Therapeutically active, substituted piperidines and pyrrolidines therapeutic compositions thereof and methods of use thereof
OwnerBo T. AF Ekenstam, Gunnar A. K. Aberginventors
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Abstract
A compound of formula ##STR1## in which m and n are a pair of integers such that m=0 or 1 and n=3-m or m=0, 1 or 2 and n=4-m, R is straight or branched C.sub.2 to C.sub.4 alkyl having a terminal hydroxy group, R.sub.1 is methyl or methoxy, R.sub.2 is methyl or ethyl and R.sub.3 is hydrogen or methyl; or a pharmaceutically acceptable salt thereof is provided, as well as compositions containing these compounds and processes for preparing them. The compounds can be used to produce topical and local anaesthetic effects in mammals and are also useful as heart anti-arrhythmic agents.
Claims23
A compound of the formula ##STR12## in which m and n are a pair of integers such that m=0 or 1 and n=3-m or m=0, 1 or 2 and n=4-m, R is straight or branched hydroxyalkyl having 2 to 4 carbons and having the hydroxy group in a terminal position, R.sub.1 is selected from the group consisting of methyl and methoxy, R.sub.2 is selected from th group consiting of methyl and ethyl and R.sub.3 is selected from the group consisting of hydrogen and methyl;
- and pharmaceutically acceptable acid addition salts thereof and quaternary N-methyl halides and quaternary N-ethyl halides thereof.
A compound selected from the group consisting of N-(2-Hydroxyethyl)pipecolinyl-2,6-dimethylanilide, its pharmaceutically acceptable acid addition salts and its optically active stereoisomers.
A compound selected from the group consisting of N-(2-Hydroxyethyl)pipecolinyl-2,4,6-trimethylanilide, its pharmaceutically acceptable acid addition salts and its optically active stereoisomers.
A compound selected from the group consisting of N-(3-Hydroxypropyl)pipecolinyl-2,6-dimethylanilide, its pharmaceutically acceptable acid addition salts and its optically active stereoisomers.
A compound selected from the group consisting of N-(2-Hydroxyethyl)pipecolinyl-2-methoxy-6-methylanilide, its pharmaceutically acceptable acid addition salts and its optically active stereoisomers.
A compound selected from the group consisting of N-(4-Hydroxybutyl)isopipecolinyl-2,4,6-trimethylanilide, its pharmaceutically acceptable acid addition salts and its optically active stereoisomers.
A compound selected from the group consisting of N-(2-Hydroxy-methylethyl)-prolyl-2,6-dimethylanilide, its pharmaceutically acceptable acid addition salts and its optically active stereoisomers.
A compound selected from the group consisting of N-(Quaternary-2-hydroxyethyl-N-methyl)pipecolinyl-2,6-dimethylanilide, its pharmaceutically acceptable acid addition salts and its optically stereoisomers.
A compound selected from the group consisting of N-(2-hydroxyethyl)prolyl-2,6-dimethylanilide, its pharmaceutically acceptable acid addition salts and its optically active stereoisomers.
Dependencies are inferred from the claim text.