IP Library Granted Patent US 12,458,643
Granted Patent B2
US 12,458,643 · App. 17/997,974 · Granted Nov 4, 2025

Antidepressant/anxiolytic drug in which PAC1 receptor antagonist is used

Inventors: Takashi Kurihara (Kagoshima, JP); Ichiro Takasaki (Toyama, JP); Hitoshi Hashimoto (Osaka, JP); Atsuko Hayata (Osaka, JP); Yusuke Shintani (Osaka, JP)
Assignees: KAGOSHIMA UNIVERSITY; OSAKA UNIVERSITY
A61K31/519A61K31/4178A61P25/22A61P25/24
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Quick Facts
Patent No.
US 12,458,643
App. No.
17/997,974
Granted
Nov 4, 2025
Kind
B2
Abstract

This invention relates to an antidepressant/anxiolytic drug comprising a compound represented by the following formula (I) or (II), wherein R 1 is a hydrogen atom, a C 1-6 -alkyl group, a C 1-6 -alkoxy group, a C 2-6 -alkenyloxy group, a halogen atom, a C 1-6 -haloalkyl group, a C 1-6 -haloalkoxy group, or a substituted or unsubstituted phenyl group; R 2 is a hydrogen atom, a C 1-6 -alkyl group, a C 1-6 -alkoxy group, a C 2-6 -alkenyloxy group, a halogen atom, a C 1-6 -haloalkyl group, a C 1-6 -haloalkoxy group, or a substituted or unsubstituted phenyl group; and R is an indazolyl group substituted with a halogen atom; a substituted or unsubstituted phenyl group; a pyrazolyl group; or a substituted or unsubstituted aralkyl group; or a salt thereof, or a solvate thereof.

Claims (20)

1 . A method for treating and/or preventing a disease that is anxiety disorder, stress disorder, and/or depression, comprising administering to a subject in need thereof an effective amount of a compound of formula (I):

wherein

R 1 is a hydrogen atom, a C 1-6 -alkyl group, a C 1-6 -alkoxy group, a C 2-6 -alkenyloxy group, a halogen atom, a C 1-6 -haloalkyl group, a C 1-6 -haloalkoxy group, or a substituted or unsubstituted phenyl group; and

R 2 is a hydrogen atom, a C 1-6 -alkyl group, a C 1-6 -alkoxy group, a C 2-6 -alkenyloxy group, a halogen atom, a C 1-6 -haloalkyl group, a C 1-6 -haloalkoxy group, or a substituted or unsubstituted phenyl group;

or a salt thereof, or a solvate thereof.

2 . The method according to claim 1 , wherein the compound of formula (I) or the salt thereof, or the solvate thereof is orally administered.

3 . A method for treating and/or preventing a disease that is anxiety disorder, stress disorder, and/or depression, comprising administering to a subject in need thereof an effective amount of a compound of formula (II):

wherein R is an indazolyl group substituted with a halogen atom; a substituted or unsubstituted phenyl group; a pyrazolyl group; or a substituted or unsubstituted aralkyl group;

or a salt thereof, or a solvate thereof.

4 . The method according to claim 3 , wherein R is an indazolyl group substituted with a halogen atom.

5 . The method according to claim 3 , wherein the halogen is chlorine.

6 . The method according to claim 3 , wherein the compound of formula (II) or the salt thereof, or the solvate thereof is orally administered.

7 . The method according to claim 4 , wherein the compound of formula (II) or the salt thereof, or the solvate thereof is orally administered.

8 . The method according to claim 5 , wherein the compound of formula (II) or the salt thereof, or the solvate thereof is orally administered.

9 . The method according to claim 1 , wherein the disease is depression.

10 . The method according to claim 1 , wherein the disease is an anxiety disorder.

11 . The method according to claim 1 , wherein the disease is a stress disorder.

12 . The method according to claim 3 , wherein the disease is depression.

13 . The method according to claim 3 , wherein the disease is an anxiety disorder.

14 . The method according to claim 3 , wherein the disease is a stress disorder.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 7, 2022
From: KURIHARA, TAKASHI; TAKASAKI, ICHIRO; HASHIMOTO, HITOSHI; HAYATA, ATSUKO; SHINTANI, YUSUKE
To: KAGOSHIMA UNIVERSITY; OSAKA UNIVERSITY
Reel/Frame 061670/0427 →
Priority Claims (1)
JP 2020-082465 · May 8, 2020 · national
Continuity (1)
Related Publication 20230181587A1 · Jun 15, 2023
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