N-pyrazole A 2A receptor agonists

Details N-pyrazole A 2A receptor agonists N-pyrazole A 2A receptor agonists

2006-12-05

2006-12-05

Crane, L. E.. (Department: 1623)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

C536S027810

Reexamination Certificate

active

07144872

ABSTRACT:
This specification discloses 2-adenosine N-pyrazole compounds having the following formula: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.

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Marumoto et al. (I), “Synthesis and Coronary Vasodilating Activity of 2-Substituted Adenosines,”Chemical&Pharmaceutical Bulletin(Japan), 23(4), 759-774 (Apr. 1975).
Marumoto et al. (II), “Synthesis and Enzymatic Activity of Adenosine 3′,5′-Cyclic Phosphate Analogues,”Chemical&Pharmaceutical Bulletin(Japan), 27(4), 990-1003 (Apr. 1979).
Persson et al., “Synthesis and Antiviral Effects of 2-Heteroaryl Substituted Adenosine and 8-Heteroaryl Guanosine Derivatives,”Bioorganic&Medicinal Chemistry, 3(10), 1377-1382 (1995).
Mager et al., “Molecular Simulation Applied to 2-(N′-Alkylidene—hydrazino)- and 2-(N′-Aralkylidenehydrazino)adenosine A2Agonists,”European Journal of Medicinal Chemistry, 30, 15-25 (1995).
Matsuda et al., “Nucleosides and Nucleotides. 103. 2-Alkynyl—adenosines: A Novel Class of Selective Adenosine A2Receptor Agonists with Potent Antihypertensive Effects,”Journal of Medicinal Chemistry, 35(1), 241-252 (Jan. 10, 1992).
[R] Marumoto et al. (I), “Synthesis and Coronary Vasodilating Activity of 2-Substituted Adenosines,” □□Chemical & Pharmaceutical Bulletin (Japan), 23(4), 759-774 (Apr. 1975).
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(T) Persson et al., “Synthesis and Antiviral Effects of 2-Heteroaryl Substituted Adenosine and 8-Heteroaryl Guanosine Derivatives,” □□Bioorganic & Medicinal Chemistry, 3(10), 1377-1382 (1995).
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(V) Matsuda et al., “Nucleosides and Nucleotides. 103. 2-Alkynyladenosines: A Novel Class of Selective Adenosine A2 Receptor Agonists with Potent Antihypertensive Effects,” Journal of Medicinal Chemistry, 35(1), 241-252 (Jan. 10, 1992).
Cristalli et al. “2-Alkynl Derivatives of Adenosine 5′N′ethyluronamide: Selective A2 Adenosie Receptor Agonists with Potent Inhibitory Activity on Platelet Aggregation”, J. Med. Chem, 37:1720-1726 (1994).
Glover, et al., “Pharmacological Stress Thallium Scintigraphy with 2-Cyclohexylmethylidenehydrazinoadenosine”, Circulation, pp. 1726-1732 (1996).

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