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filingDate 1991-09-19-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1992-02-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber IE-913302-A1
titleOfInvention Aminoesters of rapamycin
abstract A compound of structure (I), wherein R<1>, R<2>, and R<3> are each, independently, hydrogen, or R<4>; R<4> is (a), (b), or (c); R<5> is hydrogen, alkyl, aralkyl, -(CH2)qCO2R<8>, -(CH2)rNR<9>CO2R<10>, carbamylalkyl, aminoalkyl, hydroxyalkyl, guanylalkyl, mercaptoalkyl, alkylthioalkyl, indolylmethyl, hydroxypehnylmethyl, imidazoylmethyl or phenyl which is optionally mono-, di-, or tri-substituted with a substituent selected from alkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, amino, or a carboxylic acid; R<6> and R<9> are each, independently, hydrogen, alkyl, or aralkyl; R<7>, R<8>, and R<10> are each, independently, alkyl, aralkyl, fluorenylmethyl, or phenyl which is optionally mono-, di-, or tri-substituted; R<11> and R<12> are each, independently, alkyl, aralkyl, or phenyl which is optionally mono-, di-, or tri-substituted; X is (d), O, or S; R<13? and R?14> are each, independently, hydrogen or alkyl; Y is CH or N; m is 0-4; n is 0-4; p is 1-2; q is 0-4; r is 0-4; t is 0-4; u is 0-4; wherein R<5>, R<6>, m, and n are independent in each of (e) subunits when p=2; or a pharmaceutically acceptable salt thereof, with the proviso that R<1>, R<2>, and R<3> are not all hydrogen, further provided that R<1>, R<2> and R<3> are not all (a), and still further provided that t and u are not both 0 when X is O or S, which by virtue of its immuno-suppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases, and diseases of inflammation, and by virtue of its antifungal activity is useful in treating fungal infections.
priorityDate 1990-09-19-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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