Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1990-06-22
1992-03-24
Elmore, Carolyn
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
514538, 514539, 514542, 514618, 514625, 558 18, 558250, 558253, 558 9, 562426, 564162, 564182, 564192, 564209, 564294, A61K 3124, A61K 31195
Patent
active
050989340
ABSTRACT:
Novel .omega.-mercaptopropanamides and their homologs of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and ##STR2## R.sub.1 ' is selected from the group consisting of alkyl of 1 to 5 carbon atoms and aryl optionally substituted with at least one member of the group consisting of --OH, alkyl and alkoxy of 1 to 5 carbon atoms, --NO.sub.2 and halogen, n is an integer from 1 to 5, R.sub.2 is selected from the group consisting of hydrogen alkyl of 1 to 5 carbon atoms and aryl and aralkyl of 6 to 15 carbon atoms optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, --OH, halogen and --CF.sub.3, R.sub.3 is selected from the group consisting of a) hydrogen, b) phenyl optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, --OH, --NO.sub.2, halogen, --CF.sub.3, carboxymethyl, alkoxycarbonylmethyl with 1 to 5 alkoxy carbon atoms, aralkoxy of 7 to 15 carbon atoms and ##STR3## and c) a heterocycle selected from the group consisting of thiazolyl, 4,5-dihydro-thiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl, tetrazolyl, benzimidazolyl, benzothiazolyl and benzoxazolyl, all optionally substituted with alkyl of 1 to 5 carbon atoms, X and X' are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms and their salts with non-taxic, pharmaceutically acceptable acids and bases with the proviso that when R.sub.2 is hydrogen and n is 1, R.sub.3 is not phenyl optionally substituted with at least one member of the group consisting of halogen and alkyl and alkoxy of 1 to 5 carbon atoms and when R.sub.2 is methyl and n is 1, R.sub.3 is not phenyl substituted with carboxymethyl having very good analgesic activity and enkephalinase inhibiting activity.
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Delevallee Francoise
Deraedt Rogert
Vevert Jean-Paul
Elmore Carolyn
Roussel Uclaf
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