4-AMINO-IMIDAZOQUINOLINE COMPOUNDS

摘要

This invention relates to novel 4-amino-imidazoquinoline compounds of the formula;;wherein R1 to R4 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are TLR agonists and may therefore be useful as medicaments for the treatment of diseases such as cancer or infectious diseases.

主权项

1. A compound of formula I wherein R1 is C1-7-alkyl or C1-7-alkoxy-C1-7-alkyl; R2 is selected from the group consisting of hydrogen, halogen, hydroxyl, hydroxy-C1-7-alkyl, alkoxy-C1-7-alkyl, carboxyl, carboxyl-C1-7-alkyl, carboxyl-C2-7-alkenyl, aminocarbonyl-C1-7-alkyl, aminocarbonyl-C2-7-alkenyl, C1-7-alkylamino-carbonyl-C1-7-alkyl, C1-7-alkylamino-carbonyl-C2-7-alkenyl, C1-7-alkoxycarbonyl-C1-7-alkyl, C1-7-alkoxycarbonyl-C2-7-alkenyl, C1-7-alkyl-sulfonyl-C1-7-alkyl, sulfamoyl-C1-7—alkyl, C1-7-alkyl-sulfamoyl-C1-7-alkyl,
phenyl, said phenyl being unsubstituted or substituted with one, two or three groups selected from the group consisting of C1-7-alkyl, C1-7-cycloalkyl, halogen, halogen-C1-7-alkyl, halogen-C1-7-alkoxy, hydroxy, hydroxy-C1-7-alkyl, C1-7-alkoxy, cyano, carboxyl, C1-7-alkoxycarbonyl, C1-7-alkoxycarbonyl-C1-7-alkyl, C1-7-alkylsulfonyl, hydroxy-C1-7-alkylsulfonyl, C1-7-alkoxy-C1-7-alkylsulfonyl, carboxyl-C1-7-alkylsulfonyl, C1-7-alkoxy-carbonyl-C1-7-alkylsulfonyl, amino, C1-7-alkylamino, di-C1-7-alkylamino and nitro, andphenoxy, said phenoxy group being unsubstituted or substituted with one, two or three groups selected from the group consisting of C1-7-alkyl, C1-7-cycloalkyl, halogen, halogen-C1-7-alkyl, halogen-C1-7-alkoxy, hydroxy, hydroxy-C1-7-alkyl, C1-7-alkoxy, cyano, carboxyl, C1-7-alkoxycarbonyl, C1-7-alkoxycarbonyl-C1-7-alkyl, C1-7-alkyl-sulfonyl, hydroxy-C1-7-alkylsulfonyl, C1-7-alkoxy-C1-7-alkylsulfonyl, carboxyl-C1-7-alkylsulfonyl, C1-7-alkoxy-carbonyl-C1-7-alkylsulfonyl, amino, C1-7-alkylamino, di-C1-7-alkylamino and nitro; R3 is hydrogen or halogen; R4 is selected from the group consisting of
—O—(CH2)m—NHR5, and—O—(CO)—(CH2)n—NHR6,whereinm is selected from 1, 2 or 3,n is selected from 1 or 2,R5 is selected from the group consisting of hydrogen, hydroxy-C1-7-alkyl, amino-C1-7-alkyl, C1-7-alkylcarbonyl, phenylcarbonyl, heteroarylcarbonyl, carboxyl, carboxyl-C1-7-alkyl and C1-7-alkoxycarbonyl-amino-C1-7-alkyl-carbonyl, andR6 is selected from the group consisting of hydrogen, hydroxy-C1-7-alkyl, amino-C1-7-alkyl, C1-7-alkylcarbonyl, phenylcarbonyl, heteroarylcarbonyl, carboxyl, carboxyl-C1-7-alkyl and C1-7-alkoxycarbonyl-amino-C1-7-alkyl-carbonyl, or a pharmaceutically acceptable salt thereof.