Bromodomain inhibitors

1. A compound of Formula IV, or a pharmaceutically acceptable salt thereof,

wherein,

each R 12 is independently hydrogen, halogen, alkyl, or alkoxy;

R 13 is —Y—Z, wherein

Y is selected from a bond, —CH 2 —, or —CH(C 1 -C 4 alkyl)-;

Z is selected from —SO 2 R b , —N(R a )SO 2 R b , —SO 2 N(R a ) 2 , —N(R a )SO 2 N(R a ) 2 , —CON(R a ) 2 , —N(R a )CO 2 R a , —N(R a )CON(R a ) 2 , —N(R a )COR a , —OC(O)N(R a ) 2 , —OSO 2 N(R a ) 2 , or —N(R a )SO 3 R b ;

each R a is independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, or heteroarylalkyl;

R b is alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, or heteroarylalkyl;

R 16 is alkyl, alkynyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkynyl, heterocyclyl, heterocyclylalkyl, heteroaryl, or heteroarylalkyl; and

G is:

wherein,

R 22 is alkyl;

R 23 is hydrogen, halogen, or alkyl; or optionally, when R 23 is alkyl, then R 22 and R 23 join to form an optionally substituted ring;

R 25 is hydrogen, halogen, alkyl, alkoxy, or alkenyl;

R 26 is hydrogen, halogen, alkyl, alkoxy, aminoalkyl, or alkenyl; or, optionally, when R 23 is hydrogen, R 25 is not hydrogen, and R 26 is not hydrogen or halogen, then R 25 and R 26 join to form an optionally substituted ring.

2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein G is:

3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein G is:

4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein G is:

5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein G is:

6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound of Formula IV is of Formula IVa:

7. The compound of claim 6 , or a pharmaceutically acceptable salt thereof, wherein

R 13 is —Y—Z, in which Y is s a bond or —CH 2 —, Z is —SO 2 R b , —N(R a )SO 2 R b , or —SO 2 N(R a ) 2 , each R a is independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, or heteroarylalkyl, and R b is alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, or heteroarylalkyl; and

R 16 is alkyl, alkynyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkynyl, heterocyclyl, heterocyclylalkyl, heteroaryl, or heteroarylalkyl.

8. The compound of claim 6 , or a pharmaceutically acceptable salt thereof, wherein

R 13 is —Y—Z, in which Y is a bond or —CH 2 —, Z is —SO 2 R b or —N(R a )SO 2 R b , each R a is independently hydrogen or alkyl, and R b is alkyl; and

R 16 is alkyl or cycloalkylalkyl.

9. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

10. An oral dosage form comprising the pharmaceutical composition of claim 9 .

11. A method of modulating the epigenetic status of a cell comprising contacting the cell with the compound of claim 1 , or a pharmaceutically acceptable salt thereof.

12. A method for inhibiting a histone demethylase enzyme comprising contacting a histone demethylase enzyme with the compound of claim 1 , or a pharmaceutically acceptable salt thereof.

13. A method for treating cancer or neoplastic disease in a subject in need comprising administering to the subject the pharmaceutical composition of claim 9 .

14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is:

5-(1-ethyl-4-methylsulfonylindol-2-yl)-1,3-dimethylpyridin-2-one;

5-[1-(cyclopropylmethyl)-4-methylsulfonylindol-2-yl]-1,3-dimethylpyridin-2-one;

5-[1-(2-cyclopropylethyl)-4-methylsulfonylindol-2-yl]-1,3-dimethylpyridin-2-one;

4-[1-(cyclopropylmethyl)-4-methylsulfonylindol-2-yl]-2-methylisoquinolin-1-one; or

5-[1-(2-cyclopropylethyl)-4-methylsulfonylindol-2-yl]-3-methoxy-1-methylpyridin-2-one.