IP Library Granted Patent US 10,208,060
Granted Patent B2
US 10,208,060 · App. 15/513,854 · Granted Feb 19, 2019

Inhibitors of HIF prolyl hydroxylase

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Quick Facts
Patent No.
US 10,208,060
App. No.
15/513,854
Granted
Feb 19, 2019
Kind
B2
Abstract

The present invention concerns compounds of formula I or a pharmaceutically acceptable salt thereof which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.

Claims (14)

1. A compound which is:

2-(4-Hydroxy-2-oxo-1-(4-(trifluoromethyl)phenyl)-1,2,5,7-tetrahydrofuro[3,4-b]pyridine-3-carboxamido)acetic acid;

2-(1-(4-chlorophenyl)-4-hydroxy-2-oxo-1,2,5,7-tetrahydrofuro[3,4-b]pyridine-3-carboxamido)acetic acid;

2-(1-(4-fluorophenyl)-4-hydroxy-2-oxo-1,2,5,7-tetrahydrofuro[3,4-b]pyridine-3-carboxamido)acetic acid;

2-(4-hydroxy-2-oxo-1-phenyl-1,2,5,7-tetrahydrofuro[3,4-b]pyridine-3-carboxamido)acetic acid;

2-(4-hydroxy-1-(4-methoxyphenyl)-2-oxo-1,2,5,7-tetrahydrofuro[3,4-b]pyridine-3-carboxamido)acetic acid;

2-(4-hydroxy-2-oxo-1-(4-(trifluoromethoxy)phenyl)-1,2,5,7-tetrahydrofuro[3,4-b]pyridine-3-carboxamido)acetic acid;

2-(4-hydroxy-2-oxo-1-(m-tolyl)-1,2,5,7-tetrahydrofuro[3,4-b]pyridine-3-carboxamido)acetic acid;

2-(4-hydroxy-2-oxo-1-(p-tolyl)-1,2,5,7-tetrahydrofuro[3,4-b]pyridine-3-carboxamido)acetic acid;

2-(1-(4-cyanophenyl)-4-hydroxy-2-oxo-1,2,5,7-tetrahydrofuro[3,4-b]pyridine-3-carboxamido)acetic acid; and

2-(4-hydroxy-1-(5-methoxypyridin-2-yl)-2-oxo-1,2,5,7-tetrahydrofuro[3,4-b]pyridine-3-carboxamido)acetic acid;

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising a compound of claim 1 and pharmaceutically acceptable carrier.

3. A method for the treatment of anemia in a mammal which comprises administering to the mammal an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

Assignments (5)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 26, 2017
From: LIU, RONGQIANG
To: MSD R&D (CHINA) CO., LTD.
Reel/Frame 041745/0215 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 26, 2017
From: CAI, JIAQIANG; DU, XIAOXING; QUAN, WEIGUO
To: WUXI APPTEC (SHANGHAI) CO., LTD
Reel/Frame 041745/0219 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 26, 2017
From: CRESPO, ALEJANDRO; DEBENHAM, JOHN; LIU, PING; MADSEN-DUGGAN, CHRISTINA B.; SINZ, CHRISTOPHER; WANG, LIPING
To: MERCK SHARP & DOHME CORP.
Reel/Frame 041745/0233 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 26, 2017
From: WUXI APPTEC (SHANGHAI) CO., LTD.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 041745/0253 →