Abstract: The present invention provides new derivatives of perhydro-aza-heterocycles of the formula ##STR1## in which X is the oxo radical or hydrogen and the radical OR.sub.1, in which R.sub.1 is hydrogen or a substituted or unsubstituted aliphatic hydrocarbon radical, a substituted or unsubstituted araliphatic hydrocarbon radical or a substituted or unsubstituted aromatic hydrocarbon radical or an acyl radical, R.sub.2 is hydrogen or a substituted or unsubstituted aliphatic hydrocarbon radical, Y is oxygen or sulphur, n.sub.1 and n.sub.2 each are values of 1 to 3, n.sub.1 +n.sub.2 being at most four, and Ar is a substituted or unsubstituted aromatic hydrocarbon radical, and the acid addition salts, in particular the pharmaceutically acceptable acid addition salts thereof. These new substances possess valuable pharmacological properties, in particular antidepressant activity, and can be used for the treatment of mental depressions.
Abstract: A compound of formula (I): ##STR1## wherein: M IS 0 OR 1;N is 4 to 8;A is hydrogen, and when m is 0 and R.sub.5 is methyl it may also be methyl or a group CO.sub.2 B wherein B is hydrogen or CO.sub.2 B represents an ester group in which the B moiety contains from 1 to 12 carbon atoms;X is CO, protected CO, CROH in which R is hydrogen or C.sub.1-4 alkyl and in which the OH moiety may be protected; R.sub.1 is hydrogen, or CO.sub.2 R.sub.1 represents an ester group in which the R.sub.1 moiety contains 1 to 12 carbon atoms;R.sub.4 is hydrogen, C.sub.1-9 alkyl, C.sub.5-8 cycloalkyl, C.sub.5-8 cycloalkyl-C.sub.1-6 alkyl, phenyl, phenyl C.sub.1-6 alkyl, naphthyl, naphthyl C.sub.1-6 alkyl, any of which phenyl or naphthyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, or nitro groups;D is a group --CH.sub.2 --CH(R.sub.6)--CH(R.sub.7)--C(R.sub.2)(R.sub.3)--, a group--CH.sub.2 --CH(R.sub.6)--CH(R.sub.7)--CH(R.sub.8)--C(R.sub.2)(R.sub.3)--, a group--CH.sub.
Type:
Grant
Filed:
May 13, 1977
Date of Patent:
May 29, 1979
Assignee:
Beecham Group Limited
Inventors:
Richard W. Moore, Frederick Cassidy, Gordon Wootton
Abstract: Compounds of the structure: ##STR1## where A is either ##STR2## where R.sub.1 to R.sub.4 are various substituents are active as antibacterials and antifungals.
Type:
Grant
Filed:
July 18, 1977
Date of Patent:
March 20, 1979
Assignee:
Merck & Co., Inc.
Inventors:
Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel
Abstract: Compounds of the formula ##STR1## in which R.sup.4 represents an alkyl radical having from 1 to 4 carbon atoms,R.sup.5 represents a linear or branched alkylene radical having from 1 to 10 carbon atoms in the chain which may be substituted by groups which are not reactive under the applied conditions, and R.sup.6 represents hydrogen or a branched alkyl radical having from 3 to 10 carbon atoms with a secondary or tertiary N-.alpha.-C atom, are prepared by anodic alkoxylation of lactams of the formula ##STR2## with an alcohol of the formula R.sup.4 OH, in which formulae R.sup.4, R.sup.5 and R.sup.6 have the aforesaid meaning, in the presence of at least one alkali metal or tetraalkylammonium tetrafluoroborate, hexafluoroborate or nitrate as conducting salt, at a temperature of up to about 100.degree. C. in an electrolytic cell with stationary or flowing electrolyte. Some of the products are novel.
Abstract: Compounds of the formula ##STR1## in which R.sup.4 represents an alkyl radical having from 1 to 4 carbon atoms,R.sup.5 represents a linear or branched alkylene radical having from 1 to 10 carbon atoms in the chain which may be substituted by groups which are not reactive under the applied conditions, andR.sup.6 represents hydrogen or a branched alkyl radical having from 3 to 10 carbon atoms with a secondary or tertiary N-.alpha.-C atom, are prepared by anodic alkoxylation of lactams of the formula ##STR2## with an alcohol of the formula R.sup.4 OH, in which formulae R.sup.4, R.sup.5 and R.sup.6 have the aforesaid meaning, in the presence of at least one alkali metal or tetraalkylammonium tetrafluoroborate, hexafluoroborate or nitrate as conducting salt, at a temperature of up to about 100.degree. C in an electrolytic cell with stationary or flowing electrolyte. Some of the products are novel.