US 6,638,954 B2 · Δ2-1,2,3-TRIAZOLINE ANTICONVULSANTS AND THEIR ACTIVE METABOLITE ANALOGUES, THE AMINOALKYLPYRIDINES, ARE EXCITATORY AMINO ACID ANTAGONISTS AND ANTIISCHEMIC AGENTS, USEFUL IN THE TREATMENT OF CEREBRAL ISCHEMIA RESULTING FROM STROKE

Abstract

Pharmaceutical compositions comprise as the active ingredient, nonneurotixic antiischemic compounds that are highly effective by the intraperitoneal route, and that are excitatory amino acid and NMDA/sigma receptor antagonists and are selected from the group consisting of those of the formulae, wherein R2 is 4-pyridyl, 3-pyridyl, or 2-oxo-1-pyrrolidino and R1 is 3,4- or 3,5-dichloro, p- or m-chloro, p- or m-bromo, p- or m-fluoro, p- or m-trifluoromethyl, p-methyl, p-methoxy, or hydrogen, and those of the formulae, wherein R2 is 4-pyridyl or 3-pyridyl, R3 is hydrogen, methyl or ethyl and R1 is 3,4- or 3,5-dichloro, p- or m-chloro, p- or m-bromo, p- or m-fluoro, p- or m-trifluoromethyl, p-methyl, p-methoxy or hydrogen.

Claims31

Dependent claims

A non-neurotoxic antiischemic composition for the treatment of stroke in mammals, comprising as the active ingredient, an effective amount comprising from about 0.01 to about 99 wt. % of an antiischemic Δ2-1,2,3-triazoline compound, selected from the compounds of the formulae,

wherein R2 is 4-pyridyl, 3-pyridyl, or 2-pyridyl and R1 is 3,4- or 3,5-dichloro, p- or m-chloro, p- or m-bromo, p- or m-fluoro, p- or m-trifluoromethyl, p- or m-lower alkyl, p- or m-lower alkoxy or hydrogen, and a pharmaceutical carrier.

Dependencies are inferred from the claim text.

Facts

Application

09/985,318Filed 2 Nov 2001 · us provisional application

Priority

2 Nov 2000

Published

US 2002/0111371 A115 Aug 2002

Granted

28 Oct 2003

Term ends

Not estimatedThe source records don’t support an estimate.

Classification8 codes

C07D 401/04
Containing two hetero rings: directly linked by a ring-member-to-ring-member bond
A61K 31/4192
Having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole: 1,2,3-Triazoles
A61K 31/44
Having six-membered rings with one nitrogen as the only ring hetero atom: non condensed pyridines; Hydrogenated derivatives thereof
A61K 31/4439
Containing further heterocyclic ring systems: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole

Δ2-1,2,3-triazoline anticonvulsants and their active metabolite analogues, the aminoalkylpyridines, are excitatory amino acid antagonists and antiischemic agents, useful in the treatment of cerebral ischemia resulting from stroke

Life of this patent

Δ2-1,2,3-triazoline anticonvulsants and their active metabolite analogues, the aminoalkylpyridines, are excitatory amino acid antagonists and antiischemic agents, useful in the treatment of cerebral ischemia resulting from stroke

Life of this patent

Abstract

Claims31