[(4-Hydroxyl-benzo[4,5]thieno[3,2-c]pyridine-3-carbonyl)-amino]-acetic acid derivatives; HIF prolyl 4-hydroxylase inhibitors as oral erythropoietin secretagogues |
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| Authors: | Yong Rae Hong Hyun Tae Kim Seung-Chul Lee Seonggu Ro Joong Myung Cho In Su Kim Young Hoon Jung |
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| Institution: | 1. CrystalGenomics, Inc., 5F, Tower A, Korea Bio Park 694-1, Sampyeong-dong, Bundang-gu, Seongnam-si, Gyeonggi-do 463-400, Republic of Korea;2. School of Pharmacy, Sungkyunkwan University, Suwon 440-746, Republic of Korea |
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| Abstract: | A new series of PHD (HIF prolyl 4-hydroxylase) inhibitors was designed based on the X-ray co-crystal structure of FG-2216. Using a lead generation process, a series of (4-Hydroxyl-benzo4,5]thieno3,2-c]pyridine-3-carbonyl)-amino]-acetic acid derivatives was developed as potent PHD2 inhibitors. This class of compounds also showed the ability to stabilize HIF-α, to stimulate EPO secretion in in vitro studies, and to increase hematocrit, red blood cell count, and hemoglobin levels in an animal efficacy study. |
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| Keywords: | HIF-PH (PHD) Stabilizer Inhibitor Erythropoiesis |
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