CARBAMATE VON RAPAMYCIN

The invention concerns a compound of the structure wherein R and R are each, independently, hydrogen, -CONH-Ä(CR R )m(-A-(CR R )n)pÜq-B; R , R , R , R , R and R are each defined substitutents, and R may each also represent hydrogen, B is alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, hydroxyalkyl of 1-6 carbon atoms, alkylthioalkyl of 2-12 carbon atoms, alkylaminoalkyl of 2-12 carbon atoms, dialkylaminoalkyl of 3-12 carbon atoms, -OR , -SR , -CN, -COR , -CONHR , -OSO3R , -NR R , -NHCOR , -NHSO2R , or Ar; A is -CH2-, -NR -, -O-, -S-, -SO-, -PR -, -NHCO-, -NHSO- or -P(O)(R )-; Ar is naphthyl, pyridyl, quinolyl, isoquinolyl, quinoxalyl, thienyl, thionaphthyl, furyl, benzofuryl, benzodioxyl, benzoxazolyl, benzoisoxazolyl, indolyl, thiazolyl, isoxazolyl, pyrimidinyl, pyrazinyl, imidazolyl, benzopyranyl, benzÄbÜthiophenolyl, benzimidazolyl, benzthiazolyl, benzodioxolyl, piperidinyl, morpholinyl, piperazinyl, tetrahydrofuranyl, or pyrrolidinyl; wherein the Ar group 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, -SO3H -PO3H, and -CO2H; PO3H, and -CO2H; is a nitrogen containing heterocycle that may be saturated, unsaturated, or partially unsaturated, and may be optionally mono-, di-, or tri- substituted with a defined substituent, with the proviso that R and R are not both hydrogen; m=0-6; n=0-6; p=0-1; q=0-1; or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.