C-pyrazole A2A receptor agonists

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

Reexamination Certificate

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C514S045000, C514S047000, C536S027300, C536S027600, C536S027610, C536S027700

Reexamination Certificate

active

07553823

ABSTRACT:
2-adenosine C-pyrazole compounds having formula (a) and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.

REFERENCES:
patent: 3845770 (1974-11-01), Theeuwes et al.
patent: 4326525 (1982-04-01), Swanson et al.
patent: 4902514 (1990-02-01), Barclay et al.
patent: 4956345 (1990-09-01), Miyasaka et al.
patent: 4968687 (1990-11-01), Hutchison
patent: 4992445 (1991-02-01), Lawter et al.
patent: 5001139 (1991-03-01), Lawter et al.
patent: 5032252 (1991-07-01), Owen et al.
patent: 5070877 (1991-12-01), Mohiuddin et al.
patent: 5189027 (1993-02-01), Miyashita et al.
patent: 5270304 (1993-12-01), Kogi et al.
patent: 5459254 (1995-10-01), Yamaguchi et al.
patent: 5593975 (1997-01-01), Cristalli
patent: 5616345 (1997-04-01), Geoghegan et al.
patent: 5705491 (1998-01-01), Yamada
patent: 5770716 (1998-06-01), Khan et al.
patent: 5877180 (1999-03-01), Linden et al.
patent: 5939543 (1999-08-01), Morozumi et al.
patent: 6026317 (2000-02-01), Verani
patent: 6214807 (2001-04-01), Zablocki et al.
patent: 6294522 (2001-09-01), Zablocki et al.
patent: 6322771 (2001-11-01), Linden et al.
patent: 6368573 (2002-04-01), Leung
patent: 6403567 (2002-06-01), Zablocki
patent: 6448235 (2002-09-01), Linden et al.
patent: 6514949 (2003-02-01), Linden et al.
patent: 6552023 (2003-04-01), Zablocki et al.
patent: 6599283 (2003-07-01), Marzilli et al.
patent: 6605597 (2003-08-01), Zablocki et al.
patent: 6642210 (2003-11-01), Zablocki et al.
patent: 6677336 (2004-01-01), Zablocki
patent: 6770634 (2004-08-01), Zablocki et al.
patent: 6855818 (2005-02-01), Zablocki et al.
patent: 7109180 (2006-09-01), Zablocki et al.
patent: 7144872 (2006-12-01), Zablocki et al.
patent: 7183264 (2007-02-01), Zablocki
patent: 2002/0012946 (2002-01-01), Zablocki et al.
patent: 2002/0111327 (2002-08-01), Linden et al.
patent: 2002/0147174 (2002-10-01), Jones et al.
patent: 2004/0064039 (2004-04-01), Belardinelli
patent: 2004/0127533 (2004-07-01), Hart et al.
patent: 2004/0137533 (2004-07-01), Belardinelli
patent: 2005/0020915 (2005-01-01), Belardinelli et al.
patent: 2005/0175535 (2005-08-01), Belardinelli
patent: 2006/0084625 (2006-04-01), Gordi et al.
patent: 2007/0203090 (2007-08-01), Zablocki et al.
patent: 2007/0299089 (2007-12-01), Belardinelli
patent: 2008/0170990 (2008-07-01), Lieu et al.
patent: 2008/0213165 (2008-09-01), Lieu et al.
patent: 2008/0267861 (2008-10-01), Lieu et al.
patent: 965411 (1975-04-01), None
patent: 0 354 638 (1990-02-01), None
patent: S48 26038 (1973-08-01), None
patent: HEI 5 1993 9197 (1993-01-01), None
patent: WO 93/25677 (1993-12-01), None
patent: WO 98/52611 (1998-11-01), None
patent: WO 98/57651 (1998-12-01), None
patent: WO 99/63938 (1999-12-01), None
patent: WO 00/78778 (2000-12-01), None
patent: WO 00/78779 (2000-12-01), None
patent: WO 01/62979 (2001-08-01), None
patent: WO 04/11010 (2004-02-01), None
patent: WO 05/082379 (2005-09-01), None
Cerqueira, “The future of pharmacologic stress: selective A2A adenosine receptor agonists”, Am. J. Cardiol, vol. 94, No. suppl, 2004 pp. 33D-42D.
Cristalli et al., “2-Alkynl Derivatives of Adenosine 5'-N'ethyluronamide: Selective A2 Adenosine Receptor Agonists with Potent Inhibitory Activity on Platelet Aggregation”, J. Med. Chem., 37:1720-1726 (1994).
Gao, et al., “Novel Short-Acting A2A Adenosine Receptor Agonists for Coronary Vasodilation: Inverse Relationship between Affinity and Duration of Action of A2A Agonists”, Journal of Pharmacology and Experimental Therapeutics, vol. 298, pp. 209-218 (2001).
Glover et al. “Characterization of a New, Highly Selective Adenosine A2A Receptor/Agonists with Potential Use in Pharmacologic Stress Perfusion Imaging”, Circulation, vol. 110, pp. 1-311 (1999).
Glover et al., “Pharamacological Stress Thallium Scintigraphy with 2-Cyclohexylmethylidenehydrazinoadenosine”, Circulation, pp. 1726-1732 (1996).
Hendel et al., “Pharmacologic Stress SPECT Myocardial Perfusion Imaging with a Selective A2A Agonist: Results of a Pilot Study Comparing Adenosine with CVT-3146”, Circulation, Supplement IC, vol. 108, p. IV-636 (2003).
Iskandrian, A, “Adenosine Myocardial Perfusion Imaging”, The Journal of Nuclear Medicine, vol. 35, pp. 734-736 (1994).
Jadbabaie, et al. Myocardial perfusion imaging with a novel selective A2A adenosine receptor agoanists (CVT-3146): Imporant differences in radiotracer behavior, JACC, p. 443-444.
Kerensky et al. “Dose Dependent Increase in Human Coronary Blood Flow Velocity Following an IV Bolus of CVT-3146, A Novel A2A Adenosine Receptor Agonists: A Potential Agent for the Use in Pharmacological Stress Testing for Myocardial Perfusion Imaging”, Circulation, vol. 106, p. II-618 (2002).
Korolkovas, Essentials of Molecular Pharmacology-Background for Drug Design, Wiley - Interscience, New York, NY, 1970, only pp. 266-272 supplied.
Kusmic et al., “Coronary microcirculatory vasoconstriction induced by low-flow ischemia in mouse hearts is reversed by an A2A adenosine receptor”, FASEB Journal, Apr. 2007, A1227-A1228.
Koepfli et al., “Interaction of caffeine with regadenoson-induced hyperemic myocardial blood flow as measured by PET”, European Heart Journal, vo. 27 No. Supp. 1, p. 175 (Aug. 2006).
Mager, et al., “Molecular simulation applied to 2-(N'alkylidenehydrazino)- and 2-(N'- aralkylidenehydrazino) adenosine A2 Agnonists”, Eur. J. Med. Chem, 30:15-25 (1995).
Martin et al., “Pharmacology of 2-cylohexylmethylidenehydrazionoadenosine (WRC-0470), a novel, short-acting adenosine A-2A receptor agonist that produces selective coronary vasodilation”, Drup Development Research, vol. 40, No. 4, pp. 313-324 (1997).
Marumoto, et al., “Synthesis and Coronary Vasodilating Activity of 2-Substituted Adenosines”, Chem. . Pharm. Bull. 23 (4): 759-774 (1975).
Marumoto, et al., “Synthesis and Enzymatic Activity of Adenosine 3',5'-Cyclic Phosphate Analogs”, Chem. . Pharm. Bull. 27(4) 990-1003 (1979).
Matsuda, et al., “Nucleosides and Nucleotides. 103. 2-Alkynyladenoines: A Novel Class of Selective Adenosine A2 Receptor Agonists with Potent Antihypertensive Effects”, J. Med. Chem. 35:241-252 (1992).
Persson, et al., “Synthesis and Antiviral Effects of 2-Heteroaryl Substituted Adenosine and 8-Heteroaryl Substituted Guanosine Derivatives”, Bioorganic & Medicinal Chemistry, 3:1377-1382 (1998).
Riou et al., “Influence of propranolol, enalaprilat, verapamil, and caffeine on adenosine A(2A) receotir medicated coronary vasodilation”, Journal of the American College of Cardiology, col. 40, No. 9, pp. 1687-1690 (Nov. 6, 2002).
Swinyard et al., “Pharmaceutical Necessities,” Chapter 66 in Remington's Pharmaceutical Sciences, 18th Ed., Gennaro et al. (eds.), 1990, Mack Publishing Co., Easton, PA, only pp. 1318-1319 supplied.
Trochu et al. “Selective A2A Adenosine Receptor Agonist as a Coronary Vasodilator in Conscious Dogs: Potential for Use in Myocardial Perfusion Imaging,” Jour. of Cardiovasc.
Xu, et al. “Coronary Vasodilation by a Short Acting, Low Affinity A2A Adenosine Receptor Agonist in Anesthetized Closed Chest Dogs: A Second Generation of Coronary Artery Pharmacologic Stressor”, Circulation, vol. 102, No. 18, pp. 3912 (2000).
Xu, Jiang, et al. “Coronary vasodilation by a short acting, low affinity A2A adenosine receptor agonist in anesthetized closed chest dogs: a second generation of coronary artery pharmacologic atressor”, Circulation, vol. 102, No. 18, p. II 810 (2000).
Zhao et al, “Comparative Profile of Vasodilation by CVT-3146, a Novel A2A Receptor Agonist, & Adenosine in Conscious Dogs”, Jour. of Pharm & Experimental Therapeutics, p. 182-9.
Zhao et al., “Effects of caffeine on coronary vasodilation and sinus tachycardia induced by Regadenoson, a novel adenosine A2A receptor agonist, in c

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