Selective melanin-concentrating hormone type -1 receptor...

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 14/575 (2006.01) A61K 38/08 (2006.01) A61K 38/10 (2006.01) A61K 38/22 (2006.01) C07K 7/06 (2006.01) C07K 7/08 (2006.01) G01N 33/566 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2473229

The present invention features truncated hMCH analogs selectively active at MCH-1R over MCH-2R. Using amino acid numbering provided in hMCH, the featured analogs contain an X6 which is either a D-amino acid, 5-guanidinopropionic acid or its lower or higher homolog, or a derivative thereof; and a X10 which is either asparagine, glutamine, alanine, leucine, isoleucine, valine, norleucine, cyclohexylalanine, phenylalanine, (2')-naphthylalanine, tyrosine, histidine, tryptophan, lysine, serine, threonine, methionine, or a derivative thereof.

L'invention concerne des analogues de la hMCH tronquée, actifs de manière sélective sur la MCH-1R et sur la MCH-2R. Au moyen d'une numérotation d'aminoacide effectuée dans la hMCH, les analogues de l'invention contiennent un X?6¿ qui représente soit un aminoacide-D, un acide 5-guanidinepropionique ou son homologue supérieur ou inférieur, ou un de ses dérivés ; et un X?10¿ qui représente soit asparagine, glutamine, alanine, leucine, isoleucine, valine, norleucine, cyclohexylalanine, phénylalanine, (2')-naphtylalanine, tyrosine, histidine, tryptophane, lysine, sérine, thréonine, méthionine, ou un de leurs dérivés.

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