Patent ID: 6432962
Filing Date: 2002-08-13
Classification: A61K,A61P,C07D

Abstract:
A compound of the formula I wherein R1 is selected from the group consisting of halogen, haloalkyl, hydroxy, hydroxyalkyl, hydroxyalkyloxy, mercapto, cyano, carboxy, nitro, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, alkylaryl, alkoxy, aralkoxy, alkylthio, alkoxycarbonyl, alkylcarbonyloxy, alkoxycarbonyloxy, alkylsulfonyloxy, alkyloxysulfonyl, alkylcarbonylamino, aminocarboaminoalkyl, aminosulfonyl, alkylsulfonylamino, alkanoyl, alkylcarbonyl, â€”NR9R10 or â€”CONR9R10, wherein R9 and R10 are the same or different and individually represent hydrogen, alkyl or aryl;R2 represents one or more, same or different substituents selected from the group consisting of hydrogen, halogen, haloalkyl, hydroxy, hydroxyalkyl, hydroxyalkyloxy, mercapto, cyano, carboxy, nitro, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, alkylaryl, alkoxy, aralkoxy, alkylthio, alkoxycarbonyl, alkylcarbonyloxy, alkoxycarbonyloxy, alkylsulfonyloxy, alkyloxysulfonyl, alkylcarbonylamino, aminocarboaminoalkyl, aminosulfonyl, alkylsulfonylamino, alkanoyl, alkylcarbonyl, â€”NR9R10 or â€”CONR9R10, wherein R9 and R10 are the same or different and individually represent hydrogen, alkyl or aryl; R3 represents one or more, same or different substituents selected from the group consisting of hydrogen, halogen, haloalkyl, hydroxy, hydroxyalkyl, mercapto, cyano, nitro, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, aralkyl, alkylaryl, alkoxy, aralkoxy, alkylthio, alkoxycarbonyl, alkylcarbonylamino, alkylcarbonyloxy, alkoxycarbonyloxy, alkylcarbonyl â€”NR9R10 or â€”CONR9R10 wherein R9 and R10 are the same or different and individually represent hydrogen, alkyl or aryl; R4 represents hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, carboxy or aryl; R5 represents a heteroaromatic mono- or bicyclic ring system comprising 1-4 heteroatoms, except for triazine, the ring system being optionally substituted by hydrogen, halogen, haloalkyl, hydroxy, hydroxyalkyl, hydroxyalkyloxy, mercapto, cyano, carboxy, nitro, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, alkylaryl, alkoxy, aralkoxy, alkylthio, alkoxycarbonyl, alkylcarbonyloxy, alkoxycarbonyloxy, alkylsulfonyloxy, alkyloxysulfonyl, alkylcarbonylamino, aminocarboaminoalkyl, aminosulfonyl, alkylsulfonylamino, alkanoyl, alkylcarbonyl, â€”NR9R10 or â€”CONR9R10, wherein R9 and R10 are the same or different and individually represent hydrogen, alkyl or aryl; X represents oxygen, sulphur, Nâ€”OH or NR11 wherein R11 is hydrogen or alkyl; and salts thereof with pharmaceutically acceptable acids, hydrates and solvates, and optionally the N-oxides thereof wherein a nitrogen atom of the heterocyclic R5 substituent is oxidised.