Vitamin D receptor-coregulator inhibitors

Patent metadata

Field	Value
Publication number	US-10093653-B2
Application number	US-201615238305-A
Country	US
Kind code	B2
Filing date	Aug 16, 2016
Priority date	Aug 26, 2011
Publication date	Oct 9, 2018
Grant date	Oct 9, 2018

Abstract

Described herein are compounds, pharmaceutical compositions and methods for inhibiting the expression of a vitamin D receptor target gene, inhibiting interactions between the vitamin D receptor and at least one vitamin D receptor coactivator, for treating cancer in a subject, and for inhibiting angiogenesis in a subject.

First claim

The invention claimed is:

1. A compound of formula (I):

wherein:
m is 1;
p is 1;
each R 2 and R 3 is independently selected from the group consisting of alkoxy and haloalkyl.

2. The compound of claim 1 , wherein R 2 is haloalkyl.

3. The compound of claim 2 , wherein R 2 is CF 3 .

4. The compound of claim 1 , wherein R 3 is alkoxy.

5. The compound of claim 4 , wherein R 3 is methoxy.

6. A compound of formula (I):

wherein:
R 2 is CF 3 ; and
R 3 is methoxy.

7. A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier.

8. The pharmaceutical composition of claim 7 , wherein the compound is

wherein:
R 2 is CF 3 ; and
R 3 is methoxy.

9. A method of inhibiting the expression of a vitamin D receptor target gene in a sample, comprising contacting the sample with an effective amount of a compound according to claim 1 .

10. The method of claim 9 , wherein the compound is

wherein:
R 2 is CF 3 ; and
R 3 is methoxy.

11. A method of inhibiting an interaction between a vitamin D receptor and at least one vitamin D receptor coactivator in a sample, comprising contacting the sample with an effective amount of a compound according to claim 1 .

12. The method of claim 11 , wherein the compound is

wherein:
R 2 is CF 3 ; and
R 3 is methoxy.

13. A method of inhibiting angiogenesis in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound according to claim 1 .

14. The method of claim 13 , wherein the compound is

wherein:
R 2 is CF 3 ; and
R 3 is methoxy.

Assignees

• Uwm Res Foundation Inc
• Women And Infants Hospital Of Rhode Island

Inventors

• Arnold Alexander E
• Sidhu Preetpal Singh
• Nandhikonda Premchendar
• Singh Rakesh K

Classifications

• C07D209/14

  Radicals substituted by nitrogen atoms, not forming part of a nitro radical · CPC title

• A61K31/404

  Indoles, e.g. pindolol · CPC title

• C07D407/12

  linked by a chain containing hetero atoms as chain links · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• C07D209/16

  Tryptamines · CPC title