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US 12,478,615 B2Granted
Prolyl hydroxylase inhibitors and methods of use
AssigneeAkebia Therapeutics, Inc.
InventorsRichard Masaru Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
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Abstract
The present disclosure relates to HIF-1α prolyl hydroxylase inhibitors, compositions which comprise the HIF-1α prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.
Claims8
A process for preparing a compound having the formula:
- comprising:
- (a) reacting a 4-iodo-picolinic acid:
- with a glycine methyl ester hydrochloride:
- in the presence of coupling agents to form [(4-iodo-pyridine-2-carbonyl)-amino]-acetic acid methyl ester:
- and
- (b) reacting the [(4-iodo-pyridine-2-carbonyl)-amino]-acetic acid methyl ester obtained from step (a) with a 4-methylphenyl boronic acid:
- in the presence of a catalyst to form [(4-(4-methylphenyl)pyridine-2-carbonyl)amino]-acetic acid methyl ester:
4 more elements
A compound having the formula:
- or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition comprising:
- (1) a pharmaceutically acceptable excipient, and
- (2) a compound having the formula:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.