Cysteine Protease Inhibitors
AssigneeMedivir AB
InventorsMagnus Nilsson, Lourdes Oden, Pia Kahnberg, Urszula Grabowska
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Abstract
Compounds of the formula II: wherein R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R3 is H, methyl or F; Rq is trifluoromethyl and Rq′ is H or Rq and Rq′ define keto; Q is a p-(C1-C6alkylsulphonyl)phenyl- or an optionally substituted 4-(C1-C6alkyl)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.
Claims26
A compound of the Formula II:
- wherein
- R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline;
- R3 is H, methyl or F;
- Rq is CF3 with the indicated stereochemistry and Rq′ is H;
- or
- Rq and Rq′ together define keto;
- Q is
- wherein
- R4 is C1-C6 alkyl;
- R5 is H, methyl or F;
- R6 is C1-C6 alkyl;
- or a pharmaceutically acceptable salt, prodrug or N-oxide thereof.
A compound of the formula IIb:
- wherein
- R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline;
- R3 is H, methyl or F;
- Q is
- wherein
- R4 is C1-C6 alkyl;
- R5 is H, methyl or F;
- R6 is C1-C6 alkyl;
- or a pharmaceutically acceptable salt, prodrug or N-oxide thereof.
Dependencies are inferred from the claim text.