IP Library Granted Patent US 10,604,516
Granted Patent B2
US 10,604,516 · App. 14/346,914 · Granted Mar 31, 2020

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)
Assignee: National Institutes for Quantum and Radiological Science and Technology
C07D417/06A61K49/0017A61K49/0021C07D277/64C07D401/06C07D401/14C07D405/06C07D405/14C07D417/14C07F7/1804
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Quick Facts
Patent No.
US 10,604,516
App. No.
14/346,914
Granted
Mar 31, 2020
Kind
B2
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   [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.

Claims (7)

1. A compound selected from the following:

or a pharmaceutically acceptable salt thereof, or a solvate thereof.

2. The compound of claim 1 , wherein one or more atoms are a radioisotope of the atom or atoms.

3. A composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutically acceptable carrier.

4. A method of tau imaging, comprising:

(a) administering an effective dose of the compound of claim 1 , or a pharmaceutically acceptable salt thereof, or a solvate thereof, to a mammal; and

(b) imaging the brain of the mammal.

Assignments (2)
CHANGE OF NAME Recorded Nov 2, 2016
From: NATIONAL INSTITUTE OF RADIOLOGICAL SCIENCES
To: NATIONAL INSTITUTES FOR QUANTUM AND RADIOLOGICAL SCIENCE AND TECHNOLOGY
Reel/Frame 040766/0742 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 15, 2014
From: HIGUCHI, MAKOTO; SUHARA, TETSUYA; MARUYAMA, MASAHIRO; CHO, MEIEI; SHIMADA, HITOSHI
To: NATIONAL INSTITUTE OF RADIOLOGICAL SCIENCES
Reel/Frame 032676/0907 →
Continuity (1)
Related Publication 20150239878A1 · Aug 27, 2015
Cited By (2)
US 12,195,454 US 12,377,152