7,11 disubstituted camptothecin derivatives, formulations...

A - Human Necessities – 61 – K

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Details

A61K 31/4745 (2006.01) A61K 47/16 (2006.01) A61K 47/22 (2006.01) C07D 491/22 (2006.01)

Patent

CA 2188043

The novel compounds 11 hydroxy 7 ethyl camptothecin (compound 1) and 11 hydroxy 7 methoxy camptothecin (compound 2) (11,7 HECPT and 11,7 HMCPT) are active anticancer compounds which are poorly soluble in water. The present invention also claims 11,7 HECPT and 11,7 HMCPT) compositions, the synthesis of 11,7 HECPT or 11,7 HMCPT, the methods of formulation of 11,7 HECPT or 11,7 HMCPT, and the methods of use of 11,7 HECPT or 11,7 HMCPT. Additionally, the claimed invention is directed to novel dosages, schedules, and routes of administration for both the 11,7 HECPT or 11,7 HMCPT formulations to humans with various forms of cancer, Other embodiments of this invention include isolation methods and methods of synthesis of certain camptothecin derivatives.

Les nouveaux composés de la camptothécine 11 hydroxy 7 éthyle (composé 1) et 11 hydroxy 7 méthoxy (composé 2) (11,7 HECPT et 11,7 HMCPT) sont des composés actifs contre le cancer, faiblement solubles dans l'eau. La présente invention concerne également des compositions à base de 11,7 HECPT et 11,7 HMCPT, la synthèse de 11,7 HECPT et 11,7 HMCPT, des procédés de formulation et d'utilisation de ces deux composés. En outre, l'invention se rapporte à de nouveaux dosages, modes d'emploi et voies d'administration des formulations des deux composés 11,7 HECPT ou 11,7 HMCPT, destinées à l'homme atteint de diverses formes de cancer. D'autres modes de réalisation de cette invention comprennent des procédés d'isolation et de synthèse de certains dérivés de la camptothécine.

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