| abstract |
The present invention provides an adenosine A1 agonist for compounds of formula Ia wherein X is O or methylene; R1 (i) is cycloalkyl (alk) n or cycloalkenyl (alk) n, wherein the cycloalkyl or cycloalkenyl is optionally substituted with one or more halogen, hydroxy, alkyl, alkoxy, alkenyloxy, alkynyl, substituted by oxy and / or phenyl, and wherein (alk) is (C 1 -C 3) alkyl and n is 0 or 1, wherein (alk) is optionally substituted by cycloalkyl; (ii) phenyl optionally substituted with one or more atoms and / or groups selected from halogen, trifluoromethyl, cyano, alkyl, alkenyl, alkynyl, alkoxy, hydroxyalkyl, carboxy; and / or alkoxycarbonyl; (iii) at least one heteroatom-containing heterocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur optionally substituted by one or more groups selected from hydroxy, alkyl, alkoxy, alkoxycarbonyl, alkyl-; carbonyl, (aryloxy) carbonyl or -CO2 (alk) n-cycloalkyl wherein (alk) is (C1-C3) alkyl and n is 0 or 1; (iv) a linear or branched alkyl group optionally substituted with one or more halogen, hydroxy or cycloalkyl groups, and wherein optionally one or more carbon atoms of the alkyl group are independently substituted with S (= O) and / or nitrogen; n is 0, 1 or 2; (v) a group derived from a fused bicyclic ring of formula wherein A is a cycloalkane ring or a benzene ring and B is an optionally substituted benzene ring and the bicyclic ring system is attached to the 6-aminopurine moiety through an atom of ring A; R2 is hydrogen, halogen, alkyl or alkoxy; R 3 and R 4 are hydrogen, alkyl and their pharmaceutically acceptable derivatives, their pharmaceutical uses and pharmaceutical compositions containing the compounds. HE |