IP Library Granted Patent US 11,059,822
Granted Patent B2
US 11,059,822 · App. 16/349,047 · Granted Jul 13, 2021

MAGL inhibitors

Inventors: Cheryl A. Grice (Encinitas, CA); Daniel J. Buzard (San Diego, CA); Michael B. Shaghafi (San Diego, CA)
Assignee: H. LUNDBECK A/S
C07D471/10
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Quick Facts
Patent No.
US 11,059,822
App. No.
16/349,047
Granted
Jul 13, 2021
Kind
B2
Abstract

Provided herein are spirocyclic and fused bicyclic carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

Claims (44)

1. A compound having the structure of Formula (I):

wherein:

X is —O—, —S—, —SO 2 —, —N(R 3 )—, or —CH 2 —;

Y is —O— or —N(R 7 )—;

R 1 is —(CR 4 R 5 ) m —R 6 , —(CR 4 R 5 ) p —Y—(CR 4 R 5 ) q —R 6 , or —(CR 4 R 5 ) t —C 3-6 cycloalkyl—R 6 ;

each R 2 is independently selected from halogen, —CN, C 1-6 alkyl, C 1-6 haloalkyl, —C 1-6 alkyl(heterocycloalkyl), —OR 17 , and —C(O)NR 18 R 19 ;

R 3 is H or C 1-6 alkyl;

each R 4 and R 5 is each independently selected from H, F, and C 1-6 alkyl; or R 4 and R 5 , together with the carbon to which they are attached, form a C 3-6 cycloalkyl ring;

R 6 is —CO 2 R 9 , —C(O)R 10 , or —C(O)O—(CR 12 R 13 )—OC(O)R 11 ;

R 7 is H, C 1-6 alkyl, or —SO 2 R 8 ;

R 8 is C 1-6 alkyl;

R 9 is H or C 1-6 alkyl;

R 10 is C 1-6 alkyl or —NHSO 2 R 21 ;

R 11 is C 1-6 alkyl or C 1-6 alkoxy;

R 12 and R 13 is each independently H or C 1-6 alkyl;

each R 17 is independently selected from H, C 1-6 alkyl, C 1-6 haloalkyl, aminoalkyl, cycloalkyl, —C 1-6 alkyl(heterocycloalkyl), —C 1-6 alkyl—C(O)(heterocycloalkyl), optionally substituted heterocycloalkyl, optionally substituted aryl, and optionally substituted heteroaryl;

each R 18 and R 19 is independently selected from H, C 1-6 alkyl, C 1-6 haloalkyl, cycloalkyl, aryl, and heteroaryl; or R 18 and R 19 , together with the nitrogen to which they are attached, form a heterocycloalkyl ring optionally substituted with one, two, or three R 20 ;

each R 20 is independently selected from halogen, C 1-6 alkyl, C 1-6 haloalkyl, oxo, —CN, and C 3-6 cycloalkyl;

R 21 is C 1-6 alkyl;

m is 1, 2, 3 or 4;

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

p is 2, 3, or 4;

q is 1, 2, or 3; and

t is 0, 1, or 2;

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 1 is —(CR 4 R 5 ) m —R 6 .

3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein m is 1, 2, or 3.

4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein each R 4 and R 5 is H.

5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 6 is —CO 2 R 9 .

6. The compound of claim 5 , or a pharmaceutically acceptable salt thereof, wherein R 9 is H.

7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein X is —O—.

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

9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein each R 2 is independently selected from halogen, C 1-6 alkyl, and C 1-6 haloalkyl.

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

11. The compound of claim 10 , or a pharmaceutically acceptable salt thereof, wherein R 2 is —CF 3 .

12. The compound of claim 1 selected from:

or a pharmaceutically acceptable salt thereof.

13. The compound of claim 1 selected from:

or a pharmaceutically acceptable salt thereof.

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

15. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, selected from 2-(2-((8-(((1,1,1,3,3,3-hexafluoropropan-2-yl)oxy)carbonyl)-1,8-diazaspiro[4.5]decan-1-yl)methyl)-5-(trifluoromethyl)phenoxy)acetic acid.

16. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, selected from 4-(2-((8-(((1,1,1,3,3,3-hexafluoropropan-2-yl)oxy)carbonyl)-1,8-diazaspiro[4.5]decan-1-yl)methyl)-5-(trifluoromethyl)phenoxy)butanoic acid.

17. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, selected from 1-(2-((8-(((1,1,1,3,3,3-hexafluoropropan-2-yl)oxy)carbonyl)-1,8-diazaspiro[4.5]decan-1-yl)methyl)-5-(trifluoromethyl)phenoxy)cyclopropane-1-carboxylic acid.

18. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, selected from 1-((2-((8-(((1,1,1,3,3,3-hexafluoropropan-2-yl)oxy)carbonyl)-1,8-diazaspiro[4.5]decan-1-yl)methyl)-5-(trifluoromethyl)phenoxy)methyl)cyclopropane-1-carboxylic acid.

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 Feb 5, 2020
From: GRICE, CHERYL A.; BUZARD, DANIEL J.; SHAGHAFI, MICHAEL B.
To: ABIDE THERAPEUTICS, INC.
Reel/Frame 051732/0203 →
CHANGE OF NAME Recorded Jan 9, 2020
From: ABIDE THERAPEUTICS, INC.
To: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
Reel/Frame 051471/0554 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 6, 2020
From: GRICE, CHERYL A.; BUZARD, DANIEL J.; SHAGHAFI, MICHAEL B.
To: ABIDE THERAPEUTICS, INC.
Reel/Frame 051429/0118 →
Continuity (2)
Provisional Application 62423102 · Nov 16, 2016
Related Publication 20200291023A1 · Sep 17, 2020
Cited By (2)
US 12,286,421 US 12,378,219