Dextra is very pleased to announced that it has just received the French Ministére de L’Enseignement Supérieur et de la Recherche Tax Credit certificate. This is good news for any business from French companies as they will receive the full tax benefits as if Dextra was located in France.
Congratulations to Dextra, Professor George Fleet and his team for the Tetrahedron Asymmetry award for Top 25 cited authors.
Award for the paper entitled:
Looking glass inhibitors: scalable syntheses of DNJ, DMDP, and (3R)-3-hydroxy-L-bulgecinine from D-glucuronolactone and of L-DNJ, L-DMDP, and (3S)-3-hydroxy-D-bulgecinine from L-glucuronolactone. DMDP inhibits beta-glucosidases and beta-galactosidases whereas L-DMDP is a potent and specific inhibitor of alpha-glucosidases
Tetrahedron Asymmetry, Volume 21, Issue 3, 2010.
Abstract
A convenient large-scale synthesis of 1-deoxynojirimyin (DNJ) from D-glucuronolactone involves introduction of azide at C-5 with retention of configuration to give 5-azido-5-deoxy-1,2-O-isopropylidene-alpha-D-glucofuranose as a key intermediate in an overall yield of up to 72%; the same intermediate can be transformed into DMDP (2R,3R,4R,5R)-2,5-bis(hydroxymethyl)pyrrolidine-3,4-diol] and (3R)-3-hydroxy-L-bulgecinine [(2S,3R,4R,5R)-3,4-dihydroxy-5-hydroxymethyl-L-proline]. L-Glucuronolactone, a readily available L-sugar chiron, may similarly be used to access the enantiomers L-DNJ, L-DMDP, and (3S)-3-hydroxy-D-bulgecinine. A comparison of glycosidase inhibition by DMDP (an inhibitor of beta-glucosidases and beta-galactosidases) and L-DMDP (a potent and specific alpha-glucosidase inhibitor) with the corresponding enantiomeric hydroxybulgecinines is reported; DMDP and (3R)-3-hydroxy-L-bulgecinine show weak inhibition of glycogen phosphorylase.
We are pleased to announce that Dextra Laboratories Ltd will attend BIO 2012 in Boston, MA, on June 18-21, 2012.
Please arrange to see us by direct email contact to dextra@dextrauk.com, or arrange a meeting with us (NZP-Dextra) in the Partnering Program, to discuss the supply of API cGMP bile acids, nucleosides and carbohydrate derivatives for clinical trials, custom synthesis, blood purification, mannosamine derivatives and glycobiology products.
All preparations can be developed from concept through to Phase II at the Dextra, Reading, UK site and larger scale manufacturing undertaken at NZP. NZP manufactures large volumes of the key bile acid cholic acid, bile acid derivatives and GMP quality ManNAc.
National Human Genome Research Institute (NHGRI) (Bethesda, MD; www.genome.gov ) and New Zealand Pharmaceuticals Ltd (NZP) (Palmerston North, New Zealand; www.nzp.co.nz ) have partnered on a drug development project. The goal is to reduce or halt the progression of a rare disorder, Hereditary Inclusion Body Myopathy (HIBM) by treating affected patients with a small molecule therapeutic drug. HIBM primarily affects distal muscle tissue, and due to dramatically decreased muscle strength, most HIBM patients must use a wheelchair by the time they are in their 30s. NZP has licensed NHGRI’s patent portfolio related to treating HIBM and other muscle wasting diseases, as well as kidney diseases related to hyposialylation, with a monosaccharide N-Acetyl-D-mannosamine (ManNAc), also known as DEX-M74. DEX-M74 is one of the first molecules to enter development in the Therapeutics for Rare and Neglected Diseases (TRND) program (http://nctt.nih.gov/trnd ) at the National Institutes of Health (NIH). NZP and TRND are currently collaborating to complete needed pre-clinical studies for treating HIBM with DEX-M74 - these studies will be the basis of an investigational new drug application (IND) to be submitted to the Food and Drug Administration (FDA). Once the IND goes into effect, a phase I/II clinical trial is scheduled to begin at the NIH Clinical Center. That study will be led by HIBM expert and NHGRI Clinical Director, Dr. William Gahl, M.D., Ph.D.