Columbia University

Sloan-Kettering Institute for Cancer Research

Other

Tonix Pharma Holdings Limited (Bermuda)

Leland J Gershell

Thomas Allen Miller

Victoria M Richon

Paul A Marks

Ronald C Breslow

Richard A Rifkind

Sandro Belvedere

Seth Lederman

Andrew Mamoru Kawasaki

Bruce Daugherty

Darryl Rideout

The invention relates to a purified Isometheptene compound comprising the structure according to 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.

Isometheptene isomer

The present invention provides the compound having the formula: wherein each of Rand Ris, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;NH&#x2014;, or &#x2014;CH&#x2014;; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.

Cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof

Class of cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof

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New York, NY, United States of America

Leland J Gershell