Cyclacel Limited

Darwin Discovery Limited

Arakis Ltd.

Benjamin Mark Skead

Julian Scott Northen

Jonathan Charles Christian Atherton

Robin Mark Bannister

Christopher Peter Worrall

Derek John Londesbrough

Robert Westwood

Philippe Fernandes

Graham Robert Evans

Marianne Langston

Alan Rothaul

Philippe Fernades

Michal Czyzewski

Chris Atherton

John Mykytiuk

Alex Hudson

Chris Gill

The present invention relates to a process for preparing a compound of formula [I], said process comprising the steps of: formula [II]+formula [III]&#x2192;formula [I] (i) forming a reaction mixture comprising (a) a compound of formula [II], (b) a compound of formula [III] and (c) 1,2-propanediol or polyethylene glycol, or a mixture thereof, and optionally (d) a base; (ii) heating said reaction mixture to a temperature of at least about 150&#xb0; C. to form a compound of formula [I]; (iii) isolating said compound of formula [I]; and (iv) optionally converting said compound of formula [I] into salt form; wherein: Rand Rare each independently H, alkyl or haloalkyl; Rand Rare each independently H, alkyl, haloalkyl or aryl; Ris alkyl, alkenyl, cycloalkyl or cycloalkyl-alkyl, each of which may be optionally substituted with one or more OH groups; Ris selected from cyclopropylamino, cyclopropylmethylamino, cyclobutylamino, cyclobutylmethylamino and formula (A) where one of X, Y and Z is N and the remainder are CR; R, Rand each Rare independently H, alkyl or haloalkyl, wherein at least one of R, Rand Ris other than H. Further aspects of the invention relate to a highly diastereoselective process for the preparation of compounds of formula [III], a process for preparing intermediates of formula [II], and other intermediates useful in the synthesis of compounds of formula [I], and to a process for preparing the crystalline tartrate salt and free base of compounds of formula [I]. 

Process for preparing purine derivatives

The present invention relates to new crystalline forms of a purine derivative which exhibits excellent anti-tumor activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms.

Crystalline forms of a purine derivative

The present invention relates to new crystalline forms of a purine derivative which exhibits excellent anti-tumour activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms.

A method of treating an inflammatory disease or an autoimmune disease in a subject, comprises the administration of mefloquine.

Treatment of inflammatory disorders

Crystallisation of levibupivacaine and analogues thereof

A reproducible process for preparing a substantially single enantiomer (R or S) of 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexanoic acid, or an analogue thereof, thereby providing single enantiomer acid for the first time, proceeds by means of a classical salt resolution employing a resolving agent selected from an enantiomer (R or S) of a 1-arylalkylamine and (-)-quinine, and provides novel salts that are readily convertible to verapamil.

Resolution

Growing community of inventors

Cambridge, United Kingdom

Benjamin Mark Skead