Patent ID: 6153640
Filing Date: 2000-11-28
Classification: A61P,C07D

Abstract:
A compound, with a cis ring junction, selected from those of the formula (I): ##STR22## wherein: R.sub.1, R.sub.2 and R.sub.3, which may be the same or different, each independently of the others represents a substituent selected from hydrogen, halogen, linear or branched (C.sub.1 -C.sub.6)alkyl, linear or branched (C.sub.2 -C.sub.6)alkenyl, linear or branched (C.sub.2 -C.sub.6)alkynyl, hydroxy, linear or branched (C.sub.1 -C.sub.6)alkoxy, cycloalkyl, cycloalkyl-(C.sub.1 -C.sub.6)alkyl in which alkyl is linear or branched, aryl, aryl-(C.sub.1 -C.sub.6)alkyl in which alkyl is linear or branched, aryloxy, aryl-(C.sub.1 -C.sub.6)alkoxy in which alkoxy is linear or branched, linear or branched (C.sub.1 -C.sub.6)trihaloalkyl, linear or branched (C.sub.1 -C.sub.6)trihaloalkoxy, cyano, nitro, --OSO.sub.2 CH.sub.3, --OSO.sub.2 CF.sub.3, --NR.sub.6 R.sub.7, and --CO.sub.2 R.sub.6 wherein R.sub.6 and R.sub.7, which may be the same or different, each independently of the other represents a substituent selected from hydrogen, linear or branched (C.sub.1 -C.sub.6)alkyl, linear or branched (C.sub.2 -C.sub.6)alkenyl, linear or branched (C.sub.2 -C.sub.6)alkynyl, cycloalkyl, cycloalkyl-(C.sub.1 -C.sub.6)alkyl in which alkyl is linear or branched, aryl, and aryl-(C.sub.1 -C.sub.6)alkyl in which alkyl is linear or branched, or two of R.sub.1, R.sub.2 and R.sub.3 in adjacent positions represent, together with common atoms of the benzene ring to which they are bonded, a saturated or unsaturated (C.sub.4 -C.sub.8)-ring wherein one or two carbon is/are optionally replaced by one or two hetero atoms, which may be the same or different, selected from oxygen, nitrogen, and sulphur, it being understood that in the case where two of R.sub.1, R.sub.2 and R.sub.3 in adjacent positions have the meaning mentioned hereinbefore, the remaining substituent R.sub.1 or R.sub.2 or R.sub.3 takes one of the above-mentioned individual definitions of those substituents,R.sub.4 represents a group selected from hydrogen, linear or branched (C.sub.1 -C.sub.6)alkyl, linear or branched (C.sub.2 -C.sub.6)alkenyl, linear or branched (C.sub.2 -C.sub.6)alkynyl, cycloalkyl, cycloalkyl-(C.sub.1 -C.sub.6)alkyl in which alkyl is linear or branched, aryl, aryl-(C.sub.1 -C.sub.6)alkyl in which alkyl is linear or branched, heterocycloalkyl, heterocycloalkyl-(C.sub.1 -C.sub.6)alkyl in which alkyl is linear or branched, heteroaryl, and heteroaryl-(C.sub.1 -C.sub.6)alkyl in which alkyl is linear or branched,R.sub.5 represents a group selected from aryl, optionally substituted aryl, heteroaryl, and optionally substituted heteroaryl,n represents an integer of 1 to 3 inclusive,its isomers and addition salts thereof with a pharmaceutically-acceptable acid or base,cycloalkyl being understood to mean a (C.sub.3 -C.sub.8)-ring, which may be mono- or bi-cyclic, optionally having one or more unsaturated bond(s), the said unsaturated bond(s) not conferring an aromatic character on the ring, which is optionally substituted by one or more substituents, which may be the same or different, selected from halogen, and linear or branched (C.sub.1 -C.sub.6)alkyl,heterocycloalkyl being understood to mean optionally substituted cycloalkyl as defined hereinbefore and containing, in the ring, one, two or three hetero atoms, which may be the same or different, selected from oxygen, nitrogen, and sulphur,furthermore, aryl being understood to mean phenyl, naphthyl, dihydronaphthyl, tetrahydronaphthyl, indenyl, or indanyl, and optionally substituted aryl being understood to mean aryl, as defined hereinbefore, optionally substituted by one or more substituents, which may be the same or different, selected from halogen, hydroxy, linear or branched (C.sub.1 -C.sub.6)alkyl, linear or branched (C.sub.1 -C.sub.6)alkoxy, linear or branched (C.sub.1 -C.sub.6)alkenyl, cycloalkyl, adamantyl, cycloalkyl-(C.sub.1 -C.sub.6)alkyl in which alkyl is linear or branched, aryl, aryl-(C.sub.1 -C.sub.6)alkyl in which alkyl is linear or branched, aryloxy, aryl-(C.sub.1 -C.sub.6)alkoxy in which alkoxy is linear or branched, linear or branched (C.sub.1 -C.sub.6)trihaloalkyl, linear or branched (C.sub.1 -C.sub.6)trihaloalkoxy, cyano, nitro, oxo, --OSO.sub.2 CH.sub.3, --OSO.sub.2 CF.sub.3, --NR.sub.6 R.sub.7, and --CO.sub.2 R.sub.6 wherein R.sub.6 and R.sub.7 are as defined hereinbefore for formula (I),heteroaryl being likewise understood to mean aryl as defined hereinbefore containing one, two, or three heteroatoms, which may be the same or different, selected from oxygen, nitrogen, and sulphur, and optionally substituted heteroaryl being understood to mean heteroaryl as defined hereinbefore optionally substituted by one or more substituents; which may be the same or different, as defined for substitutes of aryl.