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US 5,629,336 AGranted
Use of glycine/NMDA receptor ligands for the treatment of drug dependence and withdrawal
AssigneeMerck Sharp & Dohme Corp.
InventorPeter H. Hutson
Life of this patent
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Abstract
Compounds capable of interacting with the strychnine-insensitive glycine modulatory site of the N-methyl-D-aspartate (NMDA) receptor are active in preventing or reducing dependence on dependence-inducing agents such as morphine, but lack the undesirable side-effects of agents hitherto employed for this purpose.
Claims6
A method for the treatment of dependence on an opiate dependence-inducing agent, which method comprises administering to a patient in need thereof an effective amount of a compound, or a pharmaceutically acceptable salt thereof, said compound selected from the group consisting of (a), (b), (c), (d) and (e), being:
- (a) R-(+)-3-amino-1-hydroxypyrrolidin-2-one;
- (b) a compound of formula II:
- ##STR8## wherein the substituents R and --NH.sub.2 are in a cis-configuration;
- wherein R represents a hydrocarbon group, selected from the group consisting of:
- C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl(C.sub.1-6)alkyl, aryl, aryl(C.sub.1-6)alkyl, C.sub.3-7 heterocycloalkyl, C.sub.3-7 heterocycloalkyl(C.sub.1-6)alkyl, heteroaryl and heteroaryl(C.sub.1-6)alkyl;
- wherein:
- aryl is phenyl or naphthyl;
- heterocycloalkyl is piperidyl, piperazinyl or morpholinyl;
- heteroaryl is pyridyl, quinolyl, isoquinolyl, pyridazinyl, pyrimidinyl, pyrazinyl, pyranyl, furyl, benzofuryl, thienyl, benzthienyl, imidazolyl, oxadiazolyl or thiadiazolyl;
- and wherein said hydrocarbon group can be optionally substituted by one or more groups selected from C.sub.1-6 alkyl, adamantyl, phenyl, halogen, C.sub.1-6 haloalkyl, trifluoromethyl, hydroxy, C.sub.1-6 alkoxy, aryloxy, keto, C.sub.1-3 alkylenedioxy, nitro, cyano, carboxy, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkoxycarbonyl(C.sub.1-6)alkyl, C.sub.1-6 alkylcarbonyloxy, arylcarbonyloxy, C.sub.1-6 alkylcarbonyl, arylcarbonyl, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, amino, mono- or di(C.sub.1-6)alkylamino, C.sub.1-6 alkylcarbonylamino and C.sub.1-6 alkoxycarbonylamino;
- and U represents oxygen or sulphur;
- (c) cis-3-amino-1-hydroxy-4-methylpyrrolidin-2-one;
- (d) 4-oxo-1,4-dihydroquinoline having a 2-acidic group or a group convertible thereto in vivo;
- and
- (e) 7-chloro-5-iodo-4-oxo-1,4-dihydroquinoline-2-carboxylic acid.
12 more elements
Dependencies are inferred from the claim text.