Invention Grant
- Patent Title: Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders
- Patent Title (中): 用于治疗心血管,炎症和免疫疾病的化合物和方法
-
Application No.: US08390641Application Date: 1995-02-17
-
Publication No.: US06201016B1Publication Date: 2001-03-13
- Inventor: Xiong Cai , Gurmit Grewal , Sajjat Hussoin , Aberra Fura , Ralph Scannell , Tesfaye Biftu
- Applicant: Xiong Cai , Gurmit Grewal , Sajjat Hussoin , Aberra Fura , Ralph Scannell , Tesfaye Biftu
- Main IPC: A61K3134
- IPC: A61K3134

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.
Information query