High affinity small molecule C5a receptor modulators
US6723743B1 · kind B1 · utility
Assignee
Inventors
Key dates
| Filing date | Sep 28, 2000 |
| Grant date | Apr 20, 2004 |
| Priority date | — |
| Expiry date | Oct 20, 2020 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07C2603/18
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors, preferably human C5a receptors, Preferred compounds of the invention possess one or more, and preferably two or more, three or more, four or more, or all of the following properties in that they are; 1) multi-aryl in structure (having a plurality of un-fused or fused aryl groups), 2) heteroaryl in structure, 3) orally available in vivo (such that a sub-lethal or preferably a pharmaceutically acceptable oral dose can provide a detectable in vitro effect such as a reduction of C5a-induced neutropenia), 4) comprised of fewer than four, preferably fewer than three, or fewer than two, or no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar concentrations and preferably at sub-nanomolar concentrations. Specifically exemplified representative compounds include, but are not limited to optionally substituted arylimidazoles, optionally substituted a…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.