Rapamycin oximes and hydrazones

A compound of the structure ##STR12## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONH.sub.a --{{(CR.sup.3 R.sup.4).sub.m (--A--(CR.sup.5 R.sup.6).sub.n).sub.p }.sub.q --B}.sub.r ;

• --SO.sub.2 R.sup.7 ;
• --SO.sub.3 H;
• --CHR.sup.8 O(CH.sub.2).sub.t R.sup.9 ;
• or ##STR13## R.sup.3, R.sup.4, R.sup.5, R.sup.6, and B are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, hydroxyalkyl of 1-6 carbon atoms, alkoxyalkyl of 2-12 carbon atoms, alkylthioalkyl of 2-12 carbon atoms, alkylaminoalkyl of 2-12 carbon atoms, dialkylaminoalkyl of 3-12 carbon atoms, arylalkyl of 7-10 carbon atoms, cycloalkyl of 3-8 carbon atoms, --OR.sup.10, --SR.sup.10, halogen, --CN, --NO.sub.2, --CF.sub.3, --COR.sup.10, --CO.sub.2 R.sup.10, --CONHR.sup.10, --SO.sub.2 R.sup.10, --OSO.sub.3 R.sup.10, --NR.sup.10 R.sup.11, --NHCOR.sup.10, --NHSO.sub.2 R.sup.10, or Ar;
• X is .dbd.NOR.sup.12 or .dbd.NNR.sup.12 R.sup.13 ;
• Y is O, .dbd.NOR.sup.12, or .dbd.NNR.sup.12 R.sup.13 ;
• R.sup.7, R.sup.12, and R.sup.13 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, arylalkyl of 7-10 carbon atoms, or Ar;
• R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, arylalkyl of 7-10 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, hydroxyalkyl of 1-6 carbon atoms, alkoxyalkyl of 2-12 carbon atoms, alkylthioalkyl of 2-12 carbon atoms, alkylaminoalkyl of 2-12 carbon atoms, dialkylaminoalkyl of 3-12 carbon atoms, cycloalkyl of 3-8 carbon atoms, or Ar;
• A is --CH.sub.2 --, --NR.sup.10 --, --O--, --S--, --SO--, --SO.sub.2 --, --PR.sup.10 --, --CO--, --NHCO--, --NHSO--, or --P(O)(R.sup.10)--;
• Ar is aryl which may be optionally mono-, di-, or tri- substituted with a group selected from alkyl of 1-6 carbon atoms, arylalkyl of 7-10 carbon atoms, alkoxy of 1-6 carbon atoms, cyano, halo, hydroxy, nitro, carbalkoxy of 2-7 carbon atoms, trifluoromethyl, amino, dialkylamino of 1-6 carbon atoms per alkyl group, dialkylaminoalkyl of 3-12 carbon atoms, hydroxyalkyl of 1-6 carbon atoms, alkoxyalkyl of 2-12 carbon atoms, alkylthio of 1-6 carbon atoms, --SO.sub.3 H, --PO.sub.3 H, and --CO.sub.2 H;
• ##STR14## is a nitrogen containing heterocyclic radical selected from the group consisting of pyridyl, pyrazinyl, piperidinyl, morpholinyl, piperazinyl, pyrrolidinyl, thiazolyl, pyrimidinyl, isoxazolyl, pyrrolidinyl, and imidazolyl that may be optionally mono-, di-, or tri-substituted with a group selected from alkyl of 1-6 carbon atoms, arylalkyl of 7-10 carbon atoms, alkoxy of 1-6 carbon atoms, cyano, halo, hydroxy, nitro, carbalkoxy of 2-7 carbon atoms, trifluoromethyl, amino, dialkylamino of 1-6 carbon atoms per alkyl group, dialkylaminoalkyl of 3-12 carbon atoms, hydroxyalkyl of 1-6 carbon atoms, alkoxyalkyl of 2-12 carbon atoms, alkylthio of 1-6 carbon atoms, --SO.sub.3 H, --PO.sub.3 H, and --CO.sub.2 H;
• a=0-1;
• m=0-6;
• n=0-6;
• p=0-1;
• q=0-1;
• r=1-2;
• and
• t=1-4;
• wherein R.sup.3, R.sup.4, R.sup.5, R.sup.6, A, B, m, n, p, and q are independent in each of the --CON--{{(CR.sup.3 R.sup.4).sub.m (--A--(CR.sup.5 R.sup.6).sub.n).sub.p }.sub.q --B}.sub.r subunits when r=2;
• with the proviso that R.sup.1 and R.sup.2 are not both hydrogen, and further provided that if r=2, then a=0, and if r=1, then a=1;
• or a pharmaceutically acceptable salt thereof.