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Alpha-synuclein aggregate binding agent and imaging method

A technology of synuclein and binding agent, which is applied in the field of α-synuclein aggregate binding agent and imaging, and can solve the problems of undocumented α-synuclein aggregate binding, etc.

Pending Publication Date: 2021-10-08
NAT INST FOR QUANTUM & RADIOLOGICAL SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, Patent Document 1 does not describe binding to α-synuclein aggregates

Method used

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  • Alpha-synuclein aggregate binding agent and imaging method
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  • Alpha-synuclein aggregate binding agent and imaging method

Examples

Experimental program
Comparison scheme
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Embodiment

[0260] Hereinafter, although an Example demonstrates this invention in detail, this invention is not limited to these Examples.

[0261] The following compounds were used.

[0262]

[0263]

[0264] (Preparation for BF-227)

[0265] BF-227 (i.e., 2-(2-[2-dimethylaminothiazol-5-yl]vinyl)-6-(2-[fluoro]ethoxy)benzoxazole) manufactured by NARD Research Institute , catalog number NP039-0.

[0266] (Synthesis of PBB3)

[0267]PBB3 (i.e., (2-((1E,3E)-4-(6-(methylamino)pyridin-3-yl)but-1,3-dienyl)benzo[d]thiazol-6-ol ) was synthesized by the method described in Synthesis Example 3 of Patent Document 1.

[0268] (Synthesis of C05-01)

[0269] C05-01 (i.e., ((E)-2-(4-(2-fluoro-6-(methylamino)pyridin-3-yl)but-1-en-3-ynyl)benzo[d] Thiazol-6-ol) was synthesized by the method described in Synthesis Example 23 of Patent Document 1.

[0270] (Synthesis of C05-02)

[0271] C05-02 (i.e., ((E)-5-(4-(6-(aminomethyl)benzo[d]thiazol-2-yl)but-3-en-1-ynyl)-N-methyl Pyridin-2-amine) was...

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Abstract

Provided is an alpha-synuclein aggregate binding agent having high selectivity for binding to alpha-synuclein aggregates. An alpha-synuclein aggregate binding agent containing a compound represented by formula (I), a salt acceptable as a pharmaceutical thereof, or a solvate thereof: (in formula (I), R1 and R2 each independently are selected from the group consisting of a hydrogen, alkyl, alkenyl, acyl, and hydroxyalkyl; R3 is a hydrogen or halogen; ring A is a benzene ring or a pyridine ring; ring B is formula (i) or formula (ii): R4 and R5 each independently are selected from the group consisting of a hydrogen, hydroxy, alkoxy, haloalkoxy, halohydroxyalkoxy, and aminoalkyl.).

Description

technical field [0001] The present invention relates to α-synuclein aggregate binding agents, compositions for optical imaging of α-synuclein aggregates, compositions for radiographic imaging of α-synuclein aggregates, and related to α-synuclein aggregates A diagnostic drug for a disease, or a companion diagnostic drug for the treatment or prevention of the disease, a diagnostic kit for a disease related to a substance accumulated in the brain, an optical imaging method, a radiographic method, and α-synucleus in the brain Method for screening therapeutic or preventive drugs for protein aggregate-related diseases, method for quantifying or determining accumulation of α-synuclein aggregates in brain, method for classifying and determining accumulation of substances accumulated in brain, Inhibitors of alpha-synuclein aggregation, and novel compounds. Background technique [0002] Alpha-synuclein aggregates constitute the core pathology of Parkinson's disease, dementia with Lew...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/425A61K31/443A61K31/4436A61P25/00A61P25/16A61P25/28C07D405/06C07D417/06A61K51/04
CPCA61K31/443A61P25/00A61P25/28A61P25/16C07D405/06C07D417/06C07D277/64A61K51/0455A61K49/0021C07B59/002G01N33/6896G01N33/5088G01N33/582A61K31/428A61K31/4439C09B23/107C09B57/00A61K2300/00A61K31/426A61K31/4436
Inventor 樋口真人小野麻衣子须原哲也张明荣
Owner NAT INST FOR QUANTUM & RADIOLOGICAL SCI & TECH