| abstract |
A method for inhibiting cathepsin S which comprises administering to an animal, particularly a mammal, most particularly a human being in need thereof, an effective amount of a compound of Formula I: <EMI FILE = "01029287_1" ID = "1" MFI = JPEG> in which: R1 is selected from the group consisting of: <EMI FILE = "01029287_2" ID = "2" MFI = JPEG> R2 is selected from the group consisting of: H, C1-6 alkyl, C3- cycloalkyl 6-C0-6 alkyl, Ar-C0-6 alkyl, Het-C0-6 alkyl, R9C (O) -, R9C (S) -, R9SO2-, R9OC (O) -, R9R11NC (O) -, R9R11NC ( S) -, R9 (R11) NSO2 -, <EMI FILE = "01029287_3" ID = "3" MFI = JPEG> <EMI FILE = "01029287_4" ID = "4" MFI = JPEG> R3 is selected from the group consisting of : H, C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, Het-C0-6 alkyl, Ar-C0-6 alkyl, Ar-Ar-C0-6 alkyl , Ar-Het-C0-6 alkyl, Het-Ar-C0-6 alkyl and Het-Het-C0-6 alkyl; R3 and R 'can be joined together to form a pyrrolidine, piperidine or morpholine ring; R4 is selected from the group consisting of H, C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, Het-C0-6 alkyl, R5C (O) -, R5C (S) -, R5SO2-, R5OC (O) -, R5R13NC (O) - and R5R13NC (S) -; R5 is selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6- cycloalkyl C0-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; - 2 -R6 is selected from the group consisting of H, C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl and het-C0-6 alkyl; R7 is selected from the group consisting of: H , C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, Het-C0-6 alkyl, R10C (O) -, R10C (S) -, R10SO2-, R10OC (O) - , R10R14NC (O) - and R10R14NC (S) -, R8 selects from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, Het-C0-6 alkyl and Ar-C0-6 alkyl; R9 is selected from the group consisting of: C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl, R10 is selected from the group consisting of: C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; R11 is selected from the group consisting of H, C1-6 alkyl, Ar-C0-6 alkyl and Het-C0- alkyl 6; R12 is selected from the group consisting of: H, C1-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; R13 is selected from the group consisting of: H, C1-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl, R14 is selected from the group consisting of: H, C1-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; R 'is selected from the group consisting of: H, C1-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; R' is selected from the group consisting of: H, C1-6 alkyl, Ar-alkyl C0-6 or Het-C0-6 alkyl; R '"is selected from the group consisting of: H, C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl and Het-C0- alkyl 6; X is selected from the group consisting of: CH2, S and O; Z is selected from the group consisting of: C (O) and CH2; and its pharmaceutically acceptable salts, hydrates and solvates. 1 A compound according to claim 16, in which C1-6 alkyl is selected from the group consisting of: 5-, 6- and 7-C1-6 alkyl. |