Farnesyl dibenzodiazepinone, processes for its production...

C - Chemistry – Metallurgy – 12 – N

Patent

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Details

C12N 1/20 (2006.01) A61K 31/5513 (2006.01) A61P 31/04 (2006.01) A61P 35/00 (2006.01) C07D 243/38 (2006.01) C07D 405/06 (2006.01) C12N 1/21 (2006.01) C12N 9/00 (2006.01) C12N 9/02 (2006.01) C12N 9/10 (2006.01) C12N 9/12 (2006.01) C12N 9/14 (2006.01) C12N 9/88 (2006.01) C12N 9/90 (2006.01) C12N 15/52 (2006.01) C12P 1/06 (2006.01) C12P 17/10 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2466340

This invention relates to a novel farnesylated dibenzodiazepinone, named ECO-04601, its pharmaceutically acceptable salts and derivatives, and to methods for obtaining such compounds. One method of obtaining the ECO-04601 compound is by cultivation of a novel strain of Micromonospora sp., 046-ECO11; another method involves expression of biosynthetic pathway genes in transformed host cells. The present invention further relates to Micromonospora sp. strain 046-ECO11, to the use of ECO-04601 and its pharmaceutically acceptable salts and derivatives as pharmaceuticals, in particular to their use as inhibitors of cancer cell growth, bacterial cell growth, mammalian lipoxygenase, and to pharmaceutical compositions comprising ECO-04601 or a pharmaceutically acceptable salt or derivative thereof. Finally, the invention relates to novel polynucleotide sequences and their encoded proteins, which are involved in the biosynthesis of ECO-04601.

L'invention concerne un nouveau dibenzodiazépinone </= FARNESYLATé >/= , appelé ECO-04601, ses sels acceptables pharmaceutiquement et ses dérivés, et des méthodes d'élaboration de ces composés. Une méthode d'élaboration du composé ECO-04601 repose sur la culture d'une nouvelle souche de Micromonospora sp., 046-ECO11, une autre méthode implique l'expression de gènes à voie de synthèse biologique dans des cellules hôtes transformées. Cette invention a également pour objet une souche de Micromonospora sp. 046-ECO11, l'utilisation d'ECO-04601, et de ses dérivés et sels acceptables pharmaceutiquement en tant que produits pharmaceutiques, notamment, leur utilisation comme inhibiteurs de la croissance cellulaire cancèreuse, de la croissance cellulaire bactérienne et de la lipoxygénase mammalienne, ainsi que des compositions pharmaceutiques contenant ECO-04601 ou un sel acceptable pharmaceutiquement ou un dérivé correspondant. Enfin, ladite invention a trait à de nouvelles séquences de polynucléotides et à leurs protéines codées qui sont impliquées dans la biosynthèse de ECO-04601.

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