Thiomorpholine derivatives
US4427676A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Dec 14, 1981 |
| Grant date | Jan 24, 1984 |
| Priority date | — |
| Expiry date | Dec 14, 2001 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D279/12
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.