IP Library Granted Patent US 9,670,172
Granted Patent B2
US 9,670,172 · App. 14/471,977 · Granted Jun 6, 2017

Heterocyclic compounds and methods of use

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Quick Facts
Patent No.
US 9,670,172
App. No.
14/471,977
Granted
Jun 6, 2017
Kind
B2
Abstract

This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists.

Claims (267)

1. A compound of Formulae (Ia):

or a pharmaceutically acceptable salt thereof, wherein:

A is either:

i. an aryl or heteroaryl, each having only one ring, substituted with 1, 2, or 3 substituents selected from the group consisting of halogen, CN, CF 3 , OH, C1-C6 linear or branched alkyl, C3-C6 cycloalkyl, C3-C6 cycloalkenyl, C1-C6 linear or branched hydroxyalkyl, C1-C3 linear or branched alkoxy, C3-C6 cycloalkylmethyl, —(CH 2 ) m CF 3 , ═O, —CH 2 OCH 3 , —OBn, —CO 2 H, —CO 2 -Alkyl, —NR10R11, and —CONR10R11; or

ii. an aryl or heteroaryl, each having more than one ring, optionally substituted with 1, 2, or 3 substituents selected from the group consisting of halogen, CN, CF 3 , OH, C1-C6 linear or branched alkyl, C3-C6 cycloalkyl, C3-C6 cycloalkenyl, C1-C6 linear or branched hydroxyalkyl, C1-C3 linear or branched alkoxy, C3-C6 cycloalkylmethyl, —(CH 2 ) m CF 3 , ═O, —CH 2 OCH 3 , —CH 2 OH, —OBn, —CO 2 H, —CO 2 -Alkyl, —NR10R11, and —CONR10R11;

Each R C4 , R C5 , and R C6 , is independently hydrogen, halogen, CN, CF 3 , OH, C1-C3 linear or branched alkyl, C2-C3 alkenyl, C2-C3 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloalkenyl, C1-C3 linear or branched alkoxy, —CO 2 H, —CONR10R11, or —NHCONH 2 ;

or is taken with R C7 to form the moiety

R C7 is hydrogen, C1-C6 linear or branched alkyl, C1-C6 linear or branched hydroxyalkyl, —(CR 9a R 9b ) m NR10R11, —CO 2 -Alkyl, —(CR 9a R 9b ) m O-Alkyl, —(CR 9a R 9b ) m OPO 3 Na 2 , —(CR 9a R 9b ) m O(CR 9a R 9b ) n O-Alkyl, —(CR 9a R 9b ) m O(C═O)-Alkyl, —(CR 9a R 9b ) m O(CR 9a R 9b ) n O(C═O)-Alkyl, —(C═O)CH═CH 2 , —SO 2 R C8′ ; or is taken with one of R C4 , R C5 or R C6 to form the moiety

R C8 is a linear or branched C1-C6 perhaloalkyl, a linear or branched C2-C6 perhaloalkenyl, a linear or branched C2-C6 perhaloalkynyl, a linear or branched C1-C6 alkyl having at least one halogen atom, a linear or branched C2-C6 alkenyl having at least one halogen atom, or a linear or branched C2-C6 alkynyl having at least one halogen atom;

R C8′ is a linear or branched C1-C6 alkyl, a linear or branched C1-C6 perhaloalkyl, a linear or branched C2-C6 perhaloalkenyl, a linear or branched C2-C6 perhaloalkynyl, a linear or branched C1-C6 alkyl having at least one halogen atom, a linear or branched C2-C6 alkenyl having at least one halogen atom, or a linear or branched C2-C6 alkynyl having at least one halogen atom;

Each R 9a and R 9b , where present, is independently hydrogen or C1-C6 linear or branched alkyl;

R10 and R11 are independently hydrogen, —SO 2 R C8′ , C1-C6 linear or branched alkyl, C2-C6 linear or branched alkenyl, C3-C6 cycloalkyl, or C3-C6 cycloalkenyl; or are taken together with the N to which they are attached to form a C3-C6 heterocycle, pyrrolidinone, piperidinone, oxazolidinone, oxazinanone, imidazolidinone, tetrahydropyrimidin-2(1H)-one, a 1λ 6 ,2-thiazolidine-1,1-dione, a 1,2λ 6 ,3-oxathiazolidine-2,2-dione, or a 1λ 6 ,2,5-thiadiazolidine-1,1-dione;

X is a heteroatom selected from S, O; or NR B wherein R B is hydrogen, a C1-C6 linear or branched alkyl, or a C3-C6 cycloalkyl; and

Each m and n is 1, 2 or 3.

2. The compound of claim 1 , wherein compound is of formulae (IIa):

or a pharmaceutically acceptable salt thereof, wherein:

A is a moiety selected from the group consisting of:

wherein the ring containing X is linked to ring A at any available position on ring A;

Each R C4 , R C5 , and R C6 , is independently hydrogen, halogen, CN, CF 3 , OH, C1-C3 linear or branched alkyl, C2-C3 alkenyl, C2-C3 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloalkenyl, C1-C3 linear or branched alkoxy, —CO 2 H, —CONR10R11, or —NHCONH 2 ;

or is taken with R C7 to form the moiety

R C7 is hydrogen, C1-C6 linear or branched alkyl, C1-C6 linear or branched hydroxyalkyl, —(CR 9a R 9b ) m NR10R11, —(CR 9a R 9b ) m O-Alkyl, —(CR 9a R 9b ) m OPO 3 Na 2 , —(CR 9a R 9b ) m O(CR 9a R 9b ) n O-Alkyl, —(CR 9a R 9b ) m O(C═O)-Alkyl, —(CR 9a R 9b ) m O(CR 9a R 9b ) n O(C═O)-Alkyl, —(C═O)CH═CH 2 , —SO 2 R C8′ ; or is taken with one of R C4 , R C5 or R C6 to form the moiety

R C8 is a linear or branched C1-C6 perhaloalkyl, a linear or branched C2-C6 perhaloalkenyl, a linear or branched C2-C6 perhaloalkynyl, a linear or branched C1-C6 alkyl having at least one halogen atom, a linear or branched C2-C6 alkenyl having at least one halogen atom, or a linear or branched C2-C6 alkynyl having at least one halogen atom;

R C8′ is a linear or branched C1-C6 alkyl, a linear or branched C1-C6 perhaloalkyl, a linear or branched C2-C6 perhaloalkenyl, a linear or branched C2-C6 perhaloalkynyl, a linear or branched C1-C6 alkyl having at least one halogen atom, a linear or branched C2-C6 alkenyl having at least one halogen atom, or a linear or branched C2-C6 alkynyl having at least one halogen atom;

Each R 9a and R 9b , where present, is independently hydrogen or C1-C6 linear or branched alkyl;

R10 and R11 are independently hydrogen, —SO 2 R C8′ , C1-C6 linear or branched alkyl, C2-C6 linear or branched alkenyl, C3-C6 cycloalkyl, or C3-C6 cycloalkenyl; or are taken together with the N to which they are attached to form a C3-C6 heterocycle, pyrrolidinone, piperidinone, oxazolidinone, oxazinanone, imidazolidinone, tetrahydropyrimidin-2(1H)-one, a 1λ 6 ,2-thiazolidine-1,1-dione, a 1,2λ 6 ,3-oxathiazolidine-2,2-dione, or a 1λ 6 ,2,5-thiadiazolidine-1,1-dione;

X is a heteroatom selected from S, O; or NR B wherein R B is hydrogen, a C1-C6 linear or branched alkyl, or a C3-C6 cycloalkyl; and

Each m and n is 1, 2 or 3.

3. The compound of claim 2 , wherein A is a moiety selected from the group consisting of:

4. The compound of claim 3 , wherein A is a moiety selected from the group consisting of:

5. The compound of claim 4 , wherein A is a moiety selected from the group consisting of:

6. The compound of claim 1 , wherein X is S.

7. The compound of claim 1 , wherein X is NR B , wherein R B is a linear or branched C1-C6 alkyl.

8. The compound of claim 7 , wherein R B is a linear C1-C6 alkyl selected from methyl, ethyl, n-propyl, n-butyl, n-pentyl or n-hexyl.

9. The compound of claim 7 , wherein R B is a branched C1-C6 alkyl selected from iso-propyl, iso-pentyl, and tert-butyl.

10. The compound of claim 1 , wherein the phenyl ring containing the groups R C4 , R C5 , R C6 , and —NR C7 SO 2 R C8 , is a moiety selected from:

11. The compound of claim 10 , wherein the phenyl ring containing the groups R C4 , R C5 , R C6 , and —NR C7 SO 2 R C8 , is a moiety selected from:

12. The compound of claim 1 , wherein at least one of R C4 , R C5 and R C6 is hydrogen.

13. The compound of claim 12 , wherein two of R C4 , R C5 and R C6 are hydrogen.

14. The compound of claim 12 , wherein each R C4 , R C5 and R C6 is hydrogen.

15. The compound of claim 1 , wherein at least one of R C4 , R C5 and R C6 is halogen.

16. The compound of claim 15 , wherein two of R C4 , R C5 and R C6 are halogen.

17. The compound of claim 15 , wherein each R C4 , R C5 and R C6 is halogen.

18. The compound of claim 1 , wherein one of R C4 , R C5 and R C6 is hydrogen, and the remaining two of R C4 , R C5 and R C6 are halogen.

19. The compound of claim 1 , wherein two of R C4 , R C5 and R C6 are hydrogen, and the remaining one of R C4 , R C5 and R C6 is halogen.

20. The compound of claim 1 , wherein:

A is a moiety selected from

X is S, and

the phenyl ring containing the groups R C4 , R C5 , R C6 , and —NR C7 SO 2 R C8 , is a moiety selected from:

21. The compound of claim 1 , wherein:

A is a moiety selected from

X is S, and

the phenyl ring containing the groups R C4 , R C5 , R C6 and —NR C7 SO 2 R C8 , is a moiety selected from

22. The compound of claim 1 , wherein:

A is

X is S, and

the phenyl ring containing the groups R C4 , R C5 , R C6 , and —NR C7 SO 2 R C8 , is selected from

23. The compound of claim 2 , wherein:

A is

X is S;

the phenyl ring containing the groups R C4 , R C5 , R C6 , and —NR C7 SO 2 R C8 , is selected from

24. A compound selected from the group consisting of:

1,1,1-trifluoro-N-(4-(2-(2-propylpyridin-4-yl)thiazol-4-yl)phenyl)methanesulfonamide;

1,1,1-trifluoro-N-(3-(2-(2-propylpyridin-4-yl)thiazol-4-yl)phenyl)methanesulfonamide;

N-(3-chloro-4-(2-(1-isobutyl-1H-pyrazol-)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(2-propylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(4-(2-(2-tert-butylpyridin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(1,2-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(1-propyl-1H-pyrrolo[2,3-b]pyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(2,3-dimethyl-3H-imidazo[4,5-b]pyridin-7-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(3-propyl-3H-imidazo[4,5-b]pyridin-7-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(4-(2-(3H-imidazo[4,5-b]pyridin-7-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(1,2-dipropyl-1H-pyrrolo[2,3-b]pyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(4-(2-(6-(butylamino)-2-isobutylpyrimidin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(6-(dibutylamino)-2-isobutylpyrimidin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(4-(2-(6-amino-2-isobutylpyrimidin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoromethanesulfonamide;

N-(4-(2-(2-aminopyrimidin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(2-(propylamino)pyrimidin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(2-(dibutylamino)pyrimidin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2′-propyl-2,4′-bithiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(5-propyl-1,2,4-thiadiazol-3-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(5-propyl-1,2,4-oxadiazol-3-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2′-propyl-2,5′-bithiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(5-propyl-1,3,4-thiadiazol-2-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(5-propyl-1,3,4-oxadiazol-2-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(1-isobutyl-6-oxo-1,6-dihydropyridin-3-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(4-fluoro-3-isobutylphenyl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(2-bromo-3-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3,5-dichloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

1,1,1-trifluoro-N-(4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)-2-(trifluoromethyl)phenyl)methanesulfonamide;

N-(2-cyclopropyl-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

1,1,1-trifluoro-N-(4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)-2-methylphenyl)methanesulfonamide;

1,1,1-trifluoro-N-(4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)-2-isopropylphenyl)methanesulfonamide;

N-(2-ethynyl-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(2-bromo-3-ethynyl-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(2-bromo-6-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(2-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)-6-methylphenyl)-1,1,1-trifluoromethanesulfonamide;

N-(4-(4-(2-tert-butylpyridin-4-yl)-1-methyl-1H-imidazol-2-yl)-3-chlorophenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(2-bromo-4-(1-methyl-2-(2-propylpyridin-4-yl)-1H-imidazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(2-bromo-3-chloro-4-(2-(2-propylpyridin-4-yl)-1H-imidazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(2-bromo-5-chloro-4-(1-methyl-2-(2-propylpyridin-4-yl)-1H-imidazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(4-(4-(2-tert-butylpyridin-4-yl)oxazol-2-yl)-3-chlorophenyl)-1,1,1-trifluoromethanesulfonamide;

N-(4-(2-(2-tert-butylpyridin-4-yl)oxazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(2-(dimethylamino)pyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(2-propylpyridin-4-yl)thiazol-4-yl)phenyl)-N-(trifluoromethylsulfonyl)acrylamide;

N-(3-chloro-4-(2-(2-(methylsulfonamido)pyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(2-(3,3,3-trifluoropropyl)pyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

1,1,1-trifluoro-N-(2-hydroxy-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)methanesulfonamide;

1,1,1-trifluoro-N-(2-hydroxy-4-(2-(2-propylpyridin-4-yl)thiazol-4-yl)phenyl)methanesulfonamide;

N-(4-(2-(2-tert-butylpyridin-4-yl)thiazol-4-yl)-2-hydroxyphenyl)-1,1,1-trifluoromethanesulfonamide;

1,1,1-trifluoro-N-(2-methoxy-4-(2-(2-propylpyridin-4-yl)thiazol-4-yl)phenyl)methanesulfonamide;

1,1,1-trifluoro-N-(4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)-2-methoxyphenyl)methanesulfonamide;

N-(4-(2-(2-tert-butylpyridin-4-yl)thiazol-4-yl)-2-methoxyphenyl)-1,1,1-trifluoromethanesulfonamide;

1,1,1-trifluoro-N-(4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)-3-(trifluoromethyl)phenyl)methanesulfonamide;

N-(3-chloro-4-(2-(2-neopentylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

6-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)-3-(trifluoromethyl sulfonyl)benzo[d]oxazol-2(3H)-one;

N-(3-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,2,2,2-pentafluoroethanesulfonamide;

1,1,1-trifluoro-N-(2-methoxy-4-{2-[2-(2-methylpropyl)pyridin-4-yl]-1,3-thiazol-4-yl}phenyl)methanesulfonamide;

1,1,1-trifluoro-N-{2-methoxy-4-[2-(2-propylpyridin-4-yl)-1,3-thiazol-4-yl]phenyl}methanesulfonamide;

N-{4-[2-(2-tert-butylpyridin-4-yl)-1,3-thiazol-4-yl]-2-methoxyphenyl}-1,1,1-trifluoromethanesulfonamide;

N-{4-[2-(2-benzylpyridin-4-yl)-1,3-thiazol-4-yl]-3-chlorophenyl}-1,1,1-trifluoromethanesulfonamide;

N-{4-[2-(2-aminopyridin-4-yl)-1,3-thiazol-4-yl]-3-chlorophenyl}-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(2-methanesulfonamidopyridin-4-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

1,1,1-trifluoro-N-{2-hydroxy-4-[2-(2-propylpyridin-4-yl)-1,3-thiazol-4-yl]phenyl}methanesulfonamide;

N-(3-chloro-4-{2-[2-(3,3,3-trifluoropropyl)pyridin-4-yl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(4-{2-[2-(2,2-dimethylpropyl)pyridin-4-yl]-1,3-thiazol-4-yl}-2-methoxyphenyl)-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(2-trifluoromethanesulfonamidopyridin-4-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(4-(piperidine-1-carbonyl)phenyl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[1-(3-methylbutyl)-1H-pyrazol-5-yl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-{4-[5-(2-tert-butylpyridin-4-yl)thiophen-3-yl]-3-chlorophenyl}methanesulfonamide;

N-(3-chloro-4-{2-[2-(cyclohexylmethyl)pyridin-4-yl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(naphthalen-1-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(1H-indol-6-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-(4-{2-[3-(benzyloxy)-4-(trifluoromethyl)phenyl]-1,3-thiazol-4-yl}-3-chlorophenyl)-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(2-phenylphenyl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(isoquinolin-4-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(dimethyl-1,2-oxazol-4-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-{3-[4-(2-chloro-4-trifluoromethanesulfonamidophenyl)-1,3-thiazol-2-yl]phenyl}-4-methylbenzene-1-sulfonamide;

N-{3-chloro-4-[2-(3,4-dimethoxyphenyl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(1H-indol-4-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[4-fluoro-2-(trifluoromethyl)phenyl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(2,3-dihydro-1-benzofuran-5-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[3-(hydroxymethyl)phenyl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[2-(hydroxymethyl)phenyl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[2-(piperidin-1-yl)pyridin-4-yl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(3-methylpyridin-4-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-[3-chloro-4-(2-{1H-pyrrolo[2,3-b]pyridin-4-yl}-1,3-thiazol-4-yl)phenyl]-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[3-(piperidin-1-yl)phenyl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-[3-chloro-4-(2-{5-fluoro-1H-pyrrolo[2,3-b]pyridin-4-yl}-1,3-thiazol-4-yl)phenyl]-1,1,1-trifluoromethanesulfonamide;

N-{4-[2-(1-benzothiophen-3-yl)-1,3-thiazol-4-yl]-3-chlorophenyl}-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[4-fluoro-2-(pyrrolidin-1-ylmethyl)phenyl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[2-(cyclopentylamino)pyridin-4-yl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(1H-indol-3-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(quinolin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(2-chloropyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(2-bromo-4-(2-(2-tert-butylpyridin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoromethanesulfonamide;

N-(2-bromo-4-(2-(2-propylpyridin-4-yl)-1H-imidazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(2-bromo-4-(2-(2-tert-butylpyridin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoro-N-(2-hydroxyethyl)methanesulfonamide;

N-(4-(2-(2-tert-butylpyridin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoro-N-(2-(2-oxopyrrolidin-1-yl)ethyl)methanesulfonamide;

N-(4-(2-(2-tert-butylpyridin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoro-N-(2-(2-oxooxazolidin-3-yl)ethyl)methanesulfonamide;

N-(4-(2-(2-tert-butylpyridin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoro-N-(2-(2-oxoimidazolidin-1-yl)ethyl)methanesulfonamide;

N-(2-bromo-4-(2-(2-(piperidin-1-yl)pyridin-4-yl)-1H-imidazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

2-(N-(4-(2-(2-tert-butylpyridin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoromethyl sulfonamido)ethyl acetate;

(2-(N-(4-(2-(2-tert-butylpyridin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoromethyl sulfonamido)ethoxy)methyl acetate;

N-{4-[2-(2-tert-butylpyridin-4-yl)-1,3-thiazol-4-yl]-3-chlorophenyl}-N-(2-{[4-(3-chlorophenyl)-2-oxo-1,3,2λ 5 -dioxaphosphinan-2-yl]oxy}ethyl)-1,1,1-trifluoromethanesulfonamide;

(N-(4-(2-(2-tert-butylpyridin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoromethyl sulfonamido)methyl acetate;

N-(4-(2-(2-tert-butylpyridin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoro-N-(methoxymethyl)methanesulfonamide;

N-{4-[2-(2-tert-butylpyridin-4-yl)-1,3-thiazol-4-yl]-3-chlorophenyl}-N-({[4-(3-chlorophenyl)-2-oxo-1,3,2λ 5 -dioxaphosphinan-2-yl]oxy}methyl)-1,1,1-trifluoromethanesulfonamide;

methyl 4-(2-(2-tert-butylpyridin-4-yl)thiazol-4-yl)-3-chlorophenyl(trifluoromethylsulfonyl)carbamate;

sodium (N-(4-(2-(2-tert-butylpyridin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoromethylsulfonamido)methyl phosphate;

1-(N-(3-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethylsulfonamido)ethyl isobutyrate;

N-(3-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoro-N-(2-(2-oxooxazolidin-3-yl)ethyl)methanesulfonamide;

N-(4-(2-(2-tert-butylpyridin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoro-N-(2-hydroxyethyl)methanesulfonamide;

N-(3-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoro-N-(2-(pyrrolidin-1-yl)ethyl)methanesulfonamide;

N-(3-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-N-(2-(diethylamino)ethyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-N-(2-(dimethylamino)ethyl)-1,1,1-trifluoromethanesulfonamide;

1,1,1-trifluoro-N-(3-fluoro-4-(2-(2-propylpyridin-4-yl)thiazol-4-yl)phenyl)methanesulfonamide;

N-(3-chloro-4-(2-(2-isobutylpyridin-4-yl)-1H-imidazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoro-N-(2-hydroxyethyl)methanesulfonamide;

N-(3-chloro-4-(2-(2-propylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoro-N-methylmethanesulfonamide;

1,1,1-trifluoro-N-(3-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)methanesulfonamide;

N-(2-bromo-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

1,1,1-trifluoro-N-methyl-N-(4-(2-(2-propylpyridin-4-yl)thiazol-4-yl)phenyl)methanesulfonamide;

N-(4-(2-(2-butylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide

1,1,1-trifluoro-N-(4-(2-(2-(methoxymethyl)pyridin-4-yl)thiazol-4-yl)phenyl)methanesulfonamide;

N-(4-(2-(4,6-dipropylpyridin-2-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

1,1,1-trifluoro-N-(4-(2-(4-propylpyridin-2-yl)thiazol-4-yl)phenyl)methanesulfonamide;

N-(4-(2-(2,6-dipropylpyridin-3-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(4-(2-(2-(cyclohexylmethyl)pyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

1,1,1-trifluoro-N-(4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)-3-methoxyphenyl)methanesulfonamide;

N-(3-chloro-4-(2-(2-((trifluoromethylsulfonyl)methyl)pyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(4-(2-(1H-pyrrolo[2,3-b]pyridin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(2-propyl-3H-imidazo[4,5-b]pyridin-7-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

5-(4-(2-chloro-4-(trifluoromethylsulfonamido)phenyl)thiazol-2-yl)-N-cyclopropyl-2-fluorobenzamide;

5-(4-(2-chloro-4-(trifluoromethylsulfonamido)phenyl)thiazol-2-yl)-N-cyclohexyl-2-fluorobenzamide;

N-(4-(2-(1H-indol-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(3-(piperidin-1-yl)phenyl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(2-(piperidin-1-yl)pyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(2-bromo-4-(2-(2-tert-butylpyridin-4-yl)-1H-imidazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(2-chloro-4-(2-(2-propylpyridin-4-yl)-1H-imidazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(2-bromo-5-chloro-4-(2-(2-propylpyridin-4-yl)-1H-imidazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide; and

N-(2-bromo-4-(2-(2-propylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide.

25. The compound of claim 24 , wherein the compound is selected from the group consisting of:

1,1,1-trifluoro-N-(4-(2-(2-propylpyridin-4-yl)thiazol-4-yl)phenyl)methanesulfonamide;

1,1,1-trifluoro-N-(3-(2-(2-propylpyridin-4-yl)thiazol-4-yl)phenyl)methanesulfonamide;

N-(3-chloro-4-(2-(1-isobutyl-1H-pyrazol-)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(2-propylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(4-(2-(2-tert-butylpyridin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

1,1,1-trifluoro-N-(2-methoxy-4-{2-[2-(2-methylpropyl)pyridin-4-yl]-1,3-thiazol-4-yl}phenyl)methanesulfonamide;

1,1,1-trifluoro-N-{2-methoxy-4-[2-(2-propylpyridin-4-yl)-1,3-thiazol-4-yl]phenyl}methanesulfonamide;

N-{4-[2-(2-tert-butylpyridin-4-yl)-1,3-thiazol-4-yl]-2-methoxyphenyl}-1,1,1-trifluoromethanesulfonamide;

N-{4-[2-(2-benzylpyridin-4-yl)-1,3-thiazol-4-yl]-3-chlorophenyl}-1,1,1-trifluoromethanesulfonamide;

N-{4-[2-(2-aminopyridin-4-yl)-1,3-thiazol-4-yl]-3-chlorophenyl}-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(2-methanesulfonamidopyridin-4-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

1,1,1-trifluoro-N-{2-hydroxy-4-[2-(2-propylpyridin-4-yl)-1,3-thiazol-4-yl]phenyl}methanesulfonamide;

N-(3-chloro-4-{2-[2-(3,3,3-trifluoropropyl)pyridin-4-yl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(4-{2-[2-(2,2-dimethylpropyl)pyridin-4-yl]-1,3-thiazol-4-yl}-2-methoxyphenyl)-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(2-trifluoromethanesulfonamidopyridin-4-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(4-(piperidine-1-carbonyl)phenyl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[1-(3-methylbutyl)-1H-pyrazol-5-yl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-{4-[5-(2-tert-butylpyridin-4-yl)thiophen-3-yl]-3-chlorophenyl}methanesulfonamide;

N-(3-chloro-4-{2-[2-(cyclohexylmethyl)pyridin-4-yl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(naphthalen-1-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(1H-indol-6-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-(4-{2-[3-(benzyloxy)-4-(trifluoromethyl)phenyl]-1,3-thiazol-4-yl}-3-chlorophenyl)-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(2-phenylphenyl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(isoquinolin-4-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(dimethyl-1,2-oxazol-4-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-{3-[4-(2-chloro-4-trifluoromethanesulfonamidophenyl)-1,3-thiazol-2-yl]phenyl}-4-methylbenzene-1-sulfonamide;

N-{3-chloro-4-[2-(3,4-dimethoxyphenyl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(1H-indol-4-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[4-fluoro-2-(trifluoromethyl)phenyl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(2,3-dihydro-1-benzofuran-5-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[3-(hydroxymethyl)phenyl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[2-(hydroxymethyl)phenyl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[2-(piperidin-1-yl)pyridin-4-yl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(3-methylpyridin-4-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-[3-chloro-4-(2-{1H-pyrrolo[2,3-b]pyridin-4-yl}-1,3-thiazol-4-yl)phenyl]-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[3-(piperidin-1-yl)phenyl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-[3-chloro-4-(2-{5-fluoro-1H-pyrrolo[2,3-b]pyridin-4-yl}-1,3-thiazol-4-yl)phenyl]-1,1,1-trifluoromethanesulfonamide;

N-{4-[2-(1-benzothiophen-3-yl)-1,3-thiazol-4-yl]-3-chlorophenyl}-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[4-fluoro-2-(pyrrolidin-1-ylmethyl)phenyl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[2-(cyclopentylamino)pyridin-4-yl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(1H-indol-3-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide; and

N-(3-chloro-4-(2-(quinolin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide.

26. The compound of claim 25 , wherein the compound is selected from the group consisting of:

N-(3-chloro-4-(2-(2-propylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-(4-(2-(2-tert-butylpyridin-4-yl)thiazol-4-yl)-3-chlorophenyl)-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide;

N-{4-[2-(2-benzylpyridin-4-yl)-1,3-thiazol-4-yl]-3-chlorophenyl}-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[2-(3,3,3-trifluoropropyl)pyridin-4-yl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide;

N-{3-chloro-4-[2-(1H-indol-4-yl)-1,3-thiazol-4-yl]phenyl}-1,1,1-trifluoromethanesulfonamide;

N-(3-chloro-4-{2-[2-(piperidin-1-yl)pyridin-4-yl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide; and

N-(3-chloro-4-{2-[3-(piperidin-1-yl)phenyl]-1,3-thiazol-4-yl}phenyl)-1,1,1-trifluoromethanesulfonamide.

27. A compound N-(3-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide.

28. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable vehicle.

29. A method of treating a cancer selected from the group consisting of breast cancer, prostate cancer, and liver cancer, comprising administering to an individual in need thereof a therapeutically effective amount of a compound of claim 1 .

30. The method of claim 29 , wherein the cancer is breast cancer.

31. The method of claim 29 , wherein the cancer is prostate cancer.

32. The method of claim 29 , wherein the cancer is liver cancer.

33. The pharmaceutical composition of claim 28 , wherein the compound is compound N-(3-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide.

34. The method of claim 30 , wherein the compound is compound N-(3-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide.

35. The method of claim 31 , wherein the compound is compound N-(3-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide.

36. The method of claim 32 , wherein the compound is compound N-(3-chloro-4-(2-(2-isobutylpyridin-4-yl)thiazol-4-yl)phenyl)-1,1,1-trifluoromethanesulfonamide.

Assignments (4)
CHANGE OF NAME Recorded Oct 24, 2017
From: MEDIVATION TECHNOLOGIES, INC.
To: MEDIVATION TECHNOLOGIES LLC
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RELEASE OF SECURITY INTEREST Recorded Sep 28, 2016
From: JPMORGAN CHASE BANK, N.A., AS ADMINISTRATIVE AGENT
To: MEDIVATION PROSTATE THERAPEUTICS, INC.; MEDIVATION TECHNOLOGIES, INC.
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CONFIRMATORY ASSIGNMENT Recorded Jan 18, 2016
From: CHAKRAVARTY, SARVAJIT; RAI, ROOPA; PHAM, SON MINH; PUJALA, BRAHMAM; JANGIR, RAMNIWAS; GUGULOTH, RAMBABU; SHARMA, VIJAY KUMAR
To: MEDIVATION TECHNOLOGIES, INC.
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CONFIRMATORY GRANT OF SECURITY INTEREST IN UNITED STATES PATENTS Recorded Sep 4, 2015
From: MEDIVATION TECHNOLOGIES, INC.
To: JPMORGAN CHASE BANK, N.A., AS ADMINISTRATIVE AGENT
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