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AssigneeVivacell Biotechnology Espana, S.L.
InventorsEduardo Munoz Blanco, Alberto Minassi, Maria Luz Bellido Cabello De Alba, Giovanni Appendino
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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.
A triterpene derivative of Formula (Ia) or stereoisomers, pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof,
A compound selected from the group consisting of XVIII and XIX:
A method of treating a condition or disease wherein the treatment of said condition or disease benefits from HIF-1α or HIF-2α activation, the method comprising administering to a subject in need thereof a triterpene derivative of Formula (I) or, stereoisomers, pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof,
Dependencies are inferred from the claim text.