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    • 1. 发明申请
    • ISOMETHEPTENE ISOMER
    • 异构体异构体
    • WO2014113734A3
    • 2014-11-27
    • PCT/US2014012142
    • 2014-01-17
    • TONIX PHARMACEUTICALS INCLEDERMAN SETHDAUGHERTY BRUCEGERSHELL LELAND JRIDEOUT DARRYLKAWASAKI ANDREW
    • LEDERMAN SETHDAUGHERTY BRUCEGERSHELL LELAND JRIDEOUT DARRYLKAWASAKI ANDREW
    • C07C211/21A61K31/131A61P29/00A61P37/00C07B55/00
    • C07C211/21A61K31/047A61K31/131A61K31/167A61K31/192A61K31/4045A61K31/4152A61K31/522A61K31/616A61K45/06C07B53/00C07B2200/07C07C59/285A61K2300/00
    • The invention relates to a purified Isometheptene compound comprising the structure according to Formula (I), (Formula (I)) or a hydrochloride, or a pharmaceutically acceptable addition salt thereof. In particular, the disclosure relates to the synthesis, purification and characterization of an Isometheptene isomer mucate crystal 2, wherein the Isometheptene isomer 2 is stereochemically characterized as (R)-enantiomer, respectively. The Isometheptene (R)-enantiomer activity indicates a selective centrally acting selective ligand for Imidazoline subtype 1 (I1) receptor sites; and more specifically, the disclosure provides an antihypertensive composition for treatment of migraine and other neurovascular or neurogenic pain from abdominal distress. (R)-Isometheptene enantiomer or isomer 2 may be an anti-hypertensive agent with lower side effects than the racemate form. Therefore (R)-Isometheptene is believed to be effective against episodic tension-type headaches (ETTH). The (R)-Isometheptene enantiomer or isomer 2 is believed to effectively lower blood pressure, used alone or together with other headache ameliorating drugs. Methods of synthesis and treatment are described. Regarding (R)- Isometheptene crystals data of X-ray crystallography are presented.
    • 本发明涉及包含根据式(I),(式(I))的结构或盐酸盐或其药学上可接受的加成盐的纯化的异美汀化合物。 特别地,本公开涉及异美金属异构体粘酸盐晶体2的合成,纯化和表征,其中异美金属异构体2分别立体化学表征为(R) - 对映体。 Isometheptene(R) - 对映体活性表示咪唑啉亚型1(I1)受体位点的选择性中心作用选择性配体; 更具体地说,本公开内容提供了用于治疗偏头痛和其他神经血管疼痛或神经源性疼痛免受腹部痛苦的抗高血压组合物。 (R) - 异美辛对映异构体或异构体2可以是与外消旋体形式相比具有较低副作用的抗高血压剂。 因此(R)-Isometheptene被认为对发作性紧张型头痛(ETTH)有效。 据信(R)-Isometheptene对映异构体或异构体2可有效降低血压,单独使用或与其他头痛改善药物一起使用。 描述了合成和处理的方法。 关于(R) - 异美斯汀晶体的X射线晶体学数据的介绍。
    • 2. 发明申请
    • ISOMETHEPTENE ISOMER
    • 异构异构体
    • WO2014113734A2
    • 2014-07-24
    • PCT/US2014/012142
    • 2014-01-17
    • TONIX PHARMACEUTICALS INC.LEDERMAN, SethDAUGHERTY, BruceGERSHELL, Leland J.RIDEOUT, DarrylKAWASAKI, Andrew
    • LEDERMAN, SethDAUGHERTY, BruceGERSHELL, Leland J.RIDEOUT, DarrylKAWASAKI, Andrew
    • C07C211/21A61K31/047A61K31/131A61K31/167A61K31/192A61K31/4045A61K31/4152A61K31/522A61K31/616A61K45/06C07B53/00C07B2200/07C07C59/285A61K2300/00
    • The invention relates to a purified Isometheptene compound comprising the structure according to Formula (I), (Formula (I)) or a hydrochloride, or a pharmaceutically acceptable addition salt thereof. In particular, the disclosure relates to the synthesis, purification and characterization of an Isometheptene isomer mucate crystal 2, wherein the Isometheptene isomer 2 is stereochemically characterized as (R)-enantiomer, respectively. The Isometheptene (R)-enantiomer activity indicates a selective centrally acting selective ligand for Imidazoline subtype 1 (I1) receptor sites; and more specifically, the disclosure provides an antihypertensive composition for treatment of migraine and other neurovascular or neurogenic pain from abdominal distress. (R)-Isometheptene enantiomer or isomer 2 may be an anti-hypertensive agent with lower side effects than the racemate form. Therefore (R)-Isometheptene is believed to be effective against episodic tension-type headaches (ETTH). The (R)-Isometheptene enantiomer or isomer 2 is believed to effectively lower blood pressure, used alone or together with other headache ameliorating drugs. Methods of synthesis and treatment are described. Regarding (R)- Isometheptene crystals data of X-ray crystallography are presented.
    • 本发明涉及包含根据式(I),(式(I))或盐酸盐的结构或其药学上可接受的加成盐的纯化异构体化合物。 特别地,本公开涉及异葎草酮异构体粘蛋白晶体2的合成,纯化和表征,其中异构异构体异构体2分别被立体化学表征为(R) - 对映异构体。 对映异构体异构体活性表示咪唑啉亚型1(I1)受体位点的选择性中心作用选择性配体; 并且更具体地,本公开提供了用于治疗偏头痛和其他神经血管或神经源性疼痛的抗高血压组合物。 (R) - 异亚丙基对映异构体或异构体2可以是具有低于外消旋形式的副作用的抗高血压剂。 因此(R) - 美沙芬被认为对于发作型紧张型头痛(ETTH)有效。 据信(R) - 异构体异构体2有效地降低血压,单独使用或与其他头痛改善药物一起使用。 描述合成和处理方法。 关于(R) - 异构体色素晶体的X射线晶体学数据。