Thiomorpholine derivatives

Details Thiomorpholine derivatives Thiomorpholine derivatives

1981-12-14

1984-01-24

Ford, John M.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

544 59, 544 60, 544 581, 544 587, 544 582, C07D27912, A61K 3154

Patent

active

044276761

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.sup.1 represents (lower)alkyl, R.sup.2 represents hydrogen or (lower)alkyl, R.sup.3 represents hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl(lower)alkyl, 2-tetrahydrofurylmethyl or cycloalkylmethyl and R.sup.4 represents hydrogen, hydroxy, acyloxy or a protected hydroxy group, with the proviso that when n is 0, R.sup.4 is other than hydrogen. The compounds in which n is 0 and R.sup.4 is lower alkoxy, hydroxy or acyloxy are analgesics and/or opiate antagonists and the compounds in which n is 1 and R.sup.4 is hydrogen are hypotensives or anti-hypertensives. The other compounds of formula (I) are intermediates for the pharmacologically active compounds.

REFERENCES:
patent: 2363330 (1944-11-01), Jackson et al.
patent: 2375628 (1945-05-01), D'Alelio et al.
Siegmund et al., Proc. Soc. Exp. Biol. Med., vol. 95, pp. 729-731 (1957).
Aceto et al., Brit. J. Pharmac., vol. 36, pp. 225-239 (1969).

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