发明名称 ISOMETHEPTENE ISOMER
摘要 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.
申请公布号 CA2898450(A1) 申请公布日期 2014.07.24
申请号 CA20142898450 申请日期 2014.01.17
申请人 TONIX PHARMACEUTICALS INC. 发明人 LEDERMAN, SETH;DAUGHERTY, BRUCE;GERSHELL, LELAND J.;RIDEOUT, DARRYL;KAWASAKI, ANDREW
分类号 C07C211/21;A61K31/131;A61P29/00;A61P37/00;C07B55/00 主分类号 C07C211/21
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