Pharmaceuticals for the imaging of angiogenic disorders

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 7/64 (2006.01) A61K 49/00 (2006.01) A61K 51/08 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07K 7/56 (2006.01)

Patent

CA 2324555

The present invention describes novel compounds of the formula: (Q)d-Ln-Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.

L'invention concerne des nouveaux composés de formule : (Q)¿d?-L¿n?-C¿h?, utiles pour le diagnostic et le traitement du cancer, des méthodes d'imagerie de tumeurs chez un patient, et des méthodes de traitement du cancer chez un patient. Elle porte encore sur des nouveaux composés utiles pour la surveillance du traitement de l'angiogenèse et la destruction de nouveaux vaisseaux angiogènes. Les produits pharmaceutiques sont constitués d'un fragment de ciblage qui se lie à un récepteur qui est régulé positivement pendant l'angiogenèse, d'un groupe de liaison éventuel, et d'un radioisotope efficace au plan thérapeutique ou d'un fragment imageable efficace au plan diagnostique. Le fragment imageable est un rayon gamma ou un radioisotope à émission de positrons, un agent de contraste pour imagerie par résonance magnétique, un agent de contraste aux rayons X, ou un agent de contraste aux ultrasons.

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