公开(公告)号：US12195454B2

公开(公告)日：2025-01-14

申请号：US18144547

申请日：2023-05-08

Applicant: National Institutes for Quantum and Radiological Science and Technology

Inventor： Makoto Higuchi ,  Tetsuya Suhara ,  Masahiro Maruyama ,  Meiei Cho ,  Hitoshi Shimada

IPC: C07D417/06 ,  A61K49/00 ,  C07D277/64 ,  C07D401/06 ,  C07D401/14 ,  C07D405/06 ,  C07D405/14 ,  C07D417/14 ,  C07F7/18

Abstract: The present invention provides a compound represented by the following formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein: R1 and R2 are each separately selected from the group consisting of hydrogen, alkyl, alkenyl, acyl, and hydroxyalkyl; R3 is hydrogen or halogen; ring A is a benzene ring or a pyridine ring; ring B is selected from the group consisting of the following formulas (i), (ii), (iii), and (iv): in the formula (ii), Ra is alkyl; R4 and R5 are each separately selected from the group consisting of hydrogen, hydroxy, alkoxy, haloalkoxy, halohydroxyalkoxy, and aminoalkyl; and represents a double bond or a triple bond. The above compound can be used as a molecular probe for imaging tau proteins that accumulate in the brain.

公开(公告)号：US20220133698A1

公开(公告)日：2022-05-05

申请号：US17432776

申请日：2020-01-24

Applicant: National Institutes for Quantum and Radiological Science and Technology

Inventor： Makoto Higuchi ,  Maiko Ono ,  Tetsuya Suhara ,  Meiei Cho

IPC: A61K31/426 ,  A61K31/443 ,  A61K31/4436 ,  A61P25/16 ,  A61P25/28 ,  A61K51/04

Abstract: The present invention provides an α-synuclein aggregate binding agent that has high binding selectivity for an α-synuclein aggregate.
The α-synuclein aggregate binding agent contains a compound represented by a formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof: in the formula (I), R1 and R2 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl, acyl, and hydroxyalkyl; R3 is hydrogen or halogen; the ring A is a benzene or pyridine ring; the ring B is represented by the following formula (i) or (ii): R4 and R5 are each independently selected from the group consisting of hydrogen, hydroxy, alkoxy, haloalkoxy, halohydroxyalkoxy, and aminoalkyl.

公开(公告)号：US10604516B2

公开(公告)日：2020-03-31

申请号：US14346914

申请日：2012-12-21

Applicant: National Institutes for Quantum and Radiological Science and Technology

Inventor： Makoto Higuchi ,  Tetsuya Suhara ,  Masahiro Maruyama ,  Meiei Cho ,  Hitoshi Shimada

IPC: A61B8/00 ,  A61B5/00 ,  A61B10/00 ,  C07D417/06 ,  C07F7/18 ,  C07D401/06 ,  C07D405/06 ,  C07D417/14 ,  C07D277/64 ,  A61K49/00 ,  C07D401/14 ,  C07D405/14

Abstract: The present invention provides a compound represented by the following formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof. wherein: R1 and R2 are each separately selected from the group consisting of hydrogen, alkyl, alkenyl, acyl, and hydroxyalkyl; R3 is hydrogen or halogen; ring A is a benzene ring or a pyridine ring; ring B is selected from the group consisting of the following formulas (i), (ii), (iii), and (iv): in the formula (ii), Ra is alkyl; R4 and R5 are each separately selected from the group consisting of hydrogen, hydroxy, alkoxy, haloalkoxy, halohydroxyalkoxy, and aminoalkyl; and   [Formula 3] represents a double bond or a triple bond. The above compound can be used as a molecular probe for imaging tau proteins that accumulate in the brain.

公开(公告)号：US11667628B2

公开(公告)日：2023-06-06

申请号：US17477479

申请日：2021-09-16

Applicant: National Institutes for Quantum and Radiological Science and Technology

Inventor： Makoto Higuchi ,  Tetsuya Suhara ,  Masahiro Maruyama ,  Meiei Cho ,  Hitoshi Shimada

IPC: C07D417/06 ,  C07F7/18 ,  C07D401/06 ,  C07D405/06 ,  C07D417/14 ,  C07D277/64 ,  A61K49/00 ,  C07D401/14 ,  C07D405/14

CPC classification number: C07D417/06 ,  A61K49/0017 ,  A61K49/0021 ,  C07D277/64 ,  C07D401/06 ,  C07D401/14 ,  C07D405/06 ,  C07D405/14 ,  C07D417/14 ,  C07F7/1804

Abstract: The present invention provides a compound represented by the following formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof:




wherein:



R1 and R2 are each separately selected from the group consisting of hydrogen, alkyl, alkenyl, acyl, and hydroxyalkyl;
R3 is hydrogen or halogen;
ring A is a benzene ring or a pyridine ring;
ring B is selected from the group consisting of the following formulas (i), (ii), (iii), and (iv):










in the formula (ii), Ra is alkyl;
R4 and R5 are each separately selected from the group consisting of hydrogen, hydroxy, alkoxy, haloalkoxy, halohydroxyalkoxy, and aminoalkyl; and








represents a double bond or a triple bond. The above compound can be used as a molecular probe for imaging tau proteins that accumulate in the brain.

公开(公告)号：US20200262829A1

公开(公告)日：2020-08-20

申请号：US16798226

申请日：2020-02-21

Applicant: National Institutes for Quantum and Radiological Science and Technology

Inventor： Makoto Higuchi ,  Tetsuya Suhara ,  Masahiro Maruyama ,  Meiei Cho ,  Hitoshi Shimada

IPC: C07D417/06 ,  A61K49/00 ,  C07D277/64 ,  C07D405/14 ,  C07D401/14 ,  C07D417/14 ,  C07D405/06 ,  C07D401/06 ,  C07F7/18

Abstract: The present invention provides a compound represented by the following formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof. wherein: R1 and R2 are each separately selected from the group consisting of hydrogen, alkyl, alkenyl, acyl, and hydroxyalkyl; R3 is hydrogen or halogen; ring A is a benzene ring or a pyridine ring; ring B is selected from the group consisting of the following formulas (i), (ii), (iii), and (iv): in the formula (ii), Ra is alkyl; R4 and R5 are each separately selected from the group consisting of hydrogen, hydroxy, alkoxy, haloalkoxy, halohydroxyalkoxy, and aminoalkyl; and [Formula 3] represents a double bond or a triple bond. The above compound can be used as a molecular probe for imaging tau proteins that accumulate in the brain.