N-[3-[(1R)-3-amino-1-(1-ethyl-5-methyl-6-oxopyridin-3-yl)-4-fluoroisoindol-1-yl]phenyl]-5-chloropyridine-2-carboxamide

5-[(1R)-3-amino-4-fluoro-1-[3-(5-prop-1-ynylpyridin-3-yl)phenyl]isoindol-1-yl]-1-ethyl-3-methylpyridin-2-one

N-[3-(1-amino-5-fluoro-3-methyl-4H-2,7-naphthyridin-3-yl)-4-fluorophenyl]-5-cyanopyridine-2-carboxamide

N-[3-(1-amino-5-fluoro-3-methyl-4H-2,6-naphthyridin-3-yl)-4-fluorophenyl]-5-cyanopyridine-2-carboxamide

5-[(1R)-3-amino-4,6-difluoro-1-[3-(5-prop-1-ynylpyridin-3-yl)phenyl]isoindol-1-yl]-1-ethyl-3-methylpyridin-2-one

N-[3-[(3S)-1-amino-5-fluoro-3-methyl-4H-2,6-naphthyridin-3-yl]-4-fluorophenyl]-5-cyanopyridine-2-carboxamide

I-25

N-[3-[(4S)-2-amino-4-(fluoromethyl)-5,6-dihydro-1,3-thiazin-4-yl]-4-fluorophenyl]-5-cyanopyridine-2-carboxamide

N-[3-[(4S)-2-amino-4-methyl-5,6-dihydro-1,3-thiazin-4-yl]-4-fluorophenyl]-5-cyanopyridine-2-carboxamide

5-[(1R)-3-amino-1-[3-(2-cyclopropylethynyl)phenyl]-4-fluoroisoindol-1-yl]-1-ethyl-3-methylpyridin-2-one

3-[(4S)-2-amino-4-methyl-5,6-dihydro-1,3-thiazin-4-yl]-N-(5-chloropyridin-2-yl)-4-fluorobenzamide

CHEMBL4103296

CHEMBL4097477

CHEMBL4070299

N-[3-[(4R,5R,6R)-2-amino-5-fluoro-6-[(1R)-1-fluoroethyl]-4-methyl-5,6-dihydro-1,3-oxazin-4-yl]-4-fluorophenyl]-5-(fluoromethoxy)pyrazine-2-carboxamide

US9270353, 50

US9270353, 17

N-[3-(1-amino-3-methyl-4H-2,7-naphthyridin-3-yl)-4-fluorophenyl]-5-cyanopyridine-2-carboxamide

CHEMBL4085364

I-27

N-[3-(1-amino-3-methyl-4H-2,6-naphthyridin-3-yl)-4-fluorophenyl]-5-cyanopyridine-2-carboxamide

N-[3-[(4R,5R,6R)-2-amino-5-fluoro-6-(fluoromethyl)-4-methyl-5,6-dihydro-1,3-oxazin-4-yl]-4-fluorophenyl]-5-methoxypyrazine-2-carboxamide

US8637504, 59

N-[3-[(4R,5R,6R)-2-amino-5-fluoro-6-(fluoromethyl)-4-methyl-5,6-dihydro-1,3-oxazin-4-yl]-4-fluorophenyl]-3-chloro-5-cyanopyridine-2-carboxamide

5-(3-(3-Amino-1-(1-ethyl-5-methyl-6-oxo-1,6-dihydropyridin-3-yl)-4-fluoro-1H-isoindol-1-yl)phenyl)nicotinonitrile

N-[3-[(4R,5R,6S)-2-amino-6-(1,1-difluoroethyl)-5-fluoro-4-methyl-5,6-dihydro-1,3-oxazin-4-yl]-4-fluorophenyl]-5-(fluoromethoxy)pyrazine-2-carboxamide

CHEMBL4067413

3-(3-pyrimidin-5-ylphenyl)-3-[2-(trifluoromethyl)pyridin-4-yl]isoindol-1-amine

N-[3-[(4R,5R,6R)-2-amino-5-fluoro-6-[(1S)-1-fluoroethyl]-4-methyl-5,6-dihydro-1,3-oxazin-4-yl]-4-fluorophenyl]-5-(fluoromethoxy)pyrazine-2-carboxamide

CHEMBL4084381

CHEMBL4100832

7-fluoro-3-(5-methoxy-4,6-dimethylpyridin-2-yl)-3-(3-pyrimidin-5-ylphenyl)isoindol-1-amine

3-[2-(difluoromethyl)pyridin-4-yl]-7-fluoro-3-[3-(5-prop-1-ynylpyridin-3-yl)phenyl]isoindol-1-amine

sulfonamide tricyclic analogue, 7

N-[3-[(4R,5R,6S)-2-amino-5-fluoro-6-(1-fluorocyclopropyl)-4-methyl-5,6-dihydro-1,3-oxazin-4-yl]-4-fluorophenyl]-5-(fluoromethoxy)pyrazine-2-carboxamide

5-[3-amino-4-fluoro-1-(3-pyrimidin-5-ylphenyl)isoindol-1-yl]-2-methoxy-3-methylbenzonitrile

CHEMBL4072118

N-[3-[(4R,5R,6R)-2-amino-5-fluoro-6-(fluoromethyl)-4-methyl-5,6-dihydro-1,3-oxazin-4-yl]-4-fluorophenyl]-5-fluoropyridine-2-carboxamide

N-[3-[(4S)-2-amino-6-(fluoromethyl)-4-methyl-1,3-oxazin-4-yl]-4-fluorophenyl]-5-cyanopyridine-2-carboxamide

N-[3-[(4S)-2-amino-4-methyl-5,6-dihydro-1,3-oxazin-4-yl]-4-fluorophenyl]-5-cyanopyridine-2-carboxamide

N-[3-[(4R,5R,6R)-2-amino-5-fluoro-6-(fluoromethyl)-4-methyl-5,6-dihydro-1,3-oxazin-4-yl]-4-fluorophenyl]-5-(difluoromethyl)pyrazine-2-carboxamide

5-[3-amino-4-fluoro-1-[3-(5-fluoropyridin-3-yl)phenyl]isoindol-1-yl]-1-ethyl-3-methylpyridin-2-one

N-[3-(5-amino-7-methyl-8H-1,6-naphthyridin-7-yl)-4-fluorophenyl]-5-cyanopyridine-2-carboxamide

US8637504, 76

US8999980, I-54

US9270353, 13

{3-((1r,1'R,4R)-2''-Amino-4-methoxy-3'H,5''H-dispiro-[cyclohexane-1,2'-indene-1',4''-oxazol]-6'-yl-5'',5''-d2)-5-chlorobenzonitrile}

3-(1,1-dioxo-1,2-thiazinan-2-yl)-5-(ethylamino)-2-fluoro-N-[(2S,3R)-3-hydroxy-1-phenyl-4-({[3-(trifluoromethyl)phenyl]methyl}amino)butan-2-yl]benzamide

US8637504, 16

N-[3-[(4S)-2-amino-6-(fluoromethyl)-4-methyl-1,3-oxazin-4-yl]-4-fluorophenyl]-2-(fluoromethyl)-1,3-oxazole-4-carboxamide

CHEMBL4093123

3-ethyl-N-[(2S,3R)-3-hydroxy-1-phenyl-4-({[3-(trifluoromethyl)phenyl]methyl}amino)butan-2-yl]-9-methyl-10,10-dioxo-10-thia-1,9-diazatricyclo[6.4.1.0^{4,13}]trideca-2,4(13),5,7-tetraene-6-carboxamide

N-[3-[(4S)-2-amino-6-(fluoromethyl)-4-methyl-1,3-oxazin-4-yl]-4-fluorophenyl]-2-(difluoromethyl)-1,3-oxazole-4-carboxamide

3-amino-N-[3-[(4S)-2-amino-6-(fluoromethyl)-4-methyl-1,3-oxazin-4-yl]-4-fluorophenyl]-5-(fluoromethoxy)pyrazine-2-carboxamide

CHEMBL4074071

CHEMBL4065448

N-[3-[(4S)-2-amino-4-methyl-1,3-oxazin-4-yl]-4-fluorophenyl]-5-cyanopyridine-2-carboxamide

(8R)-8-[4-(difluoromethoxy)phenyl]-3,3-difluoro-8-[3-(3-fluoropropoxy)phenyl]-2,4-dihydroimidazo[1,5-a]pyrimidin-6-amine

7,6,5 tricyclic sulfonamide, 15

(3S)-7-fluoro-3-pyridin-4-yl-3-(3-pyrimidin-5-ylphenyl)isoindol-1-amine

N-[3-[(4S)-2-amino-6-(fluoromethyl)-4-methyl-1,3-oxazin-4-yl]-4-fluorophenyl]-5-cyano-3-methylpyridine-2-carboxamide

(3S)-3-[2-(difluoromethyl)pyridin-4-yl]-5,7-difluoro-3-(3-pyrimidin-5-ylphenyl)isoindol-1-amine

5-[3-amino-4-fluoro-1-(3-pyrimidin-5-ylphenyl)isoindol-1-yl]-1-ethyl-3-methylpyridin-2-one

3-(2,6-dimethylpyridin-4-yl)-7-fluoro-3-(3-pyrimidin-5-ylphenyl)isoindol-1-amine

N-[3-[(4S)-2-amino-4,5-dimethyl-1,3-oxazin-4-yl]-4-fluorophenyl]-5-cyanopyridine-2-carboxamide

N-[3-(1-amino-8-fluoro-3-methyl-4H-2,6-naphthyridin-3-yl)-4-fluorophenyl]-5-cyanopyridine-2-carboxamide

5-[3-amino-4-fluoro-1-(3-pyrimidin-5-ylphenyl)isoindol-1-yl]-1,3-dimethylpyridin-2-one

rac-4-Fluoro-1-(pyridin-4-yl)-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine

3-(1,1-dioxo-1,2-thiazinan-2-yl)-N-[(2S,3R)-4-{[(1-ethyl-1H-pyrazol-4-yl)methyl]amino}-3-hydroxy-1-phenylbutan-2-yl]-5-(ethylamino)-2-fluorobenzamide

3-(1,1-dioxo-1,2-thiazinan-2-yl)-5-(ethylamino)-2-fluoro-N-[(2S,3R)-3-hydroxy-4-{[(3-methoxyphenyl)methyl]amino}-1-phenylbutan-2-yl]benzamide

7,6,5 tricyclic sulfonamide, 22

N-[3-[(4S)-2-amino-6-(fluoromethyl)-4-methyl-1,3-oxazin-4-yl]-4-fluorophenyl]-3-chloro-5-cyanopyridine-2-carboxamide

7-fluoro-3-(4-methoxyphenyl)-3-(3-pyrimidin-5-ylphenyl)isoindol-1-amine

8-[4-(difluoromethoxy)phenyl]-3,3-difluoro-8-[3-(2-fluoropyridin-3-yl)phenyl]-2,4-dihydroimidazo[1,5-a]pyrimidin-6-amine

8-[4-(difluoromethoxy)phenyl]-3,3-difluoro-8-[3-(4-methoxybut-1-ynyl)phenyl]-2,4-dihydroimidazo[1,5-a]pyrimidin-6-amine

sulfonamide tricyclic analogue, 15

2-(4-methoxy-3,5-dimethylphenyl)-5-methyl-2-[3-(5-prop-1-ynylpyridin-3-yl)phenyl]imidazol-4-amine

8-[4-(difluoromethoxy)phenyl]-3,3-difluoro-8-[3-(5-methoxypyridin-3-yl)phenyl]-2,4-dihydroimidazo[1,5-a]pyrimidin-6-amine

8-[4-(difluoromethoxy)phenyl]-3,3-difluoro-8-[3-(3-fluoropropoxy)phenyl]-2,4-dihydroimidazo[1,5-a]pyrimidin-6-amine

N-[3-[(4S)-2-amino-6-(methoxymethyl)-4-methyl-1,3-oxazin-4-yl]-4-fluorophenyl]-5-cyanopyridine-2-carboxamide

BMCL193669 Compound 18

(3S)-3-[2-(difluoromethyl)pyridin-4-yl]-7-fluoro-3-(3-pyrimidin-5-ylphenyl)isoindol-1-amine

7,6,5 tricyclic sulfonamide, 39

rac-1-(2-(Difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine

N-[3-[(4S)-2-amino-4-(fluoromethyl)-6-methyl-1,3-oxazin-4-yl]-4-fluorophenyl]-5-cyanopyridine-2-carboxamide

3-(1,1-dioxo-1,2-thiazinan-2-yl)-5-ethoxy-N-[(2S,3R)-3-hydroxy-1-phenyl-4-({[3-(trifluoromethoxy)phenyl]methyl}amino)butan-2-yl]benzamide

3-(2-cyclopropylpyridin-4-yl)-7-fluoro-3-(3-pyrimidin-5-ylphenyl)isoindol-1-amine

3-(1,1-dioxo-1,2-thiazinan-2-yl)-5-(ethylamino)-N-[(2S,3R)-3-hydroxy-4-{[(3-methoxyphenyl)methyl]amino}-1-phenylbutan-2-yl]benzamide

3-(1,1-dioxo-1,2-thiazinan-2-yl)-5-(ethylamino)-N-[(2S,3R)-3-hydroxy-1-phenyl-4-({[3-(trifluoromethyl)phenyl]methyl}amino)butan-2-yl]benzamide

8-[4-(difluoromethoxy)phenyl]-3,3-difluoro-8-(3-pyrimidin-5-ylphenyl)-2,4-dihydroimidazo[1,5-a]pyrimidin-6-amine

3-(1,1-dioxo-1,2-thiazinan-2-yl)-5-ethoxy-N-[(2S,3R)-3-hydroxy-1-phenyl-4-({[3-(trifluoromethyl)phenyl]methyl}amino)butan-2-yl]benzamide

7-fluoro-3-(2-methoxypyridin-4-yl)-3-(3-pyrimidin-5-ylphenyl)isoindol-1-amine

N-[3-[(4S)-2-amino-6-(fluoromethyl)-4-methyl-1,3-oxazin-4-yl]-4-fluorophenyl]-5-methoxypyrazine-2-carboxamide

(3S)-7-fluoro-3-(4-fluoro-3-pyrimidin-5-ylphenyl)-3-[2-(trifluoromethyl)pyridin-4-yl]isoindol-1-amine

(2S)-2-(4-methoxy-3,5-dimethylphenyl)-5-methyl-2-(3-pyrimidin-5-ylphenyl)imidazol-4-amine

7-fluoro-3-[3-(5-fluoropyridin-3-yl)phenyl]-3-pyridin-4-ylisoindol-1-amine

1-N-[(2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-yl]-5-(N-methylmethanesulfonamido)-3-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide

3-(1,1-dioxo-1,2-thiazinan-2-yl)-5-(ethylamino)-N-[(2S,3R)-3-hydroxy-4-[(6-methoxy-2,3-dihydro-1H-inden-1-yl)amino]-1-phenylbutan-2-yl]benzamide

N-[(2S,3R)-1-(3,5-difluorophenyl)-3-hydroxy-4-{[(3-methoxyphenyl)methyl]amino}butan-2-yl]-3-(1,1-dioxo-1,2-thiazinan-2-yl)-5-(ethylamino)benzamide

sulfonamide tricyclic analogue, 11

N-[3-(8-amino-6-methyl-5H-1,7-naphthyridin-6-yl)-4-fluorophenyl]-5-cyanopyridine-2-carboxamide

sulfonamide tricyclic analogue, 5

sulfonamide tricyclic analogue, 22

rac-4-Fluoro-1-(4-fluoro-3-(pyrimidin-5-yl)phenyl)-1-(2-(trifluoromethyl)pyridin-4-yl)-1H-isoindol-3-amine

5-[3-[3-amino-4-fluoro-1-[2-(trifluoromethyl)pyridin-4-yl]isoindol-1-yl]phenyl]pyridine-3-carbonitrile

7,6,5 tricyclic sulfonamide, 38

(8R)-3,3-difluoro-8-[3-(2-fluoro-3-methoxyphenyl)phenyl]-8-pyridin-4-yl-2,4-dihydroimidazo[1,5-a]pyrimidin-6-amine

N-[3-[(4S)-2-amino-6-(fluoromethyl)-4-methyl-1,3-oxazin-4-yl]-4-fluorophenyl]-5-(fluoromethoxy)pyrazine-2-carboxamide

6-(4-methoxyphenyl)-2-methyl-6-(3-pyrimidin-5-ylphenyl)pyrrolo[3,4-d][1,3]thiazol-4-amine

3-(1,1-dioxo-1,2-thiazinan-2-yl)-5-(ethylamino)-N-[(2S,3R)-3-hydroxy-1-phenyl-4-({[3-(trifluoromethoxy)phenyl]methyl}amino)butan-2-yl]benzamide

8-[4-(difluoromethoxy)phenyl]-3,3-difluoro-8-[3-(3-methoxyprop-1-ynyl)phenyl]-2,4-dihydroimidazo[1,5-a]pyrimidin-6-amine

3-(1,1-dioxo-1,2-thiazinan-2-yl)-N-[(2S,3R)-3-hydroxy-1-phenyl-4-({[3-(trifluoromethyl)phenyl]methyl}amino)butan-2-yl]-5-propylbenzamide

2-methyl-2-(3-pyrimidin-5-ylphenyl)-5,6-dihydro-1,3-thiazin-4-amine

7-fluoro-3-(3-pyrimidin-5-ylphenyl)-3-[2-(trifluoromethyl)pyridin-4-yl]isoindol-1-amine

3,3-difluoro-8-(4-fluoro-3-pyridin-3-ylphenyl)-8-(4-methoxy-3-methylphenyl)-2,4-dihydroimidazo[1,5-a]pyrimidin-6-amine

2-Ethyl-6-methyl-7,7-dioxo-6,7,8,9-tetrahydro-2H-7lambda*6*-thia-2,6-diaza-benzo[cd]azulene-4-carboxylic acid [(S)-1-benzyl-2-oxo-3-(tetrahydro-pyran-4-ylamino)-propyl]-amide

7,6,5 tricyclic sulfonamide, 35

2-(4-Methoxy-3,5-dimethylphenyl)-5-methyl-2-(3-(pyrimidin-5-yl)phenyl)-2H-imidazol-4-amine

sulfonamide tricyclic analogue, 25

3,3-difluoro-8-(2'-fluoro-3'-methoxybiphenyl-3-yl)-8-(pyridin-4-yl)-2,3,4,8-tetrahydroimidazo[1,5-a]pyrimidin-6-amine

bicyclic sulfonamide analogue, 11

N-[3-[(4S)-2-amino-6-(fluoromethyl)-4-methyl-1,3-oxazin-4-yl]-4-fluorophenyl]-5-cyano-3-methoxypyridine-2-carboxamide

3-(1,1-dioxo-1,2-thiazinan-2-yl)-N-[(2S,3R)-3-hydroxy-1-phenyl-4-({[3-(trifluoromethyl)phenyl]methyl}amino)butan-2-yl]-5-(propan-2-ylamino)benzamide

4-(4-amino-2-cyclopropyl-5-methylimidazol-2-yl)-2-(5-prop-1-ynylpyridin-3-yl)phenol

2-[3-(3-methoxyphenyl)phenyl]-2-methyl-5,6-dihydro-1,3-thiazin-4-amine

lysine sulfonamide analogue 9

N-[3-[(4S)-2-amino-4-cyclopropyl-6-(fluoromethyl)-1,3-oxazin-4-yl]-4-fluorophenyl]-5-cyanopyridine-2-carboxamide

3-(1,1-dioxo-1,2-thiazinan-2-yl)-N-[(2S,3R)-4-{[(1-ethyl-1H-pyrazol-4-yl)methyl]amino}-3-hydroxy-1-phenylbutan-2-yl]-5-(ethylamino)benzamide

BMCL193669 Compound 24

N-[3-[(4S)-2-amino-6-(fluoromethyl)-4-methyl-1,3-oxazin-4-yl]-4-fluorophenyl]-5-(difluoromethyl)pyrazine-2-carboxamide

sulfonamide tricyclic analogue, 13

3-Ethyl-7-methyl-8,8-dioxo-2,3,6a,7,8,9,10,10b-octahydro-1H-8lambda*6*-thia-3,7,10a-triaza-cyclohepta[de]naphthalene-5-carboxylic acid[(1S,2R)-1-benzyl-2-hydroxy-3-(3-trifluoromethyl-benzylamino)-propyl]-amide

7,6,5 tricyclic sulfonamide, 13

3-pyridin-4-yl-3-(3-pyrimidin-5-ylphenyl)isoindol-1-amine

BMCL193669 Compound 26

4-(4-amino-2-cyclopropyl-5-methylimidazol-2-yl)-2-(4-prop-1-ynylpyridin-2-yl)phenol

3-ethyl-N-[(2S,3R)-3-hydroxy-4-(methylamino)-1-phenylbutan-2-yl]-9-methyl-10,10-dioxo-10-thia-1,9-diazatricyclo[6.4.1.0^{4,13}]trideca-2,4(13),5,7-tetraene-6-carboxamide

3-(1,1-dioxo-1,2-thiazinan-2-yl)-5-(ethylamino)-N-[(2S,3R)-1-(furan-2-yl)-3-hydroxy-4-{[(3-methoxyphenyl)methyl]amino}butan-2-yl]benzamide

N-[3-[(4S)-2-amino-6-(difluoromethyl)-4-methyl-1,3-oxazin-4-yl]-4-fluorophenyl]-5-cyano-3-methylpyridine-2-carboxamide

sulfonamide tricyclic analogue, 12

6,6,5 tricyclic sulfonamide, 23

sulfonamide tricyclic analogue, 10

N-[(2S,3R)-4-[(1S)-2,3-dihydro-1H-inden-1-ylamino]-3-hydroxy-1-phenylbutan-2-yl]-3-(1,1-dioxo-1,2-thiazinan-2-yl)-5-(ethylamino)benzamide

2-(4-methoxy-3-methylphenyl)-5-methyl-2-(3-pyrimidin-5-ylphenyl)imidazol-4-amine

US8546380, 220::US8633188, 220

bicyclic sulfonamide analogue, 16

3,3-difluoro-8-(4-methoxyphenyl)-8-(3-pyrimidin-5-ylphenyl)-2,4-dihydroimidazo[1,5-a]pyrimidin-6-amine

2-cyclopropyl-5-methyl-2-[3-(5-prop-1-ynylpyridin-3-yl)phenyl]imidazol-4-amine

5-[3-(3-methoxyphenyl)phenyl]-5-methyl-2,6-dihydro-1,4-oxazin-3-amine

sulfonamide tricyclic analogue, 23

CHEMBL4092875