Novel x-conotoxin peptides (-i)

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 7/08 (2006.01) A61K 38/04 (2006.01) A61P 9/00 (2006.01) A61P 13/00 (2006.01) A61P 25/00 (2006.01) A61P 29/00 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2508129

An isolated, synthetic or recombinant .chi.-conotoxin peptide comprising the following sequence of amino acids: Xaa1 Xaa2 Gly Val Cys Cys Gly Tyr Lys Leu Cys His Pro Cys SEQ ID NO. 3 where Xaa1 is a N-terminal Xaa1 is a N-terminal pyroglutamate (pGlu) or D-pyroglutamate (DpGlu) residue; and Xaa2 is Asn or a deletion; or such a sequence in which one or more Cys is replaced with its corresponding D-amino acid and/or one or more amino acid residues other than Cys has undergone a side chain modification, or a salt, ester, amide or prodrug thereof. The invention also relates to pharmaceutical compositions comprising these peptides and the use of these peptides in the prophylaxis or treatment of conditions, such as but not limited to, pain, inflammation, incontinence, cardiovascular conditions and mood disorders.

La présente invention a trait à un peptide isolé, synthétique ou recombinant de .chi.-conotoxine comprenant la séquence d'acides aminés suivante : Xaa1 Xaa2 Gly Val Cys Cys Gly Tyr Lys Leu Cys His Pro Cys SEQ ID NO. 3, où Xaa1 est un résidu pyroglutamate (pGlu) ou D-pyroglutamate (PdGlu) N-terminal ; et Xaa2 est Asn ou une délétion ; ou une telle séquence dans laquelle un ou des Cys est/sont remplacé(s) avec son/leur acide aminé D correspondant et/ou un ou des résidus d'acide aminé autre que Cys a été soumis à une modification de chaîne latérale, ou un sel, ester, amide ou prodrogue de celui-ci. L'invention a également trait à des compositions pharmaceutiques comprenant lesdits peptides et l'utilisation desdits peptides dans la prophylaxie ou le traitement de conditions telles que, mais de manière non exclusive, la douleur, l'inflammation, l'incontinence, les conditions cardio-vasculaires ou des troubles de l'humeur.

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