# US 8,772,336 B2 · Cathepsin cysteine protease inhibitors

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- Number: US 8,772,336 B2
- Document ID: US8772336B2
- Status: Granted
- Kind: B2
- Application number: 13/649,670
- Filed: 2012-10-11
- Published: 2013-02-07
- Granted: 2014-07-08
- Earliest claimed: 2002-03-05
- Assignees: Merck Frosst Canada, Inc.; Axys Pharmaceuticals, Inc.
- Applicants: Merck Frosst Canada Inc.; Axys Pharmaceuticals, Inc.
- Inventors: Christopher I. Bayly; Cameron Black; Serge Leger; Chun Sing Li; Dan McKay; Christophe Mellon; Jacques Yves Gauthier; Vouy-Linh Truong; Cheuk Lau; Michel Therien; Michael J. Green; Bernard L. Hirschbein; James William Janc; James T. Palmer; Chitra I. Baskaran
- Web page: https://patentgrep.com/patent/US8772336B2

## CPC

- A61P 1/02: Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
- C07C 237/20: the carbon skeleton containing six-membered aromatic rings
- A61K 31/165: having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K 31/18: Sulfonamides (compounds containing a para-N-benzene-sulfonyl-N- group A61K31/63)
- A61K 31/4174: Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
- A61K 31/426: 1,3-Thiazoles
- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- A61K 31/4418: having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
- A61K 31/495: having six-membered rings with two {or more} nitrogen atoms as the only ring heteroatoms, e.g. piperazine {or tetrazines}(A61K31/48 takes precedence {; with three nitrogen atoms A61K31/53})
- A61P 3/14: for calcium homeostasis (vitamin D A61P3/02; parathyroid hormones A61P5/18; calcitonin A61P5/22; osteoporosis A61P19/10; bone metastasis A61P35/04)
- A61P 19/00: Drugs for skeletal disorders
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/04: for non-specific disorders of the connective tissue
- A61P 19/06: Antigout agents, e.g. antihyperuricemic or uricosuric agents
- A61P 19/08: for bone diseases, e.g. rachitism, Paget's disease
- A61P 19/10: for osteoporosis
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 35/04: specific for metastasis
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07C 255/25: Aminoacetonitriles
- C07C 255/29: containing cyano groups and acylated amino groups bound to the carbon skeleton
- C07C 255/46: to carbon atoms of non-condensed rings
- C07C 255/58: containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
- C07C 259/10: having carbon atoms of hydroxamic groups bound to carbon atoms of six-membered aromatic rings
- C07C 311/37: having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
- C07C 317/32: with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
- C07D 209/08: with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
- C07D 213/38: having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
- C07D 213/57: Nitriles
- C07D 213/64: attached in position 2 or 6
- C07D 213/70: Sulfur atoms
- C07D 213/89: with hetero atoms directly attached to the ring nitrogen atom
- C07D 215/12: with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D 231/12: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D 233/64: with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
- C07D 239/26: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D 241/12: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D 261/08: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D 263/32: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D 271/06: 1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
- C07D 277/28: Radicals substituted by nitrogen atoms
- C07D 277/30: Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D 295/135: with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
- C07D 295/155: with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
- C07D 307/52: Radicals substituted by nitrogen atoms not forming part of a nitro radical
- C07D 333/20: by nitrogen atoms (nitro, nitroso radicals C07D333/12)
- C07D 401/04: directly linked by a ring-member-to-ring-member bond
- C07D 417/04: directly linked by a ring-member-to-ring-member bond
- C07C 2601/02: with a three-membered ring
- C07C 2601/14: The ring being saturated
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

## Claims

### Claim 1

A method of treating osteoarthritis in a mammal in need thereof by administering to the mammal a therapeutically effective amount of a compound of the following chemical formula:
wherein R1 is hydrogen, C1-6 alkyl or C2-6 alkenyl wherein said alkyl and alkenyl groups are optionally substituted with one to six halo, C3-6 cycloalkyl, —SR9, —SR12, —SOR9, —SOR12, —SO2R9, —SO2R12, —SO2CH(R12)(R11), —OR12, —OR9, —N(R12)2, aryl, heteroaryl or heterocyclyl wherein said aryl, heteroaryl and heterocyclyl groups are optionally substituted with one or two substitutents independently selected from C1-6 alkyl, halo, hydroxyalkyl, hydroxy, alkoxy or keto;
R2 is hydrogen, C1-6 alkyl or C2-6 alkenyl wherein said alkyl and alkenyl groups are optionally substituted with one to six halo, C3-6 cycloalkyl, —SR9, —SR12, —SOR9, —SOR12, —SO2R9, —SO2R12, —SO2CH(R12)(R11), —OR12, —OR9, —N(R12)2, aryl, heteroaryl or heterocyclyl wherein said aryl, heteroaryl and heterocyclyl groups are optionally substituted with one or two substitutents independently selected from C1-6 alkyl, halo, hydroxyalkyl, hydroxy, alkoxy or keto;
or R1 and R2 can be taken together with the carbon atom to which they are attached to form a C3-8 cycloalkyl or heterocyclyl ring wherein said ring system is optionally substituted with one or two substituents independently selected from C1-6 alkyl, hydroxyalkyl, haloalkyl, or halo;
R3 is hydrogen, C1-6 alkyl or C2-6 alkenyl wherein said alkyl and alkenyl groups are optionally substituted with C3-6 cycloalkyl or one to six halo;
R4 is hydrogen, C1-6 alkyl or C2-6 alkenyl wherein said alkyl and alkenyl groups are optionally substituted with C3-6 cycloalkyl or one to six halo;
or R3 and R4 can be taken together with the carbon atom to which they are attached to form a C3-8 cycloalkyl ring, C5-8 cycloalkenyl ring, or five to seven membered heterocyclyl wherein said cycloalkyl, cycloalkenyl and heterocyclyl groups are optionally substituted with one or two substitutents independently selected from C1-6 alkyl, halo, hydroxyalkyl, hydroxy, alkoxy or keto;
R5 is selected from hydrogen or C1-6 alkyl substituted with 1-6 halo;
R6 is aryl, heteroaryl, C1-6 haloalkyl, arylalkyl or heteroarylalkyl, wherein said aryl, heteroaryl, arylalkyl and heteroarylalkyl groups are optionally substituted with one, two, or three substituents independently selected from halo, C1-6 alkyl, C1-6 haloalkyl, C3-6 cycloalkyl, haloalkoxy, —SR9, —SR12, —SOR9, —SOR12, —SO2R9, —SO2R12, —SO2CH(R12)(R11), —OR12, —N(R10)(R11), cyano, or aryl which is optionally substituted with —SO2R12;
each D is independently C1-3 alkyl, C2-3 alkenyl, C2-3 alkynyl, aryl, heteroaryl, C3-8 cycloalkyl or heterocyclyl wherein each said aryl, heteroaryl, cycloalkyl and heterocyclyl groups, which may be monocyclic or bicyclic, is optionally substituted on either the carbon or the heteroatom with one to five substituents independently selected from C1-6 alkyl, haloalkyl, halo, keto, alkoxy, —SR9, —SR12, —OR9, —OR12, N(R12)2, —SO2R9, or —SO2R10;
R7 is hydrogen;
R8 is hydrogen or C1-6 alkyl;
or R4 and R8 or can be taken together with any of the atoms to which they may be attached or are between them to form a 4-10 membered heterocyclyl ring system wherein said ring system, which may be monocyclic or bicyclic, is optionally substituted with one or two substituents independently selected from C1-6 alkyl, halo, hydroxyalkyl, hydroxy, keto, —OR10, —SR10 or —N(R10)2;
R9 is selected from the group consisting of hydrogen, aryl, aryl(C1-4)alkyl, heteroaryl, heteroaryl(C1-4)alkyl, C3-8cycloalkyl, C3-8cycloalkyl(C1-4)alkyl, and heterocyclyl(C1-4)alkyl wherein said groups can be optionally substituted with one, two, or three substituents independently selected from halo, alkoxy or —SO2R12;
R10 is hydrogen or C1-6 alkyl
R11 is hydrogen or C1-6 alkyl;
R12 is hydrogen or C1-6 alkyl which is optionally substituted with one, two, or three substituents independently selected from halo, alkoxy, cyano, —NR10 or —SR10;
n is independently selected from an integer from one to three;
or a pharmaceutically acceptable salt, stereoisomer or N-oxide derivative thereof.

### Claim 2 (depends on 1)

The method of claim 1 wherein R1 is hydrogen and R2 is hydrogen, or R1 and R2 can be taken together with the carbon atom to which they are attached to form a C3-8 cycloalkyl ring wherein said ring system is optionally substituted with one or two substituents selected from C1-6 alkyl or halo, or a pharmaceutically acceptable salt, stereoisomer or N-oxide derivative thereof.

### Claim 3 (depends on 2)

The method of claim 2 wherein R3 is C1-6 alkyl which is optionally substituted with one to six halo and R4 is hydrogen, or a pharmaceutically acceptable salt, stereoisomer or N-oxide derivative thereof.

### Claim 4 (depends on 3)

The method of claim 3 wherein R3 is n-propyl, isobutyl, 2-fluoro-2-methylpropyl, 2-trifluoromethylpropyl, 3-fluoro-2-(2-fluoromethyl)propyl, 2,2-difluoroethyl, 2,2-difluoropropyl, 3,3,3-trifluoropropyl, or 2,2-dichloroethyl and R4 is hydrogen; or a pharmaceutically acceptable salt, stereoisomer or N-oxide derivative thereof.

### Claim 5 (depends on 3)

The method of claim 3 wherein R5 is hydrogen and R6 is aryl or heteroaryl wherein said aryl or heteroaryl are optionally substituted with one, two or three substituents selected from halo or —SO2R12; or a pharmaceutically acceptable salt, stereoisomer or N-oxide derivative thereof.

### Claim 6 (depends on 3)

The method of claim 3 wherein R5 is hydrogen and R6 is C1-6 haloalkyl; or a pharmaceutically acceptable salt, stereoisomer or N-oxide derivative thereof.

### Claim 7 (depends on 6)

The method of claim 6 wherein R5 is hydrogen and R6 is trifluoromethyl or 3,3,3,2,2-pentafluoroethyl; or a pharmaceutically acceptable salt, stereoisomer or N-oxide derivative thereof.

### Claim 8 (depends on 6)

The method of claim 6 wherein n is two, each D is independently aryl or heteroaryl and R7 is —SOmCH(R10)(R11) or —SOm(Rc)(Rd), Rc and Rd are each independently hydrogen or C1-6 alkyl; or a pharmaceutically acceptable salt, stereoisomer or N-oxide derivative thereof.

### Claim 9 (depends on 1)

The method of claim 1 wherein the compound is selected from:
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-(2,2,2-trifluoro-1-phenylethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-[2,2,2-trifluoro-1-(4-fluoro-3-methylphenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1R)-2,2,2-trifluoro-1-(4-pyridin-3-ylphenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-pyridin-3-ylphenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1R)-2,2,2-trifluoro-1-(4-pyridin-4-ylphenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-pyridin-4-ylphenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1R)-2,2,2-trifluoro-1-(4-{[4-(2-fluoroethyl)piperazin-1-yl]carbonyl}phenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[2,2,2-trifluoro-1-(4-{[4-(2-fluoroethyl)piperazin-1-yl]carbonyl}phenyl)ethyl]-L-leucinamide;
N2-[1-(1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[4-(3-hydroxy-3-methylbut-1-ynyl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(3-hydroxy-3-methylbutyl)phenyl]ethyl}-L-leucinamide;
N2-[(1S)-1-(4-bromophenyl)-2,2,3,3,3-pentafluoropropyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,3,3,3-pentafluoro-1-(4-pyridin-4-ylphenyl)propyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4′-fluoro-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-((1S)-2,2,2-trifluoro-1-{4-[(1E)-3-hydroxy-3-methylbut-1-enyl]phenyl}ethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,3,3,3-pentafluoro-1-[4′-(methylthio)-1,1′-biphenyl-4-yl]propyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,3,3,3-pentafluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]propyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(1-oxidopyridin-3-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(morpholin-4-ylcarbonyl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-{[methoxy(methyl)amino]carbonyl}phenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-thien-3-ylphenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(4-methylpyridin-2-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(5-methylpyridin-2-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(2′-fluoro-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-2,2,2-trifluoroethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(hydroxymethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-[(1S)-1-(4′-cyano-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2[(1S)-1-(3′,4′-difluoro-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-L-leucinamide;
4′-{1-[1-(Cyanomethyl-carbamoyl)-3-methyl-butylamino]-2,2,2-trifluoro-ethyl}-biphenyl-2-carboxylic acid methyl ester;
4′-{1-[1-(Cyanomethyl-carbamoyl)-3-methyl-butylamino]-2,2,2-trifluoro-ethyl}-biphenyl-3-carboxylic acid methyl ester;
N1-(cyanomethyl)-N2-[(1S)-1-(3′,4′-dimethoxy-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-L leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[2′-(trifluoromethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-1-(3′,4′-dichloro-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(3′-formyl-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(2-oxo-2,3-dihydro-1,3-benzothiazol-6-yl)phenyl]ethyl}-L-leucinamide;
N2-{(1S)-1-[4-(5-bromopyridin-3-yl)phenyl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(trifluoromethoxy)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(1H-indol-4-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-pyrimidin-5-ylphenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-quinolin-3-ylphenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(1,3-thiazol-2-yl)phenyl]ethyl}-L-leucinamide;
4′-{1-[1-(Cyanomethyl-carbamoyl)-3-methyl-butylamino]-2,2,2-trifluoro-ethyl}-biphenyl-4-carboxylic acid methyl ester;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-pyrimidin-2-ylphenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(3-methylpyridin-2-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(3-furyl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-((1S)-2,2,2-trifluoro-1-{4-[3-(trifluoromethyl)pyridin-2-yl]phenyl}ethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-((1S)-2,2,2-trifluoro-1-{4-[4-(trifluoromethyl)pyridin-2-yl]phenyl}ethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-((1S)-2,2,2-trifluoro-1-{4-[5-(trifluoromethyl)pyridin-2-yl]phenyl}ethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(3′-methoxy-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1R)-2,2,2-trifluoro-1-(3′-methoxy-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N2-{(1S)-1-[4′-(acetylamino)-3′-fluoro-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(3-methylthien-2-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(3′-fluoro-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N2-{(1S)-1-[4-(5-acetylthien-2-yl)phenyl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N2-[(1S)-1-(3′-acetyl-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[3′-(trifluoromethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(5′-fluoro-2′-methoxy-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-1-(3′,5′-difluoro-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(2′,3′,5′-trifluoro-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
3-(4′-{1-[1-(Cyanomethyl-carbamoyl)-3-methyl-butylamino]-2,2,2-trifluoro-ethyl}-biphenyl-3-yl)-acrylic acid;
N2-{(1S)-1-[4-(9-anthryl)phenyl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N2-[(1S)-1-(4′-benzoyl-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-L-leucinamide;
N2-[(1S)-1-(3′-acetyl-4′-hydroxy-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-1-[2′-(cyanomethyl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[4′-(methylsulfinyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[2,2,2-trifluoro-1-(4-morpholin-4-ylphenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{(1R)-2,2,2-trifluoro-1-[4-(6-methylpyridin-3-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(6-methylpyridin-3-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[2,2,2-trifluoro-1-(5-phenylthien-2-yl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[2,2,2-trifluoro-1-(4-quinolin-8-ylphenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-pyridin-2-ylphenyl)ethyl]-L-leucinamide;
N2-{1-[4′-(aminosulfonyl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N2-{(1S)-1-[4′-(aminosulfonyl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylthio)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1R)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(morpholin-4-ylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(isopropylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-{(1S)-1-[4′-(aminosulfonyl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N2-((1S)-1-{4′-[(acetylamino)sulfonyl]-1,1′-biphenyl-4-yl}-2,2,2-trifluoroethyl)-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[2′-methyl-4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-[1-(5-bromothien-2-yl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-L-leucinamide;
N2-[1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-L-leucinamide;
4-(4′-{1-[1-(Cyanomethyl-carbamoyl)-3-methyl-butylamino]-2,2,2-trifluoro-ethyl}-biphenyl-4-yl)-piperazine-1-carboxylic acid tert-butyl ester;
N1-(cyanomethyl)-N2-[2,2,2-trifluoro-1-(4′-piperazin-1-yl-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-(2,2,2-trifluoro-1-{4′-[4-(2-hydroxyethyl)piperazin-1-yl]-1,1′-biphenyl-4-yl}ethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-(2,2,2-trifluoro-1-{4′-[4-(2-hydroxy-2-methylpropyl)piperazin-1-yl]-1,1′-biphenyl-4-yl}ethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-(1-{4-[(dimethylamino)carbonyl]phenyl}-2,2,2-trifluoroethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-[2,2,2-trifluoro-1-(4′-piperazin-1-yl-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-(1-{4-[(cyclopropylamino)carbonyl]phenyl}-2,2,2-trifluoroethyl)-L-leucinamide;
4-{1-[1-(Cyanomethyl-carbamoyl)-3-methyl-butylamino]-2,2,2-trifluoro-ethyl}-benzoic acid;
N1-(cyanomethyl)-N2-(2,2,2-trifluoro-1-{4′-[4-(2-fluoroethyl)piperazin-1-yl]-1,1′-biphenyl-4-yl}ethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-(2,2,2-trifluoro-1-{4-[(4-methylpiperazin-1-yl)carbonyl]phenyl}ethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-[2,2,2-trifluoro-1-(4-{[4-(2-hydroxy-2-methylpropyl)piperazin-1-yl]carbonyl}phenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(2-methyl-1,3-thiazol-4-yl)phenyl]ethyl}-L-leucinamide;
N2-{1-[4-(3-tert-butyl-1,2,4-triazin-5-yl)phenyl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-[2,2,2-trifluoro-1-(4-{2-[3-(methylsulfonyl)phenyl]-1,3-thiazol-4-yl}phenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-((1S)-2,2,2-trifluoro-1-{4-[2-(1H-pyrazol-4-yl)-1,3-thiazol-4-yl]phenyl}ethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-(2,2,2-trifluoro-1-{4′-[4-(methylsulfonyl)piperazin-1-yl]-1,1′-biphenyl-4-yl}ethyl)-L-leucinamide;
N2-[1-(3-bromophenyl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[4′-(methylthio)-1,1′-biphenyl-3-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[2,2,2-trifluoro-1-(3-pyridin-4-ylphenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[2,2,2-trifluoro-1-(4′-piperazin-1-yl-1,1′-biphenyl-3-yl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-3-yl]ethyl}-L-leucinamide;
N-(cyanomethyl)-1-[(2,2,2-trifluoro-1-phenylethyl)amino]cyclohexanecarboxamide;
1-{[1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino}-N-(cyanomethyl)cyclohexanecarboxamide;
N-(cyanomethyl)-1-{[2,2,2-trifluoro-1-(4′-piperazin-1-yl-1,1′-biphenyl-4-yl)ethyl]amino}cyclohexanecarboxamide;
N1-(cyanomethyl)-N2-[2,2,2-trifluoro-1-(4-piperidin-4-ylphenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[4-(4-pyridin-2-ylpiperazin-1-yl)phenyl]ethyl}-L-leucinamide;
N2-[1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-3-cyclopropylalaninamide;
N1-(cyanomethyl)-3-cyclopropyl-N2-[2,2,2-trifluoro-1-(4-pyridin-4-ylphenyl)ethyl]alaninamide;
N1-(cyanomethyl)-N2-[2,2,2-trifluoro-1-(4′-pyridin-4-yl-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1R)-2,2,2-trifluoro-1-(1,3-thiazol-2-yl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4′-methoxy-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-methoxyphenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4′-pyridin-4-yl-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-phenoxyphenyl)ethyl]-L-leucinamide;
N2-[(1S)-1-(4′-bromo-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-L-leucinamide;
N2-{(1S)-1-[4-(4-chloropyridin-3-yl)phenyl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N2-{(1S)-1-[4′-(acetylamino)-2′-methyl-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N2-[(1S)-1-(1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(6-methoxypyridin-3-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(6-methoxypyridin-2-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4″-(methylsulfonyl)-1,1′:4′,1″-terphenyl-4-yl]ethyl}-L-leucinamide;
N2-[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-3-(1-methylcyclopropyl)-L-alaninamide;
N1-(cyanomethyl)-3-(1-methylcyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-alaninamide;
N1-(cyanomethyl)-3-(1-methylcyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylthio)-1,1′-biphenyl-4-yl]ethyl}-L-alaninamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4′-methyl-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N2-[(1S)-1-(4′-acetyl-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(hydroxymethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-[1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-D-leucinamide;
N1-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-D-leucinamide;
N1-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[4′-(morpholin-4-ylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-D-leucinamide;
N1-(cyanomethyl)-N2-(2,2,2-trifluoro-1-{4′-[(methylamino)sulfonyl]-1,1′-biphenyl-4-yl}ethyl)-D-leucinamide;
N1-(cyanomethyl)-N2-{(1R)-2,2,2-trifluoro-1-[4-(1-oxidopyridin-4-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[4-(1-oxidopyridin-4-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-(2,2,2-trifluoro-1-{4-[6-(1-hydroxy-1-methylethyl)-1-oxidopyridin-3-yl]phenyl}ethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-(2,2,2-trifluoro-1-{4-[6-(methylsulfonyl)pyridin-3-yl]phenyl}ethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-(2,2,2-trifluoro-1-{4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]phenyl}ethyl)-L-leucinamide;
N2-[1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(cyanomethyl)-N2-[2,2,2-trifluoro-1-(4-piperazin-1-ylphenyl)ethyl]-L-leucinamide;
N2-{1-[3′-(acetylamino)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[4-(4-propylpiperazin-1-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[4-(piperazin-1-ylcarbonyl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[2,2,2-trifluoro-1-(4-{[4-(2-hydroxyethyl)piperazin-1-yl]carbonyl}phenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-{3-[3-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5-yl}phenyl)ethyl]-L-leucinamide;
4-{1-[1-(Cyanomethyl-carbamoyl)-3-methyl-butylamino]-2,2,2-trifluoro-ethyl}-benzoic acid methyl ester;
N1-(cyanomethyl)-N2-((1S)-2,2,2-trifluoro-1-{4-[(E)-2-quinolin-2-ylethenyl]phenyl}ethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl]ethyl}-L-leucinamide;
N2-((1S)-1-{4-[3-(5-bromopyridin-3-yl)-1,2,4-oxadiazol-5-yl]phenyl}-2,2,2-trifluoroethyl)-N1-(cyanomethyl)-L-leucinamide;
N2-[(1S)-1-(4-benzoylphenyl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(thien-2-ylcarbonyl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(1,3-thiazol-2-ylcarbonyl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-{(Z)-2-[4-(methylsulfonyl)phenyl]ethenyl}phenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-{(E)-2-[4-(methylsulfonyl)phenyl]ethenyl}phenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-isobutyrylphenyl)ethyl]-L-leucinamide;
N2-{(1S)-1-[4-(4-bromo-1,3-thiazol-2-yl)phenyl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-1-(4-cyanophenyl)-2,2,2-trifluoroethyl]-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-1-(4-ethynylphenyl)-2,2,2-trifluoroethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(2′-fluoro-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(1,3-thiazol-2-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[4′-(methylthio)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[4-(2-methylquinolin-7-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[4-(1H-indol-5-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{1-[4′-(dimethylamino)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-1-(4-{[(cyanomethyl)amino]carbonyl}phenyl)-2,2,2-trifluoroethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(1R)-1-(4-{[(cyanomethyl)amino]carbonyl}phenyl)-2,2,2-trifluoroethyl]-L-leucinamide;
N2-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[3′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
4′-{1-[1-(Cyanomethyl-carbamoyl)-3-methyl-butylamino]-2,2,2-trifluoro-ethyl}-biphenyl-4-carboxylic acid;
4′-{1-[1-(Cyanomethyl-carbamoyl)-3-methyl-butylamino]-2,2,2-trifluoro-ethyl}-biphenyl-4-carboxylic acid methoxy-methyl-amide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-({[4-(methylsulfonyl)benzyl]thio}methyl)phenyl]ethyl}-L-leucinamide;
N2-{(1S)-1-[4-(5-chloropyridin-2-yl)phenyl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N2-{(1S)-1-[3′-(aminosulfonyl)-4′-bromo-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N2-{(1S)-1-[4′-bromo-3′-(methylsulfonyl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-((1S)-2,2,2-trifluoro-1-{4-[5-methyl-6-(methylsulfonyl)pyridin-3-yl]phenyl}ethyl)-L-leucinamide;
N2-[(1S)-1-(4-{5-chloro-3-[4-(methylsulfonyl)phenyl]pyridin-2-yl}phenyl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-((1S)-2,2,2-trifluoro-1-{4-[(phenylthio)methyl]phenyl}ethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-((1S)-2,2,2-trifluoro-1-{4′-[(trifluoromethyl)sulfonyl]-1,1′-biphenyl-4-yl}ethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-{[(4-fluorobenzoyl)amino]methyl}phenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(methylsulfonyl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-1-[4′-(ethylsulfonyl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-L-leucinamide;
N2-((1S)-1-{4-[({[3-(2-chloro-6-fluorophenyl)-5-methylisoxazol-4-yl]carbonyl}amino)methyl]phenyl}-2,2,2-trifluoroethyl)-N1-(cyanomethyl)-L-leucinamide;
N2-((1S)-1-{4-[(9-chloro-3-methyl-4-oxoisoxazolo[4,3-c]quinolin-5(4H)-yl)methyl]phenyl}-2,2,2-trifluoroethyl)-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-methoxy-3′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-{(1S)-1-[4″-chloro-4′-(methylsulfonyl)-1,1′:2′,1″-terphenyl-4-yl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[2′-methoxy-4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-{(1S)-1-[2′-chloro-4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-((1S)-2,2,2-trifluoro-1-{4′-[(2-hydroxyethyl)thio]-1,1′-biphenyl-4-yl}ethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[3′-fluoro-4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-((1S)-2,2,2-trifluoro-1-{4′-[(2-hydroxyethyl)sulfonyl]-1,1′-biphenyl-4-yl}ethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[3′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-({2-[methoxy(methyl)amino]-2-oxoethyl}sulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-((1S)-2,2,2-trifluoro-1-{4′-[(2-hydroxy-2-methylpropyl)sulfonyl]-1,1′-biphenyl-4-yl}ethyl)-L-leucinamide;
N2-{(1S)-1-[4′-(aminosulfonyl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-N1-(1-cyanocyclopropyl)-L-leucinamide;
N2-[(4-bromophenyl)(2,4,6-trifluorophenyl)methyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-[(4-pyridin-4-ylphenyl)(2,4,6-trifluorophenyl)methyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[[4-(4-fluorobenzyl)phenyl](phenyl)methyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{phenyl[4-(pyridin-3-ylmethyl)phenyl]methyl}-L-leucinamide;
N2-{(4-bromophenyl) [4-(methylsulfonyl)phenyl]methyl}-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{[4-(methylsulfonyl)phenyl][4′-(methylthio)-1,1′-biphenyl-4-yl]methyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl][4-(methylsulfonyl)phenyl]methyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[2,2,2-trichloro-1-(4-glycoloylphenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[2-fluoro-1-(fluoromethyl)-1-phenylethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[4-(pyrrolidin-1-ylacetyl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[4-(piperazin-1-ylcarbonyl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-(2,2,2-trifluoro-1-{4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]phenyl}ethyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-3-(1-methylcyclopropyl)-N2-(2,2,2-trifluoro-1-{4-[1-(2-hydroxyethyl)prolyl]phenyl}ethyl)-L-alaninamide;
N2-[[4-(4-tert-butylpiperazin-1-yl)phenyl](pentafluorophenyl)methyl]-N1-(cyanomethyl)-L-leucinamide;
N-(cyanomethyl)-1-{1-[4-(4-methylpiperazin-1-yl)phenyl]ethyl}piperidine-2-carboxamide;
N2-[[4-(4-tert-butylpiperazin-1-yl)phenyl](pyridin-2-yl)methyl]-N1-(cyanomethyl)-L-leucinamide;
N2-{[4-(4-tert-butylpiperazin-1-yl)phenyl][5-(trifluoromethyl)pyridin-2-yl]methyl}-N1-(cyanomethyl)-L-leucinamide;
(4S)—N-(cyanomethyl)-4-methyl-1-[(1S)-1-(4-piperazin-1-ylphenyl)ethyl]-L-prolinamide;
(4S)—N-(cyanomethyl)-4-methyl-1-[(1R)-1-(4-piperazin-1-ylphenyl)ethyl]-L-prolinamide;
N-(cyanomethyl)-1-[(1S)-1-(4-piperazin-1-ylphenyl)ethyl]-L-prolinamide;
N-(cyanomethyl)-1-[(1R)-1-(4-piperazin-1-ylphenyl)ethyl]-L-prolinamide;
N-(cyanomethyl)-4,4-difluoro-1-[(1S)-1-(4-piperazin-1-ylphenyl)ethyl]-L-prolinamide;
N1-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-methylphenyl)ethyl]-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(1H-pyrazol-3-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(2-methyl-1,3-oxazol-4-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-pyrazin-2-ylphenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(2-methylpyridin-4-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(4-methylpyridin-3-yl)phenyl]ethyl}-L-leucinamide;
N2-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(1H-pyrazol-4-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-pyridin-4-ylphenyl)ethyl]-L-leucinamide;
N2-[(1S)-1-(3′-acetyl-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-(3′-fluoro-4′-methyl-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-((1S)-2,2,2-trifluoro-1-{5-[4-(1-hydroxy-1-methylethyl)phenyl]pyridin-2-yl}ethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,3,3,3-pentafluoro-1-[4′-(1-hydroxy-1-methylethyl)-1,1′-biphenyl-4-yl]propyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-[(1S)-2,2,3,3,3-pentafluoro-1-(4′-methyl-1,1′-biphenyl-4-yl)propyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,3,3,3-pentafluoro-1-[4-(6-methoxypyridin-3-yl)phenyl]propyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,3,3,3-pentafluoro-1-(2′-fluoro-1,1′-biphenyl-4-yl)propyl]-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-methoxy-3′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-{(1S)-1-[3′-(aminosulfonyl)-4′-methoxy-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(6-methoxypyridin-3-yl)phenyl]ethyl}-L-leucinamide;
N2-(cyanomethyl)-N2-{(1S)-2,2,3,3,3-pentafluoro-1-[4-(5-methylpyridin-2-yl)phenyl]propyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-((1S)-2,2,2-trifluoro-1-{4-[5-(methylsulfonyl)pyridin-2-yl]phenyl}ethyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(5-methylpyridin-2-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[2′-methyl-4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[5-(1H-pyrazol-3-yl)pyridin-2-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-(5-quinolin-5-ylpyridin-2-yl)ethyl]-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-(5-quinolin-6-ylpyridin-2-yl)ethyl]-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2-difluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-[(1S)-1-(4′-acetyl-1,1′-biphenyl-4-yl)-2,2,3,3,3-pentafluoropropyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N2-[(1S)-1-(1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N2-{(1S)-1-[4′-(aminosulfonyl)-1,1′-biphenyl-4-yl]-2,2,3,3,3-pentafluoropropyl}-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(1-ethoxyvinyl)phenyl]-2,2,2-trifluoroethyl}-L-leucinamide;
N2-[(1S)-1-(4-acetylphenyl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-isopropylphenyl)ethyl]-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-phenylethyl]-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(1-hydroxy-1-methylethyl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(1-methylcyclopropyl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-(2′,4′,6′-trimethyl-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N2-[(1S)-1-(6-chloropyridin-3-yl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl-L-leucinamide;
N2-{(1S)-1-[5-(4-acetylphenyl)pyridin-2-yl]-2,2,2-trifluoroethyl}-N1-(1-cyanocyclopropyl)-L-leucinamide;
N2-{(1S)-1-[6-(4-acetylphenyl)pyridin-3-yl]-2,2,2-trifluoroethyl}-N1-(1-cyanocyclopropyl)-L-leucinamide;
N2-{(1S)-1-[5-(3-acetylphenyl)pyridin-2-yl]-2,2,2-trifluoroethyl}-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-((1S)-2,2,2-trifluoro-1-{5-[4-(1-hydroxyethyl)phenyl]pyridin-2-yl}ethyl)-L-leucinamide;
N2-[(1S)-1-(1,1′-biphenyl-4-yl)-2,2,3,3,3-pentafluoropropyl]-N1-(cyanomethyl)-L-leucinamide;
N2-[(1S)-1-(4′-acetyl-1,1′-biphenyl-4-yl)-2,2,3,3,3-pentafluoropropyl]-N1-(cyanomethyl)-L-leucinamide;
N2-[(1S)-1-(1,1′-biphenyl-4-yl)-2,2,3,3,3-pentafluoropropyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N2-(1-benzyl-2,2,2-trifluoroethyl)-N1-(1-cyanocyclopropyl)-L-leucinamide;
N2-[(1S)-1-(4-tert-butylphenyl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N2-[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-4-methyl-L-leucinamide;
N2[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-4-methyl-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-((1S)-2,2,2-trifluoro-1-{4-[2-(1H-pyrazol-4-yl)-1,3-thiazol-4-yl]phenyl}ethyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(2-methyl-1,3-thiazol-4-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(2-methylpyridin-4-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(2-methylpyridin-3-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(6-methylpyridin-2-yl)phenyl]ethyl}-L-leucinamide;
N2-[(1S)-1-(3′-acetyl-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4-(1H-pyrazol-3-yl)phenyl]ethyl}-L-leucinamide;
N1-[(1S)-1-cyanoethyl]-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-[(1S)-1-cyano-3-(methylthio)propyl]-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-[(1S)-1-cyano-3-(methylsulfonyl)propyl]-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-[(1S)-1-(4-bromophenyl)-2,2,3,3,3-pentafluoropropyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,3,3,3-pentafluoro-1-[4-(6-methoxypyridin-2-yl)phenyl]propyl}-L-leucinamide;
N2-[(1S)-1-(5-bromopyridin-2-yl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-((1S)-2,2,2-trifluoro-1-{5-[4-(methylsulfonyl)phenyl]pyridin-2-yl}ethyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(1-hydroxy-1-methylethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-(6′-methyl-3,3′-bipyridin-6-yl)ethyl]-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(6-methoxypyridin-2-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(6-oxo-1,6-dihydropyridin-2-yl)phenyl]ethyl}-L-leucinamide;
(4S)—N1-(cyanomethyl)-5,5,5-trifluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
(4S)—N1-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
(4S)—N1-(cyanomethyl)-5,5,5-trifluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylthio)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
(4S)—N1-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylthio)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
(4S)—N2-[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-5,5,5-trifluoro-L-leucinamide;
(4S)—N2-[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-5,5,5-trifluoro-L-leucinamide;
N2-{(1S)-1-[4-(6-aminopyridin-3-yl)phenyl]-2,2,2-trifluoroethyl}-N1-(cyanomethyl)-L-leucinamide;
N2-[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,3,3,3-pentafluoro-1-[4-(6-methylpyridin-3-yl)phenyl]propyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,3,3,3-pentafluoro-1-[4-(6-methylpyridin-3-yl)phenyl]propyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(6-methylpyridin-3-yl)phenyl]ethyl}-L-leucinamide;
N1-cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(1-hydroxyethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(2,2,2-trifluoro-1-hydroxyethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,3,3,3-pentafluoro-1-[4′-(methylthio)-1,1′-biphenyl-4-yl]propyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,3,3,3-pentafluoro-1-[4′-(1-hydroxy-1-methylethyl)-1,1′-biphenyl-4-yl]propyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,3,3,3-pentafluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]propyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,3,3,3-pentafluoro-1-[4-(6-methoxypyridin-2-yl)phenyl]propyl}-L-leucinamide;
(4S)—N1-(cyanomethyl)-5,5,5-trifluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
(4S)—N1-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[(1S)-2,2,3,3,3-pentafluoro-1-(4′-methyl-1,1′-biphenyl-4-yl)propyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,3,3,3-pentafluoro-1-[4-(1,3-thiazol-2-yl)phenyl]propyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-[(1S)-1-(4-ethynylphenyl)-2,2,3,3,3-pentafluoropropyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-1-[4-(cyclopropylethynyl)phenyl]-2,2,2-trifluoroethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(cyclopropylethynyl)phenyl]-2,2,2-trifluoroethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(5-methyl-1,3-thiazol-2-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(1,3-thiazol-2-yl)phenyl]ethyl}-L-leucinamide;
N2-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(5-methyl-1,3-thiazol-2-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(cyclopropylethynyl)phenyl]-2,2,3,3,3-pentafluoropropyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(4-methyl-1,3-thiazol-2-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(4-methyl-1,3-thiazol-2-yl)phenyl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-1-[4-(4,5-dimethyl-1,3-thiazol-2-yl)phenyl]-2,2,2-trifluoroethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4′-(ethylsulfonyl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-(4-pyridin-3-ylphenyl)ethyl]-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-methoxy-3′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-L-alaninamide;
N2-{(1S)-1-[4′-(aminosulfonyl)-1,1′-biphenyl-4-yl]-2,2,3,3,3-pentafluoropropyl}-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-((1S)-2,2,3,3,3-pentafluoro-1-{4′-[(2-hydroxy-2-methylpropyl)sulfonyl]-1,1′-biphenyl-4-yl}propyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-alaninamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,3,3,3-pentafluoro-1-[4′-(isopropylsulfonyl)-1,1′-biphenyl-4-yl]propyl}-L-leucinamide;
N1-(1-cyano-1-methylethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-((1S)-2,2,2-trifluoro-1-{4′-[(2-hydroxy-2-methylpropyl)sulfonyl]-1,1′-biphenyl-4-yl}ethyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[2′-methyl-4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4′-(ethylsulfonyl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-L-leucinamide;
N2-{(1S)-1-[4′-(aminosulfonyl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-N1-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide;
N1-(cyanomethyl)-N2-{(S)-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl][4-(trifluoromethoxy)phenyl]methyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[(S)-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl](thien-2-yl)methyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(S)-(4′-piperazin-4-ium-1-yl-1,1′-biphenyl-4-yl)(thien-2-yl)methyl]-L-leucinamide methanesulfonate;
N1-(cyanomethyl)-N2-{(S)-(4-fluorophenyl)[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]methyl}-L-leucinamide;
N1-(cyanomethyl)-N2-{(S)-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl][4-(trifluoromethyl)phenyl]methyl}-L-leucinamide;
N2-{(S)-(4-chlorophenyl)[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]methyl}-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N2-[(S)-(4-bromophenyl)(thien-2-yl)methyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-[(S)-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl](thien-2-yl)methyl]-L-leucinamide;
N2-{(R)-(4-bromophenyl)[4-(trifluoromethoxy)phenyl]methyl}-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(S)-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl][4-(trifluoromethoxy)phenyl]methyl}-L-leucinamide;
N2-[(S)-(4-bromophenyl)(2-furyl)methyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(S)-2-furyl[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]methyl}-L-leucinamide;
N2-[1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-L-norvalinamide;
N2-{(R)-(4-bromophenyl)[4-(trifluoromethyl)phenyl]methyl}-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{1-[4′-(4-cyclopropylpiperazin-1-yl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-L-norvalinamide;
N2-[(R)-(4-bromophenyl)(4-chlorophenyl)methyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N2-[(S)-(4-bromophenyl)(3-methylthien-2-yl)methyl]-N1-(cyanomethyl)-L-leucinamide;
N2-[(S)-(4-bromophenyl)(thien-3-yl)methyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(cyanomethyl)-N2-{(S)-(2,4-difluorophenyl)[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]methyl}-L-leucinamide;
N1-(cyanomethyl)-N2-[(S)-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl](thien-3-yl)methyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(S)-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl] (3-methylthien-2-yl)methyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(S)-[4′-(4-cyclopropylpiperazin-1-yl)-1,1′-biphenyl-4-yl](3-methylthien-2-yl)methyl]-L-leucinamide;
N1-(cyanomethyl)-N2-[(S)-[4′-(4-cyclopropylpiperazin-1-yl)-1,1′-biphenyl-4-yl](thien-3-yl)methyl]-L-leucinamide;
N2-[1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-5,5,5-trifluoro-L-norvalinamide;
N1-(cyanomethyl)-5,5,5-trifluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N2-[(S)-(4-bromophenyl)(3-methylthien-2-yl)methyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-[(S)-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl] (3-methylthien-2-yl)methyl]-L-leucinamide;
N1-(cyanomethyl)-N2-{(S)-3-furyl[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]methyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N2-[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-L-norvalinamide N2-[(S)-(4-bromophenyl)(4-bromothien-2-yl)methyl]-N1-(cyanomethyl)-L-leucinamide;
N2-[(S)-(4-bromophenyl)(thien-3-yl)methyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(cyanomethyl)-N2—((S)-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]{4-[4-(methylsulfonyl)phenyl]thien-2-yl}methyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-[(S)-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl](thien-3-yl)methyl]-L-leucinamide;
N2-{(1S)-1-[4′-(aminosulfonyl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-N1-(1-cyanocyclopropyl)-L-norvalinamide;
N2-[(S)-(4-bromophenyl)(4-bromothien-2-yl)methyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N2-[(S)-[4′-(aminosulfonyl)-1,1′-biphenyl-4-yl](thien-3-yl)methyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N2-[(S)-[4′-(aminosulfonyl)-1,1′-biphenyl-4-yl](thien-3-yl)methyl]-N1-(cyanomethyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-methoxy-3′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(2-methylpyridin-4-yl)phenyl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(1H-pyrazol-3-yl)phenyl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(1-hydroxy-1-methylethyl)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(5-methylpyridin-2-yl)phenyl]ethyl}-L-norvalinamide;
2-{[(4-Bromo-phenyl)-pyridin-4-yl-methyl]-amino}-pentanoic acid cyanomethyl-amide;
2-{[(4-Bromo-phenyl)-thiazol-2-yl-methyl]-amino+}-pentanoic acid cyanomethyl-amide;
(2S)-2-[(S)-1-(4′-Acetylbiphenyl-4-yl)-2,2,2-trifluoroethylamino]-pentanoic acid (1-cyanocyclopropyl)-amide;
(2S)-2-[(S)-1-(2′,4′-Difluorobiphenyl-4-yl)-2,2,2-trifluoroethylamino]-pentanoic acid (1-cyanocyclopropyl)-amide;
(2S)-2-[(S)-1-(3′,4′-Difluorobiphenyl-4-yl)-2,2,2-trifluoroethylamino]-pentanoic acid (1-cyanocyclopropyl)-amide;
(2S)-2-[(S)-1-(3′-Chloro-4′-fluorobiphenyl-4-yl)-2,2,2-trifluoroethylamino]-pentanoic acid (1-cyano-cyclopropyl)-amide;
(2S)-2-[(S)-2,2,2-Trifluoro-1-(4′-methanesulfonylamino-biphenyl-4-yl)-ethylamino]-pentanoic acid (1-cyano-cyclopropyl)-amide;
(2S)-2-{(S)-[(4-Bromo-phenyl)-thiazol-2-yl-methyl]-amino}-4-methylpentanoic acid cyanomethyl-amide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-chloro-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-chloro-3′-methyl-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N2-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-chloro-2′-methyl-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
(2S)-2-{(S)-2,2,2-Trifluoro-1-[4-(1H-indol-5-yl)-phenyl]-ethylamino}-pentanoic acid (1-cyano-cyclopropyl)-amide;
(2S)-2-[(S)-2,2,2-Trifluoro-1-(3-′-methanesulfonylamino-biphenyl-4-yl)-ethylamino]-pentanoic acid (1-cyano-cyclopropyl)-amide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-fluoro-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-fluoro-3′-methyl-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[3′-fluoro-4′-methyl-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-trifluoromethoxy-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
(2S)-2-[(S)-2,2,2-Trifluoro-1-(4-methylbiphenyl-4-yl)-ethylamino]-pentanoic acid (1-cyanocyclopropyl)-amide;
(2S)-2-[(S)-1-(4′-Cyanobiphenyl-4-yl)-2,2,2-trifluoroethylamino]-pentanoic acid (1-cyanocyclopropyl)-amide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-methoxy-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4-(benzo[1,3]dioxol-5-yl)phenyl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methoxycarbonyl)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
(2S)-2-{(S)-[(4-Bromophenyl)-thiazol-2-yl-methyl]-amino}-1-4-methylpentanoic acid (1-cyanocyclopropyl)-amide;
(2S)-2-{(S)-[(4′-Methanesulfonyl-biphenyl-4-yl)-thiazol-2-yl-methyl]-amino}-4-methyl-pentanoic acid cyanomethyl-amide;
(2S)-2-[(S)-2,2,2-Trifluoro-1-(4′-trifluoromethyl-biphenyl-4-yl)-ethylamino]-pentanoic acid (1-cyano-cyclopropyl)-amide;
(2S)-2-[(S)-2,2,2-Trifluoro-1-(2′-trifluoromethyl-biphenyl-4-yl)-ethylamino]-pentanoic acid (1-cyano-cyclopropyl)-amide;
(2S)-2-{(S)-[(2′,4′-Difluorobiphenyl-4-yl)-thiazol-2-yl-methyl]-amino}-4-methylpentanoic acid (1-cyanocyclopropyl)-amide;
(2S)-2-{(S)-[(4′-Methanesulfonylbiphenyl-4-yl)-thiazol-2-yl-methyl]-amino}-4-methylpentanoic acid (1-cyanocyclopropyl)-amide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4-(1-oxido-2,3-dihydro-1-benzothien-5-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(1,1-dioxido-2,3-dihydro-1-benzothien-5-yl)phenyl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(1,1-dioxido-2,3-dihydro-1,2-benzisothiazol-5-yl)phenyl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfinyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(1,1-dioxido-3-oxo-2,3-dihydro-1,2-benzisothiazol-5-yl)phenyl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[2′-(1-hydroxy-1-methylethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-(1-cyanocyclopropyl)-4,4-difluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(cyanomethyl)-4,4-difluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(cyanomethyl)-4-fluoro-N2-{(1S)-2,2,2-trichloro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trichloro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4,4-difluoro-N2-{(1S)-2,2,2-trichloro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(cyanomethyl)-4,4-difluoro-N2-{(1S)-2,2,2-trichloro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
(2S)—N-(cyanomethyl)-4,4-difluoro-2-({(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}amino)butanamide;
(2S)—N-(1-cyanocyclopropyl)-4,4-difluoro-2-({(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}amino)butanamide;
(2S)—N-(1-cyanocyclopropyl)-4,4-difluoro-2-({(1S)-2,2,2-trichloro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}amino)butanamide;
(2S)—N-(cyanomethyl)-4,4-difluoro-2({(1S)-2,2,2-trichloro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}amino)butanamide;
(2S)-4,4-dichloro-N-(cyanomethyl)-2-({(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}amino)butanamide;
(2S)-4,4-dichloro-N-(1-cyanocyclopropyl)-2-({(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}amino)butanamide;
(2S)-4,4-dichloro-N-(1-cyanocyclopropyl)-2-({(1S)-2,2,2-trichloro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}amino)butanamide;
(2S)-4,4-dichloro-N-(cyanomethyl)-2-({(1S)-2,2,2-trichloro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}amino)butanamide;
N2-[(1S)-1-(1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[3′-(1-hydroxyethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-(4′-methyl-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[3′-(1-hydroxy-1-methylethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-[(1S)-1-(4′-acetyl-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide;
N2-[(1S)-1-(2′-acetyl-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(1-hydroxyethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[2′-(1-hydroxyethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(1-hydroxy-1-methylethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[2′-(1-hydroxy-1-methylethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-((1S)-2,2,2-trifluoro-1-{5-[4-(methylsulfonyl)phenyl]pyridin-2-yl}ethyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-((1S)-2,2,2-trifluoro-1-{6-[4-(methylsulfonyl)phenyl]pyridin-3-yl}ethyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-(4-{6-[(methylsulfonyl)amino]pyridin-3-yl}phenyl)ethyl]-L-leucinamide;
N1-(cyanomethyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-(4-{6-[(methylsulfonyl)amino]pyridin-3-yl}phenyl)ethyl]-L-leucinamide;
N1-(1-cyanobutyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyano-2-cyclopropylethyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyano-2-pyridin-3-ylethyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyano-3-hydroxy-3-methylbutyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(3,3-dimethyl-1-oxo-1,3-dihydro-2-benzofuran-5-yl)phenyl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(3,3-diethyl-1-oxo-1,3-dihydro-2-benzofuran-5-yl)phenyl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4-(3-oxo-1,3-dihydro-2-benzofuran-5-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(1,1-dimethyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)phenyl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(1,1-diethyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)phenyl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(3-oxo-1,3-dihydro-2-benzofuran-5-yl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4′-(1,1-dimethyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4′-(1,1-diethyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4′-(3,3-dimethyl-1-oxo-1,3-dihydro-2-benzofuran-5-yl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N2-(1-cyanocyclopropyl)-N2-{(1S)-1-[4′-(3,3-diethyl-1-oxo-1,3-dihydro-2-benzofuran-5-yl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4-(5-oxo-2,5-dihydrofuran-3-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(2,2-dimethyl-5-oxo-2,5-dihydrofuran-3-yl)phenyl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(2,2-diethyl-5-oxo-2,5-dihydrofuran-3-yl)phenyl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4-(2-oxo-2,5-dihydrofuran-3-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(5,5-dimethyl-2-oxo-2,5-dihydrofuran-3-yl)phenyl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(5,5-diethyl-2-oxo-2,5-dihydrofuran-3-yl)phenyl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4-(5-oxo-4-oxaspiro[2.4]hept-6-en-7-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4-(6-oxo-5-oxaspiro[3.4]oct-7-en-8-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4-(5-oxo-4-oxaspiro[2.4]hept-6-en-6-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4-(6-oxo-5-oxaspiro[3.4]oct-7-en-7-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-(4-quinolin-6-ylphenyl)ethyl]-L-leucinamide;
N2-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfinyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-[(1S)-1-(4′-acetyl-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-quinolin-6-ylphenyl)ethyl]-L-leucinamide;
N2-[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-4,4-difluoro-L-norvalinamide;
N1-(1-cyanocyclopropyl)-4,4-difluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylthio)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-4,4-difluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-[(1S)-1-cyano-3-(methylsulfonyl)propyl]-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-(4-quinolin-6-ylphenyl)ethyl]-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfinyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′41-hydroxyethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-[(1S)-1-(4′-acetyl-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-quinolin-6-ylphenyl)ethyl]-L-leucinamide;
N2-[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-4,4-difluoro-L-norvalinamide;
N1-(1-cyanocyclopropyl)-4,4-difluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylthio)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-4,4-difluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-((1S)-2,2,2-trifluoro-1-{4-[5-methyl-6-(methylsulfonyl)pyridin-3-yl]phenyl}ethyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-((1S)-2,2,2-trifluoro-1-{4-[6-(1-hydroxy-1-methylethyl)-5-methylpyridin-3-yl]phenyl}ethyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-(4′-fluoro-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[3′-methyl-4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4-(6-methylpyridin-3-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylthio)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(1-hydroxy-1-methylethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4-(2-methylquinolin-7-yl)phenyl]ethyl}-L-leucinamide;
N2-[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-4,4-difluoro-L-norvalinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-((1S)-2,2,2-trifluoro-1-{4′-[(1S)-1-hydroxyethyl]-1,1′-biphenyl-4-yl}ethyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-((1S)-2,2,2-trifluoro-1-{4′-[(1R)-1-hydroxyethyl]-1,1′-biphenyl-4-yl}ethyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(trifluoroacetyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[5-(2-naphthyl)pyridin-2-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-4,4-difluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylthio)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(cyanomethyl)-4,4-difluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4-(5-methyl-1,3-thiazol-2-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(1,1-dioxido-3-oxo-2,3-dihydro-1,2-benzisothiazol-5-yl)phenyl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N2-[(4-bromophenyl)(phenyl)methyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-(4′-methyl-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N2-[(1S)-1-(1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide;
N2-{(1S)-1-[4-(5-chloropyridin-2-yl)phenyl]-2,2,2-trifluoroethyl}-N1-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-(4-pyridin-4-ylphenyl)ethyl]-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-((1S)-2,2,2-trifluoro-1-{4′-[(methylsulfonyl)amino]-1,1′-biphenyl-4-yl}ethyl)-L-leucinamide;
N2-[(1S)-1-(4-bromophenyl)-2,2-difluoroethyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2-difluoro-1-[4′-(methylthio)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-(4-pyrimidin-5-ylphenyl)ethyl]-L-leucinamide;
N2-[(1S)-1-(4-acetyl-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[3′-(1-hydroxyethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-[(1S)-1-(4′-acetyl-1,1′-biphenyl-4-yl)-2,2-difluoroethyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N1-[(1S)-1-cyano-3-(methylsulfonyl)propyl]-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-(4-quinolin-6-ylphenyl)ethyl]-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfinyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(1-hydroxyethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-[(1S)-1-(4′-acetyl-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-quinolin-6-ylphenyl)ethyl]-L-leucinamide;
N2-[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-4,4-difluoro-L-norvalinamide;
N1-(1-cyanocyclopropyl)-4,4-difluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylthio)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-4,4-difluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-((1S)-2,2,2-trifluoro-1-{4-[5-methyl-6-(methylsulfonyl)pyridin-3-yl]phenyl}ethyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-((1S)-2,2,2-trifluoro-1-{4-[6-(1-hydroxy-1-methylethyl)-5-methylpyridin-3-yl]phenyl}ethyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-(4′-fluoro-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[3′-methyl-4′-(methylsulfonyl)-1, biphenyl-4-yl]ethyl}-L-leucinamide;
N2-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4-(6-methylpyridin-3-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylthio)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(1-hydroxy-1-methylethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4-(2-methylquinolin-7-yl)phenyl]ethyl}-L-leucinamide;
N2-[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]-N1-(cyanomethyl)-4,4-difluoro-L-norvalinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-((1S)-2,2,2-trifluoro-1-{4′-[(1S)-1-hydroxyethyl]-1,1′-biphenyl-4-yl}ethyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-((1S)-2,2,2-trifluoro-1-{4′-[(1R)-1-hydroxyethyl]-1,1′-biphenyl-4-yl}ethyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[4′-(trifluoroacetyl)-1,1′-biphenyl-4-yl]ethyl}-L-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2,2-trifluoro-1-[5-(2-naphthyl)pyridin-2-yl]ethyl}-L-leucinamide;
N1-(cyanomethyl)-4,4-difluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylthio)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N2-(cyanomethyl)-4,4-difluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-norvalinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4-(5-methyl-1,3-thiazol-2-yl)phenyl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(1,1-dioxido-3-oxo-2,3-dihydro-1,2-benzisothiazol-5-yl)phenyl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
N2-[(4-bromophenyl)(phenyl)methyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-(4′-methyl-1,1′-biphenyl-4-yl)ethyl]-L-leucinamide;
N2-[(1S)-1-(1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide;
N2-{(1S)-1-[4-(5-chloropyridin-2-yl)phenyl]-2,2,2-trifluoroethyl}-N1-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-(4-pyridin-4-ylphenyl)ethyl]-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-((1S)-2,2,2-trifluoro-1-{4′-[(methylsulfonyl)amino]-1,1′-biphenyl-4-yl}ethyl)-L-leucinamide;
N2-[(1S)-1-(4-bromophenyl)-2,2-difluoroethyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-2,2-difluoro-1-[4′-(methylthio)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-(4-pyrimidin-5-ylphenyl)ethyl]-L-leucinamide;
N2-[(1S)-1-(4′-acetyl-1,1′-biphenyl-4-yl)-2,2,2-trifluoroethyl]-N1-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide;
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[3′-(1-hydroxyethyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide;
N2-[(1S)-1-(4′-acetyl-1,1′-biphenyl-4-yl)-2,2-difluoroethyl]-N1-(1-cyanocyclopropyl)-L-leucinamide;
N1-(1-cyanocyclopropyl)-N2-{(1S)-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-2,2,2-trifluoroethyl}-4-fluoro-L-leucinamide;
and the pharmaceutically acceptable salts, stereoisomers and N-oxide derivatives thereof.

### Claim 10 (depends on 1)

The method of claim 1 wherein the compound is N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide or a pharmaceutically acceptable salt thereof.

### Claim 11 (depends on 1)

The method of claim 1 wherein the compound is N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfinyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide or a pharmaceutically acceptable salt thereof.

### Claim 12 (depends on 1)

The method of claim 1 wherein the compound is N1(cyanomethyl)-N2{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide or a pharmaceutically acceptable salt thereof.

### Claim 13 (depends on 1)

The method of claim 1 wherein the compound is N2{(1S)-1-[4′-(aminosulfonyl)-1,1′-biphenyl-4-yl]-2,2,2-trifluoroethyl}-N (cyanomethyl)-L-leucinamide or a pharmaceutically acceptable salt thereof.

### Claim 14

A method of treating osteoarthritis with N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide.