IP Library › Granted Patent US 8,703,759

Granted Patent B2

US 8,703,759 · App. 13/174,587 · Granted Apr 22, 2014

Fused heterocyclic compounds as ion channel modulators

Inventors: Tetsuya Kobayashi (Sunnyvale, CA); Dmitry Koltun (Foster City, CA); Gregory Notte (San Mateo, CA); Eric Parkhill (San Francisco, CA); Jeff Zablocki (Los Altos, CA)

Assignee: Gilead Sciences, Inc.

View Patent ↗

Loading inventors, assignments & file history…

Monitor This Case

Get email alerts when status or documents change.

Order Certified Copies

Most orders are placed with the USPTO same day — all within 24 business hours.

Order via The Patent Place →

Pre-filled with this patent's details

Quick Facts

Patent No.: US 8,703,759
App. No.: 13/174,587
Granted: Apr 22, 2014
Kind: B2

External Links

USPTO Patent Center↗ Full Patent PDF↗

Abstract

The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein R 1 , R 2 , R 3 , R 4 , and R 5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

Claims (343)

1. A compound Formula I:

wherein:

R 1 is aryl, pyridinyl, pyridazinyl, pyrimidinyl, quinolonyl, indazolyl, triazolopyridinyl, imidazopyridinyl, thiadiazolyl, or triazolyl; wherein said aryl, pyridinyl, pyridazinyl, pyrimidinyl, quinolonyl, indazolyl, triazolopyridinyl, imidazopyridinyl, thiadiazolyl, or triazolyl are substituted with one, two, or three substituents independently selected from the group consisting of hydroxyl, halo, —NO 2 , CN, —SF 5 , —Si(CH 3 ) 3 , —O—CF 3 , —O—R 20 , —S—R 20 , —C(O)—R 20 , —N(R 20 )(R 22 ), —C(O)—N(R 20 )(R 22 ), —N(R 20 )—C(O)—R 22 , N(R 20 )—S(O) 2 —R 26 , —S(O) 2 —R 20 , —S(O) 2 —N(R 20 )(R 22 ), C 1-3 alkoxy, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl, and

wherein said C 1-3 alkoxy, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl are optionally substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , —O—CHF 2 , aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , C(O)—O—R 20 , —CN, and —O—R 20 ;

R 2 is hydrogen, C 1-15 alkyl, C 1-8 alkoxy, —C(O)—O—R 26 , —C(O)—N(R 26 )(R 28 ), —N(R 20 )—S(O) 2 —R 20 , cycloalkyl, aryl, heteroaryl, or heterocyclyl, wherein said C 1-15 alkyl is optionally substituted with one, two, or three substituents independently selected from hydroxyl, C 1-8 alkoxy, halo, —NO 2 , O—CF 3 , —O—CHF 2 , C 2-4 alkenyl, C 2-4 alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

wherein said C 1-8 alkoxy, C 2-4 alkenyl, C 2-4 alkynyl, aryl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

wherein said C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from deuterium, hydroxyl, halo, —NO 2 , —O—CF 3 , —CF 3 , —O—CHF 2 , —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 ;

R 3 is selected from the group consisting of hydrogen, hydroxyl, halo, C 1-4 alkyl, C 1-4 alkoxy, —R 25 —N(R 20 )(R 22 ), —R 25 —O—R 20 , R 25 —C(O)—O—R 20 , —R 25 —C(O)—N(R 20 )(R 22 ), —R 25 —C(O)—O—N(R 20 )(R 22 ), —R 25 —N(R 20 )—C(O)—R 22 , and —R 25 —O—C(O)—N(R 20 )(R 22 ), and

wherein said C 1-4 alkyl is optionally substituted with one, two, or three substituents independently selected from hydroxyl, and halo;

R 4 is selected from the group consisting of hydrogen, optionally substituted C 1-4 alkyl, aryl, —CF 3 , -halo, and —O—R 24 , and

wherein said aryl is optionally further substituted with one, two, or three substituents independently selected from hydroxyl, —NO 2 , —O—CF 3 , C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

wherein said C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , —CF 3 , —O—CHF 2 , —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 ;

R 5 is selected from the group consisting of hydrogen, optionally substituted alkyl, amino, optionally substituted alkoxy, —CF 3 , —O—CF 3 , —CN, and —N(R 20 )C(O)—R 22 ;

R 20 and R 22 are in each instance independently selected from the group consisting of hydrogen, acyl, C 1-15 alkyl, C 2-15 alkenyl, C 2-15 alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl, and

wherein said C 1-15 alkyl, C 2-15 alkenyl, C 2-15 alkynyl, cycloalkyl, heterocyclyl, aryl or heteroaryl are optionally substituted with one, two, or three substituents independently selected from hydroxyl, halo, C 1-4 alkyl, mono- or dialkylamino, aminocarbonyl, —NO 2 , —SO 2 R 26 , —CN, C 1-3 alkoxy, —CF 3 , —OCF 3 , aryl, cycloalkyl, and heteroaryl; or;

when R 20 and R 22 are attached to a common nitrogen atom R 20 and R 22 may join to form a heterocyclic ring which is then optionally substituted with one, two, or three substituents independently selected from hydroxyl, halo, alkyl, aralkyl, aryl, aryloxy, aralkyloxy, mono- or dialkylamino, aminocarbonyl, —NO 2 , —SO 2 R 26 , —CN, C 1-3 alkoxy, —CF 3 , —OCF 3 , and cycloalkyl;

R 25 is in each instance independently a bond or selected from C 1-6 alkylene optionally substituted with one or two C 1-3 alkyl groups; and

R 24 , R 26 , and R 28 are in each instance independently selected from hydrogen, alkyl, aryl, or cycloalkyl, wherein the alkyl, aryl and cycloalkyl may be further substituted with from 1 to 3 substituents independently selected from hydroxyl, halo, C 1-4 alkoxy, —CF 3 , and —OCF 3 ;

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

with the proviso that the compound is not 1-(3,4-difluorobenzyl)-2-oxo-N-(3-(3-oxo-2,3-dihydro-[1,2,4]triazolo[4,3-a]pyridin-6-yl)benzyl)-1,2-dihydropyridine-3-carboxamide.

2. The compound of claim 1 , wherein R 1 is pyridinyl, pyridazinyl, pyrimidinyl, quinolonyl, indazolyl, triazolopyridinyl, imidazopyridinyl, thiadiazolyl, or triazolyl,

wherein said pyridinyl, pyridazinyl, pyrimidinyl, quinolonyl, indazolyl, triazolopyridinyl, imidazopyridinyl, thiadiazolyl, or triazolyl is substituted with one, two, or three substituents independently selected from the group consisting of hydroxyl, halo, —NO 2 , CN, —SF 5 , —Si(CH 3 ) 3 , —O—CF 3 , —O—R 20 , —S—R 20 , —C(O)—R 20 , —N(R 20 )(R 22 ), —C(O)—N(R 20 )(R 22 ), —N(R 20 )—C(O)—R 22 , —N(R 20 )—S(O) 2 —R 26 , —S(O) 2 —R 20 , —S(O) 2 —N(R 20 )(R 22 ), C 1-3 alkoxy, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl, and

3. The compound of claim 1 , wherein R 1 is aryl,

wherein said aryl is substituted with one, two, or three substituents independently selected from the group consisting of hydroxyl, halo, —NO 2 , CN, —SF 5 , —Si(CH 3 ) 3 , —O—CF 3 , —O—R 20 , —S—R 20 , —C(O)—R 20 , —N(R 20 )(R 22 ), —C(O)—N(R 20 )(R 22 ), —N(R 20 )—C(O)—R 22 , —N(R 20 )—S(O) 2 —R 26 , —S(O) 2 —R 20 , —S(O) 2 —N(R 20 )(R 22 ), C 1-3 alkoxy, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl, and

4. The compound of claim 1 , wherein R 1 is phenyl,

wherein said phenyl is substituted with one, two, or three substituents independently selected from the group consisting of hydroxyl, halo, —NO 2 , CN, —SF 5 , —Si(CH 3 ) 3 , —O—CF 3 , —O—R 20 , —S—R 20 , —C(O)—R 20 , C(O)OH, —N(R 20 )(R 22 ), —C(O)—N(R 20 )(R 22 ), —N(R 20 )—C(O)—R 22 , —N(R 20 )—S(O) 2 —R 26 , —S(O) 2 —R 20 , —S(O) 2 —N(R 20 )(R 22 ), C 1-3 alkoxy, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl, and

wherein said C 1-3 alkoxy, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, aryl, heteroaryl, cycloalkyl, and heterocyclyl are optionally substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , —O—CHF 2 , phenyl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —CN, and —O—R 20 .

5. The compound of claim 1 , wherein R 2 is hydrogen, C 1-15 alkyl, C 1-8 alkoxy, —C(O)—O—R 26 , —C(O)—N(R 26 )(R 28 ), —N(R 2 )—S(O) 2 R 20 , cycloalkyl, or heterocyclyl,

wherein said C 1-15 alkyl is optionally substituted with one, two, or three substituents independently selected from hydroxyl, C 1-8 alkoxy, halo, —NO 2 , O—CF 3 , —O—CHF 2 , C 2-4 alkenyl, C 2-4 alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

wherein said C 1-8 alkoxy, C 2-4 alkenyl, C 2-4 alkynyl, heterocyclyl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

6. The compound of claim 5 , wherein R 2 is hydrogen, C 1-15 alkyl, C 1-8 alkoxy, —C(O)—O—R 26 , —C(O)—N(R 26 )(R 28 ), and —N(R 20 )—S(O) 2 —R 20 ,

wherein said C 1-8 alkoxy, C 2-4 alkenyl, C 2-4 alkynyl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

7. A compound of Formula II:

wherein:

X is selected from the group consisting of hydroxyl, halo, —NO 2 , CN, —SF 5 , —Si(CH 3 ) 3 , —O—CF 3 , —O—R 20 , —S—R 20 , —C(O)—R 20 , C(O)OH, —N(R 20 )(R 22 ), —C(O)—N(R 20 )(R 22 ), —N(R 20 )—C(O)—R 22 , —N(R 20 )—S(O) 2 —R 26 , —S(O) 2 —R 20 , —S(O) 2 —N(R 20 )(R 22 ), C 1-3 alkoxy, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl, and

wherein said C 1-3 alkoxy, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, aryl, heteroaryl, cycloalkyl, or heterocyclyl are optionally substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , —O—CHF 2 , aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —CN, and —O—R 20 ;

R′ and R″ are each independently selected from the group consisting of hydrogen, C 1-15 alkyl, C 1-4 alkoxy, hydroxyl, halo, —NO 2 , —O—CF 3 , cycloalkyl, aryl, heteroaryl, and heterocyclyl, and;

wherein said C 1-15 alkyl is optionally substituted with one, two, or three substituents independently selected from hydroxyl, C 1-3 alkoxy, halo, —NO 2 , —O—CF 3 , —O—CHF 2 , C 2-4 alkenyl, C 2-4 alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

wherein said C 1-3 alkoxy, C 2-4 alkenyl, C 2-4 alkynyl, cycloalkyl, aryl, heterocyclyl, or heteroaryl are optionally further substituted with one, two, or three substituents independently selected from deuterium, hydroxyl, halo, —NO 2 , —O—CF 3 , C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

wherein said C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , —CF 3 , —O—CHF 2 , N(R 20 )(R 22 ), C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 ;

R 2 is hydrogen, C 1-15 alkyl, C 1-8 alkoxy, —C(O)—O—R 26 , —C(O)—N(R 26 )(R 28 ), —N(R 20 )—S(O) 2 —R 20 , cycloalkyl, aryl, heteroaryl, or heterocyclyl,

wherein said C 1-8 alkoxy, C 2-4 alkenyl, C 2-4 alkynyl, aryl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

wherein said C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from deuterium, hydroxyl, halo, —NO 2 , —O—CF 3 , —CF 3 —O—CHF 2 , —N(R 20 )(R 22 ), C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 ;

R 3 is selected from the group consisting of hydrogen, hydroxyl, halo, C 1-4 alkyl, C 1-3 alkoxy, —R 25 —N(R 20 )(R 22 ), —R 25 —O—R 20 , —R 25 —C(O)—O—R 20 , R 25 —C(O)—N(R 20 )(R 22 ), —R 25 —C(O)—O—N(R 20 )(R 22 ), —R 25 —N(R 20 )—C(O)—R 22 , and —R 25 —O—C(O)—N(R 20 )(R 22 ), and

wherein said C 1-4 alkyl is optionally substituted with one, two, or three substituents independently selected from hydroxyl and halo;

R 4 is selected from the group consisting of hydrogen, optionally substituted alkyl, aryl, —CF 3 , -halo, and —O—R 24 , and

wherein said C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , —CF 3 , —O—CHF 2 , —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 ;

R 5 is selected from the group consisting of hydrogen, optionally substituted alkyl, amino, optionally substituted alkoxy, —CF 3 , —O—CF 3 , —CN, and —N(R 20 )C(O)—R 22 ;

wherein the C 1-15 alkyl, C 2-15 alkenyl, C 2-15 alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl are optionally substituted with one, two, or three substituents independently selected from hydroxyl, halo, C 1-4 alkyl, mono- or dialkylamino, aminocarbonyl, —NO 2 , —SO 2 R 26 , —CN, C 1-3 alkoxy, —CF 3 , OCF 3 , aryl, cycloalkyl, and heteroaryl; or;

when R 20 and R 22 are attached to a common nitrogen atom R 20 and R 22 may join to form a heterocyclic ring which is then optionally substituted with one, two, or three substituents independently selected from hydroxyl, halo, alkyl, aralkyl, phenyl, phenoxy, aralkyloxy, mono- or dialkylamino, aminocarbonyl, —NO 2 , —SO 2 R 26 , —CN, C 1-3 alkoxy, —CF 3 , —OCF 3 , aryl, and cycloalkyl;

R 25 is in each instance independently a bond or selected from C 1-6 alkylene optionally substituted with one or two C 1-3 alkyl groups; and

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

8. The compound of claim 7 , wherein X is C 1-3 alkoxy or C 1-4 alkyl, and

wherein said C 1-4 alkyl is optionally substituted with one, two, or three substituents independently selected from hydroxyl, alkoxy, halo, —NO 2 , —O—CHF 2 , aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —CN, and —O—R 20 , and

wherein said C 1-3 alkoxy is optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , C(O)—N(R 20 )(R 22 )—CN, and —O—R 20 .

9. The compound of claim 8 , wherein X is OCF 3 and each of R′ and R″ is hydrogen.

10. The compound of claim 8 , wherein X is CF 3 and each of R′ and R″ is hydrogen.

11. The compound of claim 1 ,

wherein R 2 is hydrogen or C 1-15 alkyl, and

wherein said C 1-15 alkyl is optionally substituted with one, two, or three substituents independently selected from hydroxyl, C 1-8 alkoxy, halo-NO 2 , O—CF 3 , —O—CHF 2 , C 2-4 alkenyl, C 2-4 alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

12. A compound of Formula III:

wherein:

X is selected from the group consisting of hydroxyl, halo, —NO 2 , CN, —SF 5 , —Si(CH 3 ) 3 , —O—CF 3 , —S—R 20 , —C(O)—R 20 , C(O)OH, —N(R 20 )(R 22 ), —C(O)—N(R 20 )(R 22 ), —N(R 20 )—C(O)—R 22 , —N(R 20 )—S(O) 2 —R 26 , —S(O) 2 —)R 20 , —S(O) 2 —N(R 20 )(R 22 ), C 1-3 alkoxy, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl, and

wherein said alkoxy, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, aryl, heteroaryl, cycloalkyl, or heterocyclyl are optionally substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , —O—CHF 2 , aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —CN, and —O—R 20 ;

wherein said C 1-15 alkyl is optionally substituted with one, two, or three substituents independently selected from hydroxyl, alkoxy, halo, —NO 2 , —O—CF 3 , —O—CHF 2 , alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 ), —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

wherein said alkoxy, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, or heteroaryl are optionally further substituted with one, two, or three substituents independently selected from deuterium, hydroxyl, halo, —NO 2 , —O—CF 3 , C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

L is selected from the group consisting of a bond and straight or branched C 1-6 alkylene,

wherein said straight or branched C 1-6 alkylene is optionally further substituted with one, two, or three substituents independently selected from hydroxyl, alkoxy, halo, —NO 2 , —O—CF 3 , —O—CHF 2 , C 2-4 alkenyl, C 2-4 alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

wherein said alkoxy, C 2-4 alkenyl, C 2-4 alkynyl, cycloalkyl, aryl, heterocyclyl, or heteroaryl are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 ; and

Q is selected from the group consisting of hydrogen, hydroxyl, C 1-4 alkoxy, halo, —NO 2 , —O—CF 3 , —O—CHF 2 , C 2-4 alkenyl, C 2-4 alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

wherein said C 1-4 alkoxy, C 2-4 alkenyl, C 2-4 alkynyl, aryl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from deuterium, hydroxyl, halo, —NO 2 , —O—CF 3 , C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 ; and

wherein said C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , —CF 3 , —O—CHF 2 , N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 ;

R 3 is selected from the group consisting of hydrogen, hydroxyl, halo, C 1-4 alkyl, C 1-3 alkoxy, —R 25 —N(R 20 )(R 22 ), —R 25 —O—R 20 , —R 25 —C(O)—O—R 20 , —R 25 —C(O)—N(R 20 )(R 22 ), —R 25 —C(O)—O—N(R 20 )(R 22 ), —R 25 —N(R 20 )—C(O)—R 22 , and —R 25 —O—C(O)—N(R 20 )(R 22 ), and

wherein said C 1-4 alkyl is optionally substituted with one, two, or three substituents independently selected from hydroxyl and halo;

R 4 is selected from the group consisting of hydrogen, optionally substituted alkyl, aryl, —CF 3 , -halo, and —O—R 24 , and

R 5 is selected from the group consisting of hydrogen, optionally substituted alkyl, amino, optionally substituted alkoxy, —CF 3 , —O—CF 3 , —CN, and —N(R 20 )C(O)—R 22 ;

wherein the C 1-15 alkyl, C 2-15 alkenyl, C 2-15 alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl are optionally substituted with one, two, or three substituents independently selected from hydroxyl, halo, C 1-4 alkyl, mono- or dialkylamino, aminocarbonyl, —NO 2 , —SO 2 R 26 , —CN, C 1-3 alkoxy, —CF 3 , OCF 3 , aryl, cycloalkyl, and heteroaryl; or

when R 20 and R 22 are attached to a common nitrogen atom R 20 and R 22 may join to form a heterocyclic ring which is then optionally substituted with one, two, or three substituents independently selected from hydroxyl, halo, alkyl, aralkyl, phenyl, phenoxy, aralkyloxy, mono- or dialkylamino, aminocarbonyl, —NO 2 , —SO 2 R 26 , —CN, C 1-3 alkoxy, —CF 3 , —OCF 3 , aryl, and cycloalkyl;

R 25 is in each instance independently a bond or selected from C 1-6 alkylene optionally substituted with one or two C 1-3 alkyl groups; and

R 24 and R 26 are in each instance independently selected from hydrogen, alkyl, aryl, or cycloalkyl, wherein the alkyl, aryl and cycloalkyl may be further substituted with from 1 to 3 substituents independently selected from hydroxyl, halo, C 1-4 alkoxy, —CF 3 , and —OCF 3 ;

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

13. The compound of claim 12 ,

wherein L is straight or branched C 1-6 alkylene,

wherein said C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , —CF 3 , —O—CHF 2 , N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 ;

Q is selected from the group consisting of hydrogen, hydroxyl, C 1-4 alkoxy, halo, —NO 2 , —O—CF 3 , —O—CHF 2 , C 2-4 alkenyl, C 2-4 alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl-N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

wherein said C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , —CF 3 , —O—CHF 2 , —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 .

14. The compound of claim 13 , wherein R 3 is hydrogen or C 1-3 alkoxy.

15. The compound of claim 14 , wherein R 3 is hydrogen.

16. The compound of claim 13 , wherein R 4 is hydrogen or phenyl substituted with OCF 3 .

17. The compound of claim 13 , wherein R 5 is hydrogen or alkyl.

18. The compound of claim 13 , wherein each of R′ and R″ is hydrogen.

19. A compound of Formula IV:

wherein:

X is selected from the group consisting of hydroxyl, halo, —NO 2 , CN, —SF 5 , —Si(CH 3 ) 3 , —O—CF 3 , —O—R 20 , —S—R 20 , —C(O)—R 20 , —C(O)OH, —N(R 20 )(R 22 ), —C(O)—N(R 20 )(R 22 ), —N(R 20 )—C(O)—R 22 , —N(R 20 )—S(O) 2 —R 26 , —S(O) 2 —R 20 , —S(O) 2 —N(R 20 )(R 22 ), C 1-3 alkoxy, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl, and

wherein said C 1-3 alkoxy, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, aryl, heteroaryl, cycloalkyl, or heterocyclyl are optionally substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , —O—CHF 2 , phenyl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —CN, and —O—R 20 ;

L is selected from the group consisting of a bond and straight or branched C 1-6 alkylene, and

wherein said straight or branched C 1-6 alkylene is optionally further substituted with one, two, or three substituents independently selected from hydroxyl, alkoxy, halo, —NO 2 , —O—CHF 2 , C 2-4 alkenyl, C 2-4 alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

wherein said alkoxy, C 2-4 alkenyl, C 2-4 alkynyl, aryl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 ; and

wherein said C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —CF 3 , —O—CHF 2 , —N(R 20 )(R 22 ), —C(O)—R 20 , C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 ;

Q is selected from the group consisting of hydrogen, hydroxyl, alkoxy, halo, —NO 2 , —O—CF 3 , —O—CHF 2 , C 2-4 alkenyl, C 2-4 alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

wherein said alkoxy, C 2-4 alkenyl, C 2-4 alkynyl, aryl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from deuterium, hydroxyl, halo, —NO 2 , —O—CF 3 , C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 ; and

wherein said C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , —CF 3 , —O—CHF 2 , N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 ;

R 26 is in each instance independently selected from hydrogen, alkyl, aryl, or cycloalkyl, wherein the alkyl, aryl and cycloalkyl may be further substituted with from 1 to 3 substituents independently selected from hydroxyl, halo, C 1-4 alkoxy, —CF 3 , and —OCF 3 ;

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

20. The compound of claim 19 , wherein X is OCF 3 .

21. The compound of claim 19 , wherein X is CF 3 .

22. The compound of any one of claim 20 or 21 , wherein L is straight or branched C 1-6 alkylene,

wherein said C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , —CF 3 , —O—CHF 2 , —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 ; and

Q is selected from the group consisting of hydrogen, C 2-4 alkenyl, C 2-4 alkynyl, aryl, heteroaryl, cycloalkyl, and —O—R 20 , and

wherein said C 2-4 alkenyl, C 2-4 alkynyl, aryl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

wherein said C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , —CF 3 , —O—CHF 2 , —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 .

23. The compound of claim 22 , wherein Q is aryl or heteroaryl, and

wherein said aryl or heteroaryl is optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 , and

wherein said C 1-6 alkyl, C 1-4 alkoxy, aralkyl, aryl, heterocyclyl, heteroaryl, or cycloalkyl are optionally further substituted with one, two, or three substituents independently selected from hydroxyl, halo, —NO 2 , —O—CF 3 , —CF 3 , —O—CHF 2 , —N(R 20 )(R 22 ), —C(O)—R 20 , —C(O)—O—R 20 , —C(O)—N(R 20 )(R 22 ), —CN, and —O—R 20 .

24. A compound selected from the group consisting of:

2-((3-methyl-1,2,4-oxadiazol-5-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((4-methyl-1,2,5-oxadiazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-methyl-1,2,4-oxadiazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-hydroxy-3-(2-methoxyphenoxy)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-methylisoxazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((3,5-dimethylisoxazol-4-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-(trifluoromethoxy)phenyl)-2-(5-(3-(trifluoromethyl)phenyl)-1,2,4-oxadiazol-3-yl)methyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(5-methyl-1,2,4-oxadiazol-3-yl)benzyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((3-(2,6-dichlorophenyl)-1,2,4-oxadiazol-5-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(benzo[c][1,2,5]oxadiazol-5-ylmethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-(2-methoxyphenyl)-1,2,4-oxadiazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(4-(trifluoromethoxy)benzyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(quinolin-2-ylmethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(1-(3-ethyl-1,2,4-oxadiazol-5-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((3-ethyl-1,2,4-oxadiazol-5-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(pyridin-2-ylmethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((4-phenyl-1,2,5-oxadiazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-methyl-1,3,4-oxadiazol-2-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(oxazol-2-ylmethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(benzo[d]thiazol-2-ylmethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-methyl-2-phenyloxazol-4-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((4,5-dimethyloxazol-2-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-methoxy-3-(2-methoxyphenoxy)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-phenoxypropyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-methyloxazol-2-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((3-cyclopropyl-1-methyl-1H-pyrazol-5-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((1,2,4-oxadiazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-phenoxyethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((3-benzyl-1,2,4-oxadiazol-5-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

5-methoxy-2-((3-methyl-1,2,4-oxadiazol-5-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-methyl-1,2,4-oxadiazol-3-yl)methyl)-6-(3-phenoxyphenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-(4-chlorophenoxy)phenyl)-2-((5-methyl-1,2,4-oxadiazol-3-yl)methyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((3-(2-chlorophenyl)-1,2,4-oxadiazol-5-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(pyridin-2-yl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(1H-pyrazol-1-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(pyridin-2-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(2-methoxyphenoxy)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(4-chlorophenoxy)-2-hydroxypropyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(3-phenoxypyrrolidin-1-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4-chlorophenoxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4-chloro-1H-pyrazol-1-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(3-methyl-1H-pyrazol-1-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-hydroxy-3-phenoxypropyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(2,6-dimethylphenoxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4-phenyl-1H-imidazol-1-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(2-chlorophenoxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-(trifluoromethoxy)phenyl)-2-(2-(3-(trifluoromethyl)pyridin-2-yloxy)ethyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(6-methylpyridin-2-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(pyridin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4,4-difluoropiperidin-1-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(2-fluorophenoxy)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(2-chlorophenoxy)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-(4-chlorophenoxy)phenyl)-2-((3-methyl-1,2,4-oxadiazol-5-yl)methyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(3-chlorophenoxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4-fluorophenoxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(3-bromopyridin-2-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4-cyclopropylpyridin-2-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4-methylpyridin-2-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(4-fluorophenethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(3-cyclopropylpyridin-2-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(3-methylpyridin-2-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-(trifluoromethoxy)phenyl)-2-(6-(trifluoromethyl)pyridin-2-yl)methyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2,6-difluorophenethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(3-bromo-4-fluorophenyl)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-(trifluoromethoxy)phenyl)-2-(2-(6-(trifluoromethyl)pyridin-2-yloxy)ethyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-(trifluoromethoxy)phenyl)-2-(3-(2-(trifluoromethyl)phenoxy)propyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(4-fluoro-2-methoxyphenoxy)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(4-chloropyridin-3-yl)prop-2-ynyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(2-methoxyphenoxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(3-oxo-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propoxy)benzonitrile;

6-(4-(trifluoromethoxy)phenyl)-2-(3-(2-(trifluoromethyl)phenoxy)propyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

(R)-2-(3-methoxy-2-(3-(trifluoromethyl)pyridin-2-yloxy)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(pyridin-3-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(3,3′-bipyridin-6-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(p-tolyloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(4-fluorophenyl)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(chroman-2-ylmethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2,4-difluorophenethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(pyridazin-3-yloxy)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(2-chlorophenoxy)-2-methoxypropyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(pyridazin-3-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(5-methylpyrimidin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((3-methyl-1,2,4-oxadiazol-5-yl)methyl)-6-(4-(2,2,2-trifluoroethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(2-(3-methyl-1,2,4-oxadiazol-5-yl)phenoxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(pyrazin-2-yloxy)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-((5-methyl-1,2,4-oxadiazol-3-yl)methoxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((3-methyl-1,2,4-oxadiazol-5-yl)methyl)-6-(2-methyl-4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4,6-dimethylpyrimidin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(2-chlorophenoxy)-2-(pyrimidin-2-yloxy)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4-cyclopropylpyrimidin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

(S)-2-(3-methoxy-2-(3-(trifluoromethyl)pyridin-2-yloxy)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(5-chloropyrimidin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-(4-fluorophenoxy)phenyl)-2-((3-methyl-1,2,4-oxadiazol-5-yl)methyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

(3-((3-oxo-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)methyl)-1,2,4-oxadiazol-5-yl)methyl acetate;

(S)-2-(3-(2-chlorophenoxy)-2-methoxypropyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

(R)-2-(3-(2-chlorophenoxy)-2-methoxypropyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(1-methyl-1H-benzo[d]imidazol-2-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(4-fluoro-2-methoxyphenoxy)-2-hydroxypropyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(2-ethoxyphenoxy)-2-hydroxypropyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(biphenyl-2-yloxy)-2-hydroxypropyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-hydroxy-3-(3-oxo-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propoxy)benzonitrile;

2-(2-(pyridin-2-yl)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(6-methoxypyridin-2-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(4-fluoro-2-methoxyphenoxy)-2-methoxypropyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-ethoxy-3-(4-fluoro-2-methoxyphenoxy)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4-ethoxypyrimidin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-hydroxy-3-(2-methylbenzo[d]thiazol-6-yloxy)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-hydroxy-3-(2-isopropoxyphenoxy)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(4-(pyrimidin-2-yloxy)tetrahydrofuran-3-yl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((3-methyl-1,2,4-oxadiazol-5-yl)methyl)-6-(4-(trimethylsilyl)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(pyrimidin-2-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(2-oxo-3-phenoxypyrrolidin-1-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(pyrimidin-4-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(pyrazin-2-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4-phenylpyrimidin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(5-methoxypyrimidin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(3-methylpyrazin-2-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(3-bromo-6-methoxypyridin-2-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(4-fluoro-3-(oxazol-2-yl)phenyl)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-(4-chlorophenoxy)phenyl)-2-(2-(pyrimidin-2-yloxy)ethyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(4-fluoro-3-(pyridin-3-yl)phenyl)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-(4-fluorophenoxy)phenyl)-2-(2-(pyrimidin-2-yloxy)ethyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(pyrimidin-2-yloxy)ethyl)-6-(4-(trimethylsilyl)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-ethoxy-3-(2-methylbenzo[d]thiazol-6-yloxy)propyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(4-(4-ethoxypyrimidin-2-yloxy)tetrahydrofuran-3-yl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4-(dimethylamino)-5-fluoropyrimidin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(3,5-difluoro-4-phenoxyphenyl)-2-((3-methyl-1,2,4-oxadiazol-5-yl)methyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-(methoxymethyl)-1,2,4-oxadiazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(3-oxo-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)ethyloxo-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)ethoxy)pyrimidine-4-carbonitrile;

2-(2-(5-chloro-4-methoxypyrimidin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-benzoylphenyl)-2-((3-methyl-1,2,4-oxadiazol-5-yl)methyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4-(4-chlorophenoxy)pyrimidin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4-(3,3-difluoroazetidin-1-yl)-5-fluoropyrimidin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(3,4-dichlorophenyl)-2-((3-methyl-1,2,4-oxadiazol-5-yl)methyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(pyrrolo[1,2-a]pyrazin-1-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((3-((3-oxo-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)methyl)-1,2,4-oxadiazol-5-yl)methyl)isoindoline-1,3-dione;

2-((3-methyl-1,2,4-oxadiazol-5-yl)methyl)-6-(4-(trifluoromethyl)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(5-fluoropyrimidin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(2-chloropyrimidin-5-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-(4-fluorophenoxy)phenyl)-2-((5-methyl-1,2,4-oxadiazol-3-yl)methyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(isoquinolin-1-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-cyclopropyl-1,2,4-oxadiazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-(4-fluorophenoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-(pyridin-2-yl)isoxazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-(3-methylpyridin-2-yl)isoxazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-(4-fluorophenoxy)phenyl)-2-((5-(hydroxymethyl)-1,2,4-oxadiazol-3-yl)methyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(1-(3-methyl-1,2,4-oxadiazol-5-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-methyl-1,2,4-oxadiazol-3-yl)methyl)-6-(4-(trifluoromethyl)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-chlorophenyl)-2-(3-methyl-1,2,4-oxadiazol-5-yl)methyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(3,4-difluorophenyl)-2-((3-methyl-1,2,4-oxadiazol-5-yl)methyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-cinnamyl-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

(S)-2-((5-(2,2-dimethyl-1,3-dioxolan-4-yl)-1,2,4-oxadiazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((3-(methoxymethyl)-1,2,4-oxadiazol-5-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-(difluoromethyl)-1,2,4-oxadiazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(3-fluoro-4-(trifluoromethoxy)phenyl)-2-((3-methyl-1,2,4-oxadiazol-5-yl)methyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4-(2-hydroxyethoxy)pyrimidin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-(chloromethyl)-1,2,4-oxadiazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

(R)-2-((5-(2,2-dimethyl-1,3-dioxolan-4-yl)-1,2,4-oxadiazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4-(methylthio)pyrimidin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(2-(3-oxo-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)ethyloxo-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)ethoxy)pyrimidin-4-yloxy)acetonitrile;

6-(4-chloro-3-fluorophenyl)-2-((3-methyl-1,2,4-oxadiazol-5-yl)methyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-((pyrimidin-2-yloxy)methyl)-1,2,4-oxadiazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((1-methyl-1H-pyrazol-4-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((3-methylisoxazol-5-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((1-methyl-1H-pyrazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((3-ethyl-1,2,4-oxadiazol-5-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((3-ethyl-1,2,4-oxadiazol-5-yl)methyl)-6-(4-(trifluoromethyl)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((3-(methoxymethyl)-1,2,4-oxadiazol-5-yl)methyl)-6-(4-(trifluoromethyl)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((3-trideuteromethyl-1,2,4-oxadiazol-5-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-cyclopropyl-1,3,4-thiadiazol-2-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-(trifluoromethyl)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

24(5-methyloxazol-2-yl)methyl)-6-(4-(trifluoromethyl)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((4,5-dimethyloxazol-2-yl)methyl)-6-(4-(trifluoromethyl)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(imidazo[1,2-a]pyrazin-8-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-((pyridin-2-yloxy)methyl)-1,2,4-oxadiazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-((2-ethoxyphenoxy)methyl)-1,2,4-oxadiazol-3-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4-isopropoxypyrimidin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4-(2,2,2-trifluoroethoxy)pyrimidin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2-(4-(cyclopropylmethoxy)pyrimidin-2-yloxy)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-(trifluoromethoxy)phenyl)-2-(2-(5-(trifluoromethyl)pyrimidin-2-yloxy)ethyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((2-cyclopropyloxazol-4-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-cyclopropyl-1,3,4-oxadiazol-2-yl)methyl)-6-(4-(4-fluorophenoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

24(5-tert-butyloxazol-2-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

24(5-tert-butyloxazol-2-yl)methyl)-6-(4-(trifluoromethyl)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-methyl-6-(4-(trifluoromethyl)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

(R)-2-(2-(3-(4-fluorophenoxy)pyrrolidin-1-yl)ethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

5-methyl-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

5-methyl-24(3-methyl-1,2,4-oxadiazol-5-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(2,2,2-trifluoroethyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-isopropyl-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((4-methyloxazol-2-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((4-methyloxazol-2-yl)methyl)-6-(4-(trifluoromethyl)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((4-cyclopropyloxazol-2-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((4-cyclopropyloxazol-2-yl)methyl)-6-(4-(trifluoromethyl)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-chlorophenyl)-2-((5-methyloxazol-2-yl)methyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

8-methyl-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((2-methyloxazol-5-yl)methyl)-6-(4-(trifluoromethyl)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-(3-(4,5-dichloro-2-methoxyphenoxy)-2-hydroxypropyl)-6-(4-(trifluoromethyl)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

2-((5-cyclopropyloxazol-2-yl)methyl)-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one;

6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one; and

2-methyl-6-(4-(trifluoromethoxy)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one,

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

25. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a therapeutically effective amount of the compound of claim 1 or a pharmaceutically acceptable salt, ester, or stereoisomer, thereof.

Assignments (1)

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 26, 2011

From: KOBAYASHI, TETSUYA; KOLTUN, DMITRY; NOTTE, GREGORY; PARKHILL, ERIC; ZABLOCKI, JEFF

To: GILEAD SCIENCES, INC.

Reel/Frame 026969/0740 →

Continuity (2)

Provisional Application 61361056 · Jul 2, 2010

Related Publication 20120010192A1 · Jan 12, 2012