2-saccharinylmethyl phosphates, phosphonates and phosphinates useful as proteolytic enzyme inhibitors and compositions and method of use thereof

A compound having the formula ##STR21## wherein:

• R.sub.1 is hydrogen, halogen, lower-alkyl, perfluoro-lower-alkyl, perchloro-lower-alkyl, lower-alkenyl, lower-alkynyl, cyano, amino, lower-alkylamino, di-lower-alkylamino, carboxamido, lower-alkoxy, benzyloxy, hydroxy, lower-alkoxycarbonyl or phenyl;
• R.sub.2 and R.sub.3 are independently hydrogen or a substituent in any of the available 5-, 6- or 7-positions selected from the group consisting of halogen, cyano, nitro, N.dbd.B, 1-lower-alkyl-2-pyrrolyl, lower-alkylsulfonylamino, polyfluoro-lower-alkylsulfonylamino, polychloro-lower-alkylsulfonylamino, aminosulfonyl, lower-alkyl, polyfluoro-lower-alkyl, polychloro-lower-alkyl, cycloalkyl, lower-alkoxy, hydroxy, carboxy, carboxamido, hydroxy-lower-alkyl, formyl, aminomethyl, polyfluoro-lower-alkylsulfonyl, polychloro-lower-alkylsulfonyl, lower-alkylsulfonylaminosulfonyl, lower-alkoxy-poly-lower-alkyleneoxy, cycloalkyloxy, hydroxy-lower-alkoxy, benzyloxy-lower-alkoxy, polyhydroxyalkoxy, or acetal or ketal thereof, polyalkoxyalkoxy, (lower-alkoxy).sub.2 P(O)O--, --SR, --SOR, --SO.sub.2 R, --OCOR, --O--(C.sub.1-10 -alkylene)-COOR, --O--(C.sub.1-10 -alkylene)-COOH, --O--(C.sub.2-10 -alkylene)-N.dbd.B, --O--(CH.sub.2).sub.j OC(O)(CH.sub.2).sub.k --N.dbd.B, --O--(CH.sub.2).sub.j -[5-(CH.sub.2).sub.k --N.dbd.B-2-furanyl], --O--(CH.sub.2).sub.j --C.tbd.C--(CH.sub.2).sub.k --N.dbd.B', --O--(CH.sub.2).sub.j --CH.dbd.CH--(CH.sub.2).sub.k --N.dbd.B', where R is lower-alkyl, phenyl, benzyl or naphthyl, or phenyl or naphthyl substituted by from one to two substituents selected from lower-alkyl, lower-alkoxy or halogen, --N.dbd.B in each instance is amino, lower-alkylamino, di-lower-alkylamino, 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 1-piperazinyl, 4-lower-alkyl-1-piperazinyl, 4-benzyl-1-piperazinyl, 1-imidazolyl or (carboxy-lower-alkyl)amino, N.dbd.B' is amino, lower-alkylamino, di-lower-alkylamino, dibenzylamino, 1-azetidinyl, 1-pyrrolidnyl, 1-piperidinyl, 4-morpholinyl, 1-piperazinyl, 4-lower-alkyl-1-piperazinyl, 4-benzyl-1-piperazinyl, 1-imidazolyl, or --NR'(C.sub.2-10 -alkylene)-N(alkyl).sub.2 wherein R' is hydrogen or lower-alkyl, and j and k are independently an integer from 1 to 4;
• or R.sub.2 and R.sub.3 together represent a 3-atom or 4-atom unsubstituted or methylated saturated bridge bridging the carbon atoms at the 5,6 or 6,7 positions, wherein the atoms of the bridge consist of one or two carbon atoms and two of the same or different heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen;
• m and n are independently 0 or 1;
• when m and n are 1, A and B are independently hydrogen, lower-alkyl, phenyl, lower-alkoxyphenyl or benzyl, or, taken together, represent:
• ##STR22## where R.sub.7 and R.sub.8 are independently hydrogen or chlorine, R.sub.9 and R.sub.10 each is hydrogen or together represent isopropylidene, p is 0 or 1 and r is 2, 3 or 4;
• when m is 1 and n is 0, A and B are independently lower-alkyl, phenyl, benzyl or 2-pyridinyl;
• and
• when m and n are 0, A and B are independently lower-alkyl, phenyl or lower-alkoxyphenyl;
• or acid-addition salts of basic members thereof or base-addition salts of acidic members thereof.