Patent ID: 6750213
Filing Date: 2004-06-15
Classification: A61P,C07D

Abstract:
A compound of the formula: whereinR1 is selected from the group consisting of hydrogen, C1-5 alkyl, C3-8 cycloalkyl, C2-5 alkenyl, C2-5 alkynyl, C3-8 cycloalkenyl, phenyl, heteroaryl, heterocyclyl, CF3 , â€”OR6, halogen, C1-5 alkylthio, thiocyanato, cyano, â€”CO2H, â€”COOC1-5 alkyl, â€”COC1-5 alkyl, â€”CONZ2, â€”SO2NZ2, and â€”SO2C1-5 alkyl, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, phenyl, heteroaryl and heterocyclyl can be optionally substituted with C1-5 alkyl, C3-8 cycloalkyl, CF3 , phenyl, heteroaryl, heterocyclyl, â€”OR6, halogen, amino, C1-5 alkylthio, thiocyanato, cyano, â€”CO2H, â€”COOC1-5 alkyl, â€”COC1-5 alkyl, â€”CONZ2, â€”SO2NZ2 or â€”SO2C1-5 alkyl; R2 is selected from the group consisting of hydrogen, C1-5 alkyl, C3-8 cycloalkyl, C2-5 alkenyl, C2-5 alkynyl, C3-8 cycloalkenyl, phenyl, heteroaryl, heterocyclyl, CF3 , â€”OR6, halogen, C1-5 alkylthio, thiocyanato, cyano, â€”CO2H, â€”COOC1-5 alkyl, â€”COC1-5 alkyl, â€”CONZ2, â€”SO2NZ2, and â€”SO2C1-5 alkyl, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, phenyl, heteroaryl and heterocyclyl can be optionally substituted with C1-5 alkyl, C3-8 cycloalkyl, CF3 , phenyl, heteroaryl, heterocyclyl, â€”OR6, halogen, amino, C1-5 alkylthio, thiocyanato, cyano, â€”CO2H, â€”COOC1-5 alkyl, â€”COC1-5 alkyl, â€”CONZ2, â€”SO2NZ2 or â€”SO2C1-5 alkyl; R3 is selected from the group consisting of hydrogen, C1-5 alkyl, C3-8 cycloalkyl, C2-5 alkenyl, C2-5 alkynyl, C3-8 cycloalkenyl, phenyl, heteroaryl, heterocyclyl, CF3 , â€”OR6, halogen, C1-5 alkylthio, thiocyanato, cyano, â€”CO2H, â€”COOC1-5 alkyl, â€”COC1-5 alkyl, â€”CONZ2, â€”SO2NZ2, and â€”SO2C1-5 alkyl, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, phenyl, heteroaryl and heterocyclyl can be optionally substituted with C1-5 alkyl, C3-8 cycloalkyl, CF3 , phenyl, heteroaryl, heterocyclyl, â€”OR6, halogen, amino, C1-5 alkylthio, thiocyanato, cyano, â€”CO2H, â€”COOC1-5 alkyl, â€”COC1-5 alkyl, â€”CONZ2, â€”SO2NZ2 or â€”SO2C1-5 alkyl; R4 is selected from the group consisting of hydrogen, C1-5 alkyl, C3-8 cycloalkyl, C2-5 alkenyl, C2-5 alkynyl, C3-8 cycloalkenyl, phenyl, heteroaryl, heterocyclyl, CF3 , â€”OR6, halogen, C1-5 alkylthio, thiocyanato, cyano, â€”CO2H, â€”COOC1-5 alkyl, â€”COC1-5 alkyl, â€”CONZ2, â€”SO2NZ2, and â€”SO2C1-5 alkyl, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, phenyl, heteroaryl and heterocyclyl can be optionally substituted with C1-5 alkyl, C3-8 cycloalkyl, CF3 , phenyl, heteroaryl, heterocyclyl, â€”OR6, halogen, amino, C1-5 alkylthio, thiocyanato, cyano, â€”CO2H, â€”COOC1-5 alkyl, â€”COC1-5 alkyl, â€”CONZ2, â€”SO2NZ2 or â€”SO2C1-5 alkyl; R5 is selected from the group consisting of C1-5 alkyl, C3-8 cycloalkyl, C2-5 alkenyl, C2-5 alkynyl, C3-8 cycloalkenyl, phenyl, heteroaryl and heterocyclyl, wherein said alkyl, cycloalkyl, alkenyl, alkynyl, cycloalkenyl, phenyl, heteroaryl and heterocyclyl can be optionally substituted with C1-5 alkyl, C3-8 cycloalkyl, CF3 , phenyl, heteroaryl, heterocyclyl, â€”OR6, halogen, amino, C1-5 alkylthio, thiocyanato, cyano, â€”CO2H, â€”COOC1-5 alkyl, â€”COC1-5 alkyl, â€”CONZ2, â€”SO2NZ2 or â€”SO2C1-5 alkyl; X and Y are each independently selected from the group consisting of oxygen, sulfur, sulfoxide and sulfone; R6 is selected from the group consisting of hydrogen, C1-5 alkyl, benzyl, methoxymethyl, triorganosilyl, C1-5 alkylcarbonyl, alkoxycarbonyl and CONZ2; each Z is independently selected from the group consisting of hydrogen, C1-5 alkyl, and trifluoromethyl, wherein said alkyl can be optionally substituted with C1-5 alkyl, CF3 , â€”OR6, halogen, amino, C1-5 alkylthio, thiocyanato, cyano, â€”CO2H, â€”COOC1-5 alkyl, â€”COC1-5 alkyl, â€”CONV2, â€”SO2NV2 or â€”SO2C1-5 alkyl; both Zs and the nitrogen to which they are attached may be taken together to form a 3-8 membered ring, said ring may optionally contain atoms selected from the group consisting of carbon, oxygen, sulfur, and nitrogen, wherein said ring may either be saturated or unsaturated, and the carbon atoms of said ring maybe optionally substituted with one to three substituents selected from the group consisting of C1-5 alkyl, CF3 , â€”OR6, halogen, amino, C1-5 alkylthio, thiocyanato, cyano, â€”CO2H, â€”COOC1-5 alkyl, â€”COC1-5 alkyl, â€”CONV2, â€”SO2NV2, and â€”SO2C1-5 alkyl; each V is independently selected from the group consisting of C1-5 alkyl, CF3 , â€”OR6, halogen, amino, C1-5 alkylthio, thiocyanato, cyano, â€”CO2H, â€”COOC1-5 alkyl, â€”COC1-5 alkyl, and â€”SO2C1-5 alkyl; n is independently an integer from one to five; or a pharmaceutically acceptable salt or stereoisomer thereof.