IP Library Granted Patent US 10,377,695
Granted Patent B2
US 10,377,695 · App. 15/820,194 · Granted Aug 13, 2019

Metabotropic glutamate receptor positive allosteric modulators (PAMS) and uses thereof

Inventors: Raveendra Panickar Dhanya (La Jolla, CA); Douglas J. Sheffler (La Jolla, CA); Nicholas D. P. Cosford (La Jolla, CA)
Assignee: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
C07C65/40C07C49/84C07C59/90C07C69/92C07C235/46C07C235/54C07C251/48C07C255/56C07C259/10C07C311/51C07D213/50C07D213/55C07D213/64C07D213/68C07D213/70C07D213/79C07D213/80C07D239/26C07D241/12C07D241/24C07D257/04C07D271/06C07D271/07C07D277/24C07D285/08C07D285/12C07D295/108C07D295/16C07D295/26C07D307/42C07D307/54C07D307/68C07D311/16C07D333/24C07F5/025C07F5/04C07F7/025C07C2601/02C07C2601/08
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Quick Facts
Patent No.
US 10,377,695
App. No.
15/820,194
Granted
Aug 13, 2019
Kind
B2
Abstract

Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor positive allosteric modulators (PAMS), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

Claims (40)

1. A compound, or a pharmaceutically acceptable salt thereof, having the structure of formula (III):

wherein:

R 1 is —OH, —OR 4 , —NHOR 5 , —NHSO 2 R 4 , —NR 4 R 5 , or R 4 ;

or —C(═O)R 1 is a carboxylic acid bioisostere having the structure

Ring A is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

Ring B is substituted or unsubstituted 6-membered heteroaryl;

L 2 is absent or —O—(C 1 -C 6 alkylene);

R 2 is hydrogen, halogen, nitro, —CN, —OH, —OR 4 , substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted C 1 -C 6 fluoroalkyl, or substituted or unsubstituted C 3 -C 6 cycloalkyl;

R 3 is substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted C 1 -C 6 fluoroalkyl, substituted or unsubstituted C 3 -C 6 cycloalkyl, or substituted or unsubstituted aryl;

Z is —OH, —OR 4 , halogen, substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted C 1 -C 6 fluoroalkyl, or substituted or unsubstituted C 3 -C 6 cycloalkyl;

R 4 is substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted C 3 -C 6 cycloalkyl substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

R 5 is hydrogen, substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted C 1 -C 6 fluoroalkyl, substituted or unsubstituted C 3 -C 6 cycloalkyl, or substituted or unsubstituted aryl;

or R 4 and R 5 taken together with the nitrogen to which they are attached to form a substituted or unsubstituted C 2 -C 8 heterocycloalkyl;

n is 0, 1, 2, 3, 4; and

p is 0 or 1.

2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

Z is —OH, —OR 4 , halogen, or substituted or unsubstituted C 1 -C 6 alkyl.

3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

L 2 is absent or —O—(CH 2 )—.

4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

Ring A is substituted or unsubstituted aryl.

5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

Ring B is selected from a group consisting of:

6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

p is 0 and n is 0.

7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

p is 1 and n is 0.

8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

R 1 is —OH, —OCH 3 , —OCH 2 CH 3 , or —NR 4 R 5 .

9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

R 2 is hydrogen, halogen, —CN, —OH, —OR 4 , substituted or unsubstituted C 1 -C 6 alkyl, or substituted or unsubstituted C 1 -C 6 fluoroalkyl.

10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

R 3 is C 1 -C 6 alkyl or C 3 -C 6 cycloalkyl.

11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

R 3 is —CH 3 , —CH 2 CH 3 , —CH 2 CH 2 CH 3 , —CH(CH 3 ) 2 , —CH 2 CH 2 CH 2 CH 3 , —CH(CH 3 )CH 2 CH 3 , —CH 2 CH(CH 3 ) 2 , —C(CH 3 ) 3 , cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl.

12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, selected from the group consisting of:

13. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, or solvate thereof, and at least one pharmaceutically acceptable excipient.

14. A method of treating Alzheimer's disease, Parkinson's disease, Huntington's disease, Lou Gehrig's disease, in a subject in need thereof, the method comprising the step of administering to the subject the compound of claim 1 , or a pharmaceutically acceptable salt thereof.

15. A method of treating an addictive disorder in a subject in need thereof, the method comprising the step of administering to the subject the compound of claim 1 , or a pharmaceutically acceptable salt thereof.

16. The method of claim 15 , wherein the addictive disorder is nicotine addiction, alcohol addiction, opiate addiction, amphetamine addiction, methamphetamine addiction, or cocaine addiction.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 28, 2019
From: DHANYA, RAVEENDRA PANICKAR; SHEFFLER, DOUGLAS J.; COSFORD, NICHOLAS D.P.
To: SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTE
Reel/Frame 048729/0838 →
CHANGE OF NAME Recorded Mar 28, 2019
From: SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTE
To: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
Reel/Frame 048737/0720 →
Continuity (3)
Continuation 15301697
Provisional Application 61975870 · Apr 6, 2014
Related Publication 20180194710A1 · Jul 12, 2018