Disclosed herein are methods for controlling the activity of hypoxia- inducible transcription factor I -alpha (HIFla) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are phannaceutical compositions comprising HIF- la prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF -I a. Compounds used in the disclosed compositions and methods include: 1-Benzyl-3-hydroxy-4-[ 4-(2-methoxyphenyl)piperazin-1-ylmethyl]pyridin-2( 1H)-one； 1-Benzyl-3 -hydroxy-4-(thiazolidin-3-ylmethyl)pyridin-2( 1H)-one； 1-Benzyl-3-hydroxy-4-(piperidin-1-ylmethyl)pyridin-2(1H)-one and 1-(4&rsquo； -Methylbenzenesulfonyl)-3-hydroxy-4-[(2-methoxyethylamino)methyl]-pyridin-2(1H)-one.
