Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Reexamination Certificate
2006-07-11
2006-07-11
Russel, Jeffrey Edwin (Department: 1654)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
C514S017400, C530S314000, C530S324000, C530S330000
Reexamination Certificate
active
07074765
ABSTRACT:
The invention relates to compounds and methods for inhibiting human platelet aggregation, thrombosis and cell activation mediated by PAR1 and PAR4 using peptide analogs of Arg-Pro-Pro-Gly-Phe that contain one or more amino acid substitutions. The invention also includes screening methods for identifying compounds that inhibit thrombin mediated activities.
REFERENCES:
patent: 5681926 (1997-10-01), Veber et al.
patent: 5688768 (1997-11-01), Coughlin et al.
patent: 5759994 (1998-06-01), Coughlin et al.
patent: 5866681 (1999-02-01), Scarbborough
patent: 5935932 (1999-08-01), Stewart
patent: 6111075 (2000-08-01), Xu et al.
patent: 6124101 (2000-09-01), Coughlin et al.
patent: 6197541 (2001-03-01), Coughlin et al.
patent: 6436400 (2002-08-01), Xu et al.
patent: 6458923 (2002-10-01), Kyle
patent: 6515023 (2003-02-01), Barrow et al.
patent: 6544750 (2003-04-01), Schmaier
patent: 6544982 (2003-04-01), Selnick et al.
patent: 6638980 (2003-10-01), Su et al.
R. A. Houghten, et al., “Simplified Procedure For Carrying Out Simultaneous Multiple Hydrogen Fluoride Cleavages Of Protected Peptide Resins”, Int. J. Peptide Protein Res. 27, 1986, pp. 673-678.
R.B. Merrifield, “Solid Phase Peptide Synthesis. I. The Synthesis Of A Tetrapeptide”, Synthesis Of A Tetrapeptide, Jul. 20, 1963, vol. 85, pp. 2149-2154.
S. K. Fisher, et al., “Muscarinic Receptor Regulation Of Cytoplasmic Ca2+Concentrations In Human SK-N- SH Neuroblastoma Cells: Ca2+Requirements For Phospholipase C Activation”, Neuroscience Laboratory and Department of Pharmacology, University of Michigan, Ann Arbor, Michigan, Molecular Pharmacology, vol. 35, pp. 195-204 (1989).
U. B. Rasmussen, et al., “A Peptide Ligand Of the Human Thrombin Receptor Antagonizes α-Thrombin And Partially Activates Platelets”, The Journal of Biological Chemistry, vol. 268, No. 19. Jul. 5, 1993, pp. 14322-14328.
G. Salvesen, et al., “Human Low-MrKininogen Contains Three Copies Of A Cystatin Sequence That Are Divergent In Structure And In Inhibitory Activity For Cysteine Proteinases”, Biochem. J. (1986) 234, 429-434.
R.A.Houghten, “General Method for the Rapid Solid-Phase Synthesis of Large Numbers of Peptides: Specificity of Antigen-Antibody Interaction at the Level of Individual Amino Acids” Proc. Natl. Acad. Sci. USA, vol. 82, pp. 5131-5135, Aug. 1985.
W. XU, et al. “Cloning And Characterization Of Human Protease-Activated Receptor 4”, Proc. Natl. Acad. Sci. USA, vol. 95., pp. 6642-6646, Jun. 1998.
J. Kellermann, et al. “Completion Of The Primary Structure Of Human High-Molecular-Mass Kininogen, The amino acid sequence of the entire heavy chain and evidence for its evolution by gene triplication”, Eur. J. Biochem. 154, 471-478 (1986).
L.F. Brass, et al. “Structure And Function Of The Human Platelet Thrombin Receptor” The Journal Of Biological Chemistry, vol. 267, No. 20, Jul. 15, 1992, pp. 13795-13798.
T.H. Vu, et al. “Molecular Cloning Of A Functional Thrombin Receptor Reveals A Novel Proteolytic Mechanism Of Receptor Activation”, Cell, vol. 64, pp. 1057-1068, 1991.
N. Kitamura, et al., “Structural Organization Of The Human Kininogen Gene And A model For Its Evolution” The Journal of Biological Chemistry, vol. 260, No. 15, pp. 8610-8617, Jul. 15, 1985.
Y. Takagaki, et al., “Cloning And Sequence Analysis Of eDNAs For Human High Molecular Weight And Low Molecular Weight Prekininogens”, The Journal of Biological Chemistry, vol. 260, No. 14, Jul. 15, 1985, pp. 8601-8609.
M.A. Tayeh, et al., “Surface-Induced Alterations In the Kinetic Pathway For Cleavage Of Human High Molecular Weight Kininogen By Plasma Kallikrein”, The Journal of Biological Chemistry, vol. 269, No. 23, Jun. 10, 1994, pp. 16318-16325.
A.A.K. Hasan, MD. Ph.D. et al., “Bradykinin And Its Metabolite, Arg-Pro-Pro-Gly-Phe, Are Seletive Inhibitors of α-Thrombin-Induced Platelet Activation”, Circulation, vol. 94, No. 3, Aug. 1, 1996, pp. 517-528.
W.D. Ehringer, et al., “Bradykinin Antagonizes The Effects Of α-Thrombin”, Inflammation, vol. 21, No. 3, pp. 279-298, 1997.
M.R. E Silva, et al., “Bradykinin, A Hypotensive And Smooth Muscle Stimulating Factor Released From Plasma Globulin By Snake Venoms And By Trypsin”, Amer. J. Physiol., vol. 156. pp. 261-273, 1949.
F.J. Meloni, et al., “Low Molecular Weight Kininogen Binds To Platelets to Modulate Thrombin-Induced Platelet Activation”, The Journal of Biological Chemistry, vol. 266, No. 11, Apr. 15, 1991, pp. 6786-6794.
Y. Jiang, et al., “Domain 3 Of Kininogens Contains A Cell-Binding Site And A Site That Modifies Thrombin Activation Of Platelets”, The Journal of Biological Chemistry, vol. 267, No. 6, Feb. 25, 1992, pp. 3712-3717.
A.A.K. Hasan, et al., “Thrombostatin Inhibits Induced Canine Coronary Thrombosis”, Thromb Haemost 1999, vol. 82, pp. 1182-1187.
D.B. Cleary, et al., “Establishing The Inhibitory Effects Of Bradykinin On Thrombin”, Archives Of Biochemistry and Biophysics 410, (2003), pp. 96-106.
A.A.K. Hasan, et al., “Thrombostatin Inhibits Cyclic Flow Variations In Stenosed Canine Coronary Arteries”, Thromb Haemost, 2001, vol. 86, pp. 1296-1304.
Y.M. Ayala, et al., “Molecular Mapping Of Thrombin-Receptor Interactions”, Proteins: Structure, Function and Genetics, vol. 45, 2001, pp. 107-116.
A.R. Prieto, et al., “Thrombostatin, A Bradykinin Metabolite, Reduces Platelet Activation In A Model Of Arterial Wall Injury”, Cardiovascular Research 53, (2002) 984-992.
B.F. Santos, et al., “Interaction Of Viper Venom Serine Peptidases With Thrombin Receptors On Human Platelets”, FEBS Letters, 477, (2000) pp. 199-202.
C.H. Chay, et al., “A Functional Thrombin Receptor (Par 1) Is Expressed On Bone-Derived Prostate Cancer Cell Lines”, Urology, vol. 60, 2002, pp. 760-765.
Y. Jiang, et al., “Thrombin-Receptor Activation And Thrombin-Induced Brain Tolerance”, Journal of Cerebral Blood Flow & Metabolism, vol. 22, pp. 404-410 (2002).
A.AK. Hasan, et al., “Mechanisms Of Arg-Pro-Pro-Gly-Phe Inhibition Of Thrombin”, Am J Physiol Heart Circ Physiol, vol. 285, 2003, pp. H183-193.
Srikanth et al. “Reduced Rate of Bradykinin Metabolism Protects the Mouse from Thrombosis”Blood.100, 24a (2002).
Hasan et al., “The Mechanism of Thrombostatin Inhibition of Thrombin”,Blood.98, 530a, (2001).
Altrogge et al. An Assay for High-Sensitivity Detection of Thrombin Activity and Determination of Proteases Activating or Inactivating Protease-Activated Receptors. Analytical Biochemistry. 2000, vol. 277, pp. 33-45.
Dendorfer et al. Structural requirements for B2-agonists with improved degradation stability. Immunopharmacology. 1999, vol. 45, pp. 199-205.
Reissmann et al. Structure activity relationships for bradykinin antagonists on the inhibition of cytokine release and the release of histamine. Peptides. 2000, vol. 21, pp. 527-533.
Hasan Ahmed A. K.
Schmaier Alvin H.
Hobbs Ann S.
Russel Jeffrey Edwin
The Regents of the University of Michigan
Thromgen, Inc.
Venable LLP
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