abstract |
The invention provides novel thiomorpholines of the formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts wherein n represents 0 or 1, R 1 represents (lower)alkyl, R 2 represents hydrogen or (lower)alkyl, R 3 represents hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl(lower)alkyl, 2-tetrahydrofurylmethyl or cycloalkylmethyl and R 4 represents hydrogen, hydroxy, acyloxy or a protected hydroxy group, with the proviso that when n is 0, R 4 is other than hydrogen. The compounds in which n is 0 and R 4 is lower alkoxy, hydroxy or acyloxy are analgesics and/or opiate antagonists and the compounds in which n is 1 and R 4 is hydrogen are hypotensives or anti-hypertensives. The other compounds of formula (I) are intermediates for the pharmacologically active compounds. |