49 results about "Epothilones" patented technology

Recombinant nucleic acids that encode all or a portion of the epothilone polyketide synthase (PKS) are used to express recombinant PKS genes in host cells for the production of epothilones, epothilone derivatives, and polyketides that are useful as cancer chemotherapeutics, fungicides, and immunosuppressants.

The invention relates to a desorption process for epothilones, especially epothilone A and / or epothilone B, from resins and new production, work-up or purification processes or manufacturing methods for epothilones comprising said desorption process, as well as the use of certain solvents for the desorption of epothilones from resins.

Nucleic acid molecules are isolated from Sorangium cellulosum that encode polypeptides necessary for the biosynthesis of epothilone. Disclosed are methods for the production of epothilone in recombinant hosts transformed with the genes of the invention. In this manner, epothilone can be produced in quantities large enough to enable their purification and use in pharmaceutical formulations such as those for the treatment of cancer.

The present invention concerns methods for the production of pharmaceutical formulations of Epothilones suitable for being administered parenterally, such as intravenously.

The invention discloses a method for absorbing and fixing sorangium cellulosum for fermentation based on porous ceramics and belongs to the field of microbial fermentation pharmacy. The method comprises the steps that the prepared porous ceramics are processed by fermentation liquid to be dried for stand-by application; after sorangium cellulosum is cultivated through an M26 solid and a liquid medium respectively, bacterium suspension is formed; and after dilution, the bacterium suspension is inoculated in the fermentation liquid, the processed porous ceramics are added into the fermentation liquid, and shake cultivation is performed. The method for absorbing and fixing an epothilone production bacterial strain based on kieselguhr-based porous ceramics is provided by the invention, when epothilone B is in the fermentation production, sorangium cellulosum, which is the production bacterial strain of the epothilone B, is fixed, so that a solid attachment surface can be provided for a slime bacteria cell growing in a liquid environment, the method has the advantages that the fermentation production yield can be increased, the production cost of epothilone which is an anti-tumor medicine is lowered, and the operation steps are simple and easy to implement, therefore, the method can be amplified to the industrial production and establishes an experimental basis for the industrial production of epothilone.

The invention relates to the treatment of a proliferative disease, especially according to certain treatment regimens, with an epothilone, especially with epothilone A and more preferably epothilone B; as well as to the treatment of certain cancers with such an epothilone.

The invention relates to a preparation method of epothilones B. In particularly, the invention provides a technique method to prepare epothilones B through adopting 100 to 500 liters fermentor to ferment and to separate epothilones B in large scale. The invention also relates to the preparation and application of epothilones B in preparation of gleevec resistance chronic myeloid leukemia treatment drug.

The present invention provides compounds of formula (I):as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).

The invention discloses an additive for increasing the fermentative yield of epothilone, which is indoleacetic acid, indole methyl formate or indole, and the added final concentration of the additive in epothilone liquid fermentation medium is 20 plus / minus 3Mu mol / L. An experiment proves that the additive disclosed by the invention can promote thalli to absorb and utilize nutrient substances and enhance the secondary metabolism of sprangium cellulosums, so that the total amount of epothilone is increased by 2 to 19 percent on average in comparison with the total amount of epothilone not added with the additive. The additive provided by the invention reduces fermentation cost, increases the yield of epothilone, and provides another approach for epothilone production.

This invention provides the use of an Epothilone, which shows an average distribution coefficient between plasma and brain of 0.3 to 1.5 in the mouse intravenous bolus injection assay, for the preparation of a medicament for the treatment of a brain disease associated with proliferative processes.

The invention relates to the field of microbial fermentation, in particular to a preparation method of a defoamer for fermentative production of epothilone; the invention firstly synthesizes di(ethylene glycol) ethyl ether methacrylate modified silicone oil, and then mixes it with a phosphoric acid The phosphorylated polyether-modified aminosilicone oil was mixed with solid powder and reacted to prepare a defoamer suitable for the fermentation of Cystobacter celluliformis. The phosphorylated polyether-modified aminosilicone oil had a branched structure and excellent Shear resistance, suitable for the environment in the fermentation broth; in addition, the addition of polyether structure is beneficial to increase the hydrophilicity of the defoamer, increase the dispersibility of the defoamer in the fermentation broth, and is conducive to enhancing the defoaming Foam-inhibiting ability; the defoamer of the present invention has a promoting effect on the growth of C. cellulosum and the production of epothilone, and is a defoamer product suitable for the fermentation liquid of C. cellulosum.