Patent ID: 6630506
Filing Date: 2003-10-07
Classification: A61P,C07D

Abstract:
A compound having the structure whereinR1 and R2 are the same or different and are independently selected from H, alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, (alkyl or aryl)3Si (where each alkyl or aryl group is independent), cycloalkyl, cycloalkenyl, aryl, arylalkyl, aryloxy, cycloheteroalkyl, cycloheteroalkylalkyl, heteroaryl, heteroaryloxy, arylthio, arylsulfinyl, arylsulfonyl, thio, alkylthio, alkylsulfinyl, alkylsulfonyl, heteroarylthio, heteroarylsulfinyl, heteroarylsulfonyl, halogen, haloalkyl, polyhaloalkyl, polyhaloalkoxy, alkylaminocarbonyl, arylaminocarbonyl, heteroarylaminocarbonyl, acyl, carboxy, aminocarbonyl, alkylcarbonyl, alkoxycarbonyl, arylcarbonyl, heteroarylcarbonyl, cyano, tetrazolyl, imidazole, oxazole or triazole, â€”PO(R8) (R9), S(O)2R8, R9 (where R8 and R9 are the same or different and are independently hydrogen, alkyl, aryl, alkoxy, aryloxy, cycloalkyl, heteroaryl, heteroarylalkyl, heteroaryloxy, heteroarylalkoxy, cycloheteroalkyl, cycloheteroalkylalkyl, cycloheteroalkoxy, or cycloheteroalkylalkoxy); with the proviso that whenR3 is H; and R4 is H; and R5 and R6 are independently H, halogen, alkyl, alkoxy, nitro, amino, aryl, cycloheteroalkyl or heteroaryl; at least one of R1 and R2 is other than H; and where R1 and R2 may optionally be joined together to form a non-aromatic substituted or unsubstituted carbocyclic ring, a cycloalkyl or cycloalkenyl ring, or a cycloheteroalkyl ring, which ring contains 3 to 8 members; X is O, S, SO, S2, CO, or NR7 (wherein R is H, lower alkyl, alkanoyl, or â€”SO2alkyl); Y is a bond; R3, R4, R5 and R6 are the same or different and are selected from H, alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, (alkyl or aryl)3Si (where each alkyl or aryl group is independent), cycloalkyl, cycloalkenyl, aryl, arylalkyl, aryloxy, cycloheteroalkyl, cycloheteroalkylalkyl, heteroaryl, heteroaryloxy, arylthio, arylsulfinyl, arylsulfonyl, thio, alkylthio, alkylsulfinyl, alkylsulfonyl, heteroarylthio, heteroarylsulfinyl, heteroarylsulfonyl, halogen, haloalkyl, polyhaloalkyl, polyhaloalkoxy, heteroarylaminocarbonyl, acyl, carboxy, aminocarbonyl, alkylcarbonyl, alkoxycarbonyl, arylcarbonyl, heteroarylcarbonyl, cyano, tetrazolyl, imidazole, oxazole or triazole, â€”PO(R12) (R13), S(O)2R12, R13 (where R12 and R13 are the same or different and are independently hydrogen, alkyl, aryl, alkoxy, aryloxy, cycloalkyl, heteroaryl, heteroarylalkyl, heteroaryloxy, heteroarylalkoxy, cycloheteroalkyl, cycloheteroalkylalkyl, cycloheteroalkoxy, or cycloheteroalkylalkoxy), amino, alkylamino, alkenylamino, alkynylamino, arylalkylamino, arylamino, heteroarylamino, thio, alkylsulfonylamino, alkenylsulfonylamino, alkynylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkylaminocarbonyl, arylaminocarbonyl, heteroarylaminocarbonyl, hydroxy, alkylcarbonyloxy, alkylcarbonylamino, arylcarbonyloxy, arylcarbonylamino, heteroarylcarbonyloxy, heteroarylcarbonylamino, nitro, alkenylcarbonylamino, alkynylcarbonylamino, alkylaminocarbonylamino, alkenylaminocarbonylamino, alkynylaminocarbonylamino, arylaminocarbonylamino, heteroarylaminocarbonylamino, alkoxycarbonylamino, alkenyloxycarbonylamino, alkynyloxycarbonylamino, aryloxycarbonylamino, heteroaryloxycarbonylamino, aminocarbonylamino, alkylaminocarbonyloxy, 1,1-(alkoxyl or aryloxy)2alkyl (where the two aryl or alkyl substituents can be independently defined, or linked to one another to form a ring, such as 1,3-dioxane or 1,3-dioxolane), â€”NR10(C&boxH;NR11)alkyl, â€”NR10(C&boxH;NR11)alkenyl, â€”NR10(C&boxH;NR11)alkynyl, â€”NR10 (C&boxH;NR11)heteroaryl, or â€”NR10(C&boxH;NCN)-amino; where R10 and R11 are the same or different and are independently selected from hydrogen, alkyl, haloaryl, aryl, alkoxy, aryloxy, cycloalkyl, heteroaryl, arylalkyl, or cycloheteroalkyl, and optionally any two adjacent R4, R5 and R6 groups can be joined together to form a non-aromatic substituted or unsubstituted carbocyclic ring, or a cycloheteroalkyl ring or a heteroaryl ring; including pharmaceutically acceptable salts thereof, prodrug esters thereof, and all stereoisomers thereof.