Hammersmith Imanet Limited

Edward George Robins

Erik Arstad

Sajinder Kaur Luthra

Frank Brady

Bengt Langstrom

Farhad Karimi

David Robert Turton

Ian Wilson

Bo Shan

Bengt Langström

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 relates to novelF-labelled compounds which may be suitable for use as Positron Emission Tomography (PET) radiotracers, and to processes for preparation of such. TheF-labelled compounds of the invention comprise a [F]fluoroalkenyl group.

PET radiotracers

The invention provides a compound of formula (I); or a salt or solvate thereof, wherein: Ris hydrogen or Calkyl; Rand Rare each independently selected from Calkyl, [C]Calkyl, and [F]&#x2014;Cfluoroalkyl provided that at least one of Rand Ris [C]Calkyl or [F]&#x2014;Cfluoroalkyl; and Ris halo. Such compounds having use for imaging central nervous system receptors. 

Imaging 18F or 11C-labelled alkylthiophenyl guanidines

Radiolabelled acid chlorides may be synthesised by reacting a radiolabelled carboxylic acid with a solid-phase supported chlorinating agent.

Radiosynthesis of acid chlorides

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).

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London, United Kingdom

Edward George Robins