Derivatives of (2,6-diaminopurin-9-yl)-5-([1,2,4]oxadiazol-5-yl)-tetrahydrofuran-3,4-diol, intermediates and pharmaceuticals thereof, and their use for treating inflammatory diseases

摘要

A compound of formula (I); wherein: R1 and R2 independently are cycloalkyl, hydrogen, aryl2CHCH2, cycloalkylalkyl-, alkyl, arylalkyl-, R4R5N-alkyl-, alkyl-CH(CH2OH)-, arylalkyl-CH(CH2OH)-, arylalkyl-C(CH2OH)2-, cycloalkyl independently substituted by one or more- (CH2)pR6 groups, H2NC(=NH)NHalkyl-, a group of formula (III) or such a group in which one methylene carbon atom adjacent to X (or both if such exist) is substituted by methyl, -alkyl-OH, -haloalkyl, a group of formula (IV), aryl, -(CH2)fSO2NHg(alkyl)2-g or -(CH2)fSO2NHg(arylalkyl)2-g R3 is methyl,ethyl,-CH=CH2, n-propyl, -CH2CH=CH2, -CH=CHCH3, isopropenyl, cyclopropyl, cyclopropenyl, -CH(OH)CH3, -(CH2)qhalogen, -(CH2)hY(CH2)iH, -COO(CH2)lH, -CON(CH2)mH((CH2)nH), -CO(CH2)oH or -C((CH2)uH)=NO(CH2)vH Pharmaceutical compositions comprising the compound of formula (I) are also described. The compounds of formula (I) are useful for the treatment of inflammatory diseases such as asthma or chronic obstructive pulmonary disease (COPD). Also described are intermediate compounds of formulae (II), (V) and (X), wherein R1 and R3 are as defined for the compound of formula (I), above, and L, L1 and L2 represent leaving groups or protected derivatives thereof.