DAA-pyridine as peripheral benzodiazepine receptor ligand for diagnostic imaging and pharmaceutical treatment

A pharmaceutical, phenyl-based technology in the field of DAA-pyridine as a peripheral benzodiazepine receptor ligand for diagnostic imaging and drug therapy, which can solve the problem of low signal-to-noise ratio

Inactive Publication Date: 2011-06-29
BAYER SCHERING PHARMA OY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, the image produced by compound 4 has a relatively low signal-to-noise ratio

Method used

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  • DAA-pyridine as peripheral benzodiazepine receptor ligand for diagnostic imaging and pharmaceutical treatment
  • DAA-pyridine as peripheral benzodiazepine receptor ligand for diagnostic imaging and pharmaceutical treatment
  • DAA-pyridine as peripheral benzodiazepine receptor ligand for diagnostic imaging and pharmaceutical treatment

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Experimental program
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no. 1 approach

[0364] More specifically, for 18 F-marked formula I compound for obtaining 18 A first embodiment of the radiolabeling method of the F-labeled compound of formula I comprises the following steps:

[0365] - subjecting a compound of formula I with a suitable leaving group to a fluorinating agent 18 F radiolabeled to obtain 18 F labeled compound of formula I.

[0366] The term "radiolabeled" molecule as used herein generally refers to the 18 F-atoms are introduced into the molecule.

[0367] The fluorinating agent is as defined above, wherein F= 18 F.

[0368] In a second embodiment, L is [ 18 F] fluorine or [ 19 F] the synthetic method of the formula I compound of fluorine comprises the following steps:

[0369] - fluorinating the compound of formula V with F-fluorinating agent F-, to produce the compound of formula IV,

[0370]

[0371] Formula V

[0372]

[0373]Formula IV

[0374] - replacing said compound of formula IV with a compound of formula VI,

[037...

no. 2 approach

[0398] More preferably, for obtaining 18 A second embodiment of the radiolabeling method of the F-labeled compound of formula I comprises the following steps:

[0399] - with fluorinating agent 18 F radiolabels the compound of formula V to produce a compound of formula IV, and

[0400] - Substitution of the compound of formula IV by a compound of formula VI.

[0401] 18 The compound of formula IV marked by F is

[0402]

[0403] or a pharmaceutically acceptable inorganic acid or organic acid salt, hydrate, complex, ester, amide, solvate or prodrug thereof,

[0404] in

[0405] B is a leaving group;

[0406] Leaving group B is known or apparent to those skilled in the art and is derived from, but not limited to, those described or named in the following references: Synthesis (1982), p.85-125, Table 2 (p. 86; (The last item of this Table 2 should be amended to read: "n-C 4 f 9 S(O) 2 -O-nonaflat" instead of "n-C 4 h 9 S(O) 2 -O-nonaflat"), Carey and Sundberg, Org...

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PUM

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Abstract

This invention relates to novel compounds suitable for labelling or already labelled by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for therapy and diagnostic imaging by positron emission tomography (PET).

Description

technical field [0001] The present invention relates to suitable 18 F marked or has been 18 F-labeled novel compounds, methods for preparing such compounds, compositions comprising such compounds, kits comprising such compounds or compositions, and the use of such compounds, compositions or kits in therapy and by positron emission tomography (PET) for use in diagnostic imaging. Background technique [0002] Molecular imaging has the potential to detect disease progression or treatment response earlier than most traditional methods in the fields of oncology, neurology, and cardiology. Among several promising molecular imaging techniques that have been developed such as optical imaging, MRI, SPECT, and PET, PET is particularly useful for drug development due to its high sensitivity and ability to provide quantitative and kinetic data. [0003] For example, positron emitting isotopes include carbon, iodine, fluorine, nitrogen and oxygen. These isotopes can replace their non...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/81A61K31/44C07B59/00
CPCC07D213/81A61P1/04A61P19/02A61P21/02A61P25/00A61P25/08A61P25/28A61P25/30A61P29/00A61P35/00A61P37/02A61P37/08A61P9/00A61P9/10A61K31/44A61K49/06
Inventor L·莱曼A·蒂勒T·海因里希S·福尔默
Owner BAYER SCHERING PHARMA OY
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