Abstract: The invention relates to a synthesis process. This process relates to the synthesis of the compound of formula (I) according to Scheme A below: in which R1, R2 and R3, which may be identical or different, represent, individually and independently, an alkyl group, characterized by an enzymatic hydrolysis reaction that involves placing the compound of formula (II) in contact with an enzyme that performs a chemoselective hydrolysis of only one of the two ester functions of the compound of formula (II) to obtain the compound of formula (I). The invention allows the industrial preparation of the intermediate of formula (I), which may be used for the preparation of the pharmaceutical active principle repaglinide.
Abstract: The present invention relates to methods and products for improved production of the lantibiotic mersacidin. There is provided a method of producing a mersacidin variant which comprises introducing into a cell which is a ?MrsA host cell an expression vector encoding said variant, and recovering said variant from the cell culture. Preferred variants include the novel variants of Table 1, e.g. mersacidin F3W, said mersacidin F3W optionally having a further one or more variations, e.g. mersacidin F3W G8A. Also provided is a Bacillus cell which is a SigH deficient strain of Bacillus sp. HIL Y-85,54728 (NCIMB Accession Number NCIMB 41211); this cell may also be used in the production of mersacidin and its variants. Further aspects of the invention include a DNA cassette which comprises a nucleotide sequence encoding the mersacidin mrsA propeptide, and a method to transform a Bacillus HIL host cell with plasmid, which method includes the step of electroporation.
Type:
Grant
Filed:
September 25, 2006
Date of Patent:
September 22, 2009
Assignee:
Novacta Biosystems Limited
Inventors:
Michael John Dawson, Jesus Cortes Bargallo, Antony Nicholas Appleyard, Brian Arthur Michael Rudd, Steven Boakes, Gabriele Bierbaum, Anja Hoffmann, Stephanie Schmitz
Abstract: The present invention provides methods for the treatment or prophylaxis of a microbial infection of the lower intestine or colon in a subject, the method comprising administering to the subject a type-B lantibiotic. In particular, the invention provides methods for the treatment or prophylaxis of a Clostridium difficile infection. The type-B lantibiotics may include compounds selected from the group consisting of mersacidin, actagardine, plantaricin, planosporicin, ruminococcin, antibiotic 10789, michiganin and haloduracin, and derivatives and variants thereof.
Type:
Application
Filed:
January 21, 2009
Publication date:
August 13, 2009
Applicant:
Novacta Biosystems Limited
Inventors:
Sjoerd Nicolaas Wadman, Michael John Dawson, Jesus Cortes Bargallo
Abstract: The present invention relates to methods and products for improved production of the lantibiotic mersacidin. There is provided a method of producing a mersacidin variant which comprises introducing into a cell which is a ?MrsA host cell an expression vector encoding said variant, and recovering said variant from the cell culture. Preferred variants include the novel variants of Table 1, e.g. mersacidin F3W, said mersacidin F3W optionally having a further one or more variations, e.g. mersacidin F3W G8A. Also provided is a Bacillus cell which is a SigH deficient strain of Bacillus sp. HIL Y-85,54728 (NCIMB Accession Number NCIMB 41211); this cell may also be used in the production of mersacidin and its variants. Further aspects of the invention include a DNA cassette which comprises a nucleotide sequence encoding the mersacidin mrsA propeptide, and a method to transform a Bacillus HIL host cell with plasmid, which method includes the step of electroporation.
Type:
Application
Filed:
September 25, 2006
Publication date:
May 24, 2007
Applicant:
Novacta Biosystems Limited
Inventors:
Michael Dawson, Jesus Cortes Bargallo, Antony Appleyard, Brian Rudd, Steven Boakes, Gabriele Bierbaum, Anja Hoffmann, Stephanie Schmitz