IP Library › Granted Patent US 12,673,927
Granted Patent B2
US 12,673,927 · App. 17/920,679 · Granted Jul 7, 2026

Substituted aminothiazoles as DGKzeta inhibitors for immune activation

Inventors: Norbert Schmees (Berlin, DE); Ulrike Roehn (Berlin, DE); Dennis Kirchhoff (Berlin, DE); Kirstin Petersen (Berlin, DE); Thi Thanh Uyen Nguyen (Berlin, DE); Mareike Grees (Berlin, DE); Nicolas Werbeck (Freiburg, DE); Ulf Boemer (Glienicke, DE); Benjamin Bader (Berlin, DE); Detlef Stöckigt (Potsdam, DE); Dirk Kosemund (Berlin, DE); Rienk Offringa (Heidelberg, DE); Corinna Link (Mannheim, DE); Katrin Nowak-Reppel (Berlin, DE); Ulrich Rosentreter (Binnen, DE)
Assignee: Deutsches Krebsforschungszentrum
C07D277/42A61P35/00C07D277/46C07D417/06C07D417/10C07D417/12C07D417/14C07D471/08C07D487/04C07K16/2818C07K16/2827C07B2200/07
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Quick Facts
Patent No.
US 12,673,927
App. No.
17/920,679
Granted
Jul 7, 2026
Kind
B2
Abstract

The present invention covers aminothiazole compounds of general formula (I), in which R 1 , R 2 , R 3 and R 4 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of diacylglycerol kinase zeta (DGKζ) regulated disorders, as a sole agent or in combination with other active ingredients.

Claims (329)

1 . A compound of formula (I):

wherein:

R 1 is a phenyl or pyridinyl optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom, a chlorine atom, a bromine atom, cyano, difluoromethyl, trifluoromethyl, methoxy, benzyloxy, difluoromethoxy and trifluoromethoxy,

or two substituents attached to adjacent carbon atoms of the phenyl or pyridinyl of R 1 together form a bivalent group —O—CF 2 —O—;

R 2 is

wherein “*” indicates the point of attachment to the nitrogen atom to which R 2 is attached;

R 3 is methyl or —NH 2 ;

R 4 is a phenyl or pyridinyl optionally substituted with one or two substituents independently selected from the group consisting of a halogen atom, C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, —OR 9 , —N(R 10 )(R 11 ), —C(═O)—N(R 12 )(R 13 ), and —C(═O)—OR 17 ;

R 7 is a hydrogen atom or a C 1 -C 2 -alkyl;

R 8 is —C(═O)—NH 2 ;

R 9 is selected from the group consisting of a hydrogen atom, C 1 -C 2 -alkyl, benzyl, C 1 -C 2 -fluoroalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((C 1 -C 2 -alkyl)-C(═O)—O)—C 2 -alkyl-, —C(R 18 )(R 19 )—C(═O)—N(R 20 )(R 21 ), —C(═O)—N(R 20 )(R 21 ) and phenyl,

wherein the phenyl of R 9 and the phenyl within the benzyl of R 9 are optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom, a chlorine atom, cyano, and methyl;

R 10 and R 11 are independently selected from the group consisting of a hydrogen atom, C 1 -C 2 -alkyl, (C 3 -C 5 -cycloalkyl)-(C 1 -C 2 -alkyl)-, C 3 -C 7 -cycloalkyl, and (phenyl)-(C 1 -C 2 -alkyl)-O—C(═O)—,

wherein the C 3 -C 7 -cycloalkyl, and the C 3 -C 5 -cycloalkyl within the (C 3 -C 5 -cycloalkyl)-(C 1 -C 2 -alkyl)- of R 10 and R 11 are optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom, cyano, methyl, and C 1 -fluoroalkyl,

and wherein the phenyl within the (phenyl)-(C 1 -C 2 -alkyl)-O—C(═O)— of R 10 and R 11 is optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom, a chlorine atom, and a methyl,

or

R 10 and R 11 are taken together with the nitrogen atom to which they are attached to form a monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl which is optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom, cyano, methyl, and C 1 -fluoroalkyl;

R 12 and R 13 are independently selected from the group consisting of a hydrogen atom, C 1 -C 4 -alkyl, C 1 -C 2 -fluoroalkyl, C 1 -C 2 -hydroxyalkyl, (C 1 -C 4 -alkoxy)-C 2 -C 3 -alkyl-, (C 1 -C 2 -fluoroalkoxy)-C 2 -C 3 -alkyl-, (phenoxy)-C 2 -C 3 -alkyl-, C 3 -C 7 -cycloalkyl, and (phenyl)-(C 1 -C 2 -alkyl)-,

wherein the C 3 -C 7 -cycloalkyl is optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom and a methyl group,

and wherein the phenyl within the (phenoxy)-C 2 -C 3 -alkyl- and the phenyl within the (phenyl)-(C 1 -C 2 -alkyl)- are optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom, a chlorine atom, methyl, trifluoromethyl, and methoxy;

R 17 is C 1 -C 2 -alkyl;

R 18 and R 19 are independently a hydrogen atom or a methyl group;

R 20 is selected from the group consisting of a hydrogen atom, C 1 -C 3 -alkyl, and phenyl,

wherein the C 1 -C 3 -alkyl of R 20 is optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom, hydroxy, C 1 -C 3 -alkoxy, and phenyl, wherein the phenyl substituent on R 20 is optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom, a chlorine atom, and a methyl group,

and wherein the phenyl of R 20 is optionally substituted with one, two, or three substituents independently selected from the group consisting of a fluorine atom, a chlorine atom, methyl, trifluoromethyl, methoxy, and trifluoromethoxy, and

R 21 is a hydrogen atom or a C 1 -C 2 -alkyl,

or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or mixture of any of the foregoing.

2 . The compound of claim 1 , wherein:

R 1 is

wherein “**” indicates the point of attachment to the nitrogen atom to which R 1 is attached;

R 2 is

wherein “*” indicates the point of attachment to the nitrogen atom to which R 2 is attached;

R 3 is methyl or —NH 2 ;

R 4 is

wherein “#” indicates the point of attachment to the carbonyl to which R 4 is attached;

R 7 is a hydrogen atom or a C 1 -C 2 -alkyl;

R 8 is —C(═O)—NH 2 ;

R 9 is selected from the group consisting of a hydrogen atom, C 1 -C 2 -alkyl, benzyl, C 1 -C 2 -fluoroalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((C 1 -C 2 -alkyl)-C(═O)—O)—C 2 -alkyl-, —C(R 18 )(R 19 )—C(═O)—N(R 20 )(R 21 ), —C(═O)—N(R 20 )(R 21 ) and phenyl,

wherein the phenyl of R 9 and the phenyl within the benzyl of R 9 are optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom, a chlorine atom, cyano, and methyl;

R 10 and R 11 are independently selected from the group consisting of a hydrogen atom, C 1 -C 2 -alkyl, C 3 -C 7 -cycloalkyl, and (benzyl)-O—C(═O)—,

wherein the C 3 -C 7 -cycloalkyl of R 10 and R 11 is optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom, methyl, and trifluoromethyl,

and wherein the phenyl within the (benzyl)-O—C(═O)— of R 10 and R 11 is optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom, a chlorine atom, and a methyl group,

or

R 10 and R 11 are taken together with the nitrogen atom to which they are attached to form a monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl which is optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom, cyano, methyl, and trifluoromethyl;

R 12 and R 13 are independently selected from the group consisting of a hydrogen atom, C 1 -C 4 -alkyl, C 1 -C 2 -fluoroalkyl, C 1 -C 2 -hydroxyalkyl, (C 1 -C 4 -alkoxy)-C 2 -alkyl-, (C 1 -C 2 -fluoroalkoxy)-C 2 -alkyl-, (phenoxy)-C 2 -alkyl-, C 3 -C 7 -cycloalkyl, and (phenyl)-(C 1 -C 2 -alkyl)-,

wherein the phenyl within the (phenoxy)-C 2 -alkyl- and the phenyl within the (phenyl)-(C 1 -C 2 -alkyl)- of R 12 and R 13 are optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom, a chlorine atom, methyl, trifluoromethyl, and methoxy;

R 17 is C 1 -C 2 -alkyl;

R 18 and R 19 are independently a hydrogen atom or a methyl;

R 20 is benzyl or phenyl,

wherein the phenyl of R 20 and the phenyl within the benzyl of R 20 are optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom, a chlorine atom, and a methyl group,

R 21 is a hydrogen atom or a methyl,

Y 1 is —C(H)═, —C(F)═, —C(Cl)═, —C(CN)═ or —N═;

Y 2 is —C(H)═ or —N═;

Y 3 is —C(R 27 )═ or —N═,

with the proviso that if Y 2 is —N═, then Y 3 is —C(R 27 )═; and if Y 3 is —N═, then Y 2 is —C(H)═;

R 26 is selected from the group consisting of a fluorine atom, a chlorine atom, a bromine atom, cyano difluoromethyl, trifluoromethyl, methoxy, benzyloxy, difluoromethoxy, and trifluoromethoxy, and

R 27 is selected from the group consisting of a halogen atom, C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, —OR 9 , —N(R 10 )(R 11 ), —C(═O)—N(R 12 )(R 13 ) and —C(═O)—OR 17 ,

or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or mixture of any of the foregoing.

3 . The compound of claim 1 , wherein:

R 1 is

wherein “**” indicates the point of attachment to the nitrogen atom to which R 1 is attached;

R 2 is

wherein “*” indicates the point of attachment to the nitrogen atom to which R 2 is attached;

R 3 is methyl or —NH 2 ;

R 4 is

wherein “#” indicates the point of attachment to the carbonyl to which R 4 is attached;

R 7 is a hydrogen atom or a C 1 -C 2 -alkyl;

R 8 is —C(═O)—NH 2 ;

R 9 is selected from the group consisting of a hydrogen atom, C 1 -C 2 -alkyl, benzyl, C 1 -C 2 -fluoroalkyl, and phenyl,

wherein the phenyl of R 9 and the phenyl within the benzyl of R 9 are optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom, a chlorine atom, cyano, and methyl;

R 10 and R 11 are independently selected from the group consisting of a hydrogen atom, C 1 -C 2 -alkyl, and (benzyl)-O—C(═O)—,

and wherein the phenyl within the (benzyl)-O—C(═O)— of R 10 and R 11 is optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom, a chlorine atom, and a methyl,

or

R 10 and R 11 are taken together with the nitrogen atom to which they are attached to form a monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl which is optionally substituted with one or two substituents independently selected from the group consisting of a fluorine atom, cyano, methyl, and trifluoromethyl;

R 12 and R 13 are independently selected from the group consisting of a hydrogen atom, C 1 -C 2 -alkyl, (C 1 -C 4 -alkoxy)-C 2 -alkyl-, (C 1 -C 2 -fluoroalkoxy)-C 2 -alkyl-, (phenoxy)-C 2 -alkyl-, C 3 -C 7 -cycloalkyl, and (phenyl)-(C 1 -C 2 -alkyl)-;

Y 1 is —C(H)═, —C(F)═, —C(Cl)═ or —N═;

Y 2 is —C(H)═ or —N═;

Y 3 is —C(R 27 )═ or —N═,

with the proviso that if Y 2 is —N═, then Y 3 is —C(R 27 )═; and if Y 3 is —N═, then Y 2 is —C(H)═;

R 26 is selected from the group consisting of a fluorine atom, a chlorine atom, a bromine atom, difluoromethyl, methoxy, benzyloxy, difluoromethoxy, and trifluoromethoxy, and

R 27 is selected from the group consisting of a halogen atom, —OR 9 , —N(R 10 )(R 11 ), and —C(═O)—N(R 12 )(R 13 ),

or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or mixture of any of the foregoing.

4 . The compound of claim 1 , which is selected from the group consisting of:

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-bromo-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(6-methylpyridine-3-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(2-fluorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-cyano-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-chloro-3-(trifluoromethyl)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide,

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-chloro-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-4-[4-amino-2-(N-[2-amino-1-methyl-2-oxo-ethyl]-4-fluoro-anilino)thiazole-5-carbonyl]-N-methyl-benzamide;

rac-2-(N-[4-amino-5-(3-fluorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-chloro-4-methoxy-anilino)propanamide;

rac-2-(N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-methoxy-anilino)propanamide;

rac-2-(N-[4-amino-5-(2-fluoro-4-methoxy-benzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-(trifluoromethoxy)anilino]propanamide;

rac-2-(N-[4-amino-5-(3,4-difluorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(3,4-dichlorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-[N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-(trifluoromethoxy)anilino]propanamide;

(R)-2-[N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-(trifluoromethoxy)anilino]propanamide;

(S)-2-[N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-(trifluoromethoxy)anilino]propanamide;

rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-(trifluoromethyl)anilino]propanamide;

rac-2-(N-[4-amino-5-[6-(trifluoromethyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-[6-(trifluoromethyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-[6-(trifluoromethyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-chloro-2-fluoro-anilino)propanamide;

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3,4-difluoro-anilino)propanamide;

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-chloro-anilino)propanamide;

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3,4-dichloro-anilino)propanamide;

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-chloro-3-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propanamide;

rac-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propanamide;

2-(N-[4-amino-5-[4-[2-amino-1-methyl-2-oxo-ethoxy]benzoyl]thiazol-2-yl]anilino)propanamide (mixture of stereoisomers);

rac-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-chloro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-chloro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-chloro-anilino)propanamide;

rac-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-anilino)propanamide;

rac-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propanamide

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)anilino)propanamide;

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-fluoro-anilino)propanamide;

(R)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-fluoro-anilino)propanamide;

(S)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(4-methylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(4-methylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(4-methylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2,4-difluoro-anilino)propanamide;

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-methoxy-anilino)propanamide;

rac-2-[(4-amino-5-benzoyl-1,3-thiazol-2-yl)(phenyl)amino]butanamide;

rac-2-[(4-amino-5-benzoyl-1,3-thiazol-2-yl)(4-fluorophenyl)amino]butanamide;

2-(N-[4-amino-5-[4-(2-amino-1-methyl-2-oxo-ethoxy)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide (mixture of stereoisomers);

rac-2-{[4-amino-5-(4-methoxybenzoyl)-1,3-thiazol-2-yl](4-fluorophenyl)amino}butanamide;

2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-fluoro-anilino)acetamide;

2-(N-[4-amino-5-(4-methylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)acetamide;

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-fluoro-anilino)propanamide;

(R)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-fluoro-anilino)propanamide;

(S)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-fluoro-anilino)propanamide;

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-fluoro-anilino)propanamide;

(R)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-fluoro-anilino)propanamide;

(S)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-fluoro-anilino)propanamide;

rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(3-pyridyl)amino]propanamide;

(R)-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(3-pyridyl)amino]propanamide;

(S)-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(3-pyridyl)amino]propanamide;

rac-2-(N-[4-amino-5-(4-bromobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-ethyl 2-[4-[4-amino-2-(4-fluoro-N-[2-amino-1-methyl-2-oxo-ethyl]anilino)thiazole-5-carbonyl]phenoxy]acetate;

(R)-ethyl 2-[4-[4-amino-2-(4-fluoro-N-[2-amino-1-methyl-2-oxo-ethyl]anilino)thiazole-5-carbonyl]phenoxy]acetate;

(S)-ethyl 2-[4-[4-amino-2-(4-fluoro-N-[2-amino-1-methyl-2-oxo-ethyl]anilino)thiazole-5-carbonyl]phenoxy]acetate;

rac-2-(N-[4-amino-5-[4-[2-(isopropylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-(m-tolylmethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-(o-tolylmethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-[(3-chlorophenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-(3-methylanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-(2-methoxyethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-[(2-methoxyphenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-[(3-methoxyphenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-[(2-fluorophenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-[(4-fluorophenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-(ethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-(4-methylanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-[ethyl(methyl)amino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

2-(N-[4-amino-5-[4-[2-(2,3-dihydroxypropylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide (mixture of stereoisomers);

rac-2-(N-[4-amino-5-[4-[2-(4-methoxyanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-[benzyl(methyl)amino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-(4-chloroanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-[(2-chlorophenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-[(4-chlorophenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-(4-fluoroanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-[(4-methoxyphenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

2-(N-[4-amino-5-[4-[2-oxo-2-(1-phenylethylamino)ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide (mixture of stereoisomers);

rac-2-(N-[4-amino-5-[4-[2-oxo-2-(p-tolylmethylamino)ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-[methyl(2-phenylethyl)amino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-(N,2-dimethylanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-(N,4-dimethylanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[4-[2-(N,3-dimethylanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

2-(N-[4-amino-5-[4-[2-(4-chloroanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide (single stereoisomer);

2-(N-[4-amino-5-[4-[2-((2RS),3-dihydroxypropylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide (mixture of two diastereomers);

2-(N-[4-amino-5-[4-(2-amino-2-oxo-ethoxy)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide (single stereoisomer);

(R)-2-(N-[4-amino-5-[4-[2-(methylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-[4-[2-(methylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-[4-[2-(isopropylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-[4-[2-(isopropylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]phenoxy]-N-isopropyl-2-methyl-propanamide;

rac-2-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]phenoxy]-2-methyl-propanamide;

rac-2-(N-(5-benzoyl-4-methyl-thiazol-2-yl)-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-chloro-4-fluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-chloro-4-fluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-chloro-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-chloro-4-fluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-chloro-4-fluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-chloro-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propanamide;

(R)-benzyl N-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-3,4-difluoro-anilino)thiazole-5-carbonyl]phenyl]carbamate;

(S)-benzyl N-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-3,4-difluoro-anilino)thiazole-5-carbonyl]phenyl]carbamate;

rac-2-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]phenoxy]ethyl acetate;

rac-benzyl N-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]phenyl]carbamate;

(R)-benzyl N-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]phenyl]carbamate;

(S)-benzyl N-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]phenyl]carbamate;

rac-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(4-iodobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(4-phenoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(4-fluoro-N-[5-(4-methoxybenzoyl)-4-methyl-thiazol-2-yl]anilino)propanamide;

(R)-2-(4-fluoro-N-[5-(4-methoxybenzoyl)-4-methyl-thiazol-2-yl]anilino)propanamide;

(S)-2-(4-fluoro-N-[5-(4-methoxybenzoyl)-4-methyl-thiazol-2-yl]anilino)propanamide;

rac-2-(N-[4-amino-5-[4-(dimethylamino)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(pyridine-3-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(pyridine-3-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(pyridine-3-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(2-chloropyridine-4-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-(2-methylpyridine-4-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

(R)-2-(N-[4-amino-5-(2-methylpyridine-4-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(2-methylpyridine-4-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(4-pyridyl)amino]propanamide;

rac-2-(N-[4-amino-5-(2-methoxypyridine-4-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-fluoro-4-methoxy-anilino)propanamide;

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-cyano-3-fluoro-anilino)propanamide;

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-bromo-anilino)propanamide;

rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-3-chloro-4-(difluoromethoxy)anilino]propanamide;

rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(2,2-difluoro-1,3-benzodioxol-5-yl)amino]propanamide;

rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-(difluoromethoxy)-3-fluoro-anilino]propanamide;

rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-benzyloxy-anilino)propanamide;

rac-2-[N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-chloro-4-(difluoromethoxy)anilino]propanamide;

rac-2-[N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-3-chloro-4-(difluoromethoxy)anilino]propanamide;

rac-2-[N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-chloro-4-(difluoromethoxy)anilino]propanamide;

rac-2-[N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-(difluoromethoxy)-3-fluoro-anilino]propanamide;

rac-2-[N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-(difluoromethoxy)-3-fluoro-anilino]propanamide;

rac-2-[N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-(difluoromethoxy)-3-fluoro-anilino]propanamide;

rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-3-chloro-4-(trifluoromethoxy)anilino]propanamide;

rac-2-[[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-(2,2-difluoro-1,3-benzodioxol-5-yl)amino]propanamide;

rac-2-[[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-(2,2-difluoro-1,3-benzodioxol-5-yl)amino]propanamide;

rac-2-[[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-(2,2-difluoro-1,3-benzodioxol-5-yl)amino]propanamide;

rac-2-[[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-(2,2-difluoro-1,3-benzodioxol-5-yl)amino]propanamide;

rac-2-[[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-(2,2-difluoro-1,3-benzodioxol-5-yl)amino]propanamide;

rac-2-[N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-fluoro-4-(trifluoromethoxy)anilino]propanamide;

rac-2-[N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-3-fluoro-4-(trifluoromethoxy)anilino]propanamide;

rac-2-[N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-fluoro-4-(trifluoromethoxy)anilino]propanamide;

rac-2-[N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-chloro-4-(trifluoromethoxy)anilino]propanamide;

rac-2-[N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-3-chloro-4-(trifluoromethoxy)anilino]propanamide;

rac-2-[N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-chloro-4-(trifluoromethoxy)anilino]propanamide;

rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(6-methoxy-3-pyridyl)amino]propanamide;

rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-[6-(trifluoromethoxy)-3-pyridyl]amino]propanamide;

rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-[6-(difluoromethoxy)-3-pyridyl]amino]propanamide;

rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-[6-(trifluoromethyl)-3-pyridyl]amino]propanamide;

rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-[6-(difluoromethyl)-3-pyridyl]amino]propanamide;

rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(6-chloro-3-pyridyl)amino]propanamide;

rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(6-fluoro-3-pyridyl)amino]propanamide;

rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-fluoro-3-(trifluoromethoxy)anilino]propanamide;

rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-chloro-3-(trifluoromethoxy)anilino]propanamide;

rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-3-(difluoromethoxy)-4-fluoro-anilino]propanamide;

rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-chloro-3-(difluoromethoxy)anilino]propanamide;

rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-2-fluoro-4-(trifluoromethoxy)anilino]propanamide;

rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-2-chloro-4-(trifluoromethoxy)anilino]propanamide;

rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-(difluoromethoxy)-2-fluoro-anilino]propanamide;

rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-2-chloro-4-(difluoromethoxy)anilino]propanamide;

rac-2-[N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-(difluoromethyl)anilino]propanamide;

rac-2-[N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-(difluoromethyl)anilino]propanamide;

rac-2-[N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-(difluoromethyl)anilino]propanamide;

rac-2-[[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-[6-(trifluoromethoxy)-3-pyridyl]amino]propanamide;

rac-2-[[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-[6-(trifluoromethoxy)-3-pyridyl]amino]propanamide;

rac-2-[[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-[6-(difluoromethoxy)-3-pyridyl]amino]propanamide;

rac-2-[[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-[6-(difluoromethoxy)-3-pyridyl]amino]propanamide;

rac-benzyl N-[5-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]-2-pyridyl]carbamate;

rac-Ethyl 4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]benzoate;

rac-Ethyl 4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-chloro-3-fluoro-anilino)thiazole-5-carbonyl]benzoate;

rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]-N-benzyl-benzamide;

rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]-N-(2-methoxyethyl)benzamide;

rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]-N-cyclopropyl-benzamide;

rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]-N-cyclopentyl-benzamide;

rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-chloro-3-fluoro-anilino)thiazole-5-carbonyl]-N-(2-phenoxyethyl)benzamide;

rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-chloro-3-fluoro-anilino)thiazole-5-carbonyl]-N-(2-methoxyethyl)benzamide;

rac-2-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]phenoxy]-N-[(4-chlorophenyl)methyl]-2-methyl-propanamide;

rac-2-(N-[4-amino-5-(6-bromopyridine-3-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[6-(4-methyl-1-piperidyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[6-(dimethylamino)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[6-(4,4-dimethyl-1-piperidyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[6-(3,5-dimethyl-1-piperidyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[6-(1-piperidyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

rac-2-(N-[4-amino-5-[6-(4,4-difluoro-1-piperidyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propanamide;

2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide (single enantiomer);

(R)-2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide;

(S)-2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide;

2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propanamide (enantiomer 1); and

2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propanamide (enantiomer 2);

or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or mixture of any of the foregoing.

5 . A pharmaceutical composition comprising a compound of formula (I) of claim 1 , or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable excipients.

6 . A pharmaceutical combination comprising:

one or more compounds of formula (I) of claim 1 , and

one or more further active ingredients.

7 . The pharmaceutical combination of claim 6 , wherein the one or more further active ingredients comprises an immune checkpoint inhibitor.

8 . The pharmaceutical combination of claim 7 , wherein the immune checkpoint inhibitor is a PD-1/L-1 axis antagonist.

9 . The pharmaceutical combination of claim 7 , wherein the immune checkpoint inhibitor is an inhibitor of DGKα.