Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2008-02-05
2009-12-08
Shameem, Golam M (Department: 1626)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C548S469000, C548S509000
Reexamination Certificate
active
07629377
ABSTRACT:
This invention provides PAI-1 inhibiting compounds of Formula I:wherein: R1, R2, R3, and R4are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5is H, alkyl, perfluoroalkyl, aryl optionally substituted with R5, alkanoyl, aroyl optionally substituted with R8; R6is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.
REFERENCES:
patent: 3026325 (1962-03-01), Heinzelman et al.
patent: 3476770 (1969-11-01), Scherrer
patent: 3557142 (1971-01-01), Bell
patent: 3843683 (1974-10-01), Bell
patent: 4478819 (1984-10-01), Hercelin et al.
patent: 4736043 (1988-04-01), Michel et al.
patent: 4851406 (1989-07-01), Martens et al.
patent: 5151435 (1992-09-01), Bagley et al.
patent: 5164372 (1992-11-01), Matsuo et al.
patent: 5420289 (1995-05-01), Musser et al.
patent: 5482960 (1996-01-01), Berryman
patent: 5502187 (1996-03-01), Ayer et al.
patent: 5541343 (1996-07-01), Himmelsbach et al.
patent: 5612360 (1997-03-01), Boyd et al.
patent: 5859044 (1999-01-01), Dow et al.
patent: 6048875 (2000-04-01), De Nanteuil et al.
patent: 6110963 (2000-08-01), Malamas
patent: 6166069 (2000-12-01), Malamas et al.
patent: 6232322 (2001-05-01), Malamas et al.
patent: 6251936 (2001-06-01), Wrobel et al.
patent: 6302837 (2001-10-01), De Nanteuil et al.
patent: 6479524 (2002-11-01), Priepke et al.
patent: 6599929 (2003-07-01), Cho et al.
patent: 6787556 (2004-09-01), Hargreaves et al.
patent: 6800645 (2004-10-01), Cox et al.
patent: 6800654 (2004-10-01), Mayer et al.
patent: 6844358 (2005-01-01), Malamas et al.
patent: 6939886 (2005-09-01), Mayer et al.
patent: 7351730 (2008-04-01), Mayer et al.
patent: 2003/0013732 (2003-01-01), Elokdah
patent: 2003/0018067 (2003-01-01), Elokdah et al.
patent: 2003/0060497 (2003-03-01), Gerlach et al.
patent: 2003/0125371 (2003-07-01), Elokdah et al.
patent: 2004/0116488 (2004-06-01), Jennings et al.
patent: 2004/0116504 (2004-06-01), Elokdah et al.
patent: 2004/0122070 (2004-06-01), Jennings
patent: 2004/0138283 (2004-07-01), Jennings et al.
patent: 2004/0204417 (2004-10-01), Perez et al.
patent: 2005/0070584 (2005-03-01), Havran et al.
patent: 2005/0070585 (2005-03-01), Elokdah et al.
patent: 2005/0070587 (2005-03-01), Elokdah et al.
patent: 2005/0070592 (2005-03-01), Gundersen
patent: 2005/0096377 (2005-05-01), Hu
patent: 2005/0113428 (2005-05-01), Gopalsamy et al.
patent: 2005/0113436 (2005-05-01), Elokdah et al.
patent: 2005/0113438 (2005-05-01), Hu et al.
patent: 2005/0113439 (2005-05-01), Hu
patent: 2005/0119296 (2005-06-01), Elokdah et al.
patent: 2005/0119326 (2005-06-01), Havran et al.
patent: 2005/0119327 (2005-06-01), Hu
patent: 2005/0215626 (2005-09-01), Havran et al.
patent: 3147276 (1983-06-01), None
patent: 43 38 770 (1995-05-01), None
patent: 19543639 (1997-05-01), None
patent: 19753522 (1999-06-01), None
patent: 0 416 609 (1991-03-01), None
patent: 0 508 723 (1992-10-01), None
patent: 0 512 570 (1992-11-01), None
patent: 0 540 956 (1993-05-01), None
patent: 0 655 439 (1995-05-01), None
patent: 0 759 434 (1997-02-01), None
patent: 0 819 686 (1998-01-01), None
patent: 0 822 185 (1998-02-01), None
patent: 0 955 299 (1999-11-01), None
patent: 1 092 716 (2001-04-01), None
patent: 1 156 045 (2001-11-01), None
patent: 2 244 499 (1975-04-01), None
patent: 2 777 886 (1999-10-01), None
patent: 2 799 756 (2001-04-01), None
patent: 1 321 433 (1973-06-01), None
patent: 94/13637 (1994-06-01), None
patent: 94/14434 (1994-07-01), None
patent: 94/26738 (1994-11-01), None
patent: 95/10513 (1995-04-01), None
patent: 96/06840 (1996-03-01), None
patent: 96/21656 (1996-07-01), None
patent: 96/26207 (1996-08-01), None
patent: 96/32379 (1996-10-01), None
patent: 97/09308 (1997-03-01), None
patent: 97/43260 (1997-11-01), None
patent: 97/48697 (1997-12-01), None
patent: 98/08818 (1998-03-01), None
patent: 99/28297 (1999-06-01), None
patent: 99/43651 (1999-09-01), None
patent: 99/43654 (1999-09-01), None
patent: 99/43672 (1999-09-01), None
patent: 99/46260 (1999-09-01), None
patent: 99/50268 (1999-10-01), None
patent: 99/58519 (1999-11-01), None
patent: 99/61435 (1999-12-01), None
patent: 00/32180 (2000-06-01), None
patent: 00/35919 (2000-06-01), None
patent: 00/46195 (2000-08-01), None
patent: 00/46197 (2000-08-01), None
patent: 00/64876 (2000-11-01), None
patent: 00/64888 (2000-11-01), None
patent: 01/12187 (2001-02-01), None
patent: 02/030895 (2002-04-01), None
patent: 02/072549 (2002-09-01), None
patent: 03/000253 (2003-01-01), None
patent: 03/031409 (2003-04-01), None
patent: 03/068742 (2003-08-01), None
patent: 03/087087 (2003-10-01), None
patent: 2004/052854 (2004-06-01), None
Nordt, T. K. et al., “Differential Regulation by Troglitazone of Plasminogen Activator Inhibitor Type 1 in Human Hepatic and Vascular Cells,”Journal of Clinical Endocrinology and Metabolism, 85(4):1563-1568 (2000).
Aznar, J. et al., “Role of Plasminogen Activator Inhibitor Type 1 in the Pathogenesis of Coronary Artery Diseases,”Haemostasis24: 243-251 (1994).
Carmeliet, P. et al., “Plasminogen Activator Inhibitor—1 Gene-deficient Mice,”Journal of Clinical Investigation, 92: 2756-2760 (Dec. 1993).
Daci, E. et al., “Mice Lacking the Plasminogen Activator Inhibitor 1 are Protected from Trabecular Bone Loss Induced by Estrogen Deficiency,”Journal of Bone and Mineral Research, 15(8):1510-1516 (Nov. 8, 2000).
Biemond, B. J. et al., “Thrombolysis and Reocclusion in Experimental Jugular Vein and Coronary Artery Thrombosis,”Circulation, 91: 1175-1181 (1995).
Levi, M. et al., “Inhibition of Plasminogen Activator Inhibitor-1 Activity Results in Promotion of Endogenous Thrombolysis and Inhibition of Thrombus Experimental Thrombosis,”Circulation85:305-312 (1992).
Rocha, E. et al., “The Relationship Between Impaired Fibrinolysis and Coronary Heart Disease,”Fibrinolysis, 8: 294-303 (1994).
Reilly, C. et al., “Both Circulating and Clot-Bound Plasminogen Activator-1 Inhibit Endogenous Fibrinolysis in the Rat,”Arteriosclerosis and Thrombosis, 11(5): 1276-1286 (Sep./Oct. 1991).
Krishnamurti, C. et al., “Plasminogen Activator Inhibitor: A Regulator of Ancrod-Induced Fibrin Deposition in Rabbits,”Blood, 69(3): 798-803 (Mar. 1987).
Guzzo, P.R. et al., “Synthesis of a conformationally constrained threonin-valine dipeptide mimetic: design of a potential inhibitor of plasminogen activator inhibitor-1,” Tetrahedron Letters,Tetrahedron Letters, 43(1), 41-43 (2002).
U.S. Appl. No. 10/947,710, filed Sep. 23, 2004, Commons et al.
U.S. Appl. No. 10/947,711, filed Sep. 23, 2004, Gopalsamy et al.
U.S. Appl. No. 11/208,777, filed Aug. 22, 2005, Commons et al.
U.S. Appl. No. 11/208,772, filed Aug. 22, 2005, Commons.
U.S. Appl. No. 11/208,775, filed Aug. 22, 2005, Commons et al.
Aggarwal et al., “A catalytic antibody programmed for torsional activation of amide bond hydrolysis,”Chem. Eur. J., Jan. 25, 2003, 9(13), 3132-3142.
Ballantine, J. A., “The Chemistry of Bacteria,”Journal of the Chemical Society Abstracts, 1957, 2222-2227.
Charlton, Peter, “The status of plasminogen activator inhibitor-1 as a therapeutic target,”Expert Opinion on Investigational Drugs, May 1997, 6(5), 539-554.
Crandall, D. L. et al., “Characterization and comparative evaluation of a structurally unique PAI-1 inhibitor exhibiting oral in-vivo efficacy,”Journal of Thrombosis and Haemostasis, Mar. 17, 2004, 2, 1422-1428.
Da Settimo, A. et al., “Reaction of indole derivatives with bromine, substitution, oxidation, an
Crandall David LeRoy
Elokdah Hassan Mahmoud
Gundersen Eric Gould
Mayer Scott Christian
Krulandsky David
Larsen Scott
Ng Mabel
Shameem Golam M
Wyeth
LandOfFree
Substituted naphthyl indole derivatives as inhibitors of... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Substituted naphthyl indole derivatives as inhibitors of..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Substituted naphthyl indole derivatives as inhibitors of... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-4134023