IP Library Granted Patent US 7,897,612
Granted Patent B2
US 7,897,612 · App. 12/281,677 · Granted Mar 1, 2011

Substituted 1,8-naphthyridinecarboxamides for use as prolyl hydroxylase inhibitors

Assignee: Glaxosmithkline, LLC
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Quick Facts
Patent No.
US 7,897,612
App. No.
12/281,677
Granted
Mar 1, 2011
Kind
B2
Abstract

The invention described herein relates to certain bicyclic heteroaromatic N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Claims (18)

1. A compound which is:

N-{[1-(2-cyclopropylethyl)-4-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridin-3-yl]carbonyl}glycine;

N-{[4-hydroxy-1-(3-methylbutyl)-2-oxo-1,2-dihydro-1,8-naphthyridin-3-yl]carbonyl}glycine;

N-{[1-(3,3-dimethylbutyl)-4-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridin-3-yl]carbonyl}glycine;

N-{[4-hydroxy-2-oxo-1-(phenylmethyl)-1,2-dihydro-1,8-naphthyridin-3-yl]carbonyl}glycine;

N-({1-[2-(dimethylamino)ethyl]-4-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridin-3-yl]carbonyl}glycine;

N-{[1-(3,3-dimethylbutyl)-4-hydroxy-7-methyl-2-oxo-1,2-dihydro-1,8-naphthyridin-3-yl]carbonyl}glycine;

N-{[6-chloro-1-(3,3-dimethylbutyl)-4-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridin-3-yl]carbonyl}glycine;

N-{[1-(3,3-dimethylbutyl)-4-hydroxy-2-oxo-7-(trifluoromethyl)-1,2-dihydro-1,8-naphthyridin-3-yl]carbonyl}glycine;

N-{[1-(3,3-dimethylbutyl)-6-fluoro-4-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridin-3-yl]carbonyl}glycine;

N-{[6-bromo-1-(3,3-dimethylbutyl)-4-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridin-3-yl]carbonyl}glycine;

N-[(1-{[4-(1,1-dimethylethyl)phenyl]methyl}-6-fluoro-4-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridin-3-yl)carbonyl]glycine;

{[6-{[(carboxymethyl)amino]carbonyl}-8-(3,3-dimethylbutyl)-5-hydroxy-2-methyl-7-oxo-7,8-dihydro-1,8-naphthyridin-4-yl]amino}acetic acid;

N-[(1-{[4-(1,1-dimethylethyl)phenyl]methyl}-4-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridin-3-yl)carbonyl]glycine;

N-{[1-{[4-(1,1-dimethylethyl)phenyl]methyl}-4-hydroxy-2-oxo-7-(trifluoromethyl)-1,2-dihydro-1,8-naphthyridin-3-yl]carbonyl}glycine;

N-({1-[(2-chlorophenyl)methyl]-4-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridin-3-yl]carbonyl}glycine;

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt thereof and one or more of pharmaceutically acceptable carriers, diluents or excipients.

Assignments (1)
CHANGE OF NAME Recorded Nov 9, 2010
From: SMITHKLINE BEECHAM CORPORATION
To: GLAXOSMITHKLINE LLC
Reel/Frame 025337/0331 →
Continuity (2)
Provisional Application 60779737 · Mar 7, 2006
Related Publication 20090082357A1 · Mar 26, 2009