Adenosine A 3 receptor modulators

Details Adenosine A 3 receptor modulators Adenosine A 3 receptor modulators

2007-09-18

2007-09-18

Tucker, Zachary C. (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C544S251000

Reexamination Certificate

active

11169311

ABSTRACT:
The compounds of the following formula:wherein R, R2, R3and A have the meanings given in the specification, are endowed with selective A3adenosine receptor antagonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A3receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A3receptor. The compounds can be labeled, for example with fluorescent or radiolabels, and the labels used in vivo or in vitro to determine the presence of tumor cells which possess a high concentration of adenosine A3receptors.

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Baraldi et al., 2000, “Synthesis and Preliminary Biological Evaluation of [3H]-MRE 3008-F20: the First High Affinity Radioligand Antagonist for the Human A3Adenosine Receptors”, Bioorganic & Medicinal Chemestry Letters, 10, pp. 209-211.
Baraldi et al., 2000, “Pyrazolo[4,3-e]1,2,4-traizolo[1,5-c]pyrimidine Derivatives as Highly Potent and Selective Human A3Adenosine Receptor Antagonists: Influence of the Chain at the N8Pyrazole Nitrogen”, J. Med. Chem, 43, pp. 4768-4780.
Baraldi et al., 2001, “Fluorosulfonyl- and Bis-(β-chloroethyl)amino-phenylamino Functionalized Pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine Derivatives: Irreversible Antagonists at the Human A3Adenosine Receptor and Molecular Modeling Studies”, J. Med. Chem., 44, pp. 2735-2742.
Baraldi et al., 2001, “Pyrazolo[4,3-e]1,2,4-Triazolo[1,5-c]Pyrimidine Derivatives as Adenosine Receptor Ligands: A Starting Point for Searching A3Adenosine Receptor Angatonists”, Drug Development Research, 53:225-235.
Baraldi et al., 2002, “Synthesis, Biological Activity, and Molecular Modeling Investigation of New Pyrazolo[4,3,-e]-1,2,4-triazolo[1,5-c]pyrimidine Derivatives as Human A3Adenosine Receptor Antagonists”, J. Med. Chem., 45, pp. 770-780.
Jun. 27, 2005, Search Report issued in connection with EP 02 73 4202.1.

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