IP Library Granted Patent US 7,468,385
Granted Patent B2
US 7,468,385 · App. 10/498,356 · Granted Dec 23, 2008

Triazoles as oxytocin antagonists

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Quick Facts
Patent No.
US 7,468,385
App. No.
10/498,356
Granted
Dec 23, 2008
Kind
B2
Abstract

The present invention relates to triazole derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such triazole derivatives. Said triazoles are useful in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to triazole derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and/or vasopressin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin and/or vasopressin. The present invention is furthermore related to novel triazole derivatives as well as to methods of their preparation.

Claims (407)

1. The triazole derivative of Formula I:

its geometrical isomers, its optically active forms as enantiomers, diastereomers, mixtures of these and its racemate forms, as well as salts thereof, wherein:

R 1 and R 2 are independently selected from the group consisting of H, C 1 -C 6 -alkyl, aryl C 1 -C 6 -alkyl, heteroarylC 1 -C 6 -alkyl, C 3 -C 6 -cycloalkyl C 1 -C 6 -alkyl and C 3 -C 6 -heterocycloalkyl C 1 -C 6 -alkyl;

R 1 and R 2 , together with the nitrogen atom they are linked to, form a substituted or unsubstituted 5-8-membered saturated, partially unsaturated or aromatic ring containing optionally one or more additional heteroatoms selected from O, N, S;

A is C(O);

R 3 is selected from the group consisting of H, C 1 -C 6 -alkyl, aryl C 1 -C 6 -alkyl, heteroaryl C 1 -C 6 -alkyl, aryl, heteroaryl, C 3 -C 6 -cycloalkyl C 1 -C 6 -alkyl, C 3 -C 6 -heterocycloalkyl C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl;

B is S;

R 4 and R 5 are selected from the group consisting of H, C 1 -C 6 -alkyl, aryl C 1 -C 6 -alkyl, heteroaryl C 1 -C 6 -alkyl, acyl, aryl acyl, heteroaryl acyl, C 3 -C 6 -cycloalkyl C 1 -C 6 -alkyl, C 3 -C 6 -heterocycloalkyl C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl;

n is an integer from 2 to 10.

2. The triazole derivative according to claim 1 , wherein A is carbonyl.

3. The triazole derivative according to claim 1 , wherein B is sulfur.

4. The triazole derivative according to claim 1 , wherein n is an integer from 2, 3 or 4.

5. The triazole derivative according to claim 1 , wherein A is carbonyl, B is sulfur and n is an integer from 2, 3 or 4.

6. A triazole derivative according to claim 1 , selected from the group consisting of:

3-{4-benzyl-5-[(3-chlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)propanamide,

3-{4-(3-chlorophenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)propanamide,

3-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methoxypropyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[5-[(3-fluorobenzyl)sulfanyl]-4-(4-methylphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

N-(2-methoxybenzyl)-3-{4-(4-methylbenzyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}propanamide,

3-{5-[(3-fluorobenzyl)sulfanyl]-4-isobutyl-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)propanamide,

3-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methylphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[5-(benzylsulfanyl)-4-(4-methylphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[5-(benzylsulfanyl)-4-isobutyl-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-{4-(3-chlorophenyl)-5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)propanamide,

3-[5-(benzylsulfanyl)-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-{4-isobutyl-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)propanamide,

N-(2-methoxybenzyl)-3-[5-[(3-methylbenzyl)sulfanyl]-4-(tetrahydro-2-furanylmethyl)-4H-1,2,4-triazol-3-yl]propanamide,

N-butyl-3-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]propanamide,

N-(2-methoxybenzyl)-3-{4-(3-methoxyphenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}propanamide,

3-{5-[(3-chlorobenzyl)sulfanyl]-4-methyl-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)propanamide,

3-[5-[(3-fluorobenzyl)sulfanyl]-4-(tetrahydro-2-furanylmethyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-{4-allyl-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)propanamide,

3-[5-[(3-fluorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[5-(butylsulfanyl)-4-(3-methoxypropyl)-4H-1,2,4-triazol-3-yl]-N-(4-methoxybenzyl)propanamide,

N-benzyl-3-{4-(3-methoxypropyl)-5-[(2-phenoxyethyl)sulfanyl]-4H-1,2,4-triazol-3-yl}propanamide,

3-{4-benzyl-5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)propanamide,

3-[5-[(3-chlorobenzyl)sulfanyl]-4-(4-fluorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[5-(benzylsulfanyl)-4-(4-fluorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(cyclopropylmethyl)propanamide,

3-[5-[(3-cyanobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[5-(benzylsulfanyl)-4-(tetrahydro-2-furanylmethyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

N-(2-methoxybenzyl)-3-{4-(3-methoxypropyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}propanamide,

3-[4-allyl-5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[5-[(3-fluorobenzyl)sulfanyl]-4-(3-methoxypropyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-{4-(4-fluorophenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)propanamide,

3-[5-(benzylsulfanyl)-4-(3-methoxypropyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[5-[(3-fluorobenzyl)sulfanyl]-4-(4-fluorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-{4-allyl-5-[(3-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)propanamide,

3-{4-(3-chlorophenyl)-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)propanamide,

3-{4-(3-chlorophenyl)-5-[(3-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-isobutylpropanamide,

3-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-{5-[(2-chloro-4-fluorobenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-(2-furylmethyl)propanamide,

3-[5-[(3-fluorobenzyl)sulfanyl]-4-(4-methylbenzyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-{4-(3-chlorophenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-propylpropanamide,

3-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxyethyl)propanamide,

3-[5-(allylsulfanyl)-4-(4-methylbenzyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(3-methoxypropyl)propanamide,

3-{4-(3-chlorophenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-isobutylpropanamide,

N-(2-methoxybenzyl)-3-[5-[(3-methylbenzyl)sulfanyl]-4-(4-methylphenyl)-4H-1,2,4-triazol-3-yl]propanamide,

3-[5-[(2-fluorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[5-(benzylsulfanyl)-4-(4-methylbenzyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3 {4-benzyl-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)propanamide,

N-allyl-3-{4-(3-chlorophenyl)-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}propanamide,

3-[5-[(2-fluorobenzyl)sulfanyl]-4-(3-methylphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-{5-[(4-fluorobenzyl)sulfanyl]-4-isobutyl-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)propanamide,

3-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-isobutylpropanamide,

3-{4-(3-chlorophenyl)-5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-isobutylpropanamide,

N-butyl-3-[5-[(3-chlorobenzyl)sulfanyl]-4-(4-chlorophenyl)-4H-1,2,4-triazol-3-yl]propanamide,

3-[5-[(3-chlorobenzyl)sulfanyl]-4-(4-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)propanamide,

3-[5-[(2-fluorobenzyl)sulfanyl]-4-(3-methoxypropyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-{4-(3-chlorophenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(tetrahydro-2-furanylmethyl)propanamide,

3-{4-(4-chlorophenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)propanamide,

3-{4-(3-chlorophenyl)-5-[(3-cyanobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)propanamide,

N-(4-fluorobenzyl)-3-[5-[(2,3,4,5,6-pentafluorobenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]propanamide,

3-{4-allyl-5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)propanamide,

3-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methylphenyl)-4H-1,2,4-triazol-3-yl]-N-(cyclopropylmethyl)propanamide,

3-[5-[(3-chlorobenzyl)sulfanyl]-4-(tetrahydro-2-furanylmethyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)propanamide,

3-[5-(benzylsulfanyl)-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-{4-allyl-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(tetrahydro-2-furanylmethyl)propanamide,

3-[5-(allylsulfanyl)-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

N-butyl-3-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methylphenyl)-4H-1,2,4-triazol-3-yl]propanamide,

3-{4-(4-chlorophenyl)-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxyethyl)propanamide,

3-[5-(allylsulfanyl)-4-isobutyl-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[5-[(4-fluorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-{4-(3-chlorophenyl)-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)propanamide,

3-[4-benzyl-5-(butylsulfanyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[5-[(3-fluorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-isobutylpropanamide,

3-{5-[(3,5-dimethylbenzyl)sulfanyl]-4-isobutyl-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)propanamide.

3-[5-[(4-fluorobenzyl)sulfanyl]-4-(tetrahydro-2-furanylmethyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

N-butyl-3-{5-[(3-chlorobenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}propanamide,

3-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methylphenyl)-4H-1,2,4-triazol-3-yl]-N-(3-methoxypropyl)propanamide,

3-{4-(3-chlorophenyl)-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-isobutylpropanamide,

N-butyl-3-[5-[(3-methylbenzyl)sulfanyl]-4-(3-methylphenyl)-4H-1,2,4-triazol-3-yl]propanamide,

N-allyl-3-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]propanamide, 3-{4-(3-chlorophenyl)-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(tetrahydro-2-furanylmethyl)propanamide,

3-[5-(allylsulfanyl)-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[5-[(3-cyanobenzyl)sulfanyl]-4-(3-methylphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[4-benzyl-5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-{4-(4-chlorophenyl)-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)propanamide,

3-[5-[(2-fluorobenzyl)sulfanyl]-4-(4-fluorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[5-[(4-fluorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-isobutylpropanamide,

3-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methylphenyl)-4H-1,2,4-triazol-3-yl]-N-isobutylpropanamide,

3-[5-[(3-methylbenzyl)sulfanyl]-4-(4-methylphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)propanamide,

N-(2-methoxybenzyl)-3-{4-(3-methoxypropyl)-5-[(2-oxo-2-phenylethyl)sulfanyl]-4H-1,2,4-triazol-3-yl}propanamide,

3-{4-(4-chlorophenyl)-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(3-methoxypropyl)propanamide,

3-[5-[(3-fluorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-propylpropanamide,

3-[5-[(4-fluorobenzyl)sulfanyl]-4-(4-fluorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)propanamide,

3-[5-(benzylsulfanyl)-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-propylpropanamide,

N-benzyl-3-{4-(3-chlorophenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}propanamide,

3-[5-[(2-chloro-4-fluorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)propanamide,

3-{4-(3-chlorophenyl)-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-[3-(2-oxo-1-pyrrolidinyl)propyl]propanamide,

3-{4-(4-chlorophenyl)-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxyethyl)propanamide,

N-isobutyl-3-[5-[(3-methylbenzyl)sulfanyl]-4-(4-methylphenyl)-4H-1,2,4-triazol-3-yl]propanamide,

N-butyl-3-{4-(3-chlorophenyl)-5-[(3-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}propanamide,

3-{4-(3-chlorophenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(cyclopropylmethyl)propanamide,

3-[5-[(4-fluorobenzyl)sulfanyl]-4-(3-methoxypropyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

3-{4-(4-chlorophenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(3-methoxypropyl)propanamide,

3-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(4-methylphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)propanamide,

3-[5-[(3-fluorobenzyl)sulfanyl]-4-(4-methylphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)propanamide,

3-{5-[(3,5-dimethylbenzyl)sulfanyl]-4-isobutyl-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)propanamide,

3-{4-(3-chlorophenyl)-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)propanamide, 3-{4-(3-chlorophenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(4-methoxybenzyl)propanamide,

3-{4-allyl-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-benzylpropanamide,

N-(4-methoxybenzyl)-3-{4-(3-methoxyphenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}propanamide,

3-{5-[(2-fluorobenzyl)sulfanyl]-4-methyl-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)propanamide,

3-{4-(3-chlorophenyl)-5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)propanamide,

3-{4-(4-chlorophenyl)-5-[(3-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)propanamide,

3-{4-(4-chlorophenyl)-5-[(3-cyanobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)propanamide,

3-[5-[(3-cyanobenzyl)sulfanyl]-4-(4-fluorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

N-allyl-3-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methylphenyl)-4H-1,2,4-triazol-3-yl]propanamide,

3-{4-(4-chlorophenyl)-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(3-methoxypropyl)propanamide,

N-allyl-3-{4-(3-methoxyphenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}propanamide,

3-(4-(3-chlorophenyl)-5-{[4-(trifluoromethyl)benzyl]sulfanyl}-4H-1,2,4-triazol-3-yl)-N-isobutylpropanamide,

3-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(tetrahydro-2-furanylmethyl)propanamide,

3-[5-(butylsulfanyl)-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)propanamide,

N-butyl-3-{4-(4-chlorophenyl)-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}propanamide,

N-allyl-3-[5-[(3-fluorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]propanamide,

3-{4-(4-chlorophenyl)-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-[3-(2-oxo-1-pyrrolidinyl)propyl]propanamide,

3-{5-[(2-chloro-4-fluorobenzyl)sulfanyl]-4-methyl-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)propanamide,

3-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(3-methoxypropyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)propanamide,

3-{4-(3-chlorophenyl)-5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(4-methoxybenzyl)propanamide,

N-butyl-3-{4-(3-chlorophenyl)-5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}propanamide,

3-[5-[(3-methylbenzyl)sulfanyl]-4-(4-methylphenyl)-4H-1,2,4-triazol-3-yl]-N-propylpropanamide,

3-{4-(3-chlorophenyl)-5-[(3-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-propylpropanamide,

3-{4-(3-chlorophenyl)-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(4-methoxybenzyl)propanamide,

3-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(tetrahydro-2-furanylmethyl)-4H-1,2,4-triazol-3-yl]-N-(4-methoxybenzyl)propanamide,

3-{4-(4-chlorophenyl)-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)propanamide,

N-isobutyl-3-{4-(3-methoxyphenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}propanamide,

4-{5-[(3-chlorobenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)butanamide,

4-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)butanamide,

4-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)butanamide,

N-benzyl-4-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]butanamide,

N-(2-methoxybenzyl)-4-{4-(3-methoxyphenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}butanamide,

4-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methoxypropyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)butanamide,

4-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methoxypropyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)butanamide,

4-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(4-fluorobenzyl)butanamide,

4-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)butanamide,

N-(4-fluorobenzyl)-4-{4-(3-methoxyphenyl)-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}butanamide,

4-[5-[(3-fluorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-2-methoxybenzyl)butanamide,

4-{4-(3-methoxyphenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)butanamide,

N-(1,3-benzodioxol-5-ylmethyl)-4-(4-(3-methoxypropyl)-5-{[(2E)-3-phenyl-2-propenyl]sulfanyl}-4H-1,2,4-triazol-3-yl)butanamide,

4-{4-(3-chlorophenyl)-5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)butanamide,

N-benzyl-4-{4-(3-methoxyphenyl)-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}butanamide,

N-benzyl-4-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]butanamide,

N-(4-fluorobenzyl)-4-{4-(3-methoxyphenyl)-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}butanamide,

4-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-isobutylbutanamide,

N-(4-fluorobenzyl)-4-{4-(3-methoxyphenyl)-5-[(2,3,4,5,6-pentafluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}butanamide,

4-{4-(3-chlorophenyl)-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)butanamide,

4-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-propylbutanamide,

4-[5-[(4-fluorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)butanamide,

4-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(4-fluorobenzyl)butanamide,

4-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(4-methoxybenzyl)butanamide,

4-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(tetrahydro-2-furanylmethyl)butanamide,

N-benzyl-4-{4-(3-chlorophenyl)-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}butanamide,

4-[5-[(3-fluorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)butanamide,

4-{4-(3-chlorophenyl)-5-[(3-cyanobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)butanamide,

4-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(4-methoxybenzyl)butanamide,

4-[5-[(3-cyanobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)butanamide,

N-isobutyl-4-{4-(3-methoxyphenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}butanamide,

N-(4-methoxybenzyl)-4-{4-(3-methoxyphenyl)-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}butanamide,

4-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)butanamide,

N-benzyl-4-{4-(3-chlorophenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}butanamide,

4-[5-[(2-chloro-4-fluorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)butanamide,

N-allyl-4-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]butanamide,

4-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-isobutylbutanamide,

4-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(4-fluorobenzyl)butanamide,

N-benzyl-4-{4-(3-chlorophenyl)-5-[(3-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}butanamide,

N-benzyl-4-[5-(benzylsulfanyl)-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]butanamide,

4-{4-(3-chlorophenyl)-5-[(2-phenylethyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)butanamide,

4-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(3-methoxypropyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)butanamide,

N-benzyl-4-{4-(3-methoxyphenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}butanamide,

4-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-propylbutanamide,

4-{4-(3-chlorophenyl)-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(4-fluorobenzyl)butanamide,

4-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-propylbutanamide,

4-[5-[(cyclohexylmethyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)butanamide,

5-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)pentanamide,

5-{5-[(3-chlorobenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

N-(2-methoxybenzyl)-5-{4-(3-methoxypropyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

5-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-isobutylpentanamide,

5-{4-allyl-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

N-(2-methoxybenzyl)-5-[5-[(3-methylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]pentanamide,

N-(2-methoxybenzyl)-5-{5-[(3-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

5-{4-(3-chlorophenyl)-5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

5-[5-[(3-fluorobenzyl)sulfanyl]-4-(3-methoxypropyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)pentanamide,

5-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(4-fluorobenzyl)pentanamide,

5-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-isobutylpentanamide,

N-benzyl-5-{5-[(3-chlorobenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

5-{5-[(3-fluorobenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

5-[5-(benzylsulfanyl)-4-(3-methoxypropyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)pentanamide,

N-benzyl-5-{4-(3-chlorophenyl)-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

5-{4-allyl-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

5-{4-allyl-5-[(3-chlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

5-[5-(benzylsulfanyl)-4-phenyl-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)pentanamide,

5-[4-allyl-5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)pentanamide,

5-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)pentanamide,

5-[5-[(3-chlorobenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)pentanamide,

N-benzyl-5-{4-(3-chlorophenyl)-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

5-{4-allyl-5-[(3-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

N-(1,3-benzodioxol-5-ylmethyl)-5-[5-[(2-methylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)pentanamide,

5-{5-[(2-fluorobenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

5-[5-[(3-chlorobenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-(4-fluorobenzyl)pentanamide,

N-benzyl-5-{4-(3-chlorophenyl)-5-[(2,3,4,5,6-pentafluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

5-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(3-methoxypropyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)pentanamide,

5-{4-(3-chlorophenyl)-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(tetrahydro-2-furanylmethyl)pentanamide,

N-benzyl-5-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-{5-[(3-chlorobenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-(4-fluorobenzyl)pentanamide,

5-{4-(3-chlorophenyl)-5-[(3-cyanobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

5-{4-(3-chlorophenyl)-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(tetrahydro-2-furanylmethyl)pentanamide,

5-[5-(benzylsulfanyl)-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)pentanamide,

5-{5-[(3,5-dimethylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-(2-methoxyethyl)pentanamide,

5-[5-[(3-methylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)pentanamide,

N-allyl-5-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-[5-[(2-chloro-4-fluorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-isobutylpentanamide,

N-butyl-5-{5-[(3,5-dimethylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

5-{4-(3-chlorophenyl)-5-[(2,3,4,5,6-pentafluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

5-{5-[(3,5-dimethylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-[3-(2-oxo-1-pyrrolidinyl)propyl]pentanamide,

5-{5-[(3,5-dimethylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

5-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(3-methoxypropyl)-4H-1,2,4-triazol-3-yl]-N-(4-fluorobenzyl)pentanamide,

5-[5-[(3-chlorobenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-propylpentanamide,

5-{4-(3-chlorophenyl)-5-[(3-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

5-{4-allyl-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

5-[5-[(2-fluorobenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)pentanamide,

N-(4-fluorobenzyl)-5-{4-(3-methoxypropyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

5-{4-(3-chlorophenyl)-5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(4-fluorobenzyl)pentanamide,

5-{4-(3-chlorophenyl)-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(4-methoxybenzyl)pentanamide,

N-(4-methoxybenzyl)-5-{5-[(4-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

5-[5-[(3-chlorobenzyl)sulfanyl]-4-(tetrahydro-2-furanylmethyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)pentanamide,

5-{4-(3-chlorophenyl)-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-isobutylpentanamide,

5-{4-(3-methoxyphenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)pentanamide,

5-[5-[(2-chloro-4-fluorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(tetrahydro-2-furanylmethyl)pentanamide,

N-benzyl-5-{5-[(3-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

N-benzyl-5-[5-[(2-chloro-4-fluorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]pentanamide,

N-(4-fluorobenzyl)-5-[5-[(2-methylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-[5-[(3-chlorobenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-isobutylpentanamide,

N-(cyclopropylmethyl)-5-{5-[(3-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

5-{4-(3-methoxyphenyl)-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-propylpentanamide,

5-{5-[(3,5-dimethylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-(3-methoxypropyl)pentanamide,

N-benzyl-5-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-{5-[(3-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)pentanamide,

N-(4-fluorobenzyl)-5-{5-[(3-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

N-(cyclopropylmethyl)-5-{5-[(3,5-dimethylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

5-{5-[(3,5-dimethylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-propylpentanamide,

5-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)pentanamide,

N-benzyl-5-{4-(3-chlorophenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

N-benzyl-5-{5-[(4-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

5-{4-(3-chlorophenyl)-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(4-methoxybenzyl)pentanamide,

5-{4-(3-chlorophenyl)-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)pentanamide,

5-{4-(3-chlorophenyl)-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-[3-(2-oxo-1-pyrrolidinyl)propyl]pentanamide,

5-{4-(3-chlorophenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)pentanamide,

55-[5-[(3-fluorobenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)pentanamide,

5-{4-(3-chlorophenyl)-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

5-{4-allyl-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(4-fluorobenzyl)pentanamide,

N-benzyl-5-{4-(3-chlorophenyl)-5-[(2-oxo-2-phenylethyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

5-{4-(3-chlorophenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-[3-(2-oxo-1-pyrrolidinyl)propyl]pentanamide,

N-(cyclopropylmethyl)-5-{4-(3-methoxyphenyl)-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

5-{5-[(3-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-[3-(2-oxo-1-pyrrolidinyl)propyl]pentanamide,

N-allyl-5-{4-(3-chlorophenyl)-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

N-allyl-5-[5-[(2-chloro-4-fluorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-{4-(3-chlorophenyl)-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-isobutylpentanamide,

N-(4-fluorobenzyl)-5-{5-[(4-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

5-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methoxypropyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)pentanamide,

5-[5-[(2-chloro-4-fluorobenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-propylpentanamide,

N-benzyl-5-{4-(3-chlorophenyl)-5-[(3-cyanobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

5-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-propylpentanamide,

N-(2-methoxyethyl)-5-{5-[(3-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

N-[3-(2-oxo-1-pyrrolidinyl)propyl]-5-(4-phenyl-5-{[4-(trifluoromethyl)benzyl]sulfanyl}-4H-1,2,4-triazol-3-yl)pentanamide,

5-{5-[(3,5-dimethylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)pentanamide,

N-benzyl-5-{5-[(3,5-dimethylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

N-(4-fluorobenzyl)-5-[5-[(4-methylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-{4-(3-chlorophenyl)-5-[(2-oxo-2-phenylethyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(4-methoxybenzyl)pentanamide,

N-(cyclopropylmethyl)-5-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]pentanamide,

N-butyl-5-{5-[(3-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

5-{4-(3-methoxyphenyl)-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-[3-(2-oxo-1-pyrrolidinyl)propyl]pentanamide,

5-[5-(benzylsulfanyl)-4-phenyl-4H-1,2,4-triazol-3-yl]-N-(4-fluorobenzyl)pentanamide,

5-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)pentanamide,

5-[5-[(4-fluorobenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)pentanamide,

N-allyl-5-{5-[(3,5-dimethylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

N-(2-methoxybenzyl)-5-{5-[(4-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide, N-butyl-5-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(cyclopropylmethyl)pentanamide,

N-(4-fluorobenzyl)-5-[5-[(3-methylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]pentanamide,

N-(cyclopropylmethyl)-5-(4-phenyl-5-{[4-(trifluoromethyl)benzyl]sulfanyl}-4H-1,2,4-triazol-3-yl)pentanamide,

5-{4-allyl-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(4-fluorobenzyl)pentanamide,

N-isobutyl-5-[5-[(2-methylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-[3-(2-oxo-1-pyrrolidinyl)propyl]pentanamide,

5-[5-[(2-chloro-4-fluorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)pentanamide,

5-{5-[(3-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-propylpentanamide,

5-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(cyclopropylmethyl)pentanamide,

5-{4-(3-chlorophenyl)-5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)pentanamide,

N-(2-methoxyethyl)-5-{4-(3-methoxyphenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

5-{4-(3-chlorophenyl)-5-[(3-cyanobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(4-fluorobenzyl)pentanamide

5-{5-[(3-chlorobenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-isobutylpentanamide,

5-[5-(benzylsulfanyl)-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-phenylethyl)pentanamide,

N-allyl-5-{4-(3-chlorophenyl)-5-[(2,3,4,5,6-pentafluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

N-(2-methoxybenzyl)-5-[5-[(2-methylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-(4-fluorobenzyl)pentanamide,

N-isobutyl-5-{5-[(4-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

N-isobutyl-5-{5-[(3-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

5-{4-benzyl-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-[3-(2-oxo-1-pyrrolidinyl)propyl]pentanamide,

N-benzyl-5-{4-(3-methoxypropyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

5-{4-(3-chlorophenyl)-5-[(2,3,4,5,6-pentafluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-isobutylpentanamide,

N-(4-methoxybenzyl)-5-[5-[(2,3,4,5,6-pentafluorobenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]pentanamide,

N-benzyl-5-[5-(benzylsulfanyl)-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-[5-(butylsulfanyl)-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-isobutylpentanamide,

N-(cyclopropylmethyl)-5-{4-(3-methoxyphenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

5-{4-allyl-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)pentanamide,

5-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-(4-methoxybenzyl)pentanamide,

N-benzyl-5-{4-(3-chlorophenyl)-5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

5-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxyethyl)pentanamide,

N-(cyclopropylmethyl)-5-{4-(3-methoxyphenyl)-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

5-{4-(3-chlorophenyl)-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(4-fluorobenzyl)pentanamide,

5-[5-[(3-chlorobenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-(tetrahydro-2-furanylmethyl)pentanamide,

5-{4-(3-chlorophenyl)-5-[(2,3,4,5,6-pentafluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(4-methoxybenzyl)pentanamide,

5-[5-(butylsulfanyl)-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxyethyl)pentanamide,

N-benzyl-5-[5-(benzylsulfanyl)-4-phenyl-4H-1,2,4-triazol-3-yl]pentanamide,

5-{5-[(3,5-dimethylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-isobutylpentanamide,

5-{5-[(4-fluorobenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

5-{4-benzyl-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-[3-(2-oxo-1-pyrrolidinyl)propyl]pentanamide,

5-(4-(3-chlorophenyl)-5-{[(2E)-3-phenyl-2-propenyl]sulfanyl}-4H-1,2,4-triazol-3-yl)-N-isobutylpentanamide,

5-{4-(3-chlorophenyl)-5-[(3-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)pentanamide,

5-[5-[(2-methylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-propylpentanamide,

N-allyl-5-{4-(3-chlorophenyl)-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

N-butyl-5-(4-phenyl-5-{[4-(trifluoromethyl)benzyl]sulfanyl}-4H-1,2,4-triazol-3-yl)pentanamide,

5-{5-[(3-chlorobenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-(tetrahydro-2-furanylmethyl)pentanamide,

5-[5-[(4-fluorobenzyl)sulfanyl]-4-(3-methoxypropyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)pentanamide,

N-(3-methoxypropyl)-5-{5-[(3-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

N-isobutyl-5-[5-[(2-oxo-2-phenylethyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-{5-[(3-fluorobenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-(2-phenylethyl)pentanamide,

N-(2-methoxyethyl)-5-(4-phenyl-5-{[4-(trifluoromethyl)benzyl]sulfanyl}-4H-1,2,4-triazol-3-yl)pentanamide,

5-{5-[(4-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-(tetrahydro-2-furanylmethyl)pentanamide,

5-{4-(3-chlorophenyl)-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-propylpentanamide,

N-butyl-5-{4-(3-chlorophenyl)-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

5-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(3-methoxypropyl)pentanamide,

5-{4-(3-chlorophenyl)-5-[(2-oxo-2-phenylethyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(tetrahydro-2-furanylmethyl)pentanamide,

5-{5-[(3,5-dimethylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-(tetrahydro-2-furanylmethyl)pentanamide,

N-(3-methoxypropyl)-5-(4-phenyl-5-{[4-(trifluoromethyl)benzyl]sulfanyl}-4H-1,2,4-triazol-3-yl)pentanamide,

5-{4-(3-chlorophenyl)-5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

5-(4-(3-chlorophenyl)-5-{[4-(trifluoromethyl)benzyl]sulfanyl}-4H-1,2,4-triazol-3-yl)-N-[3-(2-oxo-1-pyrrolidinyl)propyl]pentanamide,

N-(4-fluorobenzyl)-5-[5-[(2-fluorobenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-[5-[(2-chloro-4-fluorobenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)pentanamide,

N-benzyl-5-[5-[(3-methylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-{4-(3-chlorophenyl)-5-[(3-cyanobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(4-methoxybenzyl)pentanamide,

5-{4-(3-chlorophenyl)-5-[(2-oxo-2-phenylethyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-isobutylpentanamide,

5-{4-benzyl-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxyethyl)pentanamide,

N-(1,3-benzodioxol-5-ylmethyl)-5-[5-[(3-chlorobenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-[5-[(3-chlorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(tetrahydro-2-furanylmethyl)pentanamide,

N-(4-methoxybenzyl)-5-[5-[(2-methylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-{4-(3-chlorophenyl)-5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-isobutylpentanamide,

5-(4-phenyl-5-{[4-(trifluoromethyl)benzyl]sulfanyl}-4H-1,2,4-triazol-3-yl)-N-propylpentanamide,

5-{4-allyl-5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

5-[5-(benzylsulfanyl)-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)pentanamide, N-benzyl-5-{4-(3-chlorophenyl)-5-[(3-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

N-(2-methoxybenzyl)-5-(4-(2-phenylethyl)-5-{[(2E)-3-phenyl-2-propenyl]sulfanyl}-4H-1,2,4-triazol-3-yl)pentanamide,

5-{4-(3-chlorophenyl)-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-propylpentanamide,

5-{4-(3-chlorophenyl)-5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(3-methoxypropyl)pentanamide,

N-butyl-5-{4-(3-chlorophenyl)-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}pentanamide,

N-benzyl-5-{5-[(2-methylbenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}pentanamide,

5-[5-[(3,5-dimethylbenzyl)sulfanyl]-4-(3-methoxyphenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxyethyl)pentanamide,

5-{4-(3-chlorophenyl)-5-[(3,5-dimethylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-isobutylpentanamide,

5-[5-(butylsulfanyl)-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(2-methoxybenzyl)pentanamide,

5-{4-allyl-5-[(3-chlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-benzylpentanamide,

5-{5-[(3-cyanobenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide,

5-{4-allyl-5-[(3-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-benzylpentanamide,

N-(1,3-benzodioxol-5-ylmethyl)-5-[5-[(2-fluorobenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-{4-allyl-5-[(3-chlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(1,3-benzodioxol-5-ylmethyl)pentanamide,

5-[5-[(3-methylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-propylpentanamide,

5-[5-[(2-fluorobenzyl)sulfanyl]-4-(tetrahydro-2-furanylmethyl)-4H-1,2,4-triazol-3-yl]-N-(3-methoxypropyl)pentanamide,

N-(2-methoxybenzyl)-5-[5-[(4-methylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]pentanamide,

5-[5-[(2-chloro-4-fluorobenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-(4-methoxybenzyl)pentanamide,

5-{5-[(3-chlorobenzyl)sulfanyl]-4-phenyl-4H-1,2,4-triazol-3-yl}-N-propylpentanamide,

5-[5-[(4-methylbenzyl)sulfanyl]-4-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-N-(tetrahydro-2-furanylmethyl)pentanamide,

5-{4-(3-chlorophenyl)-5-[(2-phenylethyl)sulfanyl]-4H-1,2,4-triazol-3-yl}-N-(2-methoxybenzyl)pentanamide and

5-[5-[(2-chloro-4-fluorobenzyl)sulfanyl]-4-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl]-N-(cyclopropylmethyl)pentanamide.

7. A pharmaceutical composition comprising the triazole derivative according to claim 1 and a pharmaceutically acceptable carrier, diluent or excipient thereof.

8. A process for the preparation of the triazole derivative according to claim 1 , comprising reacting a nucleophilic group of formula R 4 SH, wherein R 4 is defined as in claim 1 , with a triazole of formula XXXIII

wherein Z is a leaving group, and R 1 , R 2 , R 3 , A and n are defined as in claim 1 .

9. The process according to claim 8 , wherein the leaving group Z of formula XXXIII is Cl.

10. The process according to claim 8 , wherein the leaving group Z of formula XXXIII is SO 2 Me.

11. A triazole derivative of formula XXXIII:

wherein

R 1 and R 2 are independently selected from the group consisting of H, C 1 -C 6 -alkyl, aryl C 1 -C 6 -alkyl, heteroarylC 1 -C 6 -alkyl, C 3 -C 6 -cycloalkyl C 1 -C 6 -alkyl, and C 3 -C 6 -heterocycloarlkyl C 1 -C 6 -alkyl;

R 1 and R 2 , together with the nitrogen atom they are linked to, form a substituted or unsubstituted 5-8 membered saturated, partially unsaturated or aromatic ring containing optionally one or more additional heteroatoms selected from O, N, S;

A is C(O);

R 3 is selected from the group consisting of H, C 1 -C 6 -alkyl, aryl C 1 -C 6 -alkyl, heteroaryl C 1 -C 6 -alkyl, aryl, heteroaryl, C e -C 6 -cycloalkyl C 1 -C 6 -alkyl, C 3 -C 6 -heterocycloalkyl C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl,

B is S;

R 4 and R 5 are selected from the group consisting of H, C 1 -C 6 -alkyl, aryl C 1 -C 6 -alkyl, heteroaryl C 1 -C 6 -alkyl, acyl, aryl acyl, heteroaryl acyl, C 3 -C 6 -cycloalkyl C 1 -C 6 -alkyl, C 3 -C 6 -heterocycloalkyl C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl;

n is an integer from 2 to 10, and

Z is Cl or SO 2 Me.

Assignments (3)
CHANGE OF NAME Recorded Dec 3, 2009
From: LABORATOIRES SERONO SA
To: MERCK SERONO SA
Reel/Frame 023599/0944 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 11, 2007
From: APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.
To: LABORATOIRES SERONO SA
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ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 29, 2005
From: QUATTROPANI, ANNA; SCHWARZ, MATTHIAS; THOMAS, RUSSELL J.; COULTER, THOMAS
To: APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.
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