Cyclohexane derivatives

A compound of formula IA:

• ##STR20## in which formula R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, --(CHR.sup.6).sub.n CHR.sup.7 CN, --(CHR.sup.6).sub.n CHR.sup.7 CONH.sub.2, --(CHR.sup.6).sub.n CHR.sup.7 COOR.sup.8 or --(CHR.sup.6).sub.n CHR.sup.7 CH.sub.2 OH;
• R.sup.3 is unsubstituted or substituted phenyl where the substituents is/are selected from C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxy, halogen and methylene or ethylenedioxy;
• and R.sup.4' is hydrogen, alkyl or optionally substituted aryl(C.sub.1 -C.sub.6)alkyl in which the alkyl group is itself optionally substituted by C.sub.1 -C.sub.6 alkyl;
• R.sup.6 and R.sup.7 independently represent hydrogen C.sub.1 -C.sub.6 alkyl- or C.sub.7 -C.sub.16 aralkyl-, and R.sup.7 also represents hydroxy(C.sub.1 -C.sub.6)alkyl-, (C.sub.2 -C.sub.7 alkanoyloxy(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6 alkoxy)carbonyl- and R.sup.8 is hydrogen or C.sub.1 -C6 alkyl;
• with the proviso that when R.sup.3 is unsubstituted phenyl, then R.sup.1 and R.sup.4' cannot both be hydrogen.

A pharmaceutical composition comprising a compound of formula ##STR21## or a pharmaceutically acceptable salt thereof, where the dotted line represents an optional bond,

• one of R.sup.1 and R.sup.5 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.16 aralkyl, --(CHR.sup.6).sub.n CHR.sup.7 CN, --(CHR.sup.6).sub.n CHR.sup.7 CONH.sub.2, --(CHR.sup.6).sub.n CHR.sup.7 COOR.sup.8, --(CHR.sup.6).sub.n CHR.sup.7 CH.sub.2 OH wherein n is 0 or 1, R.sup.6 and R.sup.7 independently represent hydrogen, C.sub.1 -C.sub.6 alkyl- or C.sub.7 -C.sub.16 aralkyl-, and R.sup.7 also represents hydroxy(C.sub.1 -C.sub.6)alkyl-, (C.sub.2 -C.sub.7)alkanoyloxy(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6 alkoxy)carbonyl- and R.sup.8 is hydrogen or C.sub.1 -C.sub.6 alkyl;
• the other of R.sup.1 and R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.7 -C.sub.16 aralkyl;
• R.sup.3 is an optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl group;
• said heteroaryl group containing 5 to 10 ring atoms of which one or more (e.g up to 3) of said atoms are heteroatoms selected from oxygen, nitrogen and sulphur, the same or different;
• said aryl or heteroaryl radicals being optionally substituted by one or more substituents the same or different, eg substituents commonly used in pharmaceutical chemistry such as for example:
• C.sub.1 -C.sub.6 alkyl;
• C.sub.1 -C.sub.6 alkoxy or such groups substituted by C.sub.6 -C.sub.10 aryl or heteroaryl as defined above;
• halogen;
• halo C.sub.1 -C.sub.6 alkyl;
• halo C.sub.1 -C.sub.6 alkoxy;
• carboxy;
• hydroxy(C.sub.1 -C.sub.6)alkyl;
• (C.sub.1 -C.sub.6 alkoxy)carbonyl;
• amino including substituted amino, e.g mono- or di- (C.sub.1 -C.sub.6 alkyl)-amino;
• nitro;
• hydroxy;
• mercapto;
• C.sub.1 -C.sub.6 alkylthio;
• (C.sub.1 -C.sub.6)alkyl carbonyl;
• (C.sub.6 -C.sub.10 aryl)carbonyl;
• (C.sub.2 -C.sub.7)alkanoyloxy;
• (C.sub.7 -C.sub.11 )aroyloxy;
• (C.sub.1 -C6)alkylcarbonylamino, (C.sub.6 -C.sub.10 aryl)carbonylamino;
• (C.sub.2 -C.sub.7) alkoxycarbonylamino;
• C.sub.6 -C.sub.10 aryl;
• heteroaryl as defined above;
• or C.sub.1 -C.sub.2 alkylenedioxy;
• R.sup.2 and R.sup.4 independently represent hydrogen, or a group of formula --CR.sup.a R.sup.b R.sup.c where R.sup.a, R.sup.b and R.sup.c are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl, optionally substituted C.sub.6 -C.sub.10 aryl, optionally substituted heteroaryl, C.sub.1 -C.sub.6 alkyl substituted by optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl in which the substituent(s) is/are for example as illustrated above in connection with R.sup.3 ;
• or R.sup.2 also represents COR.sup.11 where R.sup.11 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or an optionally substituted (C.sub.6 -C.sub.10 aryl)alkyl or a heteroaryl alkyl radical;
• said heteroaryl group containing 5 to 10 ring atoms of which one or more (e.g up to 3) of said atoms are heteroatoms selected from oxygen, nitrogen and sulphur, the same or different;
• said aryl or heteroaryl radicals being optionally substituted by one or more substituents the same or different, eg substituents commonly used in pharmaceutical chemistry such as for example:
• C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, or such groups substituted by C.sub.6 -C.sub.10 aryl or heteroaryl as defined above;
• halogen;
• halo C.sub.1 -C.sub.6 alkyl, halo C.sub.1 -C.sub.6 alkoxy;
• carboxy;
• hydroxy(C.sub.1 -C.sub.6)alkyl C.sub.2 -C.sub.7 alkanoyloxy(C.sub.1 -C.sub.6)alkyl;
• (C.sub.1 -C.sub.6 alkoxy)carbonyl;
• amino including substituted amino, e.g mono- or di- (C.sub.1 -C.sub.6 alkyl)-amino;
• nitro;
• hydroxy;
• mercapto;
• C.sub.1 -C.sub.6 alkylthio;
• (C.sub.1 -C.sub.6 alkyl)carbonyl;
• (C.sub.6 -C.sub.10 aryl)carbonyl;
• (C.sub.2 -C.sub.7)alkanoyloxy;
• (C7-C.sub.11 )aroyloxy;
• (C.sub.1 -C.sub.6 alkyl)carbonylamino, (C.sub.6 -C.sub.10 aryl)carbonylamino;
• (C.sub.2 -C.sub.7 alkoxycarbonyl)amino;
• C.sub.6 -C.sub.10 aryl;
• heteroaryl as defined above;
• or C.sub.1 -C.sub.2 alkylenedioxy;
• one of Y and Y.sub.1 is ##STR22## where R.sup.13 represents hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.7 -C.sub.16 aralkyl;
• the other of Y and Y.sub.1 is --CHR.sup.12 -- where R.sup.12 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.7 -C.sub.16 aralkyl, or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.