Compounds that block the c5a receptor and their use in therapy

Details Compounds that block the c5a receptor and their use in therapy Compounds that block the c5a receptor and their use in therapy

C - Chemistry, Metallurgy

07

K

C07K 14/31 (2006.01) A61K 38/16 (2006.01) G01N 33/566 (2006.01)

Patent

CA 2563390

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 Xn-E-X39-K-X7~ Y-V-X11-Y-Xm, wherein Xn X39,X7 X11 and Xm 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.

La présente invention concerne des composés pouvant empêcher un contact intramoléculaire des résidus 10 à 18 à terminaison N du récepteur C5a humain avec les boucles extracellulaires de ce dernier. Plus spécifiquement, l'invention concerne des composés pouvant fixer les aspartates au niveau des positions 10, 15 et 18 et la glycine au niveau de la position 12 du récepteur C5a humain. Lesdits composés sont de préférence représentés par la formule générale Xn-E-X39-K-X7- Y-V-X11-Y-Xm, dans laquelle Xn X39,X7 X11 et Xm sont des suites d'acides aminés et les autres lettres représentent les acides aminés correspondants ou des analogues non protéinogéniques de ces derniers. L'invention concerne également leur utilisation dans la prophylaxie et la thérapie.

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