Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2008-07-29
2008-07-29
Coleman, Brenda L (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C514S217030, C514S217040, C514S217050, C514S217060, C514S217070, C514S217080, C514S217090, C514S217100, C514S217110, C540S525000, C540S596000, C540S597000, C540S598000, C540S599000, C540S601000, C540S602000, C540S603000, C540S604000
Reexamination Certificate
active
07405209
ABSTRACT:
The present invention provides 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, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound 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: 4638010 (1987-01-01), Weller, III et al.
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), Adams 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 et al.
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: 2006/0052365 (2006-03-01), Bondinell et al.
patent: 2006/0194787 (2006-08-01), Cummings et al.
patent: 0 237 082 (1987-09-01), None
patent: 0 504 938 (1992-03-01), None
patent: 0 525 420 (1993-02-01), None
patent: 0 543 310 (1993-05-01), None
patent: 0 603 873 (1994-06-01), None
patent: 0 611 756 (1994-08-01), None
patent: 0 623 592 (1994-11-01), None
patent: WO 92/04371 (1992-03-01), 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 94/24182 (1995-09-01), None
patent: WO 96/13523 (1996-05-01), None
patent: WO 96/40737 (1996-12-01), 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: WO97/49668 (1997-12-01), None
patent: WO 98/05336 (1998-02-01), None
patent: WO 98/08802 (1998-03-01), 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 00/38687 (2000-07-01), None
patent: WO 00/39115 (2000-07-01), 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 01/34153 (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 01/34160 (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 03/053331 (2003-07-01), 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., (1992), J. of Med. Chem; vol. 35, No. 23, pp. 4279-4283, especially p. 4281, col. 1, structures 1-4 and 7.
Graybill, et al., (1992), Bioorganic & Medicinal Chemistry Letters; vol. 2, No. 11, pp. 1375-1380, especially p. 1377, Scheme I.
Palmer, et al., (1995), J. of Med. Chem; 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. 48-63.
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 proteinases”, (1980), Biochem. J., 192, pp. 365-368.
Lerner, et al., “Human Cystatin C, a Cysteine Proteinase Inhibitor, Inhibits Bone Resporption 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 Resorptive Activity of Isolated Osteoclasts”, Bone, 8. pp. 305-313, 1987.
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 Involves Both Cysteine-Proteinases and Matrix Metalloproteinases”, (1992), Journal of Cellular Physiology, 150, pp. 221-231.
Shi, et al., “Molecular cloning of human cathepsin O, a novel endoproteinase and homologue of rabbit OC2”, (1995), FEBS Ltrs., 357, pp. 129-134.
Inaoka, et al., “Molecular Cloning of Human cDNA for Cathepsin K: Novel Cysteine Proteinase Predominantly Expressed in Bone”, (1995), Biochemical and Biophysical Research Communications, 206(1), pp. 89-96.
Elmore, et al., “A New Method for Determining the Absolute Molarity of Solutions of Trypsin and Chymotrypsin . . . ”, (1968), Biochem J., 107, pp. 103-107.
Barker, et al., “The Reaction of an α-Aza-Amino Acid Derivative with Chymotrypsin and Its Use as a Ligand . . . ”, (1974), Biochem J., 139, 555-563.
Gray, et al., “Nα-Ethyloxycarbonyl-α-Azaornithine Phen . . . ”, (1977), Tetrahedron, 33, p. 837-840.
Tezuka, et al., “Molecular Cloning of a Possible Cysteine Proteinase Predominantly Expressed in Osteoclasts”, (1994), J. Biolog. Chem., 269(2), pp. 1106-1109.
Gupton, et al., “Reaction of Azapeptides with Chymotrypsin-like Enzymes&#x
Cummings Maxwell David
Marquis, Jr. Robert Wells
Ru Yu
Thompson Scott Kevin
Veber Daniel Frank
Coleman Brenda L
Hall Linda E
Kinzig Charles M
SmithKline Beecham Corporation
SmithKline Beecham p.l.c.
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