848769-17-5

Upstream product

• 474012-72-1 2-[4'-(N,N-dimethylamino)phenyl]-6-tributylstannylimidazo[1,2-a]pyridine 

Relevant academic research and scientific papers

Radiosynthesis of SPECT tracers: Via a copper mediated 123I iodination of (hetero)aryl boron reagents

A general method for the copper mediated nucleophilic 123I-iodination of (hetero)aryl boronic esters and acids has been developed. The broad substrate scope of this radiosynthetic approach allows access to [123I]DPA-713, [123I]IMPY, [123I]MIBG and [123I]IPEB that are four commonly used SPECT radiotracers. Our results infer that aryl boronic reagents can now be employed as common precursors for both fluorine-18 and iodine-123 radiolabelling.

NOVEL COMPOUND HAVING AFFINITY FOR AMYLOID

It is intended to provide a compound that is effective as a diagnostic imaging probe that targets amyloid, and a diagnostic agent for Alzheimer's disease comprising the compound. Provided are a compound represented by the following formula (1), or salt thereof: wherein R1 is a radioactive halogen substituent, A1 and A2 independently represent CH or N, and a diagnostic agent for Alzheimer's disease, comprising the compound represented by the above formula or a salt thereof. The above compound and the above diagnostic agent for Alzheimer's disease transfer into brain after administration, and indicate good accumulation on amyloid deposited in the brain.

NOVEL COMPOUND WITH AMYLOID AFFINITY

A compound represented by the following formula (1), or a salt thereof: wherein R1 is a radioactive halogen substituent, 0 to 2 of A1, A2, A3 and A4 represent N, and the rest represent —(CH)— is effective as a diagnostic imaging probe targeting amyloid. A diagnostic agent for Alzheimer's disease contains a compound represented by the above formula (1) or a salt thereof. After administration to a patient, the compound and the diagnostic agent for Alzheimer's disease transfer into the patient's brain, and indicate good accumulation on amyloid deposited in the brain.

NOVEL COMPOUND HAVING AFFINITY FOR AMYLOID

A compound effective as a probe targeting amyloid for image diagnosis and a reagent comprising the compound for detecting amyloid deposited on a biological tissue are provided. Provided are a compound represented by the following formula (1): wherein R1, R2 and R3 independently represent a group selected from the group consisting of a hydrogen, hydroxyl group, alkyl substituent with 1 to 4 carbon atoms, alkoxy substituent having alkyl chain with 1 to 4 carbon atoms and halogen substituent, excluding the case where two or more of the substituents R1, R2 and R3 are hydrogen, R4 is a group selected from the group consisting of a hydrogen, hydroxy group, alkoxy substituent having alkyl chain with 1 to 4 carbon atoms and halogen substituent, and m is an integer of 1 to 4, provided that at least one of R1, R2, R3 and R4 represents a radioactive halogen substituent, and a reagent comprising the same.

NOVEL COMPOUND HAVING AFFINITY FOR AMYLOID

A compound effective as a probe targeting amyloid for image diagnosis and a reagent comprising the compound for detecting amyloid deposited on a biological tissue are provided. Provided are a compound represented by the following formula (1): wherein R1 is a group selected from the group consisting of a halogen substituent, alkyl substituent with 1 to 4 carbon atoms, alkoxy substituent having alkyl chain with 1 to 4 carbon atoms and hydroxyl group, R2 is a group selected from the group consisting of a cyano substituent, alkyl substituent with 1 to 4 carbon atoms and halogen substituent, is a group selected from the group consisting of a hydroxyl group, halogen substituent and substituent represented by the following formula: (wherein R4 is a hydrogen, halogen substituent or hydroxyl group, and m is an integer of 1 to 4), provided that a t least one of R1, R2, R3 and R4 represents a radioactive halogen, and a reagent comprising the same.

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.

DIAGNOSTIC AND REMEDY FOR DISEASE CAUSED BY AMYLOID AGGREGATION AND/OR DEPOSITION

To provide a diagnostic drug which binds specifically to an amyloid aggregate and/or an amyloid deposit, to thereby realize imaging and quantification of a disease caused by amyloid aggregation and/or deposition. The invention provides a compound represented by formula (1) : (wherein X1 represents an optionally substituted bicyclic heterocyclic group; X2 represents a hydrogen atom, a halogen atom, or a chelate-forming group; ring A represents a benzene ring or a pyridine ring; and ring B represents an optionally substituted 5-membered aromatic heterocyclic group which is bonded to the benzene ring or the pyridine ring via a carbon atom of ring B), a salt thereof, a solvate of any of these, or a transition metal coordination compound of any of these, and a diagnostic, preventive, or therapeutic drug containing the same.