Title:
ヒドロキサメートトリテルペノイド誘導体
Document Type and Number:
Japanese Patent JP6598224
Kind Code:
B2
Abstract:
Triterpenoid derivatives and compositions comprising said triterpenoids derivatives of Formula (I) are described, wherein R=-C(O)NHOH. Said triterpenoids and compositions show capacity to bind PHD2, stabilize HIF-1α and HIF-2α proteins, activate the HIF pathway in different cell types, induce angiogenesis in human endothelial vascular cell, show neuroprotective activity in vitro and in vivo, antidiabetic activity and reduce the levels of lipids in vivo, and increase the plasma levels of Erythropoietin in vivo. The triterpenoid derivatives described act also in a selective manner and do not induce Nrf2 activation, NF-κB inhibition, STAT3 inhibition, and TGR5 activation, which are known activities of the natural triterpenoid precursors. Said triterpenoid derivatives are useful in the treatment of conditions and diseases which are responsive to HIF activation such as stroke, cerebral palsy, traumatic injuries and neurodegenerative diseases; and also IBD, myocardial ischaemia–reperfusion injury, acute lung injury, diabetic and chronic wounds, organ transplantation, acute kidney injury or arterial diseases.
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Inventors:
Muñoz Blanco, Eduardo
Minassi, Alberto
Belido Caveyo de Alba, Maria Luz
Appendino, Giovanni
Minassi, Alberto
Belido Caveyo de Alba, Maria Luz
Appendino, Giovanni
Application Number:
JP2018524188A
Publication Date:
October 30, 2019
Filing Date:
October 03, 2017
Export Citation:
Assignee:
Vivacell Biotechnology Espana, S. El.
International Classes:
C07J63/00; A61K31/16; A61K31/22; A61K31/423; A61K45/00; A61P1/04; A61P3/06; A61P3/10; A61P9/00; A61P9/10; A61P11/00; A61P13/12; A61P17/02; A61P25/28; A61P37/06; C07J71/00
Domestic Patent References:
| JP2002322068A | ||||
| JP2009522353A |
Foreign References:
| WO2011085307A1 | ||||
| US20100144688 |
Other References:
WIEMANN, J. et al.,Bioorganic & Medicinal Chemistry Letters,2015年12月19日,Vol. 26,pp. 907-909
WIEMANN, J. et al.,European Journal of Medicinal Chemistry,2015年,Vol. 106,pp. 194-210
SHAN, J.-Z. et al.,Journal of Zhejiang University-Science B,2016年 9月 9日,Vol. 17, No. 9,pp. 672-682
WIEMANN, J. et al.,European Journal of Medicinal Chemistry,2015年,Vol. 106,pp. 194-210
SHAN, J.-Z. et al.,Journal of Zhejiang University-Science B,2016年 9月 9日,Vol. 17, No. 9,pp. 672-682
Attorney, Agent or Firm:
Kazuhiro Kiyohara