Patent ID: 6200985
Filing Date: 2001-03-13
Classification: A61P,C07D,C07F

Abstract:
A method for preventing or treating acute or chronic organ or tissue transplant rejection, or transplant vasculopathies in a subject in need of such treatment, which comprises administering to said subject an effective amount of a compound of formula I ##STR9##whereinR.sub.1 is alkyl, alkenyl, alkynyl, hydroxyalkyl, hydroxyalkenyl, hydroxyalkynyl, benzyl, alkoxybenzyl, or chlorobenzyl;R.sub.2 is selected from formula II or formula III: ##STR10##whereinR.sub.3 is H, alkyl, alkenyl, alkynyl, aryl, arylalkyl, hydroxyarylalkyl, hydroxyaryl, hydroxyalkyl, dihydroxyalkyl, hydroxyalkoxyalkyl, hydroxyalkylarylalkyl, dihydroxyalkylarylalkyl, alkoxyalkyl, alkylcarbonyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylaminoalkyl, alkylcarbonylaminoalkyl, arylsulfonamidoalkyl, allyl, dihydroxyalkylallyl, dioxolanylallyl, carbalkoxyalkyl, or alkylsilyl;R.sub.4 is H, methyl or together with R.sub.3 forms C.sub.2-6 alkylene;R.sub.5 is R.sub.6 O--CH.sub.2 --, wherein R.sub.6 is H, alkyl, alkenyl, alkynyl, aryl, alkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, hydroxyalkylcarbonyl, aminoalkylcarbonyl, formyl, arylalkyl, hydroxyarylalkyl, hydroxyaryl, hydroxyalkyl, dihydroxyalkyl, hydroxyalkoxyalkyl, hydroxyalkylarylalkyl, dihydroxyalkylarylalkyl, alkoxyalkyl, alkylcarbonyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxy-carbonylaminoalkyl, alkylcarbonylaminoalkyl, arylsulfonamidoalkyl, allyl, dihydroxyalkylallyl, dioxolanylallyl, or carbalkoxyalkyl;R.sub.7 CO--, wherein R.sub.7 is H, alkyl, hydroxy, alkoxy, aryloxy, amino, alkylamino, or N,N-disubstituted-amino wherein the substituents are alkyl, aryl, or arylalkyl;R.sub.8 NCH--, wherein R.sub.8 is alkyl, aryl, amino, alkylamino, arylamino, hydroxy, alkoxy, or arylsulfonylamino; or ##STR11##Y is O, (H, OH), or (H, C.sub.1-4 alkoxy); andX is OH or H;wherein ""alk"" or ""alkyl"" refers to a C.sub.1-10 aliphatic substituent optionally interrupted by an oxy linkage; and ""ar"" or ""aryl"" refers phenyl, benzyl, tolyl, and pyridyl, provided that, when X is OH, R.sub.1 is alkyl and R.sub.2 is a residue of formula 11, then R.sub.3 is other than H.