/00 , A61P3/04 , A61P3/10 , A61P15/08 , A61P15/10 , A61P43/00 , C07B53/00 , C07B61/00 , C07C67/343 , C07C69/73 , C07C69/734 , C07D209/44 , C07D211/26 , C07D211/96 , C07D217/26 , C07D295/02 , C07D295/033 , C07D309/04 , C07D335/02 , C07D401/12 , C07D405/12 , C07D409/12 , A61K31/495 , C07D43/02 , C07D49/02
CPC分类号： C07D217/26 , C07D209/44 , C07D211/26 , C07D211/96 , C07D295/033 , C07D309/04 , C07D335/02 , C07D401/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to melanocortin receptor agonist of the formula (I): which is useful in the treatment for obesity, diabetes, and male and/or female sexual dysfunction.
摘要翻译：本发明涉及式（I）的黑皮质素受体激动剂：其可用于治疗肥胖症，糖尿病和男性和/或女性性功能障碍。

6. 发明申请

US20140234403A1 LIPOSOME PRODUCTION USING ISOPROPANOL 审中-公开
标题翻译：使用异丙酚的脂肪生产
公开(公告)号：US20140234403A1
公开(公告)日：2014-08-21
申请号：US14346047
申请日：2012-09-19
申请人： Carine De Kesel , Vincent Mancuso
发明人： Carine De Kesel , Vincent Mancuso
IPC分类号： A61K9/127 , A61K47/36 , A61K47/24 , A61K47/28
CPC分类号： A61K47/24 , A61K9/127 , A61K9/1272 , A61K9/1277 , A61K47/28 , A61K47/36 , Y02A50/411
摘要： Provided are compositions and methods for producing a lipidic film. The method comprises the steps of: (i) dissolving a lipid mix in isopropanol to form a homogeneous mix; and (ii) removing the solvent from the homogeneous mix to form a lipidic film, wherein the lipid mix comprises a lipid and cholesterol.
摘要翻译：提供了用于制备脂质膜的组合物和方法。该方法包括以下步骤：（i）将脂质混合物溶解在异丙醇中以形成均匀的混合物; 和（ii）从均匀混合物中除去溶剂以形成脂质膜，其中所述脂质混合物包含脂质和胆固醇。

7. 发明申请

US20090209563A1 Pyridinoylpiperidines as 5-HT1F agonists 审中-公开
标题翻译：吡啶基哌啶作为5-HT1F激动剂
公开(公告)号：US20090209563A1
公开(公告)日：2009-08-20
申请号：US12221919
申请日：2008-08-07
申请人： Michael Philip Cohen , Daniel Timothy Kohlman , Sidney Xi Liang , Vincent Mancuso , Yao-Chang Xu
发明人： Michael Philip Cohen , Daniel Timothy Kohlman , Sidney Xi Liang , Vincent Mancuso , Yao-Chang Xu
IPC分类号： A61K31/4545 , C07D401/06 , C07D409/14 , C07D405/14 , C07D401/14 , C07D417/14 , A61K31/506 , A61P25/06
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where; R1 is C1-C6 alkyl, substituted C1-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C3 alkyl, substituted C3-C7 cycloalkyl-C1-C3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II R3 is hydrogen or C1-C3 alkyl; R4 is hydrogen, halo, or C1-C3 alkyl; R5 is hydrogen or C1-C3 alkyl; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.
摘要翻译：本发明涉及式I化合物或其药学上可接受的酸加成盐，其中： R 1是C 1 -C 6烷基，取代的C 1 -C 6烷基，C 3 -C 7环烷基，取代的C 3 -C 7环烷基，C 3 -C 7环烷基-C 1 -C 3烷基，取代的C 3 -C 7环烷基-C 1 -C 3烷基，苯基，取代的苯基，杂环或取代的杂环; R 2是氢，C 1 -C 3烷基，C 3 -C 6环烷基-C 1 -C 3烷基或式II的基团R 3是氢或C 1 -C 3烷基; R4是氢，卤素或C1-C3烷基; R5是氢或C1-C3烷基; R6是氢或C1-C6烷基; n为1〜6的整数。本发明的化合物可用于激活5-HT1F受体，抑制神经元蛋白质外渗，以及治疗或预防哺乳动物偏头痛。本发明还涉及合成式I化合物中的中间体的方法。

8. 发明授权

US07314879B2 Melanocortin receptor agonists 失效
标题翻译：黑皮质素受体激动剂
公开(公告)号：US07314879B2
公开(公告)日：2008-01-01
申请号：US10500476
申请日：2003-01-21
申请人： Ryan Thomas Backer , Caño Ivan Collado , Oscar De Frutos-Garcia , Christopher William Doecke , Matthew Joseph Fisher , Steven Lee Kuklish , Vincent Mancuso , Michael John Martinelli , Jeffrey Thomas Mullaney , Paul Leslie Ornstein , Chaoyu Xie
发明人： Ryan Thomas Backer , Caño Ivan Collado , Oscar De Frutos-Garcia , Christopher William Doecke , Matthew Joseph Fisher , Steven Lee Kuklish , Vincent Mancuso , Michael John Martinelli , Jeffrey Thomas Mullaney , Paul Leslie Ornstein , Chaoyu Xie
IPC分类号： A61K31/496 , C07D401/12 , C07D405/12 , C07D407/12
CPC分类号： C07D217/26 , C07D209/44 , C07D211/26 , C07D211/96 , C07D295/033 , C07D309/04 , C07D335/02 , C07D401/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to melanocortin receptor agonist of the formula (I): which is useful in the treatment for obesity, diabetes, and male and/or female sexual dysfunction
摘要翻译：本发明涉及式（I）的黑皮质素受体激动剂：其可用于治疗肥胖症，糖尿病和男性和/或女性性功能障碍

9. 发明授权

US07186715B2 Piperazine- and piperidine-derivatives as melanocortin receptor agonists 失效
标题翻译：哌嗪和哌啶衍生物作为黑皮质素受体激动剂
公开(公告)号：US07186715B2
公开(公告)日：2007-03-06
申请号：US10466248
申请日：2002-01-23
申请人： Karin Briner , Christopher William Doecke , Vincent Mancuso , Michael John Martinelli , Timothy Ivo Richardson , Roger Ryan Rothhaar , Qing Shi , Chaoyu Xie
发明人： Karin Briner , Christopher William Doecke , Vincent Mancuso , Michael John Martinelli , Timothy Ivo Richardson , Roger Ryan Rothhaar , Qing Shi , Chaoyu Xie
IPC分类号： A61K31/496 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
CPC分类号： A61K45/06 , C07D209/44 , C07D217/14 , C07D217/26 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction
摘要翻译：本发明涉及式I的黑皮质素受体激动剂，其可用于治疗肥胖症，糖尿病和男性和/或女性性功能障碍

10. 发明授权

US07157463B2 Substituted piperidines/piperazines as melanocortin receptor agonists 失效
标题翻译：取代的哌啶/哌嗪作为黑皮质素受体激动剂
公开(公告)号：US07157463B2
公开(公告)日：2007-01-02
申请号：US10466249
申请日：2002-01-23
申请人： Ryan Thomas Backer , Karin Briner , Christopher William Doecke , Matthew Joseph Fisher , Steven Lee Kuklish , Vincent Mancuso , Michael John Martinelli , Jeffrey Thomas Mullaney , Chaoyu Xie
发明人： Ryan Thomas Backer , Karin Briner , Christopher William Doecke , Matthew Joseph Fisher , Steven Lee Kuklish , Vincent Mancuso , Michael John Martinelli , Jeffrey Thomas Mullaney , Chaoyu Xie
IPC分类号： A61K31/496 , C07D401/12 , C07D403/12 , C07D403/14
CPC分类号： C07D401/12 , C07D209/44 , C07D217/26 , C07D401/14
摘要： The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction
摘要翻译：本发明涉及式I的黑皮质素受体激动剂，其可用于治疗肥胖症，糖尿病和男性和/或女性性功能障碍

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