Cathespin cysteine protease inhibitors

Details Cathespin cysteine protease inhibitors Cathespin cysteine protease inhibitors

2007-12-25

2007-12-25

Anderson, Rebecca (Department: 1626)

Organic compounds -- part of the class 532-570 series

Organic compounds

Nitriles

C562S450000

Reexamination Certificate

active

10568495

ABSTRACT:
This invention relates to a novel class of compounds, represented by the formula below, wherein the meanings of G, E, E, n, R1, R2, R3et R4are indicated therein, which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

REFERENCES:
patent: 2003/0232863 (2003-12-01), Bayly et al.
patent: 2439415 (2002-09-01), None
patent: WO 00/55125 (2000-09-01), None
patent: WO 01/68645 (2001-09-01), None
patent: WO 02069901 (2002-09-01), None
Robichaud, J. et al., Bioorganic & Medicinal Chemistry Letters 14, pp. 4291-4295 (2004), “Rational design of potent and selective NH-linked aryl/heteroaryl cathespin K inhibitors”.
Greenspan, PD et al., J Med. Chem, vol. 44, pp. 4524-4534 (2001), “Identification of dipeptidyl nitriles as potent and selective inhibitors of cathespin B through structure-based drug design”.
Ward, YD et al., J. Med. Chem, vol. 45, pp. 5471-5482 (2002), “Design and synthesis of dipeptide nitriles as reversible and potent cathespin S inhibitors”.
Volonterio, A et al., Organic Letters, vol. 4, No. 13, pp. 1827-1830 (2000), “Synthesis of partially modified retro and tetroinverso [NHCH(CF3)]-peptides”.

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