Treating psoriasis with transient pro-drug forms of xanthine derivatives

Abstract

Abstract Compounds of the formula: ##STR1## wherein R, which may be the same or different, represents a member selected from the group consisting of --CH 3 , --C 2 H 5 , --C 3 H 7 , iso--C 3 H 7 , --C 4 H 9 , iso--C 4 H 9 , pentyl, benzyl, allyl, 2-hydroxyethyl, cyclohexyl, 2-isobutenyl, hydroxymethyl, 2-phenylethyl and -CH 2 O-R 2 , wherein R 2 is defined infra; wherein R 1 represents a member selected from the group consisting of H, C 1 -C 7 straight or branched alkyl, CCl 3 , CBr 3 , CI 3 , ##STR2## CH 3 O--CH 2 --, (CH 3 ) 2 NCH 2 --, ##STR3## wherein R 3 represents a member selected from the group consisting of -OH, halogen (Cl, Br, I), --OCH 3 , -COOCH 3 , -NO 2 and -OCOCH 3 ; wherein ##STR4## and wherein R 2 represents a member selected from the group consisting of ##STR5## wherein R 4 is a member selected from the group consisting of C 2 -C 20 straight or branched alkyl (C 3 -C 7 preferred), --[--(CH 2 ) m --], wherein m represents an integer of from 0 to 10, ##STR6## wherein R 3 is defined as above, ##STR7## the residue of any naturally occurring amino acid, the residue of any N- substituted amino acid, wherein said substituent is any amino acid protective group cleavable via hydrogenolysis or hydrolysis (e.g., formyl, benzyloxy, carbonyl, t-butyloxycarbonyl), the residue of an N,N-C 1 -C 5 -dialkyl or cycloalkylamino acid, ##STR8## wherein n represents an integer of from 1-5 and R 5 and R 6 which may be the same or different represent C 1 -C 5 alkyl or together form a heterocyclic ring with the N atom to which they are attached (e.g., pyrolidine, piperidine, morpholine, piperazine, imidazoline, thiazolidine, isoxazolidine), imidazolyl, O-C 1 -C 8 alkyl, O-benzyl, O-phenyl and ##STR9## wherein n, R 5 and R 6 are defined as above; and wherein R 2 further represents a member selected from the group consisting of straight or branched C 1 -C 20 alkyl, ##STR10## wherein n, R 5 and R 6 are defined as above, phenyl, tolyl, xylyl, and --SO 2 --R 7 , wherein R 7 is a straight or branched C 1 -C 20 alkyl useful in treating psoriasis in warm-blooded animals are provided.

Inventors

• 👤 Nicolae S. Bodor
• 👤 Kenneth B. Sloan

Bibliographic Details