Granted Patent
B2
US 12,195,454 · App. 18/144,547 · Granted Jan 14, 2025
Compounds for imaging tau proteins that accumulate in the brain
Inventors:
Makoto Higuchi (Chiba, JP); Tetsuya Suhara (Chiba, JP); Masahiro Maruyama (Chiba, JP); Meiei Cho (Chiba, JP); Hitoshi Shimada (Chiba, JP)
C07D417/06A61K49/0017A61K49/0021C07D277/64C07D401/06C07D401/14C07D405/06C07D405/14C07D417/14C07F7/1804
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Abstract
The present invention provides a compound represented by the following formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein: R 1 and R 2 are each separately selected from the group consisting of hydrogen, alkyl, alkenyl, acyl, and hydroxyalkyl; R 3 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), R a is alkyl; R 4 and R 5 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.
Claims (12)
1. A compound, wherein the compound is:
or a pharmaceutically acceptable salt thereof, or a solvate thereof, or
or a pharmaceutically acceptable salt thereof, or a solvate thereof.
2. The compound of claim 1 , wherein compound is
or a pharmaceutically acceptable salt thereof, or a solvate thereof.
3. The compound of claim 1 , wherein compound is
or a pharmaceutically acceptable salt thereof, or a solvate thereof.
4. The compound of claim 1 , wherein one or more atoms of the compound are a radioisotope of the one or more atoms.
5. A composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutically acceptable carrier.
6. A method of tau imaging of a brain of a mammal, the method comprising:
(a) administering an effective dose of the compound of claim 1 , or a pharmaceutically acceptable salt thereof, or a solvate thereof, to the mammal; and
(b) imaging the brain of the mammal.
Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Nov 19, 2024
From: HIGUCHI, MAKOTO; SUHARA, TETSUYA; MARUYAMA, MASAHIRO; CHO, MEIEI; SHIMADA, HITOSHI
To: NATIONAL INSTITUTE OF RADIOLOGICAL SCIENCES
Reel/Frame 069330/0670 →
CHANGE OF NAME
Recorded Nov 19, 2024
From: NATIONAL INSTITUTE OF RADIOLOGICAL SCIENCES
To: NATIONAL INSTITUTES FOR QUANTUM AND RADIOLOGICAL SCIENCE AND TECHNOLOGY
Reel/Frame 069393/0646 →
Continuity (4)
Continuation
14346914
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