IP Library Granted Patent US 10,851,083
Granted Patent B2
US 10,851,083 · App. 16/295,476 · Granted Dec 1, 2020

Benzoimidazoles as prolyl hydroxylase inhibitors

Inventors: Frances Meredith Hocutt (Seattle, WA); Barry Eastman Leonard, Jr. (La Jolla, CA); Hillary M. Peltier (Evanston, CA); Victor K. Phuong (Los Angeles, CA); Michael H. Rabinowitz (San Diego, CA); Mark D. Rosen (San Diego, CA); Kyle T. Tarantino (Princeton, NJ); Hariharan Venkatesan (San Diego, CA); Lucy Xiumin Zhao (San Diego, CA)
Assignee: Janssen Pharmaceutica NV
C07D403/04C07D235/24C07D403/14C07D471/04C07D473/40C07D487/04C07D513/04
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Quick Facts
Patent No.
US 10,851,083
App. No.
16/295,476
Granted
Dec 1, 2020
Kind
B2
Abstract

The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.

Claims (9)

1. A compound having PHD inhibitor activity of the formula (I):

wherein:

n is 2-4;

each R 1 is independently selected from H, halo, —C 1-4 perhaloalkyl, trifluoroC 1-4 -alkoxy, and —SC 1-4 alkyl;

R 2 and R 3 are both H, —CF 3 , or C 1-3 alkyl;

each Z is C; or an enantiomer, a diastereomer, a racemate, or a pharmaceutically acceptable salt thereof.

2. The compound according to claim 1 , wherein R 2 and R 3 are both H.

3. The compound according to claim 1 , wherein R 2 and R 3 are both —CF 3 .

4. The compound according to claim 1 , wherein R 2 and R 3 are both C 1-3 alkyl.

Continuity (8)
Continuation 16135975 · Sep 19, 2018
Continuation 15695958 · Sep 5, 2017
Continuation 14968763 · Dec 14, 2015
Continuation 14732332 · Jun 5, 2015
Continuation 14282901 · May 20, 2014
Continuation 12990104
Provisional Application 61048531 · Apr 28, 2008
Related Publication 20190367486A1 · Dec 5, 2019
Cited By (1)
US 12,389,911