Protease inhibitors

摘要

The application discloses both the compound and the process for the synthesis of IA. For compound IA : R1 is selected from the group consisting of (see below); R2 is selected from the group consisting of: C1-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl, R9C(O)-, R9SO2-, R9R11NC(O)- and R9SO2R11NC(O)-; R3 is C1-6 alkyl; R4 is R5C(O)-; R5 is Het-C0-6alkyl; R9 is selected from the group consisting of C1-6alkyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl and Het-C0-6alkyl; R11 is selected from the group consisting of H, C1-6alkyl, ArC0-6alkyl, and Het-C0-6alkyl; R' is H; R'' is H; R''' is H; R'''' is selected from the group consisting of C1-6alkyl, C3-6cycloalkyl-C0-6alkyl, C2-6alkenyl, C2-6alkynyl, HetC0-6alkyl and ArC0-6alkyl; n is an integer from 1 to 5; Pharmaceutically acceptable salts, hydrates and solvates thereof are also included. The compound can be used in pharmaceutical compositions to treat diseases characterized by bone loss, for example, osteoporosis, periodontis, gingivitis, osteoarthritis, rheumatoid arthritis or excessive cartilage or matrix degradation. The compound can also be used in the manufacture of a medicament to treat parasitic infection such as, schistosomiasis, malaria, trypsanoma brucei, pneumocystis carinii, trypsanoma cruzi and Crithidia fusiculata.