IP Library Granted Patent US 9,487,495
Granted Patent B2
US 9,487,495 · App. 14/369,982 · Granted Nov 8, 2016

Carbamate compounds and 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 SCRIPTS RESEARCH INSTITUTE; ABIDE THERAPEUTICS
C07D295/26C07C271/10C07C271/12C07D205/04C07D207/09C07D207/14C07D213/40C07D213/55C07D215/42C07D231/12C07D231/16C07D231/56C07D241/04C07D261/08C07D263/32C07D271/06C07D295/205C07D307/79C07D317/46C07D317/58C07D401/04C07D405/14C07D407/06C07D413/06C07D471/04C07D471/10C07D487/04C07D491/107
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Quick Facts
Patent No.
US 9,487,495
App. No.
14/369,982
Granted
Nov 8, 2016
Kind
B2
Abstract

This disclosure provides compounds having the structure: wherein L 3 , R 7 , R d and p are defined herein, which are modulators of MAGL and/or ABHD6. Further provided is the use of these compounds as medicinal agents, processes for their preparation, and pharmaceutical compositions that include the disclosed compounds. The disclosure also provides a 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 (25)

1. A compound represented by:

wherein

R a and R b together with the nitrogen to which they are attached, form a 4-6 membered heterocyclic ring which may have an additional heteroatom selected from O, S, and N; wherein the 4-6 membered 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;

L 3 is C 1 -C 6 alkylene, wherein C 1 -C 6 alkylene is substituted by an additional R 7 ;

R 7 is selected from the group consisting of:

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

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

or a pharmaceutically acceptable salt or stereoisomer thereof.

2. A compound selected from the group consisting of:

or a pharmaceutically acceptable salt or stereoisomer thereof.

3. A compound selected from the group consisting of:

1,1,1,3,3,3-hexafluoropropan-2-yl 4-[bis(4-chlorophenyl)methyl]-3-methylpiperazine-1-carboxylate;

1,1,1,3,3,3-hexafluoropropan-2-yl 4-(bis(oxazol-4-yl)methyl)piperazine-1-carboxylate;

1,1,1,3,3,3-hexafluoropropan-2-yl 4-(bis(4-chloro-2-methylphenyl)methyl)piperazine-1-carboxylate;

1,1,1,3,3,3-hexafluoropropan-2-yl 4-(bis(1-methyl-1H-indazol-5-yl)methyl)piperazine-1-carboxylate; and

1,1,1,3,3,3-hexafluoropropan-2-yl 4-(di(pyridin-3-yl)methyl)piperazine-1-carboxylate;

or a pharmaceutically acceptable salt or stereoisomer thereof.

4. The compound of claim 1 , or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R 7 is optionally substituted on a free carbon by one, two, or three substituents independently selected from R h , and each R h is independently selected from the group consisting of halogen and C 1-6 alkyl (optionally substituted by one, two or three halogens).

5. The compound of claim 4 , or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R 7 is substituted on a free carbon by one, two, or three substituents independently selected from R h , and each R h is independently selected from the group consisting of halogen, and C 1-6 alkyl (optionally substituted by one, two or three halogens).

6. The compound of claim 4 , or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R 7 is

and R 7 is substituted by one or two substituents independently selected from R h , and each R h is independently selected from the group consisting of halogen and C 1-6 alkyl (optionally substituted by one, two or three halogens).

7. The compound of claim 1 , or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R 7 is unsubstituted.

8. A pharmaceutically acceptable composition comprising a compound of any one of claims 1 , 2 , 3 , and 4 - 7 , or a pharmaceutically acceptable salt or stereoisomer thereof, and a pharmaceutically acceptable excipient.

9. A method of treating pain, comprising administering to a patient in need thereof an effective amount of a compound of any one of claims 1 , 2 , 3 , and 4 - 7 , or a pharmaceutically acceptable salt or stereoisomer thereof.

Assignments (8)
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: CISAR, JUSTIN S; GRICE, CHERYL A.; JONES, TODD K.
To: ABIDE THERAPEUTICS, INC.
Reel/Frame 039828/0190 →
CONFIRMATORY LICENSE Recorded Oct 29, 2015
From: SCRIPPS RESEARCH INSTITUTE
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 037007/0414 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 20, 2015
From: NIPHAKIS, MICAH J.; CHANG, JAE WON; LUM, KENNETH M.; CRAVATT, BENJAMIN F.
To: THE SCRIPPS RESEARCH INSTITUTE
Reel/Frame 034782/0105 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 15, 2014
From: CISAR, JUSTIN S.; GRICE, CHERYL A.; JONES, TODD K.
To: ABIDE THERAPEUTICS, INC.
Reel/Frame 034509/0889 →
Continuity (2)
Provisional Application 61631558 · Jan 6, 2012
Related Publication 20150018335A1 · Jan 15, 2015