Molecules for targeting and releasing therapeutic compounds,...

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 19/00 (2006.01) A61K 38/02 (2006.01) C07K 14/47 (2006.01)

Patent

CA 2528186

The invention relates to chimera molecules for targeting and releasing therapeutic compounds in mammals, especially humans. The inventive molecules have essentially three functional segments or domains: a targeting segment that can preferentially bind to the surface of the targeted cells, a therapeutic segment comprising the biologically active compound, and a segment which binds the targeting segment and the therapeutic segment and can be cleaved onto the target site. The invention also relates to the preparation of said molecules, to synthesis intermediates or domains thereof, to pharmaceutical compositions containing the same, and to the use thereof, especially in the pharmaceutical field. The inventive molecules and compositions are especially adapted to the targeting of pathological cells in an apoptotic phase, and to the treatment of pathologies or associated tissues, especially cancers and inflammation.

La présente invention se rapporte à des molécules chimères permettant le ciblage et la libération de composés thérapeutiques chez des mammifères, notamment des humains. Les molécules de l'invention comprennent principalement trois segments ou domaines fonctionnels : un segment de ciblage, capable de se lier préférentiellement à la surface des cellules ciblées, un segment thérapeutique, comprenant le composé biologiquement actif, et un segment de liaison entre le segment de ciblage et le segment thérapeutique, le segment de liaison étant clivable sur le site cible. L'invention concerne également la préparation de ces molécules, des intermédiaires de synthèse ou domaines de celles-ci, des compositions pharmaceutiques les contenant, et leurs utilisation, en particulier dans le domaine pharmaceutique. Les molécules et compositions de l'invention sont tout particulièrement adaptées au ciblage de cellules pathologiques engagées dans une voie apoptotique, et au traitement de pathologies ou tissus associés, notamment les cancers et l'inflammation.

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