Use of substance p antagonists for the treatment of...

A - Human Necessities – 61 – K

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A61K 31/404 (2006.01) A61K 31/40 (2006.01) A61K 31/4035 (2006.01) A61K 31/435 (2006.01) A61K 31/439 (2006.01) A61K 31/445 (2006.01) A61K 31/451 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2373960

The use of antagonists of neurokirin receptors (NK-1; substance P receptors) in the treatment of adenocarcinomas, such antagonists having the following features: pA2>6.0 both in human and in murine tissues, etherocyclic non peptidergic structures, antiangiogenic effects experimentally demonstrated onto the genito-urinary tract tumors induced via orthotopic drafts of human tumoral cells either in the genito-urinary apparatus of either immunodeficient rats or mice, decrease of the tumoral mass on tumors of the genito-urinary tract induced by orthotopic drafts of tumoral cells onto tissues of the genito- urinary tract of either immunodeficient rats or mice. Preferred antagonists are FK 888, CP 96345, CP 99994, SR 140333, CGP 47899, RP 67580, MEN 11149, MEN 11467, GR 205171 or L - 703,606.

L'invention concerne l'utilisation d'antagonistes des récepteurs de neurokinine (NK-1 ; récepteurs de la substance P) afin d'établir un nouveau médicament efficace dans le traitement des adénocarcinomes, ces antagonistes étant au moins une des substances choisies parmi celles présentant les caractéristiques suivantes : pA¿2?>6,0 pour des tissus humains et de souris, des structures hétérocycliques non peptidergiques, des effets anti-angiogéniques démontrés expérimentalement sur les tumeurs du tractus génito-urinaire provoquées par implantation orthotopique de cellules tumorales humaines dans l'appareil génito-urinaire de rats ou de souris immunodéficientes, une décroissance de la masse tumorale des tumeurs du tractus génito-urinaire provoquées par implantation orthotopique de cellules tumorales sur des tissus du tractus génito-urinaire de rats ou de souris immunodéficientes.

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