IP Library Granted Patent US 12,415,782
Granted Patent B2
US 12,415,782 · App. 19/079,211 · Granted Sep 16, 2025

Heterocyclic compound and use thereof

Inventors: Yasushi Hattori (Kanagawa, JP); Yuhei Miyanohana (Kanagawa, JP); Yuichi Kajita (Kanagawa, JP); Tatsuki Koike (Kanagawa, JP); Yasutaka Hoashi (Kanagawa, JP); Norihito Tokunaga (Kanagawa, JP); Alexander Martin Pawliczek (Kanagawa, JP); Tsuneo Oda (Kanagawa, JP); Tohru Miyazaki (Kanagawa, JP); Yoshiteru Ito (Kanagawa, JP); Kohei Takeuchi (Kanagawa, JP); Keisuke Imamura (Kanagawa, JP); Takahiro Sugimoto (Kanagawa, JP)
Assignee: Takeda Pharmaceutical Company Limited
C07D207/14C07D403/06C07D407/08C07D417/06
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Quick Facts
Patent No.
US 12,415,782
App. No.
19/079,211
Granted
Sep 16, 2025
Kind
B2
Abstract

The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.

Claims (29)

1. A pharmaceutical composition comprising a pharmacologically acceptable carrier and a compound selected from the group consisting of:

N′-{(2S,3R,4S)-1-(azetidine-1-carbonyl)-4-fluoro-2-[(2-fluoro-3′-methyl[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}-N,N-dimethylsulfuric diamide;

N-[(2S,3R)-2-[(2,3′-difluoro[1,1′-biphenyl]-3-yl)methyl]-4,4-difluoro-1-(2-methylpropanoyl)pyrrolidin-3-yl]ethanesulfonamide;

N-{(2S,3R)-4,4-difluoro-1-(2-hydroxy-2-methylpropanoyl)-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}ethanesulfonamide;

N-{(2S,3R)-4,4-difluoro-1-(2-hydroxy-2-methylpropanoyl)-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}methanesulfonamide;

N-{(2S,3R)-1-(bicyclo[1.1.1]pentane-1-carbonyl)-4,4-difluoro-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}methanesulfonamide;

N-{(2S,3R)-1-(cyclopropanecarbonyl)-4,4-difluoro-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}ethanesulfonamide;

N-{(2S,3R)-4,4-difluoro-1-((1s,3R)-3-fluorocyclobutane-1-carbonyl)-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}ethanesulfonamide;

N-{(2S,3R)-4,4-difluoro-1-((1s,3R)-3-fluorocyclobutane-1-carbonyl)-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}methanesulfonamide; and

N′-{(2S,3R)-1-(azetidine-1-carbonyl)-4,4-difluoro-2-[(2-fluoro-3′-methyl[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}-N,N-dimethylsulfuric diamide;

or a salt thereof.

2. The pharmaceutical composition of claim 1 , wherein the compound is N′-{(2S,3R,4S)-1-(azetidine-1-carbonyl)-4-fluoro-2-[(2-fluoro-3′-methyl [1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}-N,N-dimethylsulfuric diamide or a salt thereof.

3. The pharmaceutical composition of claim 1 , wherein the compound is N-[(2S,3R)-2-[(2,3′-difluoro[1,1′-biphenyl]-3-yl)methyl]-4,4-difluoro-1-(2-methylpropanoyl) pyrrolidin-3-yl]ethanesulfonamide or a salt thereof.

4. The pharmaceutical composition of claim 1 , wherein the compound is N-{(2S,3R)-4,4-difluoro-1-(2-hydroxy-2-methylpropanoyl)-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}ethanesulfonamide or a salt thereof.

5. The pharmaceutical composition of claim 1 , wherein the compound is N-{(2S,3R)-4,4-difluoro-1-(2-hydroxy-2-methylpropanoyl)-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}methanesulfonamide or a salt thereof.

6. The pharmaceutical composition of claim 1 , wherein the compound is N-{(2S,3R)-1-(bicyclo[1.1.1]pentane-1-carbonyl)-4,4-difluoro-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}methanesulfonamide or a salt thereof.

7. The pharmaceutical composition of claim 1 , wherein the compound is N-{(2S,3R)-1-(cyclopropanecarbonyl)-4,4-difluoro-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}ethanesulfonamide or a salt thereof.

8. The pharmaceutical composition of claim 1 , wherein the compound is N-{(2S,3R)-4,4-difluoro-1-((1s,3R)-3-fluorocyclobutane-1-carbonyl)-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}ethanesulfonamide or a salt thereof.

9. The pharmaceutical composition of claim 1 , wherein the compound is N-{(2S,3R)-4,4-difluoro-1-((1s,3R)-3-fluorocyclobutane-1-carbonyl)-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}methanesulfonamide or a salt thereof.

10. The pharmaceutical composition of claim 1 , wherein the compound is N′-{(2S,3R)-1-(azetidine-1-carbonyl)-4,4-difluoro-2-[(2-fluoro-3′-methyl [1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}-N,N-dimethylsulfuric diamide or a salt thereof.

11. The pharmaceutical composition of claim 1 , wherein the compound is N′-{(2S,3R,4S)-1-(azetidine-1-carbonyl)-4-fluoro-2-[(2-fluoro-3′-methyl [1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}-N,N-dimethylsulfuric diamide.

12. The pharmaceutical composition of claim 1 , wherein the compound is N-[(2S,3R)-2-[(2,3′-difluoro[1,1′-biphenyl]-3-yl)methyl]-4,4-difluoro-1-(2-methylpropanoyl) pyrrolidin-3-yl]ethanesulfonamide.

13. The pharmaceutical composition of claim 1 , wherein the compound is N-{(2S,3R)-4,4-difluoro-1-(2-hydroxy-2-methylpropanoyl)-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}ethanesulfonamide.

14. The pharmaceutical composition of claim 1 , wherein the compound is N-{(2S,3R)-4,4-difluoro-1-(2-hydroxy-2-methylpropanoyl)-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}methanesulfonamide.

15. The pharmaceutical composition of claim 1 , wherein the compound is N-{(2S,3R)-1-(bicyclo[1.1.1]pentane-1-carbonyl)-4,4-difluoro-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}methanesulfonamide.

16. The pharmaceutical composition of claim 1 , wherein the compound is N-{(2S,3R)-1-(cyclopropanecarbonyl)-4,4-difluoro-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}ethanesulfonamide.

17. The pharmaceutical composition of claim 1 , wherein the compound is N-{(2S,3R)-4,4-difluoro-1-((1s,3R)-3-fluorocyclobutane-1-carbonyl)-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}ethanesulfonamide.

18. The pharmaceutical composition of claim 1 , wherein the compound is N-{(2S,3R)-4,4-difluoro-1-((1s,3R)-3-fluorocyclobutane-1-carbonyl)-2-[(2,3′,5′-trifluoro[1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}methanesulfonamide.

19. The pharmaceutical composition of claim 1 , wherein the compound is N′-{(2S,3R)-1-(azetidine-1-carbonyl)-4,4-difluoro-2-[(2-fluoro-3′-methyl [1,1′-biphenyl]-3-yl)methyl]pyrrolidin-3-yl}-N,N-dimethylsulfuric diamide.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 23, 2025
From: HATTORI, YASUSHI; MIYANOHANA, YUHEI; KAJITA, YUICHI; KOIKE, TATSUKI; HOASHI, YASUTAKA; TOKUNAGA, NORIHITO; PAWLICZEK, ALEXANDER MARTIN; ODA, TSUNEO; MIYAZAKI, TOHRU; ITO, YOSHITERU; TAKEUCHI, KOHEI; IMAMURA, KEISUKE; SUGIMOTO, TAKAHIRO
To: TAKEDA PHARMACEUTICAL COMPANY LIMITED
Reel/Frame 071804/0743 →
Priority Claims (1)
JP 2019-015488 · Jan 31, 2019 · national
Continuity (5)
Continuation 18520037 · Nov 27, 2023
Continuation 18175215 · Feb 27, 2023
Continuation 17239191 · Apr 23, 2021
Continuation 16777273 · Jan 30, 2020
Related Publication 20250243158A1 · Jul 31, 2025
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