IP Library Granted Patent US 9,957,242
Granted Patent B2
US 9,957,242 · App. 15/272,313 · Granted May 1, 2018

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 (La Jolla, CA)
Assignees: THE SCRIPPS RESEARCH INSTITUTE; ABIDE THERAPEUTICS, INC.
C07D295/205C07C271/10C07C271/12C07D205/04C07D207/09C07D207/14C07D213/38C07D213/40C07D213/55C07D215/42C07D215/46C07D231/12C07D231/16C07D231/56C07D241/04C07D261/08C07D263/32C07D271/06C07D295/26C07D307/79C07D317/46C07D317/58C07D401/04C07D401/10C07D403/10C07D405/14C07D407/06C07D413/06C07D413/10C07D471/04C07D471/10C07D487/04C07D491/107
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Quick Facts
Patent No.
US 9,957,242
App. No.
15/272,313
Granted
May 1, 2018
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 indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.

Claims (37)

1. A compound represented by:

wherein

L 3 is —CH 2 —;

R 7 is

R i and R j are independently selected from the group consisting of: H, halogen, CH 3 , C 2-6 alkyl (optionally substituted by one, two, or three moieties independently selected from R c ), and phenyl (optionally substituted by one, two, or three moieties independently selected from R c );

R i2 and R j2 are independently selected from the group consisting of: H, halogen, CH 3 , C 2-6 alkyl (optionally substituted by one, two, or three halogens), and phenyl (optionally substituted by one, two, or three moieties independently selected from R c ); and

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

or a pharmaceutically acceptable salt or stereoisomer thereof.

2. The compound of claim 1 , represented by a formula selected from the group consisting of:

3. The compound of claim 2 , represented by:

4. The compound of claim 2 , represented by:

5. The compound of claim 2 , represented by:

6. A compound selected from the group consisting of:

1,1,1,3,3,3-hexafluoropropan-2-yl 4-((5-(4-methoxyphenyl)isoxazol-3-yl)methyl)piperazine-1-carboxylate,

1,1,1,3,3,3-hexafluoropropan-2-yl 4-((5-phenylisoxazol-3-yl)methyl)piperazine-1-carboxylate,

1,1,1,3,3,3-hexafluoropropan-2-yl 4-((3-methyl-1-phenyl-1H-pyrazol-4-yl)methyl)piperazine-1-carboxylate,

1,1,1,3,3,3-hexafluoropropan-2-yl 4-((1-methyl-3-phenyl-1H-pyrazol-5-yl)methyl)piperazine-1-carboxylate,

1,1,1,3,3,3-hexafluoropropan-2-yl 4-((1-methyl-3-phenyl-1H-pyrazol-4-yl)methyl)piperazine-1-carboxylate,

1,1,1,3,3,3-hexafluoropropan-2-yl 4-((4-bromo-1-methyl-1H-pyrazol-5-yl)methyl)piperazine-1-carboxylate,

1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[3-(2-chlorophenyl)-1-methyl-1H-pyrazol-4-yl]methyl]piperazine-1-carboxylate,

1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[3-phenyl-1-(propan-2-yl)-1H-pyrazol-4-yl]methyl]piperazine-1-carboxylate,

1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[3-(2-chlorophenyl)-1-(propan-2-yl)-1H-pyrazol-4-yl]methyl]piperazine-1-carboxylate,

1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[2-methyl-6-(2-methylphenyl)pyridin-3-yl]methyl]piperazine-1-carboxylate,

1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[6-(2-fluorophenyl)-2-methylpyridin-3-yl]methyl]piperazine-1-carboxylate,

1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[2-methyl-6-(3-methylphenyl)pyridin-3-yl]methyl]piperazine-1-carboxylate,

1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[6-(3-fluorophenyl)-2-methylpyridin-3-yl]methyl]piperazine-1-carboxylate,

1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[6-methyl-5-(2-methylphenyl)pyridin-2-yl]methyl]piperazine-1-carboxylate,

1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[5-(3-fluorophenyl)pyridin-2-yl]methyl]piperazine-1-carboxylate,

1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[5-(2-fluorophenyl)-6-methylpyridin-2-yl]methyl]piperazine-1-carboxylate,

1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[5-(3-fluorophenyl)-6-methylpyridin-2-yl]methyl]piperazine-1-carboxylate,

and

1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[6-methyl-5-(3-methylphenyl)pyridin-2-yl]methyl]piperazine-1-carboxylate;

or a pharmaceutically acceptable salt thereof.

7. A pharmaceutically acceptable composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

8. A method of treating pain in a patient in need thereof, comprising administering to the patient in need thereof an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

9. A pharmaceutically acceptable composition comprising a compound of claim 6 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

10. A method of treating pain in a patient in need thereof, comprising administering to the patient in need thereof an effective amount of a compound of claim 6 , or a pharmaceutically acceptable salt thereof.

Assignments (6)
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 →
MERGER Recorded Mar 23, 2021
From: ABIDE THERAPEUTICS, INC.
To: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
Reel/Frame 057434/0784 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 4, 2018
From: NIPHAKIS, MICAH J.; CHANG, JAE WON; LUM, KENNETH M.; CRAVATT, BENJAMIN F.
To: THE SCRIPPS RESEARCH INSTITUTE
Reel/Frame 045438/0804 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 22, 2016
From: NIPHAKIS, MICAH J.; CHANG, JAE WON; LUM, KENNETH M.; CRAVATT, BENJAMIN F.
To: THE SCRIPPS RESEARCH INSTITUTE
Reel/Frame 040108/0184 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 22, 2016
From: CISAR, JUSTIN S; GRICE, CHERYL A.; JONES, TODD K.
To: ABIDE THERAPEUTICS, INC.
Reel/Frame 039829/0980 →
Continuity (3)
Continuation 14369982
Provisional Application 61631558 · Jan 6, 2012
Related Publication 20170073320A1 · Mar 16, 2017