IP Library Granted Patent US 10,093,630
Granted Patent B2
US 10,093,630 · App. 15/312,998 · Granted Oct 9, 2018

Pyrazole compounds and methods of making and using same

Inventors: Dale L. Boger (La Jolla, CA); Katerina Otrubova (San Diego, CA); Justin S. Cisar (San Diego, CA); Cheryl A. Grice (Encinitas, CA); Todd K. Jones (Solana Beach, CA)
Assignees: ABIDE THERAPEUTICS, INC.; THE SCRIPPS RESEARCH INSTITUTE
C07D231/14C07D401/12C07D403/12C07D405/12C07D417/12C07D491/107
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Quick Facts
Patent No.
US 10,093,630
App. No.
15/312,998
Granted
Oct 9, 2018
Kind
B2
Abstract

Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of one or more of MAGL, ABHD6, and FAAH. Furthermore, the subject compounds and compositions are useful for the treatment of, for example, pain, solid tumors and/or obesity.

Claims (23)

1. A compound of Formula (I):

wherein:

R 1 is optionally substituted phenyl;

R 2 is phenyl optionally substituted with one or more groups independently selected from alkyl, —O— alkyl, alkenyl, alkynyl, halo, fluoroalkyl, cyano, nitro, aryl, —O-aryl, aralkyl, —O-aralkyl, carbocyclyl, heterocyclyl, heterocyclylalkyl, and heteroaryl;

R 3 is H; and

R 4 is phenyl optionally substituted with one or more groups independently selected from alkyl, halo, and fluoroalkyl;

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

2. The compound of claim 1 , or a solvate, hydrate, tautomer, N-oxide, or pharmaceutically acceptable salt thereof, wherein R 4 is phenyl substituted with one or more groups independently selected from alkyl, halo, and fluoroalkyl.

3. The compound of claim 2 , or a solvate, hydrate, tautomer, N-oxide, or pharmaceutically acceptable salt thereof, wherein R 4 is phenyl substituted with one group selected from alkyl, halo, and fluoroalkyl.

4. The compound of claim 1 , or a solvate, hydrate, tautomer, N-oxide, or pharmaceutically acceptable salt thereof, wherein R 4 is phenyl substituted with one halo.

5. The compound of claim 2 , or a solvate, hydrate, tautomer, N-oxide, or pharmaceutically acceptable salt thereof, wherein R 2 is phenyl optionally substituted with one or two groups independently selected from alkyl, —O-alkyl, halo, fluoroalkyl, aryl, —O-aryl, aralkyl, —O— aralkyl, heterocyclyl, and heterocyclylalkyl.

6. The compound of claim 5 , or a solvate, hydrate, tautomer, N-oxide, or pharmaceutically acceptable salt thereof, wherein R 2 is phenyl substituted with one or two groups independently selected from alkyl, halo, and fluoroalkyl.

7. The compound of claim 6 , or a solvate, hydrate, tautomer, N-oxide, or pharmaceutically acceptable salt thereof, wherein R 2 is phenyl substituted with one halo.

8. The compound of claim 6 , or a solvate, hydrate, tautomer, N-oxide, or pharmaceutically acceptable salt thereof, wherein R 1 is phenyl optionally substituted with one or more groups independently selected from alkyl, halo, and fluoroalkyl.

9. The compound of claim 6 , or a solvate, hydrate, tautomer, N-oxide, or pharmaceutically acceptable salt thereof, wherein R 1 is phenyl substituted with one or more groups independently selected from alkyl, halo, and fluoroalkyl.

10. The compound of claim 6 , or a solvate, hydrate, tautomer, N-oxide, or pharmaceutically acceptable salt thereof, wherein R 1 is phenyl substituted with one or two groups independently selected from alkyl, halo, and fluoroalkyl.

11. The compound of claim 6 , or a solvate, hydrate, tautomer, N-oxide, or pharmaceutically acceptable salt thereof, wherein R 1 is phenyl substituted with one group selected from alkyl, halo, and fluoroalkyl.

12. The compound of claim 6 , or a solvate, hydrate, tautomer, N-oxide, or pharmaceutically acceptable salt thereof, wherein R 1 is unsubstituted phenyl.

13. The compound of claim 1 selected from:

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

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

15. A method of therapeutically treating a disorder selected from the group consisting of a solid tumor cancer, obesity, Down's syndrome, Alzheimer's disease, and inflammation, in a patient in need thereof, comprising administering a therapeutically effective amount of a compound of claim 1 , or a solvate, hydrate, tautomer, N-oxide, or a pharmaceutically acceptable salt thereof, to the patient.

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

Assignments (5)
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 5, 2017
From: CISAR, JUSTIN S.; GRICE, CHERYL A.; JONES, TODD K.
To: ABIDE THERAPEUTICS, INC.
Reel/Frame 041866/0511 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 5, 2017
From: BOGER, DALE L.; OTRUBOVA, KATERINA
To: THE SCRIPPS RESEARCH INSTITUTE
Reel/Frame 041866/0531 →
Continuity (2)
Provisional Application 62001491 · May 21, 2014
Related Publication 20170190669A1 · Jul 6, 2017
Cited By (1)
US 12,258,340