Compounds that Block the C5a Receptor and Their Use in Therapy
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United States of America Patent
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Issued Date -
Sep 25, 2008
app pub date -
Apr 15, 2005
filing date -
Apr 16, 2004
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Abstract
The present invention relates to compounds that are able to prevent intramolecular contact of the N-terminal residues 10 to 18 of human C5aR with the extracellular loops thereof. More specifically the invention relates to compounds that are able to bind the aspartates in positions 10, 15 and 18 and the glycine in position 12 of the human C5aR. Such compounds are preferably of the general formula X.sub.n-E-X.sub.39-K-X.sub.7Y-V-X.sub.11-Y-X.sub.m, wherein X.sub.nX.sub.39, X.sub.7X.sub.11 and X.sub.m are stretches of amino acids and the other letters represent the corresponding amino acids or non-proteinogenic analogs thereof. The invention further relates to their use in prophylaxis and therapy.
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