Cycloaliphatic compounds, analgesic compositions thereof and method of use thereof as analgesics
AssigneeGlaxo Group Limited
InventorDerek P. Reynolds
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AssigneeGlaxo Group Limited
InventorDerek P. Reynolds
Estimating the term…
Compounds are disclosed of general formula (I) ##STR1## in which R.sub.1 represents a hydrogen atom, a halogen atom or a group OR.sub.2, in which R.sub.2 represents a hydrogen atom, an alkyl group or an acyl group, R.sub.3 represents hydrogen or an alkyl, alkenyl or aryl group, R.sub.4 and R.sub.5 which may be the same or different, each represents a hydrogen atom or an alkyl, alkenyl or alkynyl group optionally substituted by an aryl or cycloalkyl group; or R.sub.4 and R.sub.5 together with the nitrogen atom may form a saturated four to seven membered ring, with the provisos that, when R.sub.4 and R.sub.5 simultaneously represent hydrogen atoms then (i) when R.sub.1 is hydrogen then R.sub.3 is not methyl and (ii) the compounds are the .beta.-isomers; and their physiologically acceptable salts. Compounds of formula (I) may be prepared from the corresponding .alpha.- or .beta.-configuration alcohols, from an aziridine intermediate or by a variety of alkylation procedures whereby the group R.sub.4 and/or R.sub.5 is introduced. The compounds (I) and their salts have analgesic activity and may be formulated as pharmaceutical compositions in conventional manner.
A compound of the formula (I):
2.beta.-Methylamino-1-phenylcyclopentanol, propanoate ester, hydrogen sulphate or hydrogen maleate.
A compound selected from 2.beta.-dimethylamino-1-phenylcyclopentanol propanoate;
A compound of the formula (I):
A compound of the formula (I)a:
Dependencies are inferred from the claim text.