Compounds of the formula II:
wherein
R
2
is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline;
R
3
is H, methyl or F;
Rq is trifluoromethyl and Rq′ is H or Rq and Rq′ define keto;
Q is a p-(C
1
-C
6
alkylsulphonyl)phenyl- or an optionally substituted 4-(C
1
-C
6
alkyl)piperazin-1-yl-thiazol-4-yl- moiety have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
II式化合物:其中R2为亮
氨酸、
异亮氨酸、环己基甘
氨酸、O-甲基苏
氨酸、4-
氟亮
氨酸或3-甲氧基缬
氨酸的侧链;R3为H、甲基或F;Rq为三
氟甲基,Rq′为H或Rq和Rq′定义酮基;Q为p-(C1-C6烷基磺酰基)苯基-或一个可选择取代的4-(C1-C6烷基)
哌嗪-1-基
噻唑-4-基-部分,用于治疗由于卡托普斯底蛋白K的不当表达或激活而表现出的疾病,例如骨质疏松症、骨关节炎、类风湿性关节炎或骨转移。