IP Library Granted Patent US 9,278,960
Granted Patent B2
US 9,278,960 · App. 14/356,080 · Granted Mar 8, 2016

Quinoline carboxamide and quinoline carbonitrile derivatives as mGluR2-negative allosteric modulators, compositions, and their use

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Quick Facts
Patent No.
US 9,278,960
App. No.
14/356,080
Granted
Mar 8, 2016
Kind
B2
Abstract

The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, R Q , -L-, R 1 , n, R 2 , and R 3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.

Claims (28)

1. A compound selected from the group consisting of:

or a stereoisomer thereof, or a pharmaceutically acceptable salt of said compound or said stereoisomer.

2. A compound having a structure:

3. A pharmaceutical composition comprising the compound of claim 2 and a pharmaceutically acceptable carrier.

4. A compound having a structure:

in the form of a pharmaceutically acceptable salt.

5. A pharmaceutical composition comprising the compound of claim 4 in the form of a pharmaceutically acceptable salt and a pharmaceutically acceptable carrier.

6. A compound having a structure:

7. A pharmaceutical composition comprising the compound of claim 6 and a pharmaceutically acceptable carrier.

8. A compound having a structure:

in the form of a pharmaceutically acceptable salt.

9. A pharmaceutical composition comprising the compound of claim 8 in the form of a pharmaceutically acceptable salt and a pharmaceutically acceptable carrier.

10. A compound having a structure:

11. A pharmaceutical composition comprising the compound of claim 10 and a pharmaceutically acceptable carrier.

12. A compound having a structure:

in the form of a pharmaceutically acceptable salt.

13. A pharmaceutical composition comprising the compound of claim 12 in the form of a pharmaceutically acceptable salt and a pharmaceutically acceptable carrier.

14. A compound having a structure:

or a stereoisomer thereof.

15. A pharmaceutical composition comprising the compound of claim 14 or a stereoisomer thereof, and a pharmaceutically acceptable carrier.

16. A compound having a structure:

or a stereoisomer thereof, wherein said compound or said stereoisomer is in the form of a pharmaceutically acceptable salt.

17. A pharmaceutical composition comprising the compound of claim 16 or a stereoisomer thereof, wherein said compound or said stereoisomer is in the form of a pharmaceutically acceptable salt, and a pharmaceutically acceptable carrier.

18. A compound having a structure:

19. A pharmaceutical composition comprising the compound of claim 18 and a pharmaceutically acceptable carrier.

20. A compound having a structure:

in the form of a pharmaceutically acceptable salt.

21. A pharmaceutical composition comprising the compound of claim 20 in the form of a pharmaceutically acceptable salt and a pharmaceutically acceptable carrier.

Assignments (2)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 24, 2015
From: BUNGARD, CHRISTOPHER JAMES; CONVERSO, ANTONELLA; DELEON, PABLO; HANNEY, BARBARA; HARTINGH, TIMOTHY JOHN; MANIKOWSKI, JESSE JOSEF; MANLEY, PETER J.; MEISSNER, ROBERT; MENG, ZHAOYANG; PERKINS, JAMES J.; RUDD, MICHAEL T.; SHU, YOUHENG
To: MERCK SHARP & DOHME CORP.
Reel/Frame 035963/0618 →