Patent ID: 6696470
Filing Date: 2004-02-24
Classification: A61P,C07D

Abstract:
A compound according to the formula (Iâ€²): or a pharmaceutically effective salt thereof, whereinX is selected from the group consisting of O, S, S(O) and S(O)2; R1 is selected from the groups consisting of (a) hydrogen, halo, R5â€”, C2-6 alkenyl, C2-6 alkynyl, hydroxy-R5â€”, R5â€”Oâ€”, R5â€”Sâ€”, R5â€”Oâ€”R5â€”, mercapto-R5â€”, R5â€”Sâ€”R5â€”, â€”NH2, R5â€”NHâ€”, (R5)2â€”Nâ€” or a heterocyclic group optionally substituted by one or two substituents selected from C1-4 alkyl, phenyl, and pyridyl; (b) Arâ€”, Arâ€”R5â€”, Arâ€”C2-6 alkenyl, Arâ€”C2-6 alkynyl, Arâ€”Oâ€”, Arâ€”Oâ€”Arâ€”, Arâ€”Oâ€”Arâ€”Oâ€”, Arâ€”Oâ€”R5â€”, Arâ€”R5â€”Oâ€”, Arâ€”Sâ€”, Arâ€”R5â€”Sâ€”, Arâ€”NHâ€”, (Ar)2â€”R5â€”, Arâ€”R5â€”NHâ€”, Arâ€”R5â€”N(R5)â€” or (Ar)2â€”Nâ€”; (c) R5â€”C(O)â€”, â€”NO2, cyano, NH2â€”C(O)â€”, R5â€”NHâ€”C(O)â€”, (R5)2â€”Nâ€”C(O)â€”, Arâ€”C(O)â€”, (Arâ€”R5)2â€”Nâ€”C(O)â€”, Arâ€”R5â€”C(O)â€”, Arâ€”NHâ€”C(O)â€”, Arâ€”R5â€”NHâ€”C(O)â€”, R5â€”S(O)2â€” or R5â€”S(O)â€”; and (d) R5â€”C(O)â€”NHâ€”, Arâ€”C(O)â€”NHâ€”, Arâ€”R5â€”C(O)â€”NHâ€” or H2Nâ€”C(O)â€”NHâ€”; wherein Ar is aryl or heteroaryl optionally substituted by one or two substituents selected from C1-4 alkyl, halo-substituted C1-4 alkyl, halo-substituted C1-4 alkoxy, C1-4 alkylthio, nitro, hydroxy, amino and halo; and â€”A1â€”B1â€”A2â€”, together with the carbon atoms to which A1 and A2 are attached, defines a ring having 4 to 8 carbon atoms, said ring being optionally substituted with acetyl-, carboxyl-, â€”C(O)â€”NH2, â€”C(O)â€”OR5, â€”C(O)â€”NHR5, hydroxy, R5â€”, C1-4 alkoxy-, R5â€”NHâ€”, or (R5)2â€”NHâ€”, wherein A1 and A2 are independently, a direct bond or C1-6 alkylene, and B1 is carbonyl; each occurence of R4 is selected independently from hydrogen, halo, R5â€”, hydroxy-R5â€”, R5â€”Oâ€”R5â€”, R5â€”C(O)â€”, R5â€”Oâ€”C(O)â€”, and R5â€”NHâ€”C(O)â€”; m is 0,1,2,3 or 4; and R5, if present, is C1-6 alkyl optionally substituted by up to four halogen atoms.