Loading patent…
AssigneeTonix Pharmaceuticals, Inc.
InventorsSETH LEDERMAN, BRUCE DAUGHERTY, LELAND J. GERSHELL, DARRYL RIDEOUT, ANDREW KAWASAKI
Estimating the term…
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.
A purified racemic Isometheptene compound comprising the structure according to Formula (I),
An (S)-Isometheptene mucate salt comprising the structure according to Formula (II):
An (R)-Isometheptene mucate salt comprising the structure according to Formula (III):
A composition comprising a purified Isometheptene enantiomer or pharmaceutically acceptable addition salt or hydrochloride thereof;
A composition, comprising a (R)-Isometheptene enantiomer or hydrochloride or pharmaceutically acceptable addition salt thereof, and one or more pharmaceutical substances selected from the group consisting of acetaminophen, ibuprofen, aspirin, caffeine, dichloralphenazone, naproxen, and sumatriptan succinate;
A method of treatment of hypertension comprising administering a therapeutic amount of a composition comprising Isometheptene (R)-enantiomer mucate salt, and a pharmaceutically acceptable carrier, to a patient in need of such treatment.
A method of treatment of migraine comprising administering to a patient in need of such treatment, a therapeutic amount of a composition comprising (R)-Isometheptene enantiomer mucate salt combined with an active ingredient selected from acetaminophen, ibuprofen, aspirin, caffeine, dichloralphenazone, naproxen, and sumatriptan succinate;
A method for nitric oxidase inhibition comprising administering to a patient in need of such treatment, a therapeutic amount of a composition comprising Isometheptene (R)-enantiomer mucate salt combined with an active ingredient selected from acetaminophen, ibuprofen, aspirin, caffeine, dichloralphenazone, naproxen, and sumatriptan succinate;
A method for producing a composition comprising the steps of mixing a therapeutically effective amount of (R)-Isometheptene mucate salt with an anti-inflammatory substance selected from the group consisting of acetaminophen, ibuprofen, aspirin, dichloralphenazone, naproxen, and sumatriptan succinate;
An oral dosage comprising the composition comprising a therapeutic amount of (R)-Isometheptene in a controlled release formulation comprising coated or uncoated capsules.
A therapeutic controlled release formulation comprising a drug selected from pure (R)-Isometheptene within or on a core coated with a biodegradable material.
Dependencies are inferred from the claim text.