Tricyclic diazepine vasopressin antagonists and oxytocin antagonists

A compound selected from Formula I:

• ##STR293## wherein;
• A--B is ##STR294## the moiety ##STR295## represents a fused phenyl or fused substituted phenyl optionally substituted by one or two substituents selected from (C.sub.1 -C.sub.3) lower alkyl, halogen, amino, (C.sub.1 -C.sub.3) lower alkoxy, or (C.sub.1 -C.sub.3) lower alkylamino;
• the moiety:
• ##STR296## is a five-membered aromatic (unsaturated) fused nitrogen-containing heterocyclic ring wherein D, E, and F are carbon and wherein the carbon atoms may be optionally substituted by a substituent selected from halogen, (C.sub.1 -C.sub.3) lower alkyl, hydroxy, COCCl.sub.3, COCF.sub.3, ##STR297## --CHO, amino, (C.sub.1 -C.sub.3) lower alkoxy, (C.sub.1 -C.sub.3) lower alkylamino, CONH (C.sub.1 -C.sub.3) lower alkyl, or --CON›lower alkyl (C.sub.1 -C.sub.3)!.sub.2,
• R.sub.b is independently selected from H, --CH.sub.3, or --C.sub.2 H.sub.5 ;
• q is 1 or 2;
• R.sup.3 is the moiety ##STR298## wherein Ar is a moiety selected from the group ##STR299## and X is selected from O, S, NH, --NCH.sub.3, or --N--COCH.sub.3 ;
• R.sub.4 is selected from H, lower alkyl (C.sub.1 -C.sub.3), --CO-lower alkyl (C.sub.1 -C.sub.3), SO.sub.2 lower alkyl (C.sub.1 -C.sub.3), or the moieties of the formulae:
• ##STR300## R.sub.1 and R.sup.2 are, independently, H, (C.sub.1 -C.sub.3) lower alkyl, (C.sub.1 -C.sub.3) lower alkoxy, or halogen;
• R.sub.5 is H, (C.sub.1 -C.sub.3) lower alkyl, (C.sub.1 -C.sub.3) lower alkoxy or halogen;
• R.sup.6 is selected from:
• (a) moieties of the formula:
• ##STR301## wherein cycloalkyl is defined as C.sub.3 to C.sub.6 cycloalkyl, cyclohexenyl or cyclopentenyl;
• n is 0-2;
• R.sub.a is independently selected from H, --CH.sub.3, --C.sub.2 H.sub.5, ##STR302## --(CH.sub.2)q-O-lower alkyl (C.sub.1 -C.sub.3), or --CH.sub.2 CH.sub.2 OH;
• R.sub.b is as hereinbefore defined;
• q is 1 or 2;
• (b) a moiety of the formula:
• ##STR303## where R.sub.2 is as hereinbefore defined;
• (c) a moiety of the formula:
• ##STR304## wherein J is R.sub.a,lower alkyl (C.sub.1 -C.sub.8) branched or unbranched, lower alkenyl (C.sub.2 -C.sub.8) branched or unbranched, --O-lower alkyl (C.sub.1 -C.sub.8) branched or unbranched, --O-lower alkenyl (C.sub.2 -C.sub.8) branched or unbranched, tetrahydrofuran, tetrahydrothiophene, or --CH.sub.2 --K wherein K is halogen, (C.sub.1 -C.sub.3) lower alkoxy, tetrahydrofuran, tetrahydrothiophene or the heterocyclic ring moiety:
• ##STR305## wherein D, E, F and G are selected from carbon or nitrogen and wherein the carbon atoms may be optionally substituted with halogen, (C.sub.1 -C.sub.3)lower alkyl, hydroxy, --CO-lower alkyl (C.sub.1 -C.sub.3), CHO, (C.sub.1 -C.sub.3)lower alkoxy, or --CO.sub.2 -lower alkyl (C.sub.1 -C.sub.3);
• and
• R.sub.a and R.sub.b are as hereinbefore defined;
• (d) a moiety selected from those of the formulae:
• ##STR306## wherein R.sub.c is selected from halogen, (C.sub.1 -C.sub.3)lower alkyl, --O-lower alkyl (C.sub.1 -C.sub.3), OH ##STR307## q is 1 or 2;
• R.sub.a and R.sub.b are as hereinbefore defined;
• wherein Ar' is selected from the group:
• ##STR308## wherein W' is selected from O, S, NH, N-lower alkyl (C.sub.1 -C.sub.3), --NHCO-lower alkyl (C.sub.1 -C.sub.3), or NSO.sub.2 -lower alkyl (C.sub.1 -C.sub.3);
• R.sup.7 is selected from H, lower alkyl (C.sub.1 -C.sub.3), halogen, --O-lower alkyl (C.sub.1 -C.sub.3), or CF.sub.3 ;
• R.sup.8 and R.sup.9 are independently selected from hydrogen, lower alkyl (C.sub.1 -C.sub.3), S-lower alkyl (C.sub.1 -C.sub.3), halogen, --NH-lower alkyl (C.sub.1 -C.sub.3), --OCF.sub.3, --CN, --OH, --S--CF.sub.3, --NO.sub.2, NH.sub.2, or --O-lower alkyl (C.sub.1 -C.sub.3);
• R.sup.10 is H, halogen, or lower alkyl-(C.sub.1 -C.sub.3);
• and the pharmaceutically acceptable salts, esters and pro-drug forms thereof.