Azole derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 487/04 (2006.01) A61K 31/53 (2006.01) A61K 31/70 (2006.01) C07H 15/26 (2006.01)

Patent

CA 2082462

A B S T R A C T Compounds of the formula I:- Image I wherein: X is O, S or N:H; n is O or an integer of from 1 to 3; R1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl; R2 is CH2R3, NHR4, SO2NR5YNR6R7 or R8, in which R3 is hydroxy, (1-4C)alkoxy or (1-4C)alkylsulphonyl; R4 is (1-4C)alkylsulphonyl, (1-4C)haloalkylsulphonyl, formyl, carbamoyl or 2,6-dichloro-4-(2-(1,1- dimethylethyl)amino-1-hydroxyethyl)phenyl; R5 is hydrogen or (1-4C)alkyl; Y is CO or (1-6C)alkylene; R6 and R7 are independently (1-4C)alkyl, or R6 is hydrogen and R7 is (1-4C)alkyl, (1-4C)haloalkyl, phenyl(1-4C)alkyl or, when Y is (1-6C)alkylene, is (1-4C)alkylamino- carbonyl or (5-6C)cycloalkylaminocarbonyl; and R8 is a sugar residue of formula II in which R9 represents hydrogen, methyl or hydroxymethyl and m is 2 or 3; A is N or CT in which T is hydrogen or (1-4C)alkyl; or a pharmaceutically acceptable salt thereof, processes for their manufacture and pharmaceutical compounds containing them. The compounds are useful as adenosine antagonists.

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