abstract |
The invention concerns a compound of the structuren n wherein R¹ and R² are each, independently, hydrogen, n-CONH-[(CR³R⁴) m (-A-(CR⁵R⁶) n ) p ] q -B;n n R³, R⁴, R⁵, R⁶, R⁹ and R 1O are each defined substitutents, and R³⁻⁶ may each also represent hydrogen, nB 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, -OR⁷, -SR⁷, -CN, -COR⁷, -CONHR⁷, -OSO₃R⁷, -NR⁷R⁸, -NHCOR⁷, -NHSO₂R⁷, or Ar; nA is -CH₂-, -NR⁷-, -O-, -S-, -SO-, -PR⁷-, -NHCO-, -NHSO- or -P(O)(R⁷)-; nAr is naphthyl, pyridyl, quinolyl, isoquinolyl, quinoxalyl, thienyl, thionaphthyl, furyl, benzofuryl, benzodioxyl, benzoxazolyl, benzoisoxazolyl, indolyl, thiazolyl, isoxazolyl, pyrimidinyl, pyrazinyl, imidazolyl, benzopyranyl, benz[b]thiophenolyl, 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; nPO₃H, and -CO₂H;n n 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 R¹ and R² are not both hydrogen; nm=0-6; n=0-6; p=0-1; q=0-1; nor a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent. |