Protease inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S211030, C514S217030, C514S217050, C514S217060, C514S217070, C514S217080, C514S217090, C514S217100, C514S217110, C540S525000, C540S596000, C540S597000, C540S598000, C540S599000, C540S601000, C540S602000, C540S603000, C540S604000

Reexamination Certificate

active

07071184

ABSTRACT:
The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.

REFERENCES:
patent: 4038247 (1977-07-01), Muller et al.
patent: 4447419 (1984-05-01), Quadro
patent: 4518528 (1985-05-01), Rasnick
patent: 4638101 (1987-01-01), Rosenquist
patent: 4749792 (1988-06-01), Natarajan et al.
patent: 4994471 (1991-02-01), Lalinde et al.
patent: 5057525 (1991-10-01), Van Daele
patent: 5142056 (1992-08-01), Kempe et al.
patent: 5206251 (1993-04-01), Khanna et al.
patent: 5216168 (1993-06-01), Khanna et al.
patent: 5374637 (1994-12-01), Van Daele
patent: 5395824 (1995-03-01), Higuchi et al.
patent: 5422359 (1995-06-01), Ando et al.
patent: 5424325 (1995-06-01), Ando et al.
patent: 5501969 (1996-03-01), Hastings et al.
patent: 5523313 (1996-06-01), Nunami et al.
patent: 5585387 (1996-12-01), Lu et al.
patent: 5668128 (1997-09-01), Tsubotani et al.
patent: 5830850 (1998-11-01), Gelb et al.
patent: 5861298 (1999-01-01), DeBouck et al.
patent: 5902882 (1999-05-01), Matzinger et al.
patent: 5948669 (1999-09-01), Feild et al.
patent: 5998470 (1999-12-01), Halbert et al.
patent: 6057362 (2000-05-01), Yamashita
patent: 6232342 (2001-05-01), Carr et al.
patent: 6274336 (2001-08-01), Abdel-Meguid et al.
patent: 6284777 (2001-09-01), Halbert et al.
patent: 6331542 (2001-12-01), Carr et al.
patent: 6369077 (2002-04-01), Marquis, Jr. et al.
patent: 6566373 (2003-05-01), Gribble et al.
patent: 6583137 (2003-06-01), Marquis, Jr. et al.
patent: 2003/0044399 (2003-03-01), Cummings, Jr. et al.
patent: 2004/0034013 (2004-02-01), Cummings et al.
patent: 2004/0229863 (2004-11-01), Cummings et al.
patent: 86/67002 (1987-07-01), None
patent: 2033497 (1991-01-01), None
patent: EP 0 237 082 (1987-09-01), None
patent: EP 0 504 938 (1992-03-01), None
patent: EP 0 525 420 (1993-02-01), None
patent: EP 0 603 873 (1994-06-01), None
patent: EP 0 611 756 (1994-08-01), None
patent: EP 0 623 592 (1994-11-01), None
patent: 2570686 (1997-01-01), None
patent: WO 92/04371 (1992-03-01), None
patent: EP 0 543 310 (1993-05-01), None
patent: WO 94/00095 (1994-01-01), None
patent: WO 94/04172 (1994-03-01), None
patent: WO 94/23033 (1994-10-01), None
patent: WO 95/05192 (1995-02-01), None
patent: WO 95/24182 (1995-09-01), None
patent: WO 96/13523 (1996-05-01), None
patent: WO 96/40737 (1996-12-01), None
patent: WO 97/16177 (1997-05-01), None
patent: WO 97/16433 (1997-05-01), None
patent: WO 97/47642 (1997-12-01), None
patent: WO 97/47643 (1997-12-01), None
patent: WO 97/49668 (1997-12-01), None
patent: WO9749668 (1997-12-01), None
patent: WO 98/05336 (1998-02-01), None
patent: WO 98/08802 (1998-03-01), None
patent: WO 98/12211 (1998-03-01), None
patent: WO 98/46582 (1998-10-01), None
patent: WO 98/48799 (1998-11-01), None
patent: WO 98/49152 (1998-11-01), None
patent: WO 98/50342 (1998-11-01), None
patent: WO 99/11637 (1999-03-01), None
patent: WO 99/53039 (1999-10-01), None
patent: WO 99/59526 (1999-11-01), None
patent: WO 99/59570 (1999-11-01), None
patent: WO 99/64399 (1999-12-01), None
patent: WO 99/66925 (1999-12-01), None
patent: WO 00/09653 (2000-02-01), None
patent: WO 00/29408 (2000-05-01), None
patent: WO 01/34160 (2000-05-01), None
patent: WO 00/38687 (2000-07-01), None
patent: WO 00/39115 (2000-07-01), None
patent: WO 00/47563 (2000-08-01), None
patent: WO 00/49011 (2000-08-01), None
patent: WO 00/54769 (2000-09-01), None
patent: WO 00/58296 (2000-10-01), None
patent: WO 01/07436 (2001-02-01), None
patent: WO 01/34153 (2001-05-01), None
patent: WO 01/34154 (2001-05-01), None
patent: WO 01/34155 (2001-05-01), None
patent: WO 01/34156 (2001-05-01), None
patent: WO 01/34157 (2001-05-01), None
patent: WO 01/34158 (2001-05-01), None
patent: WO 01/34159 (2001-05-01), None
patent: WO 01/34565 (2001-05-01), None
patent: WO 01/34566 (2001-05-01), None
patent: WO 01/34599 (2001-05-01), None
patent: WO 01/70232 (2001-09-01), None
patent: WO 02/17924 (2002-03-01), None
patent: WO 02/092563 (2002-11-01), None
patent: WO 03/0267770 (2003-04-01), None
patent: WO 03/045909 (2003-06-01), None
patent: WO 03/053331 (2003-07-01), None
patent: WO 03/097593 (2003-11-01), None
patent: WO 03/099844 (2003-12-01), None
patent: WO 03/103574 (2003-12-01), None
patent: WO 03/104257 (2003-12-01), None
patent: WO 04/017911 (2004-03-01), None
patent: WO 2005/013909 (2005-02-01), None
patent: WO 2005/034838 (2005-04-01), None
patent: 829141 (1983-08-01), None
patent: 839532 (1985-06-01), None
patent: 873821 (1987-11-01), None
Bossard, et al., (1996), J. of Bio. Chem;, vol. 271, No. 21, pp. 12517-12524.
Bromme, et al., (1996), Biochemical Journal, vol. 315, pp. 85-89, especially abstract, Figure 1.
Velasco, et al., (1994), J. of Bio. Chem; Vol. 269, No. 43, pp. 27136-27142, especially the abstract.
Magrath, et al., (1994), J. of Med. Chem; vol. 35, No. 23, pp. 4279-4283, especially p. 4281, column 1, structures 1-4 and 7.
Graybill, et al., (1992), Bioorganic & Medicinal Chemistry Letter; vol. 2, No. 11, pp. 1375-1380, especially p. 1377, Scheme 1.
Palmer, et al., (1995), J. of Med. Cheml; vol. 38, No. 17, pp. 3193-3196.
Danheiser, (1995), Genetic Engineering News; vol. 15, No. 17, pp. 1-1 and 35-36.
Rasnick, (1996), Perspectives in Drug Discovery & Design; vol. 6, pp. 47-63.
Potempa, et al., “Host andPorphyromonas gingivalisproteinases in periodontitis: A biochemical model of infection and tissue destruction”, (1994), Perspectives in Drug Discovery and Design, vol. 2, pp. 445-458.
Drake, et al., “Cathepsin K, but Not Cathepsins B, L, or S, Is Abundantly Expressed in Human Osteoclasts”, (1996), J. of Biological Chemistry, 271(21). pp. 12511-12516.
Bromme, et al., “Human Cathepsin 02, a Matrix Protein-degrading Cysteine Protease Expressed in Osteoclasts”, (1996), J. of Biological Chemistry, 271(4), pp. 2126-2132.
Delaisse, et al., “In Vivo and In Vitro Evidence for the Involvement of Cysteine Proteinases in Bone Resorption”, (1984), Biochemical and Biophysical Research Communications, 125(2), pp. 441-447.
Delaisse, et al., “Inhibition of bone resorption in culture by inhibitors of thiol procinases”, (1980), Biochem. J., 192, pp. 365-368.
Lerner, et al., “Human Crystatin C, a Cysteine Proteinase Inhibitor, Inhibits Bone Resorption In Vitro Stimulated by Parathyroid Hormone and Parathyroid Hormone-Related Peptide of Malignancy”, (1992), J. of Bone and Mineral Research, 7(4), pp. 433-439.
Hill, et al., “Inhibition of Bone Resorption by Selective Inactivators of Cysteine Proteinases”, (1994), J. of Cellular Biochemistry, 56, pp. 118-130.
Delaise, et al., “The Effects of Inhibitors of Cysteine-Proteinases and Collagenase on the Pesorptive Activity of Isolated Osteoclasts”, Bone, 8, pp. 305-313 (q987).
Borg, et al, “Synthesis of 1,2,4-Oxadiazole-, 1,3,4,-Oxadiazole-, and 1,2,4-Triazole-Derived Dipeptidomietics”, J. Org. Chem., 60, pp. 3112-3120 (1995).
Boden, et al, “Total Synthesis of Lissoclinamide 5, a Cytotoxic Cyclic Peptide from the TunicateLissoclinum patella”, (1994), Tetrahedron. Ltrs., 35(44), pp. 8271-8274.
Everts, et al., “Degradation of Collagen in the Bone-Resorbing Compartment Underlying the Osteoclast Involved Both Cysteine-Proteinases and Matrix Metalloproteinases”, (1992), Journal of the Cellular Physiology, 150, pp, 221.231.
Shi, et al., “Molecular cloning of human cathepsin O, a novel endoproteinase and homolog

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