Nitrogen bridge tetrahydroisoquinolines

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546140, A61K 3147, C07C40114

Patent

active

052409392

ABSTRACT:
Muscle relaxant nitrogen bridge tetrahydroisoquinolines are disclosed. The novel compounds are represented by the formula ##STR1## wherein A is ##STR2## M represents --(CH.sub.2).sub.n --Z--(CH.sub.2).sub.n or ##STR3## R is a C.sub.1-3 alkoxy group, or adjacent Rs are a methylenedioxy group, R.sub.1 is lower alkyl; n is 1-6;
m is 2 or 3; p is 1-3; Z is --N.sup.+ (R.sub.2 R.sub.3)--, --N(R.sub.4)--, ##STR4## and --N[(CH.sub.2).sub.n --A--R.sub.5 ]--; R.sub.2 and R.sub.3 are independently lower alkyl groups wherein a carbon atom within the chain may be replaced by a heteroatom, lower cycloalkyl, lower cycloalkyl lower alkyl, aryl, aryl lower alkyl, a 4- to 6-member heteroring or may be combined with the nitrogen to form a heteroring; R.sub.4 is a straight- or branched- chain C.sub.1-10 alkyl wherein a carbon atom within the chain may be replaced by a heteroatom, lower cycloalkyl, lower cycloalkyl lower alkyl, aryl, or a heteroring, which groups may be substituted or unsubstituted; or ##STR5## R.sub.5 is lower alkyl or lower alkenyl; Y is hydrogen, lower alkyl wherein a carbon atom within the chain may be replaced by a heteroatom, lower alkoxy, aryl, aryloxy, lower cycloalkyl, lower cycloalkyl lower alkyl, a 4- to 6-member heteroring or --NR.sub.2 R.sub.3 ; X.sup.- is a pharmaceutically acceptable anion, and optically active forms thereof, meso forms thereof, cis-trans isomeric forms thereof and racemates thereof.

REFERENCES:
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patent: 4235906 (1980-01-01), Savarese et al.
patent: 4701460 (1987-10-01), El-Sayad et al.
patent: 4761418 (1988-08-01), Swaringen, Jr. et al.

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