C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/476.1, 260/4
C07D 295/04 (2006.01) C07D 295/084 (2006.01)
Patent
CA 1049530
ABSTRACT OF THE DISCLOSURE The present invention relates to pharmaceutical compositions which on administration to mammals are capable of producing a psychotropic effect and is particular, produce a mood elevating effect without causing substantial side effects such as those associated with anti-cholinergic agents. Accordingly, the present invention provides pharmaceutical compositions which comprise pharmaceutically acceptable carriers in associa- tion with compounds of the formula (III): Image (III) wherein R1 is hydrogen atom or a group R9 or CO.R9 wherein R9 is C1=6 alkyl, phenyl or benzyl group or such a group .omega.-substituted by a group NR10-R11 where R10 is hydrogen atom or a methy, ethyl or benzyl group and R11 is a hydrogen atom or a methyl or ethyl group or is attached to R10 so that NR10R11 is a pyrrolidyl, piperidyl, morpholino or hexamethylenimino group; R2 is a hydrogen atom or a methyl or ethyl group; R3 is a hydrogen atom or a methy, ethyl, propyl or benzyl group; R4 is a hydrogen atom or a methyl or ethyl group or is attached to R3 so that NR3R4 is a pyrrolidyl, piperidyl, morpholino, N-methyl- piperazino or hexamethylenimino group; R5 is a hydrogen, fluorine, chlorine or bromine atom or a methyl, ethyl, propyl, butyl, benzyl, trifluormethyl, hydroxy, methoxy, ethoxy, propoxy, benzyloxy, acetoxy, propionoxy, amino, methylamino ethylamino, dimethylamino, diethylamino, carboxyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, nitro or methylthiol group; R6, R7 and R8 which may be the same or different are each a hydrogen, flourine, chlorine or bromine atom or a methyl, ethyl, methoxy, ethoxy, acetoxy, hydroxy or trifluoro-methyl group; or salt or solvent thereof. The process of preparation comprises the condensation of an amine of the formula HNR3R4 with a compound of the formula (V) : Image (V) or a salt thereof wherein R5, R6, R7 and R8 are as defined in relation to formula (III); Y is a group displaceable by a neucleophile and X is a group CR2OR1 or a suitable precursor thereof; and thereafter if desired, converting any of the groups R1, R2, R3, R4, R5, R6, R7 and R8 to alternative groups R1, R2, R3, R4, R5, R6, R7 and R8 by known methods and if X is a precursor of CR2OR1, converting X to CR2OR1 by known methods.
192963
Clark Judith A.
Hadley Michael S.
Beecham Group Limited
Na
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