# US 7,612,060 B2 · Triazoles and methods of use

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- Number: US 7,612,060 B2
- Document ID: US7612060B2
- Status: Granted
- Kind: B2
- Application number: 11/247,046
- Filed: 2005-10-11
- Published: 2006-05-11
- Granted: 2009-11-03
- Earliest claimed: 2004-10-13
- Assignees: Amgen Inc.
- Inventors: Toshihiro Aya; Guolin Cai; Jian J. Chen; Derin D'Amico; Thomas Nguyen; Wenyuan Qian
- Web page: https://patentgrep.com/patent/US7612060B2

## CPC

- C07D 401/14: containing three or more hetero rings
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 1/18: for pancreatic disorders, e.g. pancreatic enzymes
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 7/10: Antioedematous agents; Diuretics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 9/12: Antihypertensives
- A61P 11/02: Nasal agents, e.g. decongestants
- A61P 11/06: Antiasthmatics
- A61P 13/10: of the bladder
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 27/02: Ophthalmic agents
- A61P 27/06: Antiglaucoma agents or miotics
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/12: Antivirals
- A61P 35/04: specific for metastasis
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 403/06: linked by a carbon chain containing only aliphatic carbon atoms
- C07D 403/14: containing three or more hetero rings
- C07D 405/14: containing three or more hetero rings
- C07D 409/14: containing three or more hetero rings
- C07D 471/04: Ortho-condensed systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

## Claims

### Claim 1

A compound of Formula (I):
wherein:
t is 1;
X is selected from —NH— or —NRd— where Rd is C1-8alkyl or C1-4haloalkyl;
is:
A is a group of formula (a):
where:
R1 is a 5-, 6-, 7-, or 8-membered saturated, partially saturated or unsaturated monocyclic, a saturated, partially saturated or unsaturated 8-, 9-, 10- or 11-membered bicyclic, or 12-, 13-, 14- or 15-membered tricyclic hydrocarbon ring containing 0, 1, 2, 3 or 4 atoms selected from N, O and S, wherein the carbon and sulfur atoms of the ring are substituted by 0, 1 or 2 oxo groups and the ring is substituted by 0, 1, 2 or 3 substituents selected from R6, R7 or R8 independently selected from basic moieties, and additionally substituted by 0, 1, 2 or 3 substituents selected from R6, R7 and R8 which are selected from Rg, C1-8alkyl, C1-4haloalkyl, hydroxyalkyl, cyano, nitro, —C(═O)Rb, —C(═O)ORb, —C(═O)NRaRa, —C(═NRa)NRaRa, —ORa, —OC(═O)Rb, —OC(═O)NRaRa, —OC(═O)N(Ra)S(═O)2Rb, —OC2-6alkylNRaRa, —OC2-6alkylORa, —SRa, —S(═O)Rb, —S(═O)2Rb, —S(═O)2NRaRa, —S(═O)2N(Ra)C(═O)Rb, —S(═O)2N(Ra)C(═O)ORb, —S(═O)2N(Ra)C(═O)NRaRa, —NRaRa, —N(Ra)C(═O)Rb, —N(Ra)C(═O)ORb, —N(Ra)C(═O)NRaRa, —N(Ra)C(═NRa)NRaRa, —N(Ra)S(═O)2Rb, —N(Ra)S(═O)2NRaRa, —NRaC2-6alkylNRaRa and —NRaC2-6alkylORa, and the ring is additionally substituted by 0, 1, 2, 3, 4 or 5 substituents selected from R6, R7, R8, R9 and R10 which are independently selected from Br, Cl, F and I;
R2 is a saturated, partially saturated or unsaturated 5-, 6- or 7-membered monocyclic or 6-, 7-, 8-, 9-, 10- or 11-membered bicyclic hydrocarbon ring containing 0, 1, 2, 3 or 4 atoms selected from N, O and S, wherein the carbon atoms of the ring are substituted by 0, 1 or 2 oxo groups and the ring is substituted by 0, 1, 2 or 3 substituents selected from Re, Rg, C1-4haloalkyl, halo, cyano, nitro, —C(═O)Rb, —C(═O)ORb, —C(═O)NRaRa, —C(═NRa)NRaRa, —ORa, —OC(═O)Rb, —OC(═O)NRaRa, —OC(═O)N(Ra)S(═O)2Rb, —OC2-6alkylNRaRa, —OC2-6alkylORa, —SRa, —S(═O)Rb, —S(═O)2Rb, —S(═O)2NRaRa, —S(═O)2N(Ra)C(═O)Rb, —S(═O)2N(Ra)C(═O)ORb, —S(═O)2N(Ra)C(═O)NRaRa, —NRaRa, —N(Ra)C(═O)Rb, —N(Ra)C(═O)ORb, —N(Ra)C(═O)NRaRa, —N(Ra)C(═NRa)NRaRa, —N(Ra)S (═O)2Rb, —N(Ra)S(═O)2NRaRa, —NRaC2-6alkylNRaRa and —NRaC2-6alkylORa, and the ring is additionally substituted by 0, 1, 2, 3, 4 or 5 substituents independently selected from Br, Cl, F and I;
R3, R3a, R4 and R5 are independently in each instance selected from H, C1-3alkyl, C1-3haloalkyl, —OH, F, Cl, Br and I; or
R3 and R3a together form oxo;
Rx is selected from H, F, Cl, (C1-C3)haloalkyl, and (C1-C3)alkyl;
Ra is independently, at each instance, H or Rb;
Rb is independently, at each instance, phenyl, benzyl or C1-6alkyl, the phenyl, benzyl and C1-6alkyl being substituted by 0, 1, 2 or 3 substituents selected from halo, C1-4alkyl, C1-3haloalkyl, —OC1-4alkyl, —NH2, —NHC1-4alkyl, —N(C1-4alkyl)C1-4alkyl.
Rd is independently at each instance C1-8alkyl, C1-4haloalkyl, halo, cyano, nitro, —C(═O)Rb, —C(═O)ORb, —C(═O)NRaRa, —C(═NRa)NRaRa, —ORa, —OC(═O)Rb, —OC(═O)NRaRa, —OC(═O)N(Ra)S(═O)2Rb, —OC2-6alkylNRaRa, —OC2-6alkylORa, —SRa, —S(═O)Rb, —S(═O)2Rb, —S(═O)2NRaRa, —S(═O)2N(Ra)C(═O)Rb, —S(═O)2N(Ra)C(═O)ORb, —S(═O)2N(Ra)C(═O)NRaRa, —NRaRa, —N(Ra)C(═O)Rb, —N(Ra)C(═O)ORb, —N(Ra)C(═O)NRaRa, —N(Ra)C(═NRa)NRaRa, —N(Ra)S(═O)2Rb, —N(Ra)S(═O)2NRaRa, —NRaC2-6-alkylNRaRa or —NRaC2-6alkylORa;
Re is independently at each instance C1-6alkyl substituted by 0, 1, 2 or 3 substituents independently selected from Rd and additionally substituted by 0 or 1 substituents selected from Rg; and
Rg is independently at each instance a saturated, partially saturated or unsaturated 5-, 6- or 7-membered monocyclic or 6-, 7-, 8-, 9-, 10- or 11-membered bicyclic hydrocarbon ring containing 0, 1, 2, 3 or 4 atoms selected from N, O and S, wherein the carbon atoms of the ring are substituted by 0, 1 or 2 oxo groups and the ring is substituted by 0, 1, 2 or 3 substituents selected from C1-8alkyl, C1-4haloalkyl, halo, cyano, nitro, —C(═O)Rb—C(═O)ORb, —C(═O)NRaRa, —C(═NRa)NRaRa, —ORa, —OC(═O)Rb, —OC(═O)NRaRa, —OC(═O)N(Ra)S(═O)2Rb, —OC2-6alkylNRaRa, —OC2-6alkylORa, —SRa, —S(═O)Rb, —S(═O)2Rb, —S(═O)2NRaRa, —S(═O)2N(Ra)C(═O)Rb, —S(═O)2N(Ra)C(═O)ORb, —S(═O)2N(Ra)C(═O)NRaRa, —NRaRa, —N(Ra)C(═O)Rb, —N(Ra)C(═O)ORb, —N(Ra)C(═O)NRaRa, —N(Ra)C(═NRa)NRaRa, —N(Ra)S(═O)2Rb, —N(Ra)S(═O)2NRaRa, —NRaC2-6alkylNRaRa and —NRaC2-6alkylORa, and the ring is additionally substituted by 0, 1, 2, 3, 4 or 5 substituents independently selected from Br, Cl, F and I; or
a pharmaceutically-acceptable salt thereof;
wherein the basic moieties are independently selected from amino, cycloalkylaminoC1-6alkyl, cycloalkylC1-6alkylamino-C1-6alkyl, heterocyclylaminoC1-6alkyl, heterocyclylC1-6alkylaminoC1-6alkyl, arylaminoC1-6alkyl, arylC1-6alkylaminoC1-6alkyl, C1-6-alkylamino-C1-6-alkoxy, C1-6-alkylamino-C1-6-alkoxy-C1-6-alkoxy, aminoC1-6alkoxy, aminoC1-6alkyl, C1-6alkylaminoC1-6alkyl, C1-4-alkylamino-C2-6-alkenyl, 5-8 membered nitrogen-containing heterocyclyl-C2-6-alkenyl, heterocyclyl-C1-6alkylamino-C2-6alkyl, 5-6 membered heterocyclyloxy, 4-6 membered nitrogen-containing heterocyclyl and 5-7 membered nitrogen-containing heterocyclyl-alkyl; and wherein each of said basic moieties is substituted by 0, 1, 2 or 3 groups independently selected from halo, —NH2, hydroxyl, cyano, —CF3, C1-6alkylamino, oxo, C1-6alkoxy, C2-6alkenyl, C2-6alkynyl, diC1-6alkylamino, C1-6alkyl, substituted C1-6alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, substituted saturated or partially saturated heterocyclyl and unsubstituted saturated or partially saturated heterocyclyl, wherein each substituted C1-6alkyl, substituted aryl, substituted heteroaryl, and substituted saturated or partially saturated heterocyclyl is substituted by 0, 1, 2 or 3 groups independently selected from halo, —NH2, hydroxyl, cyano, C1-6alkylamino, C1-6haloalkyl, oxo, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, or diC1-6alkylamino.

### Claim 2 (depends on 1)

The compound of claim 1 wherein R1 is a saturated, partially saturated or unsaturated 8-, 9-, 10- or 11-membered bicyclic or 12-, 13-, 14- or 15-membered tricyclic hydrocarbon ring containing 0, 1, 2, 3 or 4 atoms selected from N, O and S, wherein the carbon and sulfur atoms of the ring are substituted by 0, 1 or 2 oxo groups and the ring is substituted by R6, R7 or R8 independently selected from basic moieties, and additionally substituted by 0, 1, 2 or 3 substituents selected from R6, R7 and R8 which are selected from Rg, C1-8alkyl, C1-4haloalkyl, cyano, nitro, —C(═O)Rb, —C(═O)ORb, —C(═O)NRaRa, —C(═NRa)NRaRa, —ORa, —OC(═O)Rb, —OC(═O)NRaRa, —OC(═O)N(Ra)S(═O)2Rb, —OC2-6alkylNRaRa, —OC2-6alkylORa, —SRa, —S(═O)Rb, —S(═O)2Rb, —S(═O)2NRaRa, —S(═O)2N(Ra)C(═O)Rb, —S(═O)2N(Ra)C(═O)ORb, —S(═O)2N(Ra)C(═O)NRaRa, —NRaRa, —N(Ra)C(═O)Rb, —N(Ra)C(═O)ORb, —N(Ra)C(═O)NRaRa, —N(Ra)C(═NRa)NRaRa, —N(Ra)S(═O)2Rb, —N(Ra)S(═O)2NRaRa, —NRaC2-6alkylNRaRa and —NRaC2-6alkylORa, and the ring is additionally substituted by 0, 1, 2, 3, 4 or 5 substituents selected from R6, R7, R8, R9 and R10 which are independently selected from Br, Cl, F and I; and
Rx is H.

### Claim 3 (depends on 2)

The compound of claim 2 wherein and R3 and R3a together form oxo.

### Claim 4 (depends on 3)

The compound of claim 3 wherein:
R5 is hydrogen; and
R1 is:
wherein:
X1 is N or CR6;
X2 is N or CR7;
X3 is N or CR8;
X4 is N or CH; wherein no more than two of X1, X2, X3 and X4 is N; and
the C ring is a saturated or partially saturated 6- or 7-membered ring containing 0, 1 or 2 atoms selected from N, O and S, wherein the carbon and sulfur atoms of the ring are substituted by 0, 1 or 2 oxo groups and the ring is substituted by 0 or 1 substituents selected from Rg, C1-8alkyl, C1-4haloalkyl, cyano, nitro, —C(═O)Rb, —C(═O)ORb, —C(═)NRaRa, —C(═NRa)NRaRa, —ORa, —OC(═O)Rb, —OC(═O)NRaRa, —OC(═O)N(Ra)S(═O)2Rb, —OC2-6alkylNRaRa, —OC2-6alkylORa, —SRa, —S(═O)Rb, —S(═O)2Rb, —S(═O)2NRaRa, —S(═O)2N(Ra)C(═O)Rb, —S(═O)2N(Ra)C(═O)ORb, —S(═O)2N(Ra)C(═O)NRaRa, —NRaRa, —N(Ra)C(═O)Rb, —N(Ra)C(═O)ORb, —N(Ra)C(═O)NRaRa, —N(Ra)C(═NRa)NRaRa, —N(Ra)S(═O)2Rb, —N(Ra)S(═O)2NRaRa, —NRaC2-6alkylNRaRa and —NRaC2-6alkylORa, and the ring is additionally substituted by 0, 1, 2 or 3 substituents independently selected from Br, Cl, F and I.

### Claim 5 (depends on 3)

The compound of claim 3 wherein:
R5 is hydrogen;
R1 is:
where R7 is a basic moiety; and
X is —NH—.

### Claim 6 (depends on 5)

The compound of claim 5 wherein R7 is selected from amino, aminomethyl, isopropylaminomethyl, t-butylaminomethyl, 2-t-butylaminoethyl, 2-tert-butylamino-1-methyl-ethyl, 1-tert-butylaminoethyl, 1-(tert-butylamino-methyl)-vinyl, 1-(piperidin-1-ylmethyl)-vinyl, N-isobutyl-aminomethyl, N-isobutyl-aminoethyl, (2,2-dimethyl)propylaminomethyl, N-isopropyl-N-ethylaminomethyl, N-isopropyl-N-methylaminomethyl, N-t-butyl-N-methyl-aminomethyl, N-iso-butyl-N-methylaminomethyl, N-t-butyl-N-ethylaminomethyl, N-isobutyl-N-methylaminomethyl, N-t-butyl-N-isopropylaminomethyl, N,N-di(isopropyl)-aminomethyl, N,N-dimethylaminomethyl, N,N-diethylaminomethyl, N,N-di(t-butyl)-aminomethyl, cyclopropylaminomethyl, cyclopropylaminoethyl, cyclopropylmethyl-aminomethyl, cyclopropylmethylaminoethyl, cyclobutylaminomethyl, cyclobutylaminoethyl, cyclobutylmethylaminomethyl, cyclobutylmethylaminoethyl, 4,5-dihydro-imidazolyl, 1-piperidinylmethyl, 4-fluoropiperidin-1-ylmethyl, 4,4-difluoropiperidin-1-ylmethyl, 3-hydroxypiperidin-1-ylmethyl, 4-hydroxypiperidin-1-ylmethyl, 4-(piperidin-1-yl)-piperidinylmethyl, 4-(dimethylamino)piperidin-1-ylmethyl, 2,6-dimethylpiperidin-1-ylmethyl, 4-morpholinylmethyl, 1-pyrrolidinylmethyl, 2-methylpyrrolidin-1-ylmethyl, 2,5-dimethyl-pyrrolidin-1-ylmethyl, piperazin-1-ylmethyl, azocan-1-ylmethyl, azepan-1-ylmethyl, (7-azabicyclo[2.2.1]hept-7-yl)methyl, (1,3,3-trimethyl-6-azabicyclo[3.2.1]oct-6-yl)methyl, 2-piperidinyl and 4-methylpiperazin-1-ylmethyl; and
R2 is phenyl substituted by 1, 2 or 3 substituents selected C1-6alkyl, C1-4haloalkyl, halo, cyano, or nitro.

### Claim 7

A compound selected from the group consisting of:
(R)-3-((1-((R)-7-cyclopropylaminomethyl-3,4-dihydro-2H-chromen-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-methylbenzenesulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-7-tert-butylaminomethyl-3,4-dihydro-2H-chromen-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-methylbenzenesulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-7-cyclopropylmethylamino-3,4-dihydro-2H-chromen-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-methylbenzenesulfonyl)-piperazin-2-one;
(R)-3-((1-((R)-6-((2,2-dimethylethylamino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-methylbenzenesulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-methylbenzenesulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-4-(3,4-dichlorobenzenesulfonyl)-3-((1-((R)-1-(4-(piperidin-1-ylmethyl)phenyl)-ethyl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((cyclopentyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-tosyl-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((4-fluoro-piperidin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(phenylsulfonyl)-3,4-dihydro-pyrazin-2(1H)-one;
(R)-4-(4-chlorophenyl-sulfonyl)-3-((1-((R)-6-((4-fluoro-piperidin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)piperazin-2-one;
(R)-3-((1-((R)-6-((4-fluoro-piperidin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-methoxyphenylsulfonyl)piperazin-2-one;
(R)-4-(4-chlorophenyl-sulfonyl)-3-((1-((R)-6-((4-fluoro-piperidin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((4-fluoro-piperidin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-methoxyphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((cyclopentyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(phenylsulfonyl)piperazin-2-one;
(R)-3-((1-((R)-6-((cyclopentyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-(trifluoromethyl)phenyl-sulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((cyclopentyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(phenylsulfonyl)-3,4-dihydro-pyrazin-2(1H)-one;
(R)-4-(4-chlorophenyl-sulfonyl)-3-((1-((R)-6-((cyclopentyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)piperazin-2-one;
(R)-3-((1-((R)-6-((cyclopentyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-methoxyphenylsulfonyl)piperazin-2-one;
(R)-4-(4-chlorophenyl-sulfonyl)-3-((1-((R)-6-((cyclopentylamino)methyl)-1,2,3,4-tetra-hydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((cyclopentyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-methoxyphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((tert-butyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(phenylsulfonyl)piperazin-2-one;
(R)-3-((1-((R)-6-((tert-butyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-(trifluoromethyl)phenyl-sulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((tert-butyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(phenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((tert-butyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-chlorophenylsulfony)piperazin-2-one;
(R)-3-((1-((R)-6-((tert-butyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-methoxyphenyl-sulfonyl)piperazin-2-one;
(R)-3-((1-((R)-6-((tert-butyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-chlorophenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((tert-butyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-methoxyphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((neopentyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-tosyl-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((neopentyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(phenylsulfonyl)piperazin-2-one;
(R)-3-((1-((R)-6-((neopentyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-(trifluoromethyl)phenyl-sulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((neopentyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(phenylsulfonyl)-3,4-dihydro-pyrazin-2(1H)-one;
(R)-4-(4-chlorophenylsulfonyl)-3-((1-((R)-6-((neopentylamino)methyl)-1,2,3,4-tetra-hydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-piperazin-2-one;
(R)-4-(4-chlorophenyl-sulfonyl)-3-((1-((R)-6-((neopentylamino)methyl)-1,2,3,4-tetra-hydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-4-(4-methoxyphenyl-sulfonyl)-3-((1-((R)-6-((neopentylamino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydro-pyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((4-methyl-piperazin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-tosyl-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((4-methyl-piperazin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(phenylsulfonyl)piperazin-2-one;
(R)-3-((1-((R)-6-((4-methyl-piperazin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-(trifluoromethyl)phenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((4-methyl-piperazin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(phenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-4-(4-chlorophenyl-sulfonyl)-3-((1-((R)-6-((4-methylpiperazin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)piperazin-2-one;
(R)-4-(4-methoxyphenyl-sulfonyl)-3-((1-((R)-6-((4-methylpiperazin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)piperazin-2-one;
(R)-4-(4-chlorophenyl-sulfonyl)-3-((1-((R)-6-((4-methylpiperazin-1-yl)methyl)-1,2,3,4-tetrahydro-naphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-4-(4-methoxyphenyl-sulfonyl)-3-((1-((R)-6-((4-methylpiperazin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((isobutyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-tosyl-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((isobutyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(phenylsulfonyl)piperazin-2-one;
(R)-3-((1-((R)-6-((isobutyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-(trifluoromethyl)phenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((isobutyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(phenylsulfonyl)-3,4-dihydropyrazin-2(1H1)-one;
(R)-4-(4-chlorophenyl-sulfonyl)-3-((1-((R)-6-((isobutylamino)methyl)-1,2,3,4-tetra-hydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)piperazin-2-one;
(R)-3-((1-((R)-6-((isobutyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-methoxyphenylsulfonyl)piperazin-2-one;
(R)-4-(4-chlorophenyl-sulfonyl)-3-((1-((R)-6-((isobutylamino)methyl)-1,2,3,4-tetra-hydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((isobutyl-amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-methoxyphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((4-fluoro-piperidin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-tosyl-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-((4-fluoro-piperidin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(phenylsulfonyl)piperazin-2-one;
(R)-3-((1-((R)-6-((4-fluoro-piperidin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-(trifluoro-methyl)phenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-(4-(4,5-dihydro-1H-imidazol-2-yl)phenethyl)-1H-1,2,3-triazol-4-yl)methyl)-4-tosylpiperazin-2-one;
(R)-4-(3,4-dichlorophenylsulfonyl)-3-((1-((R)-3-isobutyl-1,2,3,4,7,8,9,10-octahydrobenzo[f]isoquinolin-7-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-4-(3,4-dichlorophenylsulfonyl)-3-((1-((R)-2-isobutyl-1,2,3,4,6,7,8,9-octahydro-benzo[g]isoquinolin-6-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-2-((1-((R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-1-tosyl-1,2-dihydropyrido[2,3-b]pyrazin-3(4H)-one;
(R)-3-((1-((R)-6-chloro-1,1-dioxothiochroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3,4-dichlorophenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-4-(3,4-dichlorophenyl-sulfonyl)-3-((1-((R)-1,2,3,4,7,8,9,10-octahydro-benzo[f]isoquinolin-7-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-4-(3,4-dichlorophenyl-sulfonyl)-3-((1-((R)-1,2,3,4,6,7,8,9-octahydro-benzo[g]isoquinolin-6-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-4-(3,4-dichlorophenyl-sulfonyl)-3-((1-((R)-3-isobutyl-1,2,3,4,7,8,9,10-octahydro-benzo[f]isoquinolin-7-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(S)-4-(3,4-dichlorophenyl-sulfonyl)-3-((1-((S)-2-(2-(piperidin-1-yl)ethyl)-5,6,7,8-tetrahydroquinazolin-5-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-4-(3,4-dichlorophenyl-sulfonyl)-3-((1-((S)-2-(2-(piperidin-1-yl)ethyl)-5,6,7,8-tetrahydroquinazolin-5-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-4-(3,4-dichlorophenyl-sulfonyl)-3-((1-((R)-2-(2-(piperidin-1-yl)ethyl)-5,6,7,8-tetrahydroquinazolin-5-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(S)-4-(3,4-dichlorophenyl-sulfonyl)-3-((1-((R)-2-(2-(piperidin-1-yl)ethyl)-5,6,7,8-tetrahydroquinazolin-5-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-methyl 5-(4-(((R)-3-oxo-1-tosylpiperazin-2-yl)methyl)-1H-1,2,3-triazol-1-yl)-5,6,7,8-tetrahydronaphthalene-2-carboxylate;
(S)-4-(3,4-dichlorophenyl-sulfonyl)-3-((1-((S)-2-(2-(4-methylpiperidin-1-yl)ethyl)-5,6,7,8-tetrahydroquinazolin-5-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-4-(3,4-dichlorophenyl-sulfonyl)-3-((1-((S)-2-(2-(4-methylpiperidin-1-yl)ethyl)-5,6,7,8-tetrahydroquinazolin-5-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(S)-4-(3,4-dichlorophenyl-sulfonyl)-3-((1-((R)-2-(2-(4-methylpiperidin-1-yl)ethyl)-5,6,7,8-tetrahydroquinazolin-5-yl)-1H-1,2,3-triazol-4-yl)-methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-4-(3,4-dichlorophenyl-sulfonyl)-3-((1-((R)-2-(2-(4-methylpiperidin-1-yl)ethyl)-5,6,7,8-tetrahydroquinazolin-5-yl)-1H-1,2,3-triazol-4-yl)-methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-(((S)-2-(hydroxymethyl)pyrrolidin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-tosyl-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-(((R)-2-(hydroxymethyl)pyrrolidin-1-yl)methyl)-1,2,3,4-tetrahydro-naphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-tosyl-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydro-naphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-tosyl-3,4-dihydropyrazin-2(1H)-one;
(R)-2-((1-((R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydro-naphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-1-tosyl-1,2-dihydropyrido[2,3-b]pyrazin-3(4H)-one;
(R)-3-((1-((R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydro-naphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-tosyl-3,4-dihydropyrido[3,2-b]pyrazin-2(1H)-one;
(R)-4-(3,4-dichlorophenyl-sulfonyl)-3-((3-((R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-3H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-4-(3,4-dichlorophenyl-sulfonyl)-3-((1-((R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
methyl 4-((R)-1-(4-(((R)-1-(3,4-dichlorophenylsulfonyl)-3-oxo-1,2,3,4-tetrahydropyrazin-2-yl)methyl)-1H-1,2,3-triazol-1-yl)ethyl)benzoate;
(R)-methyl 5-(4-(((R)-1-(3,4-dichlorophenylsulfonyl)-3-oxo-1,2,3,4-tetrahydropyrazin-2-yl)methyl)-1H-1,2,3-triazol-1-yl)-5,6,7,8-tetrahydro-naphthalene-2-carboxylate;
(R)-3-((1-(4-(4,5-dihydro-1H-imidazol-2-yl)phenethyl)-1H-1,2,3-triazol-4-yl)methyl)-4-tosylpiperazin-2-one;
(R)-3-((1-(4-(4H-1,2,4-triazol-3-yl)phenethyl)-1H-1,2,3-triazol-4-yl)methyl)-4-tosylpiperazin-2-one;
(R)-3-((1-(4-(4,5-dihydro-1H-imidazol-2-yl)phenethyl)-1H-1,2,3-triazol-4-yl)methyl)-4-tosyl-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-(4-(4,5-dihydro-1H-imidazol-2-yl)phenethyl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-methoxyphenylsulfonyl)piperazin-2-one;
(R)-3-((1-((R)-6-(((S)-2-(hydroxymethyl)pyrrolidin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-tosylpiperazin-2-one;
(R)-3-((1-((R)-6-(((R)-2-(hydroxymethyl)pyrrolidin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-tosylpiperazin-2-one;
(R)-4-(3,4-dichlorophenyl-sulfonyl)-3-((1-((R)-3-(2,2,2-trifluoroacetyl)-,2,3,4,7,8,9,10-octahydrobenzo[f]isoquinolin-7-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-4-(3,4-dichlorophenyl-sulfonyl)-3-((1-((R)-2-(2,2,2-trifluoroacetyl)-,2,3,4,7,8,9,10-octahydrobenzo[h]isoquinolin-7-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-4-(3,4-dichlorophenyl-sulfonyl)-3-((1-((R)-2-isobutyl-1,2,3,4,6,7,8,9-octahydro-benzo[g]isoquinolin-6-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
(R)-3-((1-((S)-2-(2-(azepan-1-yl)ethyl)-5,6,7,8-tetrahydro-quinazolin-5-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3,4-dichloro-phenylsulfonyl)-3,4-dihydro-pyrazin-2(1H)-one;
(R)-3-((1-((R)-2-(2-(azepan-1-yl)ethyl)-5,6,7,8-tetrahydro-quinazolin-5-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3,4-dichloro-phenylsulfonyl)-3,4-dihydro-pyrazin-2(1-H)-one;
4-(naphthalen-2-ylsulfonyl)-3-((1-(7-(2-piperidin-1-ylethyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
4-(naphthalen-2-ylsulfonyl)-3-((1-(7-(dimethylaminomethyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
4-(naphthalen-2-ylsulfonyl)-3-((1-(7-(piperidin-1-ylmethyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
4-(naphthalen-2-ylsulfonyl)-3-((1-(7-(4-methylpiperazin-1-ylmethyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
4-(naphthalen-2-ylsulfonyl)-3-((1-(7-(diethylaminomethyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
4-(naphthalen-2-ylsulfonyl)-3-((1-(7-(4,5-dihydroimidazol-2-ylmethyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
4-(naphthalen-2-ylsulfonyl)-3-((1-(7-(2-ethylmethylaminoethyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
4-(naphthalen-2-ylsulfonyl)-3-((1-(7-(2-piperazin-1-ylethyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(5,6,7,8-tetrahydronaphth-2-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(2-quinolyl sulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(phenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(2-chlorophenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-chlorophenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-chlorophenylsulfonylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-methoxyphenylsulfonyl ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3,5-dichlorophenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-methoxyphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-fluorophenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(biphen-3-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(biphen-4-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-methylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(2,3,4-trichlorophenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(2,4,5-trichlorophenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3,4-dichlorophenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-t-butylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(naphtha-1-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-methylnaphth-1-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(phenylethen-1-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(benzo[1,2,5]oxadiazol-5-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(5-(dimethylamino)naphth-1-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(5-chloro-3-methylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(benzothiazol-2-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(2,3,4,5,6-pentamethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(6-methoxy-2-naphthylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-chloro-4-methylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(5-methoxy-3-methylbenzothien-2-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(6-methoxy-3-methylbenzothien-2-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(5-chloro-3-methylbenzothien-2-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-methylbenzothien-2-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(2,4-dichloro-5-methylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3,5-dichloro-4-methylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(2,4-dichloro-3-methylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(7-methoxy-2-naphthylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(6-fluoroethoxy-2-naphthylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-methyl-5-trifluoromethoxybenzofur-2-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-methyl-5-methoxybenzofur-2-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(5-chloro-benzo[1,2,5]oxadiazol-4-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-methyl-5-trifluoromethoxybenzothien-2-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(6-ethoxy-2-naphthylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(2-Cl4-CF3-phenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(6-bromonaphthylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-methylbenzofur-2-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-chlorobenzothien-2-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(5-chloro-benzo[1,2,5]thiadiazol-4-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(5-chloro-1,3-dimethyl-1H-pyrazol-4-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(2,3-dichlorothien-5-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(2,5-dichlorothien-3-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(5-chloro-2-naphthylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-butoxyphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3,5-di(trifluoromethyl)phenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(5-(isoxazol-3-yl)thien-2-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(2-chlorothien-5-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-chloro-benzo[1,2,5]oxadiazol-7-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(2,4-dichloro-6-methylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(2,4,6-trimethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(2,5-dimethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-chloro-2,5-dimethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(2,5-dichlorophenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-chloro-2,5-dimethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3,4-difluorophenylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-chloro-4-fluorophenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(2-methyl-5-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-methylcyclohexylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3,5-dimethylbenzothien-2-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(5-fluoro-3-methylbenzothien-2-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(5-methylbenzothien-2-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(5-chloro-3-methylbenzofur-2-ylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-((isopropyl(methyl)amino)methyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-pyridylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(3-isopropyl-7-(1-methylpiperidin-2-yl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(2,2-dimethyl-7-(1-methylpiperidin-2-yl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-(piperidin-2-yl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(2,2-dimethyl-7-(methylaminomethyl)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-(dimethylaminomethyl)-1,2,3,4-tetrahydonaphth-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-(piperidin-1-ylaminomethyl)-1,2,3,4-tetrahydonaphth-2-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(5-(piperidin-1-yl)methylindan-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(6-(4-methylpiperazin-1-yl)methylindan-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(4-(piperazin-1-yl)methylindan-1-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(2-(diethylaminomethyl)-5,6,7,8-tetrahydoquinolin-5-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(2-(isopropylaminomethyl)-5,6,7,8-tetrahydoquinolin-8-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(2-(t-butylaminomethyl)-5,6,7,8-tetrahydoisoquinolin-8-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-(morpholin-4-ylmethyl)-quinolin-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(1-methyl-2-oxo-6-(piperidin-1-yl)methylindol-3-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-(dimethylaminomethyl)-1,2,3,4-tetrahydonaphth-2-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-(diethylaminomethyl)-4,5,6,7-tetrahydobenzofur-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-(4-morpholinylmethyl)-4,5,6,7-tetrahydobenzothien-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(7-(aminomethoxy)chroman-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(4-4-(4,5-dihydro-1H-imidazol-2-yl)-phenylethyl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((4-4-(4,5-dihydro-1H-imidazol-2-yl)-phenyl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one;
3-((1-(4-(aminopropyl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one; and
3-((1-(4-(aminoethyl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)-4-(3-trifluoromethylphenylsulfonyl)-3,4-dihydropyrazin-2(1H)-one; or
a pharmaceutically acceptable salt thereof.

### Claim 8 (depends on 1)

A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of claim 1.