| 摘要 |
<P>PROBLEM TO BE SOLVED: To provide low molecular weight, non-peptidic, non-peptidomimetic, organic compounds that can act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also such ligands that can act as antagonists or inverse agonists of complement C5a receptors. <P>SOLUTION: The compound possesses the following properties: (1) a polycyclic aryl structure; (2) a heteroaryl structure; (3) a pharmaceutically acceptable oral dose which can detect an effect in vivo; (4) amide bonds fewer than four or preferably no amide bonds, and (5) inhibitory capacity inhibiting leukocyte chemotaxis at nanomolar, preferably sub-nanomolar concentration. There also are provided pharmaceutical compositions comprising such compounds and the use of such compositions in treating a variety of inflammatory and immune system disorders. <P>COPYRIGHT: (C)2012,JPO&INPIT |
