Benzodiazepine analogs

A compound of Formula:

• ##STR11## wherein:
• R.sup.1 is H, C.sub.1 -C.sub.6 linear or branched alkyl, loweralkenyl, lower alkynyl, X.sup.12 -COOH, --X.sup.12 COOR.sup.6, --X.sup.11 -cycloloweralkyl, --X.sup.12 NR.sup.4 R.sup.5, --X.sup.12 CONR.sup.4 R.sup.5, --X.sup.12 CN, or --X.sup.11 CX.sub.3.sup.10 ;
• R.sup.2 is H, loweralkyl, substituted or unsubstituted phenyl (wherein the substituents may be 1 or 2 of halo, loweralkyl, loweralkoxy, loweralkythio, carboxyl, carboxyloweralky, nitro, --CF.sub.3, or hydroxy), 2-,3-, or 4-pyridyl;
• R.sup.3 is ##STR12## --NH(CH.sub.2).sub.2 --.sub.3 NHCOR.sup.7, ##STR13## --X.sup.11 NR.sup.18 SO.sub.2 (CH.sub.2).sub.q R.sup.7 ;
• R.sup.4 and R.sup.5 are independently H or R.sup.6 or in combination with the N of the NR.sup.4 R.sup.5 group form an unsubstituted or mono or disubstituted, saturated or unsaturated, 4-7 membered heterocyclic ring, wherein said heterocyclic ring may contain a second heteroatom selected from O and NCH.sub.3 and the substituents(s) is/are independently selected from C.sub.1 -C.sub.4 alkyl;
• R.sup.6 is loweralkyl, cycloloweralkyl, substituted or unsubstituted phenyl, or substituted or unsubstituted phenylloweralkyl wherein the phenyl or phenylloweralkyl substituents may be 1 or 2 of halo, loweralkyl, loweralkoxy, nitro, or CF.sub.3 ;
• R.sup.7 is ##STR14## R.sup.8 is H, loweralkyl, cycloloweralkyl, --X.sup.13 CONH.sub.2, --X.sup.13 COOR.sup.6, --X.sup.13 COOH, --X.sup.13 -cycloloweralkyl, or --X.sup.13 NR.sup.4 R.sup.5,
• R.sup.15 is H, or loweralkyl,
• R.sup.18 is H or loweralkyl;
• n is 1-6,
• 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, --X.sup.11 COOR.sup.6, X.sup.11 COOH, or --X.sup.11 NR.sup.4 R.sup.5,
• X.sup.2 is H or X.sup.3, with the proviso that when X.sup.2 is H, then X.sup.4 is NX.sup.5 COOH or NX.sup.5 COOR.sup.6 wherein X.sup.5 is a linear alkyl chain of 2 to 6 carbon atoms, any carbon atom of which may be additionally substituted with a linear or branched alkyl group of 1 to 3 carbon atoms;
• X.sup.3 is O(CH.sub.2).sub.n COOR.sup.6, O(CH.sub.2).sub.n COOH, (CH.sub.2).sub.n COOR.sup.6, (CH.sub.2).sub.n COOH, COOR.sup.6, or X.sup.12 OR.sup.6 ;
• X.sup.4 is S,O, CH.sub.2, or NR.sup.8 ;
• X.sup.7 is O,S, HH, or NR.sup.15 with the proviso that X.sup.7 can be NR.sup.15 only when R.sup.1 is not H;
• X.sup.8 is H, loweralkyl;
• X.sup.9 and X.sub.a.sup.9 are independently NR.sup.18 or O;
• X.sup.10 is F, Cl, or Br;
• X.sup.11 is absent or C.sub.1-4 linear or branched alkyl alkylidene;
• X.sup.12 is C.sub.1-4 linear or branched alkylidene,
• X.sup.13 is linear or branched alkylidene.