IP Library Granted Patent US 10,899,737
Granted Patent B2
US 10,899,737 · App. 16/334,335 · Granted Jan 26, 2021

Piperazine carbamates and methods of making and using same

Inventors: Cheryl A. Grice (Encinitas, CA); Daniel J. Buzard (San Diego, CA); Michael B. Shaghafi (San Diego, CA); Olivia D. Weber (San Diego, CA)
Assignee: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
C07D401/10A61K45/06A61P1/00A61P23/00A61P25/28A61P29/00C07D205/04C07D207/09C07D207/16C07D211/26C07D211/58C07D211/60C07D211/62C07D231/12C07D241/04C07D265/30C07D295/205C07D309/08C07D333/38C07D333/40C07D401/04C07D403/10C07D403/14C07D405/10C07D413/10C07D471/06C07D471/10C07D487/04C07D487/08C07D487/10
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Quick Facts
Patent No.
US 10,899,737
App. No.
16/334,335
Granted
Jan 26, 2021
Kind
B2
Abstract

Provided herein are piperazine carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or ABHD6. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

Claims (27)

1. A compound of Formula (III):

wherein:

X is —N(R 2 )(R 3 ), —C 1-6 alkyl-N(R 4 )(R 5 ), or —C(O)N(R 4 )(R 5 );

each R 1 is independently halogen, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 alkoxy, C 1-6 haloalkoxy, C 3-8 cycloalkyl, —OH, or —CN;

R 2 and R 3 , together with the nitrogen to which they are attached, form

(i) a C 2-8 heterocycloalkyl; or

(ii) a C 2-8 heteroaryl;

wherein the C 2-8 heterocycloalkyl or the C 2-8 heteroaryl is substituted with one R 6 and optionally substituted with one or two additional substituents selected from halogen, C 1-6 alkyl, C 1-6 haloalkyl, and C 1-6 alkoxy;

R 4 and R 5 , together with the nitrogen to which they are attached, form

(i) a C 2-8 heterocycloalkyl; or

(ii) a C 2-8 heteroaryl;

wherein the C 2-8 heterocycloalkyl or the C 2-8 heteroaryl is substituted with one R 7 and optionally substituted with one or two additional substituents selected from halogen, C 1-6 alkyl, C 1-6 haloalkyl, and C 1-6 alkoxy;

R 6 is —C 1-6 alkyl-CO 2 H or —N(R 8 )—C 1-6 alkyl-CO 2 H;

R 7 is —CO 2 H, —C 1-6 alkyl-CO 2 H, or —N(R 9 )—C 1-6 alkyl-CO 2 H;

R 8 is H or C 1-6 alkyl;

R 9 is H or C 1-6 alkyl; and

p is 0, 1, 2, 3, or 4;

or a pharmaceutically acceptable salt or solvate thereof.

2. The compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof, wherein X is —N(R 2 )(R 3 ).

3. The compound of claim 2 , or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 and R 3 , together with the nitrogen to which they are attached, form a C 2 -C 8 heterocycloalkyl substituted with one R 6 .

4. The compound of claim 3 , or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 and R 3 , together with the nitrogen to which they are attached, form a C 2 -C 8 heterocycloalkyl selected from:

5. The compound of claim 4 , or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is —CH 2 CO 2 H.

6. The compound of claim 4 , or a pharmaceutically acceptable salt or solvate thereof, wherein each R 1 is independently halogen or C 1-6 haloalkyl.

7. The compound of claim 6 , or a pharmaceutically acceptable salt or solvate thereof, wherein each R 1 is C 1-6 haloalkyl.

8. The compound of claim 7 , or a pharmaceutically acceptable salt or solvate thereof, wherein p is 1.

9. The compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof, selected from:

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

Assignments (4)
CORRECTIVE ASSIGNMENT TO CORRECT THE THE RECEIVING PARTY NAME PREVIOUSLY RECORDED AT REEL: 055679 FRAME: 0885. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Jun 11, 2021
From: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
To: H. LUNDBECK A/S
Reel/Frame 056544/0697 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 23, 2021
From: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
To: H. LUNDBECK A/S.
Reel/Frame 055679/0885 →
CHANGE OF NAME Recorded Jan 22, 2020
From: ABIDE THERAPEUTICS, INC.
To: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
Reel/Frame 051588/0454 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 25, 2019
From: GRICE, CHERYL A.; BUZARD, DANIEL J.; SHAGHAFI, MICHAEL B.; WEBER, OLIVIA D.
To: ABIDE THERAPEUTICS, INC.
Reel/Frame 048995/0294 →
Continuity (2)
Provisional Application 62396561 · Sep 19, 2016
Related Publication 20190202801A1 · Jul 4, 2019
Cited By (1)
US 12,286,421