Industrial Research Limited

Ark Therapeutics Limited

Arktherapeutics Group, Plc

Ashley Jarvis

David Lawrence Selwood

Basil Hartzoulakis

Ian Zachary

Chris Chapman

Haiyan Jia

Michelle Tickner

Lili Cheng

Katie Ellard

Rosemary Lynch

Jamie Nally

Mark Stewart

Gary Brian Evans

Keith Clinch

Gavin Frank Painter

Anthony Mitchell

Paul Andrew Benjes

John Adrian Dickison

The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.

Arginine derivatives with NP-1 antagonistic activity

The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists. 

Arginine derivatives with NP-I antagonistic activity

A novel method for the preparation of a compound of formula (I) from an N&#x2014;protected-D-mannosamine. A compound of formula (I) is a useful intermediate for the preparation of kiftnensine, a potent and selective mannosidase inhibitor. The method includes protecting the hydroxyl group at the C-6 position of an N&#x2014;protected-D-mannosamine, to give a 6&#x2014;O&#x2014;protected&#x2014;N&#x2014;protected-D-mannosamine; reducing the C-1 anomeric carbon atom of the 6&#x2014;O&#x2014;protected&#x2014;N&#x2014;protected-D-mannosamine to give a 6&#x2014;O&#x2014;protected&#x2014;N&#x2014;protected-D-mannitol; protecting the four hydroxyl groups of the 6&#x2014;O&#x2014;protected&#x2014;N&#x2014;protected-D-mannitol; and removing the nitrogen atom protecting group and optionally removing the C-6 oxygen atom protecting group to give the compound of formula (I): where Rand Rare each independently protecting groups which, together with the oxygen atoms to which they are attached, form a 5-, 6-, 7- or 8-membered ring; and Ris hydrogen or a protecting group.

Process for preparing kifunensine intermediate and kifunensine therefrom

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London, United Kingdom

Ashley Jarvis