IP Library Granted Patent US 11,142,526
Granted Patent B2
US 11,142,526 · App. 16/642,717 · Granted Oct 12, 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); Todd K. Jones (San Diego, CA)
Assignee: H. LUNDBECK A/S
C07D471/10A61P1/00A61P25/02A61P25/06A61P25/08C07D401/12C07D409/12C07D487/04C07D519/00
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Quick Facts
Patent No.
US 11,142,526
App. No.
16/642,717
Granted
Oct 12, 2021
Kind
B2
Abstract

Provided herein are compounds and compositions useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

Claims (30)

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

wherein:

Y is —CH 2 — or —C(O)—;

Z is C 3-6 cycloalkyl;

R 3 is a 5- to 6-membered heteroaryl ring or a 9- to 10-membered bicyclic heteroaryl ring; wherein the 5- to 6-membered heteroaryl ring and the 9- to 10-membered bicyclic heteroaryl ring are optionally substituted with one, two, or three R 4 ;

each R 4 is independently selected from C 1-6 alkyl, halogen, —CN, C 1-6 haloalkyl, C 3-8 cycloalkyl, C 2-9 heterocycloalkyl, —C 1-6 alkyl-(C 2-9 heterocycloalkyl), phenyl, —CH 2 -phenyl, C 1-9 heteroaryl, —OR 7 , —CO 2 R 6 , and —CH 2 CO 2 R 6 ; wherein C 2-9 heterocycloalkyl, —C 1-6 alkyl(C 2-9 heterocycloalkyl), phenyl, and C 1-9 heteroaryl are optionally substituted with one or two R 5 ; or two adjacent R 4 form a 6-membered cycloalkyl or 6-membered heterocycloalkyl ring, wherein the cycloalkyl and heterocycloalkyl ring are optionally substituted with one or two R 5 ;

each R 5 is independently selected from halogen, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 heteroalkyl, C 1-6 alkoxy, C 3-8 cycloalkyl, —C 1-6 alkyl(C 3-8 cycloalkyl), C 2-9 heterocycloalkyl, —CO 2 R 6 , —CH 2 CO 2 R 6 , and —C 1-6 alkyl(C 2-9 heterocycloalkyl) optionally substituted with C 1-6 alkyl;

each R 6 is independently selected from H and C 1-6 alkyl;

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

R 11 is H, C 1-6 alkyl, or —C 1-6 alkyl-O—C 1-6 alkyl;

R 12 is C 1-6 alkyl;

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

v is 0 or 1;

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 13 is H.

3. The compound of claim 1 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or pharmaceutically acceptable salt thereof, wherein v is 0.

4. The compound of claim 1 , wherein Y is —C(O)—.

5. The compound of claim 1 , wherein R 11 is C 1-6 alkyl.

6. The compound of claim 1 , wherein R 12 is —CH 3 .

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

8. The compound of claim 1 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or pharmaceutically acceptable salt thereof, wherein R 3 is a 9- to 10-membered bicyclic heteroaryl ring optionally substituted with one, two, or three R 4 .

9. The compound of claim 8 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or pharmaceutically acceptable salt thereof, wherein R 3 is a 9-membered bicyclic heteroaryl ring substituted with one, two, or three R 4 .

10. The compound of claim 8 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or pharmaceutically acceptable salt thereof, wherein R 3 is a 9-membered bicyclic heteroaryl ring substituted with one or two R 4 , wherein each R 4 is independently selected from halogen, C 1-6 alkyl, and C 1-6 haloalkyl.

11. The compound of claim 8 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or pharmaceutically acceptable salt thereof, wherein R 3 is an unsubstituted 9-membered bicyclic heteroaryl ring.

12. The compound of claim 8 , or a solvate, hydrate, tautomer, N-oxide, stereoisomer, or pharmaceutically acceptable salt thereof, wherein R 3 is selected from:

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.

16. A method of treating a disease or disorder in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof, wherein the disease or disorder is selected from migraine, epilepsy/seizure disorder, neuromyelitis optica (NMO), Tourette syndrome, persistent motor tic disorder, persistent vocal tic disorder, and abdominal pain associated with irritable bowel syndrome.

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.; JONES, TODD K.
To: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
Reel/Frame 054846/0484 →
Continuity (2)
Provisional Application 62551721 · Aug 29, 2017
Related Publication 20200255427A1 · Aug 13, 2020