Compounds of formula (I), are cannabinoid CB1 receptors, useful, inter
alia in the treatment of obesity:
wherein A.sub.1 is hydrogen, --COOH, or tetrazolyl, and A.sub.2 is
hydrogen, --COOH, tetrazolyl, --CN, --CF.sub.3, --COR.sub.6,
--SO.sub.2R.sub.6, --OR.sub.7, --NR.sub.7R.sub.8, --NHCOR.sub.6, and
--NR.sub.7SO.sub.2R.sub.8 provided that one of A.sub.1 and A.sub.2 is
either --COOH or tetrazolyl; p is 0 or 1 and A.sub.3 is phenyl or
cycloalkyl, either of which is optionally substituted with R.sub.4 and/or
R.sub.5; q is 0 or 1; R.sub.1 is a bond, or
--(CH.sub.2).sub.aB.sub.1(CH.sub.2).sub.b-- wherein a and b are
independently 0, 1, 2 or 3 provided that a+b is not greater than 4, and
B.sub.1 is --CO--, --O--, --S--, --SO--, --SO.sub.2--, --CH.sub.2--,
--CHOH-- or --NR.sub.7--; R.sub.2 is a bond,
--CH.sub.2).sub.aB.sub.1(CH.sub.2).sub.b-- or
--[(CH.sub.2).sub.aB.sub.1(CH.sub.2).sub.b].sub.n-A.sub.4-[(CH.sub.2).sub-
.cB.sub.2(CH.sub.2).sub.d].sub.m-- wherein a, b, and B.sub.1 are as
defined for R.sub.1; B.sub.2 is as defined for B.sub.1, c and d are
independently 0, 1, 2 or 3; with the proviso that a+b+c+d is not greater
than 6, n and m are independently 0 or 1 and A.sub.4 is a monocarbocyclic
or monoheterocyclic ring, having 3 to 8 ring atoms, optionally
substituted with one or more of --F, --Cl, --Br, --CN, --CF.sub.3,
C.sub.1-C.sub.4 alkyl, cycloalkyl, --OR.sub.9, oxo or --NR.sub.7R.sub.8;
R.sub.3 is hydrogen, C.sub.1-C.sub.4 alkyl, cycloalkyl, --CF.sub.3,
--OR.sub.9, --NR.sub.7R.sub.8, --(CH.sub.2).sub.sCOR.sub.6,
--(CH.sub.2).sub.sSO.sub.2R.sub.6, --(CH.sub.2).sub.sNR.sub.7COR.sub.6,
--(CH.sub.2).sub.sNR.sub.7COOR.sub.8,
--(CH.sub.2).sub.sNR.sub.7SO.sub.2R.sub.6, wherein s is 1, 2, 3 or 4;
R.sub.4 and R.sub.5 independently --R.sub.9, --CN, --F, --Cl, --Br,
--OR.sub.9, --NR.sub.7R.sub.8, --NR.sub.7COR.sub.6,
--NR.sub.7SO.sub.2R.sub.6, --COR.sub.6, --SR.sub.9, --SOR.sub.9,
--SO.sub.2R.sub.6, (C.sub.1-C.sub.4 alkyl)OR.sub.9, --(C.sub.1-C.sub.4
alkyl)NR.sub.7R.sub.8, --(C.sub.1-C.sub.4 alkyl)NR.sub.7COR.sub.6,
C.sub.1-C.sub.4 alkyl)NR.sub.7COOR.sub.8, --(C.sub.1-C.sub.4
alkyl)NR.sub.7SO.sub.2R.sub.6, --(C.sub.1-C.sub.4 alkyl)COR.sub.6,
--(C.sub.1-C.sub.4 alkyl)SO.sub.2R.sub.6, --NR.sub.7COOR.sub.8, or
[N--(C.sub.1-C.sub.4 alkyl)]-tetrazolyl; R.sub.6 is C.sub.1-C.sub.4
alkyl, cycloalkyl, --CF.sub.3 or --NR.sub.7R.sub.8; R.sub.7 and R.sub.8
are independently hydrogen, C.sub.1-C.sub.4 alkyl or cycloalkyl; and
R.sub.9 is hydrogen, C.sub.1-C.sub.4 alkyl, cycloalkyl, fully or
partially fluorinated C.sub.1-C.sub.4 alkyl.
