IP Library Granted Patent US 10,953,008
Granted Patent B2
US 10,953,008 · App. 16/996,314 · Granted Mar 23, 2021

Substituted pyrazolo[1,5-a]pyrazines as negative allosteric modulators of group II metabotropic glutamate receptor

Inventors: Yohei Ikuma (Osaka, JP); Kengo Tojo (Osaka, JP); Ryo Fukazawa (Osaka, JP); Shuji Masumoto (Osaka, JP)
Assignee: SUMITOMO DAINIPPON PHARMA CO., LTD.
A61K31/4985A61P25/28C07D519/00
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 10,953,008
App. No.
16/996,314
Granted
Mar 23, 2021
Kind
B2
Abstract

Provided are a compound that is useful for the prevention of and/or as a treatment agent for a disease in which a group II mGlu receptor is involved; and a medical application of said compound. Provided is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof.

Claims (24)

1. A compound selected from the group consisting of:

(7S)-3-(imidazo[1,2-a]pyridin-6-yl)-7-methyl-5-[4-(trifluoromethyl)phenyl]-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one;

(7S)-3-(imidazo[1,2-a]pyridin-6-yl)-7-methyl-5-[3-chloro-4-fluorophenyl]-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one;

(7S)-3-(3-fluoroimidazo[1,2-a]pyridin-6-yl)-7-methyl-5-[4-(trifluoromethyl)phenyl]-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one; and

(7S)-7-methyl-3-(3-methylimidazo[1,2-a]pyridin-6-yl)-5-[4-(trifluoromethyl)phenyl]-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one,

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein the compound is (7S)-3-(imidazo[1,2-a]pyridin-6-yl)-7-methyl-5-[4-(trifluoromethyl)phenyl]-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one, or a pharmaceutically acceptable salt thereof.

3. The compound of claim 1 , wherein the compound is (7S)-3-(imidazo[1,2-a]pyridin-6-yl)-7-methyl-5-[3-chloro-4-fluorophenyl]-6,7-dihydropyrazolo [1,5-a]pyrazin-4(5H)-one, or a pharmaceutically acceptable salt thereof.

4. The compound of claim 1 , wherein the compound is (7S)-3-(3-fluoroimidazo[1,2-a]pyridin-6-yl)-7-methyl-5-[4-(trifluoromethyl)phenyl]-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one, or a pharmaceutically acceptable salt thereof.

5. The compound of claim 1 , wherein the compound is (7S)-7-methyl-3-(3-methylimidazo[1,2-a]pyridin-6-yl)-5-[4-(trifluoromethyl)phenyl]-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one, or a pharmaceutically acceptable salt thereof.

6. A pharmaceutical composition comprising one or more pharmaceutically acceptable excipients and the compound of claim 1 , or a pharmaceutically acceptable salt thereof.

7. The pharmaceutical composition of claim 6 , wherein the pharmaceutically composition further comprises one or more additional medicaments.

8. A method for negatively modulating allosteric activity of a Group II metabotropic glutamate receptor in a patient, comprising administering to a patient in need thereof a therapeutically effective amount of the compound according to claim 1 , or a pharmaceutically acceptable salt thereof.

9. The method of claim 8 , wherein the Group II metabotropic glutamate receptor is metabotropic glutamate receptor subtype 2.

10. The method of claim 8 , wherein the patient has a disease involving Group II metabotropic glutamate receptor selected from the group consisting of a psychiatric disease and a neurodegenerative disease.

11. The method of claim 10 , wherein the psychiatric disease or neurodegenerative disease is selected from the group consisting of major depressive disorder, depressive disorder, bipolar disorder, a bipolar-related disorder, anxiety disorder, posttraumatic stress disorder, obsessive-compulsive disorder, acute stress disorder, schizophrenia, autism spectrum disorder, Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, obesity, seizure, tremor, pain, and sleep disorder.

12. The method of claim 10 , wherein the psychiatric disease or neurodegenerative disease is selected from the group consisting of major depressive disorder, depressive disorder, bipolar disorder, a bipolar-related disorder, anxiety disorder, posttraumatic stress disorder, obsessive-compulsive disorder, acute stress disorder, schizophrenia, autism spectrum disorder, and sleep disorder.

13. The method of claim 10 , wherein the psychiatric disease or neurodegenerative disease is selected from the group consisting of major depressive disorder, depressive disorder, bipolar disorder, a bipolar-related disorder, anxiety disorder, posttraumatic stress disorder, obsessive-compulsive disorder, and acute stress disorder.

14. The method of claim 10 , wherein the psychiatric disease or neurodegenerative disease is selected from the group consisting of Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, obesity, seizure, tremor, and pain.

15. The method of claim 8 , wherein the compound is (7S)-3-(imidazo[1,2-a]pyridin-6-yl)-7-methyl-5-[4-(trifluoromethyl)phenyl]-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one, or a pharmaceutically acceptable salt thereof.

16. The method of claim 8 , wherein the compound is (7S)-3-(imidazo[1,2-a]pyridin-6-yl)-7-methyl-5-[3-chloro-4-fluorophenyl]-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one, or a pharmaceutically acceptable salt thereof.

17. The method of claim 8 , wherein the compound is (7S)-3-(3-fluoroimidazo[1,2-a]pyridin-6-yl)-7-methyl-5-[4-(trifluoromethyl)phenyl]-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one, or a pharmaceutically acceptable salt thereof.

18. The method of claim 8 , wherein the compound is (7S)-7-methyl-3-(3-methylimidazo[1,2-a]pyridin-6-yl)-5-[4-(trifluoromethyl)phenyl]-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one, or a pharmaceutically acceptable salt thereof.

19. The method of claim 10 , wherein the method further comprises administering to the patient one or more antipsychotic drugs.

Assignments (1)
CHANGE OF NAME Recorded Nov 21, 2022
From: SUMITOMO DAINIPPON PHARMA CO., LTD.
To: SUMITOMO PHARMA CO., LTD.
Reel/Frame 061972/0730 →
Priority Claims (1)
JP 2017-225364 · Nov 24, 2017 · national
Continuity (2)
Continuation 16764962
Related Publication 20210030754A1 · Feb 4, 2021