IP Library Granted Patent US 11,161,856
Granted Patent B2
US 11,161,856 · App. 16/642,713 · Granted Nov 2, 2021

Spirocycle compounds and methods of making and using same

Inventors: Cheryl A. Grice (Encinitas, CA); Olivia D. Weber (San Diego, CA); Daniel J. Buzard (San Diego, CA); Michael B. Shaghafi (San Diego, CA)
Assignee: H. LUNDBECK A/S
C07D519/00C07D211/58C07D401/12C07D471/10
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Quick Facts
Patent No.
US 11,161,856
App. No.
16/642,713
Granted
Nov 2, 2021
Kind
B2
Abstract

Provided herein are compounds of the formula: and compositions comprising the same, which are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

Claims (31)

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

wherein:

Y is —CH 2 —;

R 1 is H or C 1-6 alkyl;

R 2 is H or C 1-6 alkyl;

each R 3 is independently selected from C 1-6 alkyl, halogen, —CN, C 1-6 haloalkyl, —SF 5 , and —OR 7 ;

R 4 is selected from

each R 7 is independently selected from H, C 1-6 alkyl, C 1-6 haloalkyl, C 3-8 cycloalkyl, and -C 1-6 alkyl-C 3-8 cycloalkyl;

a, b, c, and d are independently 0 or 1;

e is 0, 1, or 2;

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

n is 0 or 1;

m is 0 or 1;

p is 0, 1, or 2; and

q is 0, 1, or 2; provided that when q is 0, then p is 2;

or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or pharmaceutically acceptable salt thereof, wherein R 4 is

3. The compound of claim 1 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or pharmaceutically acceptable salt thereof, wherein R 4 is

4. The compound of claim 1 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or pharmaceutically acceptable salt thereof, wherein R 1 is H.

5. The compound of claim 1 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or pharmaceutically acceptable salt thereof, wherein R 2 is H.

6. The compound of claim 1 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or pharmaceutically acceptable salt thereof, wherein R 1 and R 2 are both H.

7. The compound of claim 1 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or pharmaceutically acceptable salt thereof, wherein each R 3 is independently selected from halogen and C 1-6 haloalkyl.

8. The compound of claim 1 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or pharmaceutically acceptable salt thereof, wherein each R 3 is independently selected from C 1-6 haloalkyl.

9. The compound of claim 1 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or pharmaceutically acceptable salt thereof, wherein each R 3 is —CF 3 .

10. The compound of claim 1 , wherein w is 1.

11. The compound of claim 1 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or pharmaceutically acceptable salt thereof, wherein m is 1, n is 1, q is 1, and p is 1.

12. The compound of claim 1 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or pharmaceutically acceptable salt thereof, wherein m is 1, n is 1, q is 0, and p is 2.

13. The compound of claim 1 selected from:

or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or a pharmaceutically acceptable salt thereof.

14. A pharmaceutical composition comprising a compound of claim 1 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

15. A method of treating pain in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a compound of claim 1 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or a pharmaceutically acceptable salt thereof.

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 →
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 Jan 7, 2021
From: GRICE, CHERYL A.; WEBER, OLIVIA D.; BUZARD, DANIEL J.; SHAGHAFI, MICHAEL B.
To: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
Reel/Frame 054846/0368 →
Continuity (2)
Provisional Application 62551714 · Aug 29, 2017
Related Publication 20210214375A1 · Jul 15, 2021