1-aryl-4-substituted isoquinolines

Details 1-aryl-4-substituted isoquinolines 1-aryl-4-substituted isoquinolines

2011-03-29

2011-03-29

Davis, Zinna N (Department: 1625)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

C546S144000

Reexamination Certificate

active

07915288

ABSTRACT:
1-aryl-4-substituted isoquinoline or 1-aryl-3,4-disubstituted isoquinoline analogues of Formula I and Formula II, as follows:wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I and II 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 1-aryl-4-substituted isoquinolines or 1-aryl-3,4-disubstituted isoquinolines, which are useful as probes for the localization of C5a receptors.

REFERENCES:
patent: 4260611 (1981-04-01), Bartmann et al.
patent: 4282223 (1981-08-01), Bartmann et al.
patent: 6114530 (2000-09-01), Yuan et al.
Henry R. A. J., “Reactions of Epimeric 2,2'-diacetyl-1,1',2,2'-tetrahydro-1,1'-biisoquinolines”, J. Org. Chem., vol. 37, No. 21, pp. 3206-3209, 1972.

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