Methods for improving the antagonistic/agonistic properties...

C - Chemistry – Metallurgy – 07 – K

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Details

C07K 14/575 (2006.01) A61K 38/22 (2006.01) G01N 33/68 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2427490

The present invention relates to a method for improving the antagonistic/agonistic properties of peptidic antagonists/agonists of the corticotropin-releasing factor receptor (CRFR). Further, the present invention relates to an antagonist of the ligand of the corticotropin-releasing factor receptor (CRFR) comprising or alternatively consisting of the amino acid sequence of astressin wherein at least Ala at position 11 is replaced by another amino acid. Further, the present invention relates to an antibody directed against the agonist or antagonist of the present invention. Also described is an anti-idiotypic antibody which is directed against the antibody(ies) of the invention. The present invention also relates to a pharmaceutical or diagnostic composition comprising the antagonist, the agonist, the antibody(ies) and/or the anti-idiotypic antibody of the invention. Furthermore, the present invention relates to a kit comprising the agonist, the antagonist, the antibody(ies) and/or the anti-idiotypic antibody of the present invention. Also described is the use of the agonist, the antagonists, the antibody(ies) and/or the anti-idiotypic antibody of the invention for the preparation of a pharmaceutical composition for the treatment, diagnosis and/or prevention of corticotropin-releasing factor receptor-associated diseases. The present invention also relates to a method of refining the agonist and/or the antagonists of the present invention by means of peptidomimetics and synthesizing the refined compound. Furthermore, the present invention relates to a method of formulating the agonist/antagonist of the invention into a pharmaceutical composition.

L'invention concerne une méthode permettant d'améliorer les propriétés antagonistes/agonistes des antagonistes/agonistes peptidiques du récepteur de la corticolibérine (CRFR) ; un antagoniste du ligand du récepteur de la corticolibérine (CRFR) comprenant ou constitué alternativement de la séquence d'acides aminés de l'astressine dans lequel Ala en position 11 est remplacé par un autre acide aminé ; un anticorps dirigé contre l'agoniste ou l'antagoniste selon l'invention ; un anticorps anti-idiotypique qui est dirigé contre le ou les anticorps selon l'invention ; une composition pharmaceutique ou diagnostique comprenant l'antagoniste, l'agoniste, le ou les anticorps et/ou l'anticorps anti-idiotypique selon l'invention ; une trousse comprenant l'agoniste, l'antagoniste, le ou les anticorps et/ou l'anticorps anti-idiotypique selon l'invention ; l'utilisation de l'agoniste, des antagonistes, du ou des anticorps et/ou de l'anticorps anti-idiotypique selon l'invention pour la préparation d'une composition pharmaceutique pour le traitement, le diagnostic et/ou la prévention des maladies associées au récepteur de la corticolibérine ; une méthode permettant d'affiner l'agoniste et/ou les antagonistes selon l'invention au moyen de peptidomimétiques et de synthétiser le composé affiné ; une méthode permettant de formuler l'agoniste/antagoniste selon l'invention en une composition pharmaceutique.

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