Selective adenosine receptor agents

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 473/04 (2006.01) A61K 31/52 (2006.01) C07D 473/06 (2006.01)

Patent

CA 2038747

Xanthine derivatives which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo. Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate. The subject group of compounds which are of the following general formula: Image including the (R) and (S) enantiomers and racemic mixtures thereof, and the pharmaceutically acceptable salts thereof, Wherein R1 and R2 are each independently (C1-C4)lower alkyl or (C2-C4)lower alkenyl, Z is: Image R3 is (C1-C3)lower alkyl, nitro, amino, hydroxy, fluoro, bromo or chloro, m is zero or an integer from 1 to 4, n is an integer from 1 to 4, and X is H or OH.

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