N9-cyclopentyl-substituted adenine derivatives

Details N9-cyclopentyl-substituted adenine derivatives N9-cyclopentyl-substituted adenine derivatives

C - Chemistry, Metallurgy

07

D

167/220, 260/242

C07D 473/00 (2006.01) A61K 31/52 (2006.01) C07D 303/46 (2006.01)

Patent

CA 1288431

4-16170/+/CGC 1233 N9-Cyclopentyl-substituted adenine derivatives Abstract: The compounds of the formula I Image (I) wherein R, R3 nd R5 independently represent hydrogen or hydroxy provided that at least one of R, R3 and R5 represents hydroxy; R1 represents hydrogen, lower alkyl, C3-C7alkenyl, hydroxy-lower alkyl, C3-C6cycloalkyl, C3-C6cycloalkyl-lower alkyl, 2-norbornyl, 2-nor- bornyl-lower alkyl, aryl, aryl-lower alkyl, aryl-C3-C6cycloalkyl, 9-fluorenyl or 9-fluorenyl-lower alkyl; or R1 represents a bicyclic benzo-fused 5 or 6-membered saturated carbocyclic radical or a benzo-fused 5 or 6-membered saturated heterocyclic radical containing a heteroatom selected from oxygen and sulfur directly attached to the fused benzene ring, any said bicyclic radicals being optionally substituted on the benzo portion by lower alkyl, lower alkoxy or halogen R2 represents hydrogen, halogen, -SR1 or -N(R9)R1 in each of which R1 has meaning as defined hereinbefore provided that R1 in -SR1 does not represent hydrogen; R9 represents hydrogen or lower alkyl; R4 represents hydroxymethyl provided that R2 does not represent either hydrogen or -NHR1 in which R1 represents either hydrogen or lower alkyl; or R4 represents lower alkoxymethyl, lower alkylthiomethyl or -CONHR6 in which R6 represents lower alkyl, aryl-lower alkyl, C3-C6cycloalkyl or hydroxy-lower alkyl; pharmaceutically acceptable ester derivatives thereof in which free hydroxy groups are esterified in form of a pharmaceutically acceptable ester; and salts thereof; methods for their preparation; and their use as adenosine receptor agonists are disclosed.

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