Contrast agent for imagining myocardial perfusion

A technology of imaging agents and pharmacy, which is used in radioactive preparations in vivo, drug combinations, introduction of heterocyclic compound isotopes, etc.

Inactive Publication Date: 2014-10-22
RESPIRATORIUS AB (PUBL)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently, single photon emission computed tomography (SPECT) is the mainstay of CAD imaging, but improved diagnostic methods are still needed

Method used

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  • Contrast agent for imagining myocardial perfusion
  • Contrast agent for imagining myocardial perfusion
  • Contrast agent for imagining myocardial perfusion

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0054] Synthesis of Imaging Compounds.

[0055] Example 1

[0056]

[0057] N-[[3-fluoro-4-(2-fluoroethoxymethyl)phenyl]methyl]-2-methyl-1,8-naphthyridine-3-carboxamide

[0058] Will have 19mg 2-[[2-fluoro-4-[[(2-methyl-1,8-naphthyridine-3-carbonyl) amino] methyl] phenyl] methoxy] ethyl 4-methylbenzene Sulfonate (0.036mmol), 26mg Kryptofix 222 (4,7,13,16,21,24-hexaoxa-1,10-diazabicyclo[8.8.8]-di A flask of a solution of hexadecane) (0.069 mmol) and 4 mg KF (0.069 mmol) in 1.0 ml dry MeCN was added to a preheated oil bath and heated at 90 C for 30 min. The reaction mixture was cooled to room temperature and diluted with water. The mixture was extracted twice with EtOAc. The combined organic phases were washed with brine, dried (MgSO4) and concentrated. Flash chromatography gave 9.6 mg (72%).

[0059] 1 H NMR (CDCl 3 )δ8.97(dd,1H),8.03(s,1H),8.01(m,1H),7.42(m,2H),7.19(dd,1H),7.13(m,1H),7.08(t,1H ), 4.67(m,2H), 4.65(s,3H), 4.53(m,1H), 3.80(m,1H), 3.73(m,1H).

[0060]...

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Abstract

The present disclosure is directed to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a compound linked to an imaging moiety, wherein said compound binds MC-1, and scanning the patient using diagnostic imaging. The invention also relates to kits comprising said compound or precursor compounds linked or not linked to an imaging moiety.

Description

technical field [0001] The present disclosure is directed to imaging agents, pharmaceutical compositions, and methods for imaging myocardial perfusion, comprising administering to a patient a compound linked to an imaging moiety, wherein the compound binds MC-1, and scanning this site using diagnostic imaging patient. The invention also relates to kits comprising said imaging agents or precursor compounds linked or not to an imaging moiety. Background technique [0002] Coronary artery disease (CAD) is the leading cause of death in the Western world. Imaging techniques for diagnosis and prognosis are very important for treating CAD to reduce mortality. Imaging to evaluate myocardial blood flow to determine necessary treatment, usually surgery, is a critical part of CAD healthcare. Currently, single photon emission computed tomography (SPECT) is the mainstay of CAD imaging, but improved diagnostic methods are still needed. [0003] Heart cells, myocardium have very high i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/10A61K51/04C07D471/04A61K101/02
CPCC07D471/04A61K51/0455C07B59/002A61P43/00A61K49/10A61K51/04A61K49/00
Inventor 马丁·约翰森
Owner RESPIRATORIUS AB (PUBL)
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