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1. WO2012058174 - NOVEL THIAZOLE-CARBOXAMIDE DERIVATIVES AS PDK1 INHIBITORS

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[ EN ]

WHAT IS CLAIMED IS:

1. A compound selected from the group consisting of:

1 -[4 ,5 -difluoro-2~[ [ [2-( 1 H-pyrazol-4-y l)-4 -thiazolyl] carbonyl] amino]pheny 1] -4-(methylamino)-4-piperidinecarboxamide;

1 - [ 5 -hy droxy-2- [ [ [2-( 1 H-pyrazol-4-y l)-4-thiazoly 1] carbonyl] amino]phenyl]-4- (methylamino)-4-piperidinecarboxamide;

1 - [5 -methoxy-2 - [ [ [2-( 1 H-pyrazol -4-yl)-4-thiazoly 1] carbonyl] amino]phenyl ] -4-(methylamino)-4-piperidinecarboxamide;

l-[4-amino-5-fluoro-2-[[[2-(l-methyl-lH-pyrazol-4-yl)-4-thiazolyl]carbonyl]amino]phenyl]-4-(methylamino)-4-piperidinecarboxamide;

1 - [5-hydroxy-2-[ [ [2-( 1 -methyl- 1 H-pyrazol-4-yl)-4-thiazolyl]carbonyl]amino]phenyl]-4-(methylamino)-4-piperidinecarboxamide;

1 -[4-amino-5-fluoro-2- [[[2- [6-( 1 -methylethoxy)-3-pyridinyl] -4-1hiazolyl]carbonyl]amino]phenyl]-4-(methyIamino)-4-piperidinecarboxamide;

1 - [3 -fluoro-2- [ [ [2-( 1 -methyl- 1 H-pyrazol-4-yl)-4-thiazolyl] carbonyl]amino] phenyl] -4-(methyIamino)-4-piperidinecarboxamide;

1 - [3 ,5-difluoro-2-[ [[2-( 1 -methyl- 1 H-pyrazol-4-yl)-4-thiazolyl]carbonyl]amino]phenyl]-4-(methylamino)-4-piperidinecarboxamide;

l-[2,3-difluoro-6-[[[2-(l-methyl-lH-pyrazol-4-yl)-4-thiazolyl]carbonyl]amino]phenyl]-4-(methylamino)~4-piperidinecarboxamide;

1 - [5 -hydroxy-2- [ [[2- [4-(2-methoxyethoxy)phenyl] -4-thiazolyl] carbonyl] amino]phenyl] -4-(methylamino)-4-piperidinecarboxamide;

1- [2-[[[2-(233-dihydro-5-benzofuranyl)-4-thiazolyl]carbonyl]amino]-5-hydroxyphenyl]-4-(methylamino)-4-piperidinecarboxamide ;

1 - [4-amino-2-fluoro-6-[ [ [2-( 1 H-pyrazol-4-yl)-4-thiazolyl] carbonyl] amino]pheny 1] -4-(methylamino)-4-piperidinecarboxamide;

1 -[5~amino~3 - [[[2-( 1 H-pyrazol-4-yl)-4-thiazolyl]carbonyl]amino] -2-pyridinyl] -4-(methylamino)-4-piperidinecarboxamide;

l-[4-amino-2-fluoro-6-[[[2-(l -methyl- 1 H~pyrazol-4-yl)~4-thiazolyl] carbonyl] amino]phenyl] -4-(methylamino)-4-piperidinecarboxamide;

2- (4 -amino- 1 H-pyrazol- 1 -yl)-N- (5-amino-2-(4-carbamoyl-4 -(methylamino)piperidin- 1 -yl)phenyl)thiazole-4-carboxamide;

1 - [4-amino-2 - [ [ [2-( 1 H-pyrazol-4-yl)-4-thiazoly 1] carbonyl]amino]pheny 1] -4 -(methylamino)-4-piperidinecarboxamide;

l-[4-hydroxy-2-[[[2-(lH-pyrazol-4-yl)-4-thiazolyl]carbonyl]amino]phenyl]-4-(methylamino)-4-piperidinecarboxamide ;

1 - [4-hydroxy-2- [[ [2-( 1 -methyl- 1 H-pyrazol-4-yl)-4-thiazoly 1] carbonyl]amino]phenyl]~4- (methylammo)-4-piperidinecarboxamide;

4-(methylamino)-l-[5-methyl-2-[[[2-(l^^

piperidinecarboxamide ;

N-[4-amino-2-(l -methyl-2,4-dioxo-l ,3,84riazaspiro[4.5]dec-8-yl)phenyl]-2-(l H-pyrazol-4-yl)-4-thiazolecarboxarmde;

1 - [5-amino-2- [ [[2-( 1 H-pyrazol-4-yl)-4-thiazoly 1] carbonyl] amino]pheny 1] -4-(methyl amino)-4-piperidinecarboxamide;

1 - [4-cyano-2-[ [ [2-( 1 H-pyrazol-4-yl)-4-thiazolyl] carbonyl] amino] phenyl] -4 -(methylamino)-4-piperidinecarboxamide;

l~[4-amino-2-fluoro-6-[[[2-(3-pyridinyl)-4-thiazolyl]carbonyl]amino]phenyl]-4-(methylamino)-4-piperidinecarboxamide;

l-[4,5-diamino-2-[[[2-(lH-pyrazol-4-yl)-4-thiazolyl]carbonyl]amino]phenyl]-4-(methylami 4-piperidinecarboxamide;

1 -[4-arnino~2-£!uoro-6-[[[2-(2-methyl-4-pyridinyl)-4-thiazolyl]carbonyl]arnino]phenyl]-4-(methylamino)-4-piperidinecarboxarmde;

1 -[4-amino-2-[[[2-(l -methyl-1 H-pyrazol-5-yl)-4-thiazolyl]carbonyl]amino]phenyl]-4-(methylamino)-4-piperidmecarboxamide;

l-[4-amino-2-[[[2-(6-hydroxy-3-pyridmyl)-4-thiazolyl]carbonyl]amino]pl enyl]-4-(methylamino)~4-piperidinecarboxamide;

1 - [4-amino-2- [ [ [2~(2~amino-5 -pyr imidinyl)-4-thiazolyl]carbonyI] amino] phenyl] -4-(methylamino)-4-piperidinecarboxamide;

l-[4-amino-2-[[[2-(5-pyrimidinyl)-4-thiazolyl]carbonyl]amino]phenyl]-4-(methylamino)-4-piperidinecarboxamide ;

l-[4-amino-2-[[[2-[2-(trifluororaethyl)-4-pyridinyl]-4-thiazolyl]carbonyl]amino]phenyl]-4-(memylamino)-4-piperidinecarboxamide ;

1 - [4-amino-2-[ [[2-[6-(trifluoromethyl)-3 -pyridinyl] -4-thiazolyl]carbonyl] amino]phenyl] -4-(methylamino)-4-piperidinecarboxamide;

l-[4-amino-2-[[[2-(2-hydroxy-5-pyrimidinyl)-4-thiazolyl]carbonyl]amino]phenyl]-4-(methylamino)-4-piperidinecarboxamide;

l-[4-amino-2-[[[2-[l-methyl-3-(trifluoromethyl)-lH-pyrazol-5-yl]-4-thiazolyl]carbonyl]amino]phenyl]-4-(methylamino)-4-piperidinecarboxamide;

N-[5-amino-2-(2}9-diazaspiro[5.5]undec-9-yl)phenyl]-2-[l-methyl-3-(trifluoromethyl)-lH-pyrazol-5 -yl] -4-thiazolecarboxamide ;

l-[4-amino-2-[[[2-(3,5-dimethyl-4-isoxazolyl)-4-thiazolyl]carbonyl]amino]phenyl]-4- (methylamino)-4-piperidinecarboxamide;

N - [5 -amino-2-(2,9-di azaspiro [5.5] undec-9-yl)phenyl] ~2- [ 3 - (tr i fmoromethy 1)- 1 H-pyrazol- 5 -yl] -4-thiazolecarboxamide;

1 - [4-ami no-2- [[ [2-(2-methyl-3 -pyri diny^

4-piperidinecarboxamide;

N-[5-amino-2-(2J8-diazaspiro[4.5]dec-8-yl)-3-pyridinyl]-2~(lH-pyrazol-4-yl)-4-thiazolecarboxamide;

N- [5 -amino-2-(2 ,8-di azaspiro [4.5] dec-2-y l)-3 -pyridinyl] -2-( 1 H-pyrazol-4-y l)-4-thiazolecarboxarnide;

N-[5-amino-2-(2J9-diazaspiro[5.5]undec-2-yl)-3-pyridinyl]-2-(lH-pyrazoI-4-yl)-4-thiazolecarboxamide;

N-[5-amino-2-(2,9-diazaspiro[5.5]undec-9-yl)-3-pyridinyl]-2-(lH-pyrazol-4-yl)-4-thiazolecarboxamide;

1 -[4-amino-2-[[[2-(4-ammo- 1 H-pyrazol- 1 -yi)-4-thiazolyl]carbonyl] amino] -6-fluorophenyl] -4-(methylamino)-4-piperidinecarboxamide;

1 2-[[[2-(4-amino-lH-pyrazol-l-yl)-4-thiazolyl]carbonyl]amino]-5-hydroxyphenyl]-4-(methylamino)-4-piperidinecarboxamide;

l-[4-amino-2-fluoro-6-[[[2-(4-methyM

(methylamino)-4-piperidinecarboxamide;

l~[4-amino-2-fluoro-6-[[[2-(lH-pyrazol-l-yl)-4-thiazolyl3carbonyl]amino]phenyl]-4-(methylamino)-4-piperidinecarboxamide;

1 -[4-amino-2-fluoro-6- [[ [2-(3 -oxo- 1 -piperazinyl)-4-thiazolyl] carbonyl] aminojphenyl] -4-(methylamino)-4-piperidinecarboxamide; and

l-[4-amino-2-fluoro-6-[[[2-(4-morpholmyl)-4-thiazolyl]carbonyl]amino]phenyl3-4-(methylamino)-4-piperidinecarboxamide;

Or a stereoisomer thereof;

Or a pharmaceutically acceptable salt thereof;

Or a pharamceutically acceptable salt of the stereoisomer thereof.

2. A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 1 and a pharmaceutically acceptable carrier and optionally other therapeutic ingredients.

3. Use of a compound according to claim 1 for the preparation of a

medicament for the treatment of cancer.

4. A method of treating a disease by inibiting PDK-l , comprising administering a therapeutically effective amount of a compound of claim 1.