A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
167/228
A61K 31/445 (2006.01)
Patent
CA 1316112
ABSTRACT ANXIOLYTIC COMPOSITIONS CONTAINING DIOXOPIPERIDINE DERIVATIVES Phenyl-3-aminoalkyl-4-methyl-2,6-dioxopiperidines of the Formula I Image (I) wherein: R1 represents hydrogen or C1-C4 alkyl; n is 1 or 2; R2 represents hydrogen or methyl, provided that one R2 is hydrogen when n is 2; R3 represents hydrogen or C1-C2 alkyl; R4 represents C1-C2 alkyl; R5 and R6 independently represent hydrogen or methyl; m is 0 to 3; and each Y is in a meta or para position and independently represents hydroxy, C1-C2 alkoxy, C1-C2 alkyl, C1-C2 hydroxyalkyl, halogen, or trifluoromethyl, provided that hydroxy and alkoxy are not in the para position, and pharmacologically acceptable salts thereof have anxiolytic activity. At least some of the compounds are ten orders more potent than diazepam, exhibit an effective dose range in the order of millions fold, and cause dose related effects without sedative side effects. The presently preferred compound is 3-(3'methoxyphenyl)-3-(3"-N,N-dimethylaminopropyl) -4,4-dimethyl-2,6-dioxopiperidine (AGN 2979).
546240
Costall Brenda
Gittos Maurice Ward
British Technology Group Limited
Sim & Mcburney
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