Epoxy-guaiane derivatives and treatment of cancer

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 493/08 (2006.01) A61K 31/35 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2711434

Disclosed are englerins and derivatives (I) thereof useful in the treatment of a number of cancers, particularly renal cancer, as well as pharmaceutical compositions and method of treating a patient with the use of these derivatives. The englerins, for example Englerin A and Englerin B, can be isolated from the plant Phyllanthus engleri or produced by synthetic methods. An example of the englerin derivative is 2'-chloroenglerin A, which has the structure (II), wherein double bond 'a' is E, Z, or a mixture of E and Z.

L'invention concerne des englérines et des dérivés (I) de celles-ci utiles dans le traitement de plusieurs cancers, en particulier le cancer du rein, de même que des compositions pharmaceutiques et des procédés de traitement d'un patient par l'utilisation de ces dérivés. Les englérines, par exemple l'englérine A et l'englérine B, peuvent être isolés du végétal Phyllanthus engleri ou produit par des procédés synthétiques. Un exemple de dérivé d'englérine et de la 2'-chloroenglérine A, qui a la structure (II), dans laquelle une double liaison "a" est E, Z, ou un mélange de E et Z.

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