Patent ID: 6579874
Filing Date: 2003-06-17
Classification: A61P,C07D

Abstract:
A compound of formula (I) whereina is N or C; b is CH when a is N, or O when a is C; &boxH; denotes a single or a double bond dependent upon whether the azole ring is an imidazole or an oxazole ring; Z is N or CH; W is â€”NR6â€”Yâ€”, â€”Oâ€” or â€”Sâ€”, where R6 is H, C1-C4alkyl, C3-C8cycloalkyl, C3-C8cycloalkylC1-C3alkyl, C6-C18aryl, C3-C18heteroaryl, C7-C19aralkyl or C4-C19heteroaralkyl and â€”Yâ€” is C1-C4alkylene or a direct bond; R2 is phenyl, optionally substituted by one or more substituents, each of which is, independently, selected from halo, CF3, cyano, amido or thioamido, carboxylate or thiocarboxylate, C1-C4alkoxy, C1-C4alkyl, or NH2 which is optionally mono- or di-N-C1-C4alkyl substituted; R3 is H, halogen, C1-C10alkyl, C1-C4alkenyl, C3-C10cycloalkyl, C3-C18heterocycloalkyl, C6-C18aryl, C3-C18heteroaryl or methyleneaminoguanidinyl, each of which, except H and halogen, is optionally substituted by up to 4 substituents separately selected from C1-C4alkyl optionally substituted by hydroxy, halogen, halo-substituted-C1-C4alkyl, hydroxy, C1-C4alkoxy, C1-C4alkylthio, carboxy, optionally C1-C6alkyl or C1-C6alkoxy substituted carbonyl, optionally mono- or di-N-C1-C4alkyl substituted amino, or by N-heterocyclyl having from 5- to 7-ring atoms and optionally having a further hetero atom; and R5 is C6-C18aryl, C3-C18heteroaryl or C3-C12cycloalkyl each of which is optionally substituted by up to 4 substituents separately selected from C1-C4alkyl, halogen, halo substituted C1-C4alkyl, hydroxy, C1-C4alkoxy, C1-C4alkylthio, or optionally mono- or di-N-C1-C4alkyl substituted amino, or by N-heterocyclyl having from 5- to 7-ring atoms and optionally having a further hetero atom; or pharmaceutically-acceptable esters thereof, or acid addition salts thereof, or, when said compound comprises one or more free hydroxyl groups, the pharmaceutically-acceptable prodrug esters thereof, which are cleavable under physiological conditions to release the compound having one or more free hydroxyl groups.