Imidazole derivatives and methods of use thereof for improving the pharmacokinetics of a drug

Patent metadata

Field	Value
Publication number	US-9981969-B2
Application number	US-201414895406-A
Country	US
Kind code	B2
Filing date	Jun 2, 2014
Priority date	Jun 7, 2013
Publication date	May 29, 2018
Grant date	May 29, 2018

Abstract

The present invention relates to Imidazole Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, B, Y, R 1 and R 2 are as defined herein. The present invention also relates to compositions comprising at least one Imidazole Derivative, and methods of using the Imidazole Derivatives for inhibiting CYP450 3A. Inhibition of CYP450 3A can be used to improve the pharmacokinetics of a drug that is metabolized by CYP450 3A4.

First claim

What is claimed is:

1. The compound, having the formula (Ic);

or a pharmaceutically acceptable salt thereof,
wherein:
n is 1 or 2;
R 3 is selected from H, halo and C 1 -C 6 alkyl;
R 4 is selected from H, halo and C 1 -C 6 alkyl;
each occurrence of R a is independently H, methoxy, halo or methyl; and
each occurrence of R b is independently H, methoxy, halo or methyl.

2. The compound of claim 1 , wherein n is 1.

3. The compound of claim 1 , wherein n is 2.

4. A compound having the structure:

or a pharmaceutically acceptable salt thereof.

5. A pharmaceutical composition comprising an effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.

Assignees

• Merck Sharp & Dohme

Inventors

• Coburn Craig A
• Maletic Milana
• Luo Yunfu
• Qi Zhiqi
• Li Chunsing
• Yu Tingting
• Soll Richard

Classifications

• A61P31/18

  for HIV · CPC title

• A61P31/12

  Antivirals · CPC title

• C07D401/14

  containing three or more hetero rings · CPC title

• C07D471/04

  Ortho-condensed systems · CPC title

• C07D413/14

  containing three or more hetero rings · CPC title