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Richmond, Australia

Marcuccio S.M.,Advanced Molecular Technologies Ltd. | Epa R.,Advanced Molecular Technologies Ltd. | White J.M.,University of Melbourne | Deadman J.J.,Avexa Ltd
Organic Process Research and Development | Year: 2011

Apricitabine is a novel inhibitor of the HIV virus reverse transcriptase polymerase which is currently in clinical development for the treatment of AIDS. A new process for the preparation of apricitabine is presented which requires only three steps from 2-(R)-benzoyloxymethyl-1,3-oxathiolane. The new process produces the cis-(2R,4R) isomer in greater than 99% diastereomeric excess by preferential crystallisation of the conglomerate form of the novel 2-(R)-benzoyloxymethyl-4-(R)-(N-benzoylcytosin-1-yl)-1,3-oxathiolane intermediate without requiring chromatography. Deprotection of the intermediate in 88% yield then gives chiral apricitabine, in 30% overall yield. The new method avoids a lengthy salt formation/-break stage, does not require toluene sulphonic acid, and introduces no new byproduct to the manufacturing process. © 2011 American Chemical Society. Source


Spencer J.,University of Greenwich | Patel H.,University of Greenwich | Callear S.K.,University of Southampton | Coles S.J.,University of Southampton | Deadman J.J.,Avexa Ltd
Tetrahedron Letters | Year: 2011

A library of pyridines and pyrimidines has been synthesised in excellent yields employing microwave and flow chemistry methodologies. Work-up bottlenecks have been facilitated substantially by the use of supported reagents and many of the final compounds have been studied in the solid state by single crystal X-ray diffraction. © 2011 Elsevier Ltd. All rights reserved. Source


Patent
AVEXA Ltd | Date: 2012-09-13

The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.


Patent
AVEXA Ltd | Date: 2012-02-27

The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided.


Patent
AVEXA Ltd | Date: 2010-04-23

The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided.

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