Hammersmith Imanet Limited

Ge Healthcare Limited

Ge Healthcare as

Frank Brady

Sajinder Kaur Luthra

Erik Arstad

Yongjun Zhao

Alexander Mark Gibson

Edward George Robins

Nicholas Toby Jeffery

Alan Cuthbertson

Bengt Langstrom

Harry John Wadsworth

Magne Solbakken

Farhad Karimi

Duncan George Wynn

Bo Shan

Ian Wilson

Nicholas Toby Jeffrey

James Millar Gillies

Duncan Wynn

Bengt Langström

Erik Hammersmith Imanet Limited Arstad

Magne Amersham Health As Solbakken

Sajinder K Hammersmith Imanet Limited Luthra

Nicholas T Hammersmith Imanet Limited Jeffery

Duncan Ge Healthcare Limited Wynn

Alexander Mark Ge Healthcare Limited Gibson

Alan Amersham Health As Cuthbertston

This invention relates to the miniaturization of radiosyntheses onto microfabricated devices, and in particular to use of microfabricated devices for radiosynthesis, isolation, and analysis of radiotracers for use in Positron Emission Tomography (PET).

Use of microfabricated devices

The present invention provides novel tetracyclic indole compounds of Formula (I) either as in vivo imaging agents or as therapeutic agents. A method for the preparation of the in vivo imaging agent compound is also provided by the invention, as well as a precursor for use in said method. Pharmaceutical compositions comprising the compounds of the invention are additionally provided. Where the pharmaceutical composition comprises a compound suitable for in vivo imaging, a kit is provided for the preparation of the pharmaceutical composition. In a further aspect, use of the compound for in vivo imaging or treatment of conditions associated with PBR is provided. 

Tetracyclic indole derivatives as in vivo imaging agents and having peripheralbenzodiazepine receptor affinity (PBR)

The invention provides a process for the production of anF-labelled tracer which comprises treatment of a solid support-bound precursor of formula (I) SOLID SUPPORT-LINKER-X-TRACER (I) wherein X is a group which promotes nucleophilic substitution at a specific site on the attached TRACER and the TRACER is of formula (A). 

Solid-phase fluorination of benzothiazoles

The invention relates to novel processes for the purification of radiolabelled tracers, using a solid-support bound scavenger group. The general concept being illustrated by the scheme:

Purification methods

A method for coating the internal surfaces of a reaction vessel having a small internal diameter comprises the steps of (i) introducing into the reaction vessel a solution of one or more monomers in a suitable solvent; (ii) introducing a flow of an inert gas through the reaction vessel; and (iii) initiating polymerization of the monomer solution.

Method for coating the internal surface of a reaction vessel

The invention relates to a process for the production of an [F]fluorohaloalkane which comprises treatment of a solid support-bound precursor of formula (I):SOLID SUPPORT-LINKER-SO&#x2014;O&#x2014;(CH)X&#x2003;&#x2003;(I)wherein n is an integer of from 1 to 7 and X is chloro, bromo or iodo;withFto produce the [F]fluorohaloalkane of formula (II)F&#x2014;(CH)&#x2014;X&#x2003;&#x2003;(II)wherein n and X are as defined for the compound of formula (I), optionally followed by

[object Object]

The invention relates to a process for the production of anF-labelled tracer which comprises treatment of a solid support-bound precursor of formula (I): SOLID SUPPORT-LINKER-I-TRACER (I) Ywherein the TRACER is of formula (A): or an amine protected derivative thereof, wherein Yis an anion, preferably trifluoromethylsulphonate (triflate) anion; and Ris either (i) a group CH&#x2014;NPPin which Pand Pare each independently hydrogen or a protecting group, or (ii) a carbonyl group; withFto produce the labelled tracer of formula (II) or an amine protected derivative thereof, wherein Ris as defined for the compound of formula (I).

Solid-phase fluorination of uracil and cytosine

The invention relates to compounds of formula: (I) or a salt or solvate thereof, wherein: Ris &#x2014;CHRor [F]&#x2014;Cfluoroalkyl wherein Ris hydrogen or Calkyl; Ris hydrogen or Calkyl; Ris halo; and Ris halo, Calkylthio, or Calkyl; and their use for imaging central nervous system (CNS) receptors. 

Imaging compounds

The invention provides a process for preparation of a fluorohaloalkane, preferably an [F]fluorohaloalkane of formula (I) wherein X is halo and n is an integer of from 1 to 6; which comprises: reaction of the corresponding organosilicon compound of formula (II): wherein n is as defined for the compound of formula (I); and R', R&#x2033;, and R&#x2032;&#x2033; are independently selected from Calkyl and Chaloalkyl; and R&#x2033; may alternatively be the group: with a compound of formula (III): wherein X is as defined for the compound of formula (I) and Y is halo. Intermediates having use in such processes are also claimed. 

Chemical process

The invention relates to a process for the production of an [F]fluorohaloalkane which comprises treatment of a solid support-bound precursor of formula (I): SOLID SUPPORT-LINKER-SO&#x2014;O&#x2014;(CH)X (I) wherein n is an integer of from (1) to (7) and X is chloro, bromo or iodo; withFto produce the [F]fluorohaloalkane of formula (II)F&#x2014;(CH)&#x2014;X (II) wherein n and X are as defined for the compound of formula (I), optionally followed by (i) removal of excessF, for example by ion-exchange chromatography; and/or (ii) removal of organic solvent.

The invention relates to compounds of formula (I); wherein Rand Rindependently selected from Calkyl; P, P, P, and Pare each independently hydrogen or a protecting group; and their use in the preparation ofF-labelled 6-L-fluorodopa 

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London, United Kingdom

Frank Brady