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Tricyclic indole derivatives as PBR ligands

A technology of precursor compound and compound, applied in the fields of radiopharmaceutical composition, synthesis of said precursor compound, positron-emission tomography imaging, preparation of said precursor compound and said PET tracer, It can solve the problems of low non-specific binding specificity, unknown role of metabolites, etc.

Active Publication Date: 2014-12-24
GE HEALTHCARE LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, (R)-[ 11 C] PK 11195 Known to have high protein binding and low specificity for nonspecific binding
Furthermore, the role of its radiolabeled metabolites is not known, and quantification of binding requires complexation modes

Method used

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  • Tricyclic indole derivatives as PBR ligands
  • Tricyclic indole derivatives as PBR ligands
  • Tricyclic indole derivatives as PBR ligands

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preparation example Construction

[0029] Preparation of precursor compounds

[0030] The precursor compounds of the invention may be obtained by a number of different routes, each forming a separate aspect of the invention.

[0031] Accordingly, the present invention provides a first process for the preparation of a precursor compound of formula I as defined herein, wherein said process comprises:

[0032] (i) providing a racemic mixture of said precursor compound of formula I and a compound of formula II as defined herein:

[0033] (II);

[0034] where R 2 As above for R 1 defined by, and R 1 and R 2 same;

[0035] (ii) separating said precursor compound of formula I from said compound of formula II.

[0036] The step of "separating" said precursor compound of formula I from said compound of formula II is carried out by enantiomeric separation techniques. Suitable enantiomeric separation techniques include high performance liquid chromatography (HPLC), supercritical fluid chromatography (SFC), simul...

Embodiment 1

[0113] Example 1 describes the synthesis of a racemic mixture comprising a precursor compound of Formula I and an enantiomer of Formula II.

Embodiment 2

[0114] Example 2 describes the synthesis of a non-radioactive racemic mixture comprising a non-radioactive analog of a PET tracer of the present invention as well as its alternative enantiomers.

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Abstract

The present invention provides a PET tracer that has improved properties for imaging the peripheral benzodiazepine receptor (PBR) as compared with known such PET tracers. The present invention also provides a precursor compound useful in the preparation of the PET tracer of the invention and methods for the preparation of said precursor compound and said PET tracer. Also provided by the present invention is a radiopharmaceutical composition comprising the PET tracer of the invention. Methods for using the PET tracer and the radiopharmaceutical composition are also provided.

Description

[0001] Technical Field of the Invention [0002] The present invention relates to in vivo imaging of peripheral benzodiazepine receptors (PBR), particularly positron emission tomography (PET) imaging. Indole-based PET tracers that provide high affinity binding to PBR, have good absorption in the brain after administration, and have excellent selective binding to PBR. The present invention also provides a precursor compound that can be used to synthesize the PET tracer of the present invention, and a method for synthesizing the precursor compound. Other aspects of the invention include a method of synthesizing a PET tracer of the invention comprising the use of a precursor compound of the invention, a kit for performing the method, and a cassette for performing the method in an automated format. Furthermore, the present invention provides a radiopharmaceutical composition comprising the PET tracer of the present invention, as well as methods of using said PET tracer. Backgroun...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D209/80C07D495/04A61K51/04
CPCC07D209/88A61K51/0446C07D209/80
Inventor R.阿查纳思S.巴拉吉S.M.费尔韦D.曼齐拉斯U.莫卡帕蒂D.奥谢亚J.M.帕斯莫尔B.单W.J.特里格H.J.瓦德斯沃思A.M.卡达维帕兰普穆罕默德
Owner GE HEALTHCARE LTD
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