The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Mar. 29, 2011
Filed:
May. 06, 2005
Kyungae Lee, Newton, MA (US);
Jun Yuan, Guilford, CT (US);
George D. Maynard, Clinton, CT (US);
Alan Hutchison, Madison, CT (US);
Scott Mitchell, East Haven, CT (US);
Kyungae Lee, Newton, MA (US);
Jun Yuan, Guilford, CT (US);
George D. Maynard, Clinton, CT (US);
Alan Hutchison, Madison, CT (US);
Scott Mitchell, East Haven, CT (US);
Novartis International Pharmaceutical Ltd., Hamilton, BM;
Abstract
1-aryl-4-substituted isoquinoline or 1-aryl-3,4-disubstituted isoquinoline analogues of Formula I and Formula II, as follows: wherein R, R, R, R, R, 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.