956499-76-6

Upstream product

• 20511-12-0 2-amino-5-iodopyridine 
• 61791-99-9 2-bromo-4-hydroxyacetophenone 
• 2491-38-5 2-bromo-1-(4'-hydroxyphenyl)-1-ethanone 

Downstream Products

• 958641-70-8 2-[4-(2-fluoroethoxy)phenyl]-6-iodoimidazo[1,2-a]pyridine 
• 958641-87-7 2-[4-(2-t-butyldiphenylsiloxyethoxy)phenyl]-6-iodoimidazo[1,2-a]pyridine 
• 958641-90-2 2-[4'-(3''-t-butyldimethylsiloxypropoxy)phenyl]-6-iodoimidazo[1,2-a]pyridine 
• 958641-68-4 2-[4'-(3''-fluoropropoxy)phenyl]-6-iodoimidazo[1,2-a]pyridine 
• 958641-74-2 2-[4-(2-hydroxyethoxy)phenyl]-6-iodoimidazo[1,2-a]pyridine 
• 958641-83-3 2-[4-(3-hydroxypropoxy)phenyl]-6-iodoimidazo[1,2-a]pyridine 
• 1027045-54-0 2-(4′-methoxyphenyl)-6-tributylstannylimidazo[1,2-a]pyridine 
• 958641-72-0 2-[4′-(2-fluoroethoxy)phenyl]-6-tributylstannylimidazo[1,2-a]-pyridine 
• 958641-75-3 2-[4′-(2-hydroxyethoxy)phenyl]-6-tributylstannylimidazo[1,2-a]pyridine 
• 958641-84-4 2-[4′-(3-hydroxypropoxy)phenyl]-6-tributylstannylimidazo[1,2-a]pyridine 

Relevant academic research and scientific papers

Design, Synthesis, and Preliminary Evaluation of SPECT Probes for Imaging β-Amyloid in Alzheimer's Disease Affected Brain

In this study, we synthesized of a series of 2-phenyl- and 2-pyridyl-imidazo[1,2-a]pyridine derivatives and examine their suitability as novel probes for single-photon emission computed tomography (SPECT)-based imaging of β-amyloid (Aβ). Among the 11 evaluated compounds, 10 showed moderate affinity to Aβ(1-42) aggregates, exhibiting half-maximal inhibitory concentrations (IC50) of 14.7 ± 6.07-87.6 ± 39.8 nM. In vitro autoradiography indicated that 123I-labeled triazole-substituted derivatives displayed highly selective binding to Aβ plaques in the hippocampal region of Alzheimer's disease (AD)-affected brain. Moreover, biodistribution studies performed on normal rats demonstrated that all 123I-labeled probes featured high initial uptake into the brain followed by a rapid washout and were thus well suited for imaging Aβ plaques, with the highest selectivity observed for a 1H-1,2,3-triazole-substituted 2-pyridyl-imidazopyridine derivative, [123I]ABC577. This compound showed good kinetics in rat brain as well as moderate in vivo stability in rats and is thus a promising SPECT imaging probe for AD in clinical settings.

USE OF NOVEL COMPOUND HAVING AFFINITY FOR AMYLOID, AND PROCESS FOR PRODUCTION OF THE SAME

The invention provides a reagent for detecting amyloid in a biological tissue which can be detect amyloid in vitro and in vivo with high sensitivity using a compound which has affinity with amyloid and is suppressed in toxicity such as mutagenicity. The reagent for detecting amyloid deposited in a biological tissue comprises a compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represents a carbon or nitrogen; R1 is a halogen substituent; R2 is a halogen substituent; and m is an integer or 0 to 2, provided that at least one of R1 and R2 is a radioactive halogen substituent, at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 and A4.

USE OF NOVEL COMPOUND HAVING AFFINITY FOR AMYLOID, AND PROCESS FOR PRODUCTION OF THE SAME

The invention provides a reagent for detecting amyloid in a biological tissue which can detect amyloid in vitro and in vivo with high sensitivity using a compound which has affinity with amyloid and is suppressed in toxicity such as mutagenicity. The reagent for detecting amyloid deposited in a biological tissue comprises the compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represent a carbon or a nitrogen, and R3 is a group represented by the following formula: wherein R1 is a radioactive halogen substituent; m is an integer of 0 to 4; and n is an integer of 0 or 1, provided that at least one of A1, A3, A3 and A4 represents a carbon, and R5 binds to a carbon represented by A1, A2, A3 or A4.

UTILIZATION OF NOVEL COMPOUNDS WITH AMYLOID AFFINITY AND METHOD OF PRODUCING THE SAME

The invention provides a reagent for detecting amyloid deposited in a biological tissue which can detect amyloid in vitro and in vivo with high sensitivity using a compound which has affinity with amyloid and is suppressed in toxicity such as mutagencity. The reagent for detecting amyloid deposited in a biological tissue comprises a compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represent carbon or nitrogen; R1 is a radioactive halogen substituent; R2 is a group selected from the group consisting of hydrogen, hydroxyl group, methoxy group, carboxyl group, amino group, N-methylamino group, N,N-dimethylamino group and cyano group; and m is an integer of 0 to 2, provided that at least one of A1, A2, and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 and A4.

USE OF NOVEL COMPOUND HAVING AFFINITY FOR AMYLOID, AND PROCESS FOR PRODUCTION OF THE SAME

The invention provides a reagent which can detect amyloid in vitro and in vivo with high sensitivity using a compound which has affinity with amyloid. The reagent for detecting amyloid deposited in a biological tissue comprises the compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represent a carbon or nitrogen, R1 is a group selected from the group consisting of a hydrogen, hydroxyl group, carboxyl group, sulfuric acid group, amino group, nitro group, cyano group, non-radioactive halogen substituent, alkyl substituent with 1 to 4 carbon atoms and alkoxy substituent, with 1 to 4 carbon atoms, and R2 is a radioactive halogen substituent, provided that at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 or A4.

NOVEL COMPOUND HAVING AFFINITY FOR AMYLOID

The present invention provides a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagencity. Provided is a compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represents a carbon or nitrogen; R1 is a halogen substituent; R2 is a halogen substituent; and m is an integer of 0 to 2, provided that at least one of R1 and R2 is a radioactive halogen substituent, at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 or A4 as well as a low-toxic diagnostic agent comprising a compound represented by the preceding formula or a salt thereof.

NOVEL COMPOUND HAVING AFFINITY TO AMYLOID

The invention relates to a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagenicity, and also relates to a low-toxic diagnostic agent for Alzheimer's disease containing the compound. The compound is represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represent a carbon or a nitrogen, and R3 is a group represented by the following formula: wherein R1 is a radioactive halogen substituent; m is an integer of 0 to 4; and n is an integer of 0 or 1, provided that at least one of A1, A2, A3 and A4 represents a carbon, and R3 binds to a carbon represented by A1, A2, A3 or A4.

NOVEL COMPOUND HAVING AFFINITY FOR AMYLOID

A compound that has affinity with amyloid, exhibits sufficiently rapid clearance from normal tissues, and is suppressed in toxicity such as mutagenicity is provided, which is represented by the following formula (1): or a salt thereof, wherein R1 is a group selected from hydrogen, hydroxyl group, carboxyl group, sulfate group, amino group, nitro group, cyano group, an alkyl substituent with one to 4 carbon atoms or an alkoxy substituent with one to 4 carbon atoms; R2 is a radioactive halogen substituent; and m is an integer of 0 to 2, and a low-toxic diagnostic agent for Alzheimer's disease comprising a compound represented by the above formula or a salt thereof is also provided.

NOVEL COMPOUNDS WITH AFFINITY FOR AMYLOID

It is intended to provide a compound effective as an image diagnosis probe targeting amyloid and a diagnostic agent for Alzheimer's disease comprising the compound. Provided is a compound represented by the following formula or a salt thereof: wherein A1, A2, A3 and A4 independently represents a carbon or nitrogen, R1 is a group selected from the group consisting of hydrogen, hydroxyl group, carboxyl group, sulfuric acid group, amino group, nitro group, cyano group, non-radioactive halogen substituents, alkyl substituents with 1-4 carbon atoms and alkoxy substituents with 1-4 carbon atoms, and R3 is a radioactive halogen substituent, provided that at least one of A1 A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 or A4, as well as a diagnostic agent for Alzheimer's disease comprising the compound represented by the above formula or a salt thereof.