3-substituted-aminomethyl-3-substituted-oxy-17a-methyl-17a-l...

C - Chemistry – Metallurgy – 07 – J

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C07J 73/00 (2006.01) A61K 31/58 (2006.01)

Patent

CA 2046527

ABSTRACT OF THE DISCLOSURE 3-SUBSTITUTED-AMINOMETHYL-3-SUBSTITUTED-OXY-17A- METHYL-17A-LOWER-ALKYL-17A-AZA-D-HOMOL-5-ALPHA-ANDROSTANES This invention pertains to novel 3-substituted-aminomethyl-3-substi- tuted-oxy-17a-methyl-17a-lower-alkyl-17a-aza-D-homo-5-alpha-androstane compounds useful as muscle relaxants, methods for preparing such com- pounds, and methods for administering muscle relaxation, wherein the novel compounds are represented the general Formula: Image (1) including optically active isomeric forms, and pharmaceutically accept- able acid addition salts thereof, therein: R is selected from the group consisting of hydrogen, lower-alkyl, lower-alkyl carbonyl, and di(lower-alkyl)amino carbonyl; R1 is selected from the group consisting of: di(lower-alkyl)sub- stituted amino; lower-cycloalkyl lower-alkyl, lower-alkyl substituted amino;, 1-piperidinyl; 1-pyrrolidinyl; 1-hexamethyleneimino; 4-morphol- inyl; 1-piperazinyl, 1-(4-methylpiperazinyl), tri(lower-alkyl)substituted amino, 1-(1-methylpiperidinyl); 1-(1-methylpyrrolidinyl); and 1-(4,4-di- methylpiperazinyl). each lower-alkyl group having from 1 to 6 carbon atoms; R2 is a lower-alkyl group having from 1 to 4 carbon atoms; and X- is a pharmaceutically acceptable anion.

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