IP Library Granted Patent US 9,718,789
Granted Patent B2
US 9,718,789 · App. 15/010,925 · Granted Aug 1, 2017

Substituted triazoles and methods relating thereto

Inventors: Neil J. Ashweek (San Diego, CA); John P. Williams (San Diego, CA); Deborah Slee (Cardiff, CA); Manisha Moorjani (San Diego, CA)
Assignee: Neurocrine Biosciences, Inc.
C07D249/04C07D401/12C07D403/04C07D405/04C07D413/04
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Quick Facts
Patent No.
US 9,718,789
App. No.
15/010,925
Granted
Aug 1, 2017
Kind
B2
Abstract

Substituted 1,2,3-triazole compounds are disclosed which have utility in the treatment of a variety of neurological disorders. The compounds provided herein have the general structure: wherein R 1 , R 2 , R 3 and n are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound provided herein in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for treating neurological disorders in a subject in need thereof.

Claims (23)

1. A compound having the following structure (A):

or a stereoisomer, ester, solvate, or pharmaceutically acceptable salt thereof,

wherein:

R 1 and R 2 taken together with the N to which they are attached, form a 5-6 member nonaromatic heterocycle wherein the 5-6 member nonaromatic heterocycle may be substituted with 0-3 R 4 ;

R 3 at each occurrence is Cl, F, C 1-4 alkyl, —OC 1-4 alkyl or trifluoromethyl;

R 4 at each occurrence is C 1-4 alkyl; and

n is 0-3.

2. The compound of claim 1 , wherein n is 1.

3. The compound of claim 1 , wherein n is 2.

4. The compound of claim 1 , wherein R 3 is Cl, F, or trifluoromethyl.

5. The compound of claim 1 , wherein R 3 is C 1-4 alkyl or —OC 1-4 alkyl.

6. The compound of claim 1 , wherein n=1 or 2 and R 3 is F.

7. The compound of claim 1 , wherein n is 1 and R 3 is F.

8. The compound of claim 1 , wherein R 4 is absent.

9. The compound of claim 1 , wherein n is 2 and each occurrence of R 3 is F.

10. The compound of claim 1 , wherein R 3 is C 1-4 alkyl, —OC 1-4 alkyl, trifluoromethyl, or Cl.

11. The compound of claim 1 , wherein the heterocycle formed by R 1 and R 2 taken together is piperidine.

12. The compound of claim 1 , wherein the heterocycle formed by R 1 and R 2 taken together is morpholine.

13. The compound of claim 1 , wherein the heterocycle formed by R 1 and R 2 taken together is piperazine, oxazolidine, or pyrrolidine.

14. The compound of claim 1 , wherein R 4 is methyl or ethyl.

15. The compound of claim 1 , wherein the compound is 4-{1-[(2,6-difluorophenyl)methyl]-1H-1,2,3-triazol-4-yl}morpholine.

16. The compound of claim 1 , wherein the compound is 1-[(2,6-difluorophenyl)methyl]-4-(pyrrolidin-1-yl)-1H-1,2,3-triazole.

17. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent.

Assignments (2)
CONFIRMATORY GRANT OF SECURITY INTEREST IN UNITED STATES PATENTS Recorded May 26, 2026
From: NEUROCRINE BIOSCIENCES, INC.
To: JPMORGAN CHASE BANK, N.A.
Reel/Frame 075670/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 2, 2017
From: ASHWEEK, NEIL J.; WILLIAMS, JOHN P.; SLEE, DEBORAH; MOORJANI, MANISHA
To: NEUROCRINE BIOSCIENCES, INC.
Reel/Frame 042209/0852 →
Continuity (3)
Provisional Application 62110415 · Jan 30, 2015
Provisional Application 62259314 · Nov 24, 2015
Related Publication 20160221968A1 · Aug 4, 2016