Novel adenosine antagonists useful in treatment of e.g. neurodegenerative, pulmonary, renal and cardiovascular disorders

摘要

3,8-Disubstituted-xanthines (I) are new. They are prepared via new intermediates (IA). 3-alk(en or yn)yl-8-(alkyl or bridged cycloalkyl)-xanthines (I). as racemates, enantiomers, diastereomers and mixtures, and their addition salts are new: a or b = double bond; R<1> = H; 1-6C alkyl; 3-6C alkenyl; or 3-6C alkynyl; R<2> = 1-6C alkyl, 3-6C alkenyl or 3-6C alkynyl substituted with OR<6>, SO2R<6>, OCOR<9>, COOR<9>, NR<7>R<8>, O(CH2)2-NR<7>R<8>, CONR<7>R<8>, OCH2CONR<7>R<8> or O(CH2)2-CONR<7>R<8> or optionally substituted with C-bonded 5-6 membered heterocyclic ring containing 1-4 O, N and/or S atoms and optionally substituted with 1-4C alkyl or benzyl; R<3> = 1-6C alkyl optionally substituted with OH; or norbornanyl, norbornenyl, adamantyl or noradamantyl optionally substituted with Me or OH; R<4> and R<5> (not present simultaneously) = H or benzyl optionally substituted with 1-3 OMe; R<6> = H or 3-6C cycloalkyl or 1-4C alkyl optionally substituted with OR<9> or OCOR<9>; R<7> and R<8> = H; SO2R<6>; 1-4C alkyl; COR<9>; or COOR<9>; or NR<7>R<8> forms a 5-6 membered ring containing a further N atom or an O atom and optionally substituted with 1-4C alkyl or benzyl; compounds are excluded when R<1> = R<2>. Independent claims are also included for the following: (1) the preparation of compounds (I); and (2) the intermediates of formula (IA): R<2>' = H or 1-6C alkyl, 3-6C alkenyl or 3-6C alkynyl substituted with CN, halo, 1-6C alkoxy, CH3SO2O, CF3SO2O or p-tosyloxy.