Use of xanthines as immunosuppressants and to inhibit allograft reactions
A family of compounds effective in suppressing lymphocyte activation is comprised of 7-(oxoalkyl)1,3-dialkyl xanthines, other than denbufylline, of the formula in which R1 and R2 are the same or different and are selected from the group consisting of straight-chain or branched alkyl radicals with 2 to 6 carbon atoms, cyclohexyl, alkoxyalkyl and hydroxyalkyl radicals, and A represents a hydrocarbon radical with up to 4 carbon atoms which can be substituted by a methyl group. Another family of effective compounds is comprised of compounds of the formula wherein at least one of R1 and R3 is eithera) a branched hydroxyalkyl group of the formula in which R4 stands for an alkyl group with 1 to 3 carbon atoms and n stands for a whole number from 2 to 5, the other R1 or R3 group that lay optionally be present stands for a hydrogen atom or an aliphatic hydrocarbon group R5 with up to 6 carbon atoms, whose carbon chain may be interrupted by up to 2 oxygen atoms or may be substituted with a hydroxy or oxo group, orb) an oxoallyl group of the formula wherein R6 is C1-C6 and p is 2, 3 or 4, the remaining R1 or R3 being as defined above, and R2 is an alkyl group C1-C4; The suppression of lymphocyte activation is indicated in humans afflicted with autoimmune disease.
Fred Hutchinson Cancer Research Center
A A
A61K A61K
inventional inventional
Jack W. James A. William J.
Singer Bianco Novick, Jr.