SETH LEDERMAN,BRUCE DAUGHERTY,LELAND J. GERSHELL,DARRYL RIDEOUT,ANDREW KAWASAKI
申请号：
MX2015009268
公开号：
MX2015009268A
申请日:
2014.01.17
申请国别(地区):
MX
年份:
2015
代理人:
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.La invención se refiere a un compuesto de isometepteno purificado que comprende la estructura según la formula (I), (6- metilamino -2- metilhepteno) o un clorhidrato, o una sal de adición farmacéuticamente aceptable del mismo. En particular, la descripción se refiere a la síntesis, purificación y caracterización de u cristal de mucato de isómero 2 de isometepteno, en donde el isómero 2 isometeptero se caracteriza estereoquímicamente como enantiómero (R) de isometepteno indica un ligando selectivo que actua de manera central selectivo para sitios del receptor de imidazolina subtipo 1 (I1)； y más específicamente, la descripción proporciona una composición antihipertensora para el tratamiento de la migraña y otro dolor neu
