Patent ID: 6608084
Filing Date: 2003-08-19
Classification: A61P,C07D

Abstract:
A compound of general formula (I): wherein:R1 represents R3â€”L3â€”Ar1â€”L4â€”Z3â€”; R2 represents hydrogen, halogen, C1-4alkyl or C1-4alkoxy; R3 represents alkyl, alkenyl allynyl, aryl, arylalkyl, arylalkenyl, arylalkynyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkylalkynyl, cycloalkenyl, cycloalkenylalkyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, heteroarylalkynyl, heterocycloalkyl or heterocycloalylalkyl; R5 represents hydrogen or C1-4alkyl; R7 and R7a are each independently hydrogen or C1-4alkyl; R8 represents hydrogen, alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl; R9 represents alkyl, aryl, cycloalkyl, heteroaryl or heterocycloalkyl, or alkyl substituted by aryl, carboxy, cycloalkyl, heteroaryl, heterocycloallyl, â€”S(O)mR3, â€”C(&boxH;O)â€”NY4Y5 or â€”NY4Y5; R10 represents hydrogen, R3 or alkyl substituted with alkoxy, cycloalkyl, hydroxy, mercapto, alkylthio or â€”NY4Y5; R14 represents alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, hetetoarylalkyl, heterocycloalkyl or heterocycloalkylalkyl; A1 represents a methylene or ethylene linkage; Ar1 represents arylene; L1 represents: an allylene linkage optionally substituted by (a) carboxy, hydroxy, mercapto, R3, â€”N(R8)â€”C(&boxH;O)â€”R9, â€”N(R8)â€”C(&boxH;O)â€”OR9, â€”N(R8)â€”SO2â€”R9 or â€”NY4Y5, or by (b) alkyl substituted by carboxy, hydroxy, mercapto, S(O)mR9, â€”C(&boxH;O)â€”NY4Y5 or â€”NY4Y5; L3 represents an â€”NR5â€”C(&boxH;Z)â€”NR5â€” linkage; L4 represents an alkylene chain; Y1 and Y2 are independently hydrogen, alkenyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl or heteroarylalkyl; or the group â€”NY1Y2 may form a cyclic amine; Y4 and Y5 are independently hydrogen, alkenyl, alkyl, alkynyl, aryl, cycloalkenyl, cycloalkyl, heteroaryl, heterocycloalkyl, or alkyl substituted by alkoxy, aryl, cyano, cycloalkyl, heteroaryl, heterocycloalkyl, hydroxy, oxo, â€”NY1Y2, or one or more â€”CO2 R8 or â€”C(&boxH;O)â€”NY1Y2 groups; or the group â€”NY4Y5 may form a 5- to 7-membered cyclic amine which (i) may be optionally substituted with one or more substituents selected from alkoxy, carboxamido, carboxy, hydroxy, oxo, or a 5-, 6- or 7-membered cyclic acetal derivative thereof, or R10; (ii) may also contain a after heteroatom selected from O, S, SO2, or NY6; and (iii) may also be fused to additional aryl, heteroaryl, heterocycloalkyl or cycloalkyl rings to form a bicyclic or tricyclic ring system; Y6 represents hydrogen, alkyl, aryl, arylalkyl, â€”C(&boxH;O)â€”R14, â€”C(&boxH;O)OR14 or SO2R14; Z is an oxygen or sulphur atom; Z1 is C(R7)(R7a); Z3 is C(&boxH;O) or OC(&boxH;O); m is an integer 1 or 2; and Y is carboxy; and their ester prodrugs; and phamaceutically acceptable salts and solvates of such compounds and their ester prodrugs.