Triazolobenzodiazepines and pharmaceutical use

A compound of the formula:

• ##STR28## wherein R.sup.1 is H, OH, loweralkyl, cycloloweralkyl, loweralkynyl, loweralkenyl, substituted or unsubstituted phenyl(wherein the substituents are 1 or 2 of halo, loweralkyl, loweralkoxy, or hydroxy), --(CH.sub.2).sub.m NR.sup.4 R.sup.5, CX.sub.3.sup.10, or --(CH.sub.2).sub.n COOR.sup.6 ;
• R.sup.2 is H, loweralkyl, substituted or unsubstituted phenyl (wherein the substitutents are 1 or 2 of halo, loweralkyl, loweralkoxy, loweralkylthio, carboxyl, carboxyloweralkyl, nitro, --CF.sub.3, ##STR29## or hydroxy), or --(CH.sub.2).sub.m COOR.sup.6 ;
• R.sup.3 is --(CH.sub.2).sub.n R.sup.7, ##STR30## R.sup.4 and R.sup.5 are independently H, loweralkyl, or cycloloweralkyl or are connected to form a hetero ring ##STR31## wherein n is 2-6;
• R.sup.6 is H, loweralkyl, cycloloweralkyl, substituted or unsubstituted phenyl (wherein the substituents are 1 or 2 of halo, loweralkyl, loweralkoxy, nitro, or CF.sub.3), or substituted or unsubstituted phenylloweralkyl (wherein the substituents are 1 or 2 of halo, loweralkyl, loweralkoxy, nitro, or CF.sub.3);
• R.sup.7 and R.sub.a.sup.7 are independently .alpha.- or .beta.-naphthyl, substituted or unsubstituted phenyl (wherein the substituents are 1 to 2 of halo, --NO.sub.2, --OH, --NR.sup.4 R.sup.5, cyano, phenyl, trifluoromethyl, acetylamino, acetyloxy, loweralkylthio, SCF.sub.3, --C.tbd.CH, CH.sub.2 SCF.sub.3, OCHF.sub.2, SH, S-phenyl, PO.sub.3 H, or loweralkoxy), ##STR32## (with the proviso that q is not 0 or 1 in --(CH.sub.2).sub.n NH(CH.sub.2).sub.q R.sup.7 and that q is not 0 in ##STR33## when R.sup.7 or R.sub.a.sup.7 is ##STR34## R.sup.8 is H, loweralkyl, cycloloweralkyl, --(CH.sub.2).sub.m CONH.sub.2, --(CH.sub.2).sub.m COOR.sup.6, --(CH.sub.2).sub.n -cycloloweralkyl, --(CH.sub.2).sub.m NR.sub.4 R.sub.5, ##STR35## R.sup.9 and R.sup.10 are independently H, --OH, or --CH.sub.3 ;
• R.sup.11 and R.sup.12 are independently loweralkyl or cycloloweralkyl;
• R.sup.13 is H, loweralkyl, acyl, O, or cycloloweralkyl;
• R.sup.14 is loweralkyl or phenylloweralkyl;
• R.sup.18 is H, loweralkyl, or acyl;
• m is 1-4;
• n is 0-4;
• p is 0 when its adjacent is unsaturated or when R.sup.3 is =CHR.sup.7, and it is 1 when its adjacent is saturated, except that when R.sup.13 is O, p=1 and is unsaturated;
• q is 0-4;
• r is 1 or 2;
• X.sup.1 is H, --NO.sub.2, CF.sub.3 CN, OH, loweralkyl, halo, loweralkylthio, loweralkoxy, --(CH.sub.2).sub.n COOR.sup.6, --NR.sup.4 R.sup.5, or ##STR36## X.sup.2 and X.sup.3 are independently H, --OH, --NO.sub.2, halo, loweralkylthio, loweralkyl, loweralkoxy or ##STR37## X.sup.4 is S, O, CH.sub.2, or NR.sup.8 ;
• X.sup.5 is H, CF.sub.3, CN, --COOR.sup.6, NO.sub.2, or halo;
• X.sup.6 is O or HH;
• X.sup.8 is H or loweralkyl;
• X.sup.9 and X.sub.a.sup.9 are independently NR.sup.18, O
• X.sup.10 is F, Cl, Br;
• is a saturated or unsaturated bond, such that both bonds in the seven-membered ring of Formula I may be saturated (single bonds), but both may not be unsaturated (double bonds),
• and the pharmaceutically acceptable salts thereof.