Binding Function 3 (BF3) site compounds as therapeutics and methods for their use

Patent metadata

Field	Value
Publication number	US-10633338-B2
Application number	US-201916426406-A
Country	US
Kind code	B2
Filing date	May 30, 2019
Priority date	Apr 9, 2014
Publication date	Apr 28, 2020
Grant date	Apr 28, 2020

Abstract

Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provide.

First claim

What is claimed is:

1. A compound having the structure of Formula II:

wherein,
L 1 is H;
L 2 is H, Cl, F or Br;
L 3 is H, Cl, F or Br;
L 4 is C(O)NHCH 3 , CF 3 ,

L 5 is H;
L 6 is H;
L 7 is H;
L 9 is Cl, F or Br;
L 9 is Cl, F or Br; and
L 10 is Cl, F or Br.

2. The compound of claim 1 , wherein
L 2 is H, Cl or F; and
L 3 is H, Cl or F.

3. The compound of claim 1 , wherein
L 2 is H, Cl or F;
L 3 is H, Cl or F;
L 8 is Cl or F;
L 9 is Cl or F; and
L 10 is Cl or F.

4. The compound of claim 1 , wherein
L 2 is H, Cl or F;
L 3 is H, Cl or F;
L 8 is F;
L 9 is F; and
L 10 is F.

5. The compound of claim 1 , wherein
L 4 is C(O)NHCH 3 .

6. The compound of claim 1 , wherein
L 4 is CF 3 ,

7. The compound of claim 1 , wherein
L 2 is H, Cl or F;
L 3 is H, Cl or F;
L 4 is C(O)NHCH 3 , CF 3 ,

L 8 is Cl or F;
L 9 is Cl or F; and
L 10 is Cl or F.

8. The compound of claim 1 , wherein
L 2 is H, Cl or F;
L 3 is H, Cl or F;
L 4 is C(O)NHCH 3 ;
L 8 is Cl or F;
L 9 is Cl or F, and
L 10 is Cl or F.

9. The compound of claim 1 , wherein
L 2 is H, Cl or F;
L 3 is H, Cl or F;
L 4 is C(O)NHCH 3 or CF 3 ;
L 8 is Cl or F;
L 9 is Cl or F; and
L 10 is Cl or F.

10. The compound of claim 1 , wherein
L 2 is H, Cl or F;
L 3 is H, Cl or F;
L 4 is C(O)NHCH 3 ,

L 8 is Cl or F;
L 9 is Cl or F, and
L 10 is Cl or F.

11. The compound of claim 1 , wherein
L 2 is H, Cl or F;
L 3 is H, Cl or F;
L 4 is C(O)NHCH 3 , CF 3 or

L 9 is Cl or F;
L 9 is Cl or F; and
L 10 is Cl or F.

12. The compound of claim 1 , wherein the compound is:

13. A pharmaceutical composition comprising a compound or pharmaceutically acceptable salt thereof according to claim 1 and a pharmaceutically acceptable excipient.

14. The pharmaceutical composition of claim 13 , wherein the compound is selected from:

15. A method of modulating AR activity, the method comprising (a) administering a compound of claim 1 to a subject in need thereof.

16. The method of claim 15 , wherein the modulating AR activity is for the treatment of prostate cancer.

Assignees

• Univ British Columbia
• Univ Fraser Simon

Inventors

• Rennie Paul
• Tcherkassov Artem
• Young Robert N
• Andre Christophe M

Classifications

• C07D413/04

  directly linked by a ring-member-to-ring-member bond · CPC title

• A61P5/28

  Antiandrogens · CPC title

• C07D405/14

  containing three or more hetero rings · CPC title

• C07D209/10

  with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring · CPC title

• C07D417/14

  containing three or more hetero rings · CPC title