3-substituted-6-aryl pyridines

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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Reexamination Certificate

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07863454

ABSTRACT:
3-substituted-6-aryl pyridines of Formula I are provided:wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.

REFERENCES:
Balant et al., “Metabolic Considerations, etc.,” in Manfred ed., Burger's Medicinal Chemistry and Drug Discovery, 5th ed. vol. 1:Principles and Practice, John Wiley & Sons, Inc., 1995.
Vippagunta et al.m “Crystalline Solids”, Advanced Drug Delivery Reviews 48 (2001) 3-26.
Jain et al., “Polymorphism in Pharmacy”, Indian Drugs, 1986, 23(6), 315-329.
Guillory (in Brittain ed.), “Polymorphism, etc.,” NY: Marcel Dekker, Inc., 1999, 1-2, 183-226.

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