1-aryl-4-substituted isoquinolines
US7915288B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | May 6, 2005 |
| Grant date | Mar 29, 2011 |
| Priority date | — |
| Expiry date | Jan 27, 2028 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D413/14
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.