IP Library Granted Patent US 11,530,189
Granted Patent B2
US 11,530,189 · App. 17/195,351 · Granted Dec 20, 2022

Carbamate compounds and methods of making and using same

Inventors: Justin S. Cisar (San Diego, CA); Cheryl A. Grice (Encinitas, CA); Todd K. Jones (Solana Beach, CA); Micah J. Niphakis (San Diego, CA); Jae Won Chang (San Diego, CA); Kenneth M. Lum (San Diego, CA); Benjamin F. Cravatt (San Diego, CA)
Assignees: H. LUNDBECKA/S; THE SCRIPPS RESEARCH INSTITUTE
C07D295/205A61P25/22C07C271/10C07C271/12C07D205/04C07D207/09C07D207/14C07D213/38C07D213/40C07D213/55C07D215/42C07D215/46C07D231/12C07D231/16C07D231/56C07D241/04C07D261/08C07D263/32C07D271/06C07D295/26C07D307/79C07D317/46C07D317/58C07D401/04C07D401/10C07D403/10C07D405/14C07D407/06C07D413/06C07D413/10C07D471/04C07D471/10C07D487/04C07D491/107
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 11,530,189
App. No.
17/195,351
Granted
Dec 20, 2022
Kind
B2
Abstract

This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from post-traumatic stress disorder comprising administering a disclosed compound or composition.

Claims (32)

1. A method of treating epilepsy in a subject in need thereof, the method comprising administering to the subject an effective amount of a compound represented by:

wherein

L 3 is a bond, —CH 2 —, —S(O) 2 —, or —C(O)—;

R 7 is phenyl; wherein R 7 is optionally substituted by one, two, or three moieties independently selected from R h ;

R a and R b are independently selected, for each occurrence, from the group consisting of hydrogen and C 1-3 alkyl; wherein C 1-3 alkyl is optionally substituted by one or more substituents selected from halogen, cyano, oxo, hydroxyl, heterocycle, and phenyl;

or R a and R b , when they occur together with the nitrogen to which they are attached, form a 4-6 membered saturated heterocyclic ring, which may have an additional heteroatom selected from O, S, and N, or a spirocyclic ring selected from 8-oxa-2-azaspiro[4.5]decane and 2,8-diazaspiro[4.5]decane, wherein the 4-6 membered saturated heterocyclic ring or the spirocyclic ring are optionally substituted by one or more substituents selected from the group consisting of halogen, cyano, oxo, C 1-6 alkyl, —S(O) w —C 1-6 alkyl (where w is 0, 1 or 2), hydroxyl, —C(O)—C 1-6 alkyl, —NH 2 , and —NH—C(O)—C 1-6 alkyl;

R c is selected from the group consisting of halogen, hydroxyl, C 1-6 alkyl (optionally substituted by one, two, or three halogens), and C 1-6 alkoxy (optionally substituted by one, two, or three halogens); and

R h is selected from the group consisting of: halogen, phenyl (optionally substituted by one, two, or three moieties each independently selected from R c ), hydroxyl, cyano, C 1-6 alkyl (optionally substituted by one, two or three halogens), C 1-6 alkoxy (optionally substituted by one, two or three halogens), R a R b N—, R a —C(O)NR a —, R a R b N—SO 2 —, R a R b N—C(O)—, R a —S(O) w — (wherein w is 0, 1 or 2), R a —SO 2 —NR b —, and heteroaryl (optionally substituted by one, two or three moieties each independently selected from R c );

or a stereoisomer or pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein L 3 is a —CH 2 —.

3. The method of claim 1 , wherein L 3 is a —CH 2 —; and R h is selected from the group consisting of: halogen, phenyl (optionally substituted by one, two, or three moieties each independently selected from halogen, methyl, ethyl, propyl, t-butyl, and CF 3 ), C 1-6 alkyl (optionally substituted by one, two or three halogens), C 1-6 alkoxy (optionally substituted by one, two or three halogens), R a R b N—, R a R b N—C(O)—, and heteroaryl (optionally substituted by one, two or three moieties each independently selected from C 1-6 alkyl or halogen).

4. The method of claim 1 , wherein L 3 is a —CH 2 —; and R h is selected from the group consisting of: halogen, C 1-6 alkyl (optionally substituted by one, two or three halogens), C 1-6 alkoxy (optionally substituted by one, two or three halogens), and R a R b N—.

5. The method of claim 4 , wherein R 7 is substituted by two moieties independently selected from R h .

6. The method of claim 1 , wherein L 3 is a —CH 2 —; and R 7 is substituted by R a R b N— and a moiety selected from the group consisting of: halogen, C 1-6 alkyl (optionally substituted by one, two or three halogens), and C 1-6 alkoxy (optionally substituted by one, two or three halogens).

7. The method of claim 6 , wherein R a and R b , together with the nitrogen to which they are attached, form a 4-6 membered saturated heterocyclic ring, which may have an additional heteroatom selected from O, S, and N, and the 4-6 membered saturated heterocyclic ring is optionally substituted by one or more substituents selected from the group consisting of halogen, cyano, oxo, C 1-6 alkyl, —S(O) w —C 1-6 alkyl (where w is 0, 1 or 2), hydroxyl, —C(O)—C 1-6 alkyl, —NH 2 , and —NH—C(O)—C 1-6 alkyl.

8. The method of claim 7 , wherein the 4-6 membered saturated heterocyclic ring is selected from azetidine, pyrrolidine, piperidine, piperazine, and morpholine, and the 4-6 membered saturated heterocyclic ring is optionally substituted by one or more substituents selected from the group consisting of halogen, cyano, oxo, C 1-6 alkyl, —S(O) w —C 1-6 alkyl (where w is 0, 1 or 2), hydroxyl, —C(O)—C 1-6 alkyl, —NH 2 , and —NH—C(O)—C 1-6 alkyl.

9. The method of claim 7 , wherein the 4-6 membered saturated heterocyclic ring is pyrrolidine.

10. The method of claim 7 , wherein the 4-6 membered saturated heterocyclic ring is morpholine.

11. The method of claim 7 , wherein the 4-6 membered saturated heterocyclic ring is piperidine.

12. The method of claim 1 , wherein L 3 is a —CH 2 —; and R h is selected from the group consisting of: halogen, phenyl (optionally substituted by one, two, or three moieties each independently selected from halogen, methyl, ethyl, propyl, t-butyl, and CF 3 ), C 1-6 alkyl (optionally substituted by one, two or three halogens), C 1-6 alkoxy (optionally substituted by one, two or three halogens), and heteroaryl (optionally substituted by one, two or three moieties each independently selected from C 1-6 alkyl or halogen).

13. The method of claim 12 , wherein R 7 is substituted by two moieties independently selected from R h .

14. The method of claim 1 , wherein L 3 is a —CH 2 —; and R h is selected from the group consisting of: halogen, C 1-6 alkyl (optionally substituted by one, two or three halogens), C 1-6 alkoxy (optionally substituted by one, two or three halogens), and R a R b N—C(O)—.

15. The method of claim 14 , wherein R 7 is substituted by two moieties independently selected from R h .

16. The method of claim 1 , wherein L 3 is —S(O) 2 —.

17. The method of claim 1 , wherein L 3 is —C(O)—.

18. The method of claim 1 , wherein L 3 is a bond.

19. The method of claim 1 , wherein the compound is 1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[2-(morpholin-4-yl)-4-(trifluoromethyl)phenyl]-methyl]piperazine-1-carboxylate, or a pharmaceutically acceptable salt thereof.

20. The method of claim 1 , wherein the compound is 1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[3-fluoro-2-(morpholin-4-yl)phenyl]4-methyl]piperazine-1-carboxylate, or a pharmaceutically acceptable salt thereof.

21. The method of claim 1 , wherein the compound is 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate, or a pharmaceutically acceptable salt thereof.

22. The method of claim 1 , wherein the compound is 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(3-acetamidopyrrolidin-1-yl)-4-chlorobenzyl)piperazine-1-carboxylate, or a solvate, hydrate, stereoisomer, or pharmaceutically acceptable salt thereof.

23. The method of claim 1 , wherein the compound is 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(4-chloro-2-(8-oxa-2-azaspiro[4.5]decan-2-yl)benzyl)piperazine-1-carboxylate, or a solvate, hydrate, or pharmaceutically acceptable salt thereof.

24. The method of claim 1 , wherein the compound is 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(4-chloro-2-(4-(methylsulfonyl)piperazin-1-yl)benzyl)piperazine-1-carboxylate, or a solvate, hydrate, or pharmaceutically acceptable salt thereof.

Assignments (5)
CORRECTIVE ASSIGNMENT TO CORRECT THE 1ST INVENTOR'S MIDDLE INITIAL NAME PREVIOUSLY RECORDED AT REEL: 055639 FRAME: 0644. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT . Recorded Oct 28, 2021
From: CISAR, JUSTIN S.; GRICE, CHERYL A.; JONES, TODD K.
To: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
Reel/Frame 057964/0991 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 26, 2021
From: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
To: H. LUNDBECK A/S
Reel/Frame 057919/0419 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 15, 2021
From: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
To: H. LUNDBECK A/S
Reel/Frame 058240/0547 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 18, 2021
From: NIPHAKIS, MICAH J.; CHANG, JAE WON; LUM, KENNETH M.; CRAVATT, BENJAMIN F.
To: THE SCRIPPS RESEARCH INSTITUTE
Reel/Frame 055639/0530 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 18, 2021
From: CISAR, JUSTIN C.; GRICE, CHERYL A.; JONES, TODD K.
To: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
Reel/Frame 055639/0644 →
Continuity (6)
Continuation 16717813 · Dec 17, 2019
Continuation 15925517 · Mar 19, 2018
Continuation 15272313 · Sep 21, 2016
Continuation 14369982
Provisional Application 61631558 · Jan 6, 2012
Related Publication 20210188793A1 · Jun 24, 2021