Patent ID: 6544984
Filing Date: 2003-04-08
Classification: A61P,C07D

Abstract:
A compound of Formula 1:â€‰whereinR is selected from hydrogen, (C1-C3) alkyl, â€”CN, â€”ORâ€², â€”SRâ€², â€”CF3, â€”OCF3, Cl, F, â€”N(Râ€²)CO(C1-C3)alkyl, â€”N(Râ€²)(Râ€²), NO2, â€”CONH2, â€”SO2NH2, â€”SO2N(Râ€²)(Râ€²), â€”N(Râ€²)COCH2Oâ€”(C1-C3)alkyl, wherein Râ€² is (C1-C3) alkyl or hydrogen; R4 is (C2-C6) alkyl-Oâ€” containing one triple bond, â€‰wherein Râ€³ is hydrogen, â€”CH2OH, (C1-C6)alkyl, (C1-C6)alkyl-Oâ€”CH2â€”, (C1-C6)alkyl-Sâ€”CH2â€”, (C1-C6)alkyl-NHâ€”CH2â€”, [(C1-C3)alkyl]2-NCH2â€”, (C3-C6)cycloalkyl-Oâ€”CH2â€”, [(C1-C3) alkyl]2-Nâ€”(CH2)2-4NHCH2â€”, [(C1-C3) alkyl]2-Nâ€”(CH2)2-4N(CH3)CH2â€”, â€‰â€‰R1 and R2 are each, independently, hydrogen or C1-C3 alkyl, R3 is (C1-C8)alkyl, NH2CH2COâ€”, (C1-C6)alkylNHCH2COâ€”, HO(CH2)mCOâ€”, HCOâ€”, Aryl(CH2)nCOâ€”, Heteroaryl(CH2)nCOâ€”, (C1-C3)alkyl-Oâ€”(CH2)nCOâ€”, (C1-C3)alkylCOâ€”, (C1-C3)alkylCOâ€”NHCH2COâ€”, (C3-C7)cycloalkylCOâ€”, (C1-C3)alkylSO2â€”, Aryl(CH2)nSO2â€”, Heteroaryl(CH2)nSO2â€”, (C1-C3)alkyl-Oâ€”(CH2)mâ€”SO2â€”, (C1-C3)alkyl-Oâ€”(CH2)mâ€”, (C1-C3)alkyl-Oâ€”(C1-C3)alkyl-Oâ€”(C1-C3)alkylâ€”, HOâ€”(C1-C3)alkyl-Oâ€”(C1-C3)alkyl-, Aryl-Oâ€”CH2COâ€”, Heteroaryl-Oâ€”CH2COâ€”, ArylCH&boxH;CHCOâ€”, HeteroarylCH&boxH;CHCOâ€”, (C1-C3)alkylCH&boxH;CHCOâ€”, â€‰Aryl(C1-C3)alkyl-, Heteroaryl(C1-C3)alkyl-, ArylCH&boxH;CHCH2â€”, HeteroarylCH&boxH;CHCH2â€”, (C1-C6)alkylCH&boxH;CHCH2â€”, â€‰Râ€²OCH2CH(ORâ€²)COâ€”, (Râ€²OCH2)2C(Râ€²)COâ€”, â€‰[(C1-C6)alkyl]2-Nâ€”(C1-C6)alkyl COâ€”, or (C1-C6)alkyl-NHâ€”(C1-C6)alkylCOâ€”; whereinm=1 to 3; n=0 to 3 Aryl is â€‰Heteroaryl is â€‰whereinX is hydrogen, halogen, (C1-C3) alkyl or â€”OCH3, and R and Râ€² are as defined above; L is hydrogen, (C1-C3)alkyl, â€”CN, â€”ORâ€², â€”SRâ€², â€”CF3, â€”OCF3, Cl, F, â€”N(Râ€²)CO(C1-C3)alkyl, N(Râ€²)(Râ€²), â€”NO2, â€”CONH2, â€”SO2NH2, â€”SO2N(Râ€²)(Râ€²), â€”N(Râ€²)COCH2Oâ€”(C1-C3)alkyl, â€‰M is â€‰â€‰â€ƒor N(Râ€²)(Râ€²) where Râ€² is as defined above; W is O, S, NH or N(C1-C3)alkyl; Y is hydrogen, F, Cl, CF3 or OCH3; and Xâ€² is halogen, hydrogen, (C1-C3)alkyl, Oâ€”(C1-C3)alkyl, or â€”CH2OH; and pharmaceutically acceptable salts thereof.