DISCLOSED HEREIN ARE METHODS FOR CONTROLLING THE ACTIVITY OF HYPOXIA-INDUCIBLE TRANSCRIPTION FACTOR 1-ALPHA (HIF-1α) 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 PHARMACEUTICAL COMPOSITIONS COMPRISING HIF-1α PROLYL HYDROXYLASE INHIBITORS USEFUL IN TREATING DISEASES, CONDITIONS, AND/OR SYNDROMES RELATED THERETO THE ACTIVITY OF HIF-1α.