Adenosine A3 receptor agonists

Details Adenosine A3 receptor agonists Adenosine A3 receptor agonists

2005-07-05

2005-07-05

Wilson, James O. (Department: 1623)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

C536S027230, C536S027610, C536S027630

Reexamination Certificate

active

06914053

ABSTRACT:
Disclosed are novel adenosine A3receptor agonists of Formula I:wherein:R is hydrogen or lower alkyl;R1is optionally substituted lower alkoxy or optionally substituted cycloalkyloxy;R2is hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted trialkylsilyl; andR3is hydroxymethyl or R4R5NC(Q)—;in which R4and R5are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, or optionally substituted heteroaryl.

REFERENCES:
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patent: WO 00/78779 (2000-12-01), None
(R) Volpini et al., “N6-Alkyl-2-alkynyl Derivatives of Adenosine as Potent and Selective Agonists at the Human Adenosine A3 Receptor and a Starting Point for Searching A2B Ligands,” Journal of Medicinal Chemistry, 45(15), 3271-3279 (Jul. 18, 2002).
(S) Baraldi et al., “Synthesis and and Biological Activity of a New Series of N6-Arylcarbamoyl, 2(Ar)alkynyl-N6-arylcarbamoyl, and N6-Carboxamido Derivatives . . . ,” Journal of Medicinal Chemistry, 41(17), 3174-3185 (Aug. 13, 1998).
(T) Siddiqi et al., “Search for New Purine- and Ribose-Modified Adenosine Analogues as Selective Agonists and Antagonists a Adenosine Receptors, ” Journal of Medicinal Chemistry, 38(7), 1174-1188 (Mar. 31, 1995).
(U) Klotz et al. (l), “2-Substituted N-ethylcarboxamidoadenosine Derivatives as High-Affinity Agonists at A3 Adenosine Receptors,” Naunyn-Schmiedeberg's Archives of Pharmacology, 360(2), 103-108 (1999); published online on Jul. 13, 1999.
(V) Klotz et al. (II), “Comparative Pharmacology of Human Adenosine Receptor Subtypes—Characterization of Stably Transfected Receptors in CHO Cells,” Naunyn-Schmiedeberg's Archives of Pharmacology, 357(1), 1-9 (1998).
(W) Stu Borman, “A3 Receptors,” Science & Technology Section of Chemical & Engineering News, 79(7), 37-40 (Feb. 12, 2001).
Volpini et al., “N6-Alkyl-2-alkynyl Derivatives of Adenosine as Potent and Selective Agonists at the Human Adenosine A3Receptor and a Starting Point for Searching A2BLigands,”Journal of Medicinal Chemistry, 45(15), 3271-3279 (Jul. 18, 2002).
Baraldi et al., “Synthesis and and Biological Activity of a New Series of N6-Arylcarbamoyl, 2(Ar)alkynyl-N6-arylcarbamoyl, andN6-Carboxamido Derivatives of Adenosine-5'-N-ethyluronamide as A1and A3Adenosine Receptor Agonists,”Journal of Medicinal Chemistry, 41(17), 3174-3185 (Aug. 13, 1998).
Siddiqi et al., “Search for New Purine- and Ribose-Modified Adenosine Analogues as Selective Agonists and Antagonists at Adenosine Receptors,”Journal of Medicinal Chemistry, 38(7), 1174-1188 (Mar. 31, 1995).
Klotz et al. (I), “2-Substituted N-ethylcarboxamidoadenosine Derivatives as High-Affinity Agonists at A3Adenosine Receptors,”Naunyn-Schmiedeberg's Archives of Pharmacology, 360(2), 103-108 (1999); published online on Jul. 13, 1999.
Klotz et al. (II), “Comparative Pharmacology of Human Adenosine Receptor Subtypes—Characterization of Stably Transfected Receptors in CHO Cells,”Naunyn-Schmiedeberg's Archives of Pharmacology, 357(1), 1-9 (1998).
Stu Borman, “A3Receptors,” Science & Technology Section ofChemical&Engineering News, 79(7), 37-40 (Feb. 12, 2001).
Klotz et al: “2-Substituted N-Ethylcarboxamidoadenosine Derivatives as High-Affinity Agonists at Human A3 Adenosine Receptors”, Nauny-Schmiedeberg's Archives of Pharmacology, Springer, Berlin, DE., vol. 360, No. 2, 1999, pp. 103-108 XP000984051, ISSN: 0028-1298, compound 8, tables 1,2 (Jul. 13, 1999).
Baraldi et al: “Novel N6-(Substituted-phenylcarbamoyl) Adenosine-5'-Uronamides as Potent Agonist for A2 Adenosine Receptors”, Journal of Medicinal Chemistry, American Chemical Society, Washington, US, vol. 39, No. 3, (Feb. 1996), pp. 802-806, XP002913657, ISSN: 0022-2623, conclusions on p. 804, pp. 803, col. 2, paragraph 4; (Publ. ACS Abstr; Dec. 15, 1995).

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