A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/52 (2006.01) A61K 38/19 (2006.01)
Patent
CA 2056800
HOE 90/S 046 ABSTRACT OF THE DISCLOSURE A family of compounds effective in inhibiting the ef- fects of allograft reaction, such as graft versus host reac- tion (GVHR), in a human is comprised of 7-(oxoalkyl) 1,3- dialkyl xanthines of the formula Image (I) 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 Image (II) wherein at least one of R1 and R3 is either a) a branched hydroxyalkyl group of the formula Image , 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 and R3 group that may 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, or b) an oxoallyl group of the formula Image 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 inhibition of GVHR is indicated in human transplant recipients.
Bianco James A.
Novick William J. Jr.
Singer Jack W.
Bereskin & Parr
Fred Hutchinson Cancer Research Center (the)
Hoechst Marion Roussel Inc.
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