C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/292, 260/323
C07D 207/02 (2006.01) C07D 207/12 (2006.01) C07D 207/24 (2006.01) C07D 211/04 (2006.01) C07D 211/42 (2006.01) C07D 211/46 (2006.01) C07D 211/54 (2006.01) C07D 211/74 (2006.01) C07D 223/02 (2006.01) C07D 223/08 (2006.01) C07D 491/04 (2006.01)
Patent
CA 1112242
Abstract of the Disclosure The present invention provides processes for the pro- duction of new derivatives of perhydro-aza-heterocycles of the formula Image (I) in which X is the oxo radical or hydrogen and the radical OR1, in which R1 is hydrogen, lower alkyl, carboxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, carbamoyl-lower alkyl, N- lower alkylcarbamoyl-lower alkyl, N,N-di-lower alkylcarbamoyl- lower alkyl or cyano-lower alkyl and also phenyl, or phenyl- lower alkyl or phenoxy-lower alkyl which are unbranched or branched at the .alpha.-carbon atom, it being possible, in each case, for phenyl to be unsubstituted or substituted by lower alkyl, lower alkoxy, halogen, trifluoromethyl, lower alkoxy- carbonyl, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylcarbamoyl or cyano, or in which R1 is acyl, and acyl is the group -C(=O)-R1 in which R is lower alkyl, lower alkoxy- lower alkyl or halogeno-lower alkyl, or phenyl or phenyl-lower alkyl, in which phenyl, in each case, can be substituted by lower alkyl, lower alkoxy, halogen and/or trifluoromethyl, R2 is hydrogen or a lower aliphatic hydrocarbon radical, Y is oxygen or sulphur, n1 and n2 each are values of 1 to 3, n1 + n2 being at most four, and Ar is phenyl, naphthyl, tetrahydro- naphthyl or anthryl, in which, in each case, phenyl or an aromatic ring of naphthyl or anthryl can be unsubstituted or substituted by lower alkyl, hydroxyl, lower alkoxy, halogen, trifluormethyl, lower alkoxycarbonyl, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylcarbamoyl, nitro or cyano, it being possible, in each case, for 1, 2 or 3 of these substi- tuents to be present and for these substitutents to be either identical or different and of acid addition salts thereof. These new substances possess valuable pharmacological proper- ties, in particular antidepressant activity, and can be used, in the form of pharmaceutical compositions, for the treatment of mental depressions.
285793
Fetherstonhaugh & Co.
Novartis Ag
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