Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders
US5681966A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Jun 7, 1995 |
| Grant date | Oct 28, 1997 |
| Priority date | — |
| Expiry date | Jun 7, 2015 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D307/14
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Enantiomerically enriched disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.