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15β-substituted estrone derivatives as selective inhibitors of 17β-hydroxysteroid-dehydrogenases, method of preparation and use thereof
专利权人:
USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I.;USTAV MOLEKULARNI GENETIKY AKADEMIE VED CR, V.V.I.;UNIVERZITA PALACKEHO V OLOMOUCI;HELMHOLTZ ZENTRUM MUNCHEN
发明人:
Martin Kotora,Eva Prchalova,Jerzy Adamski,Gabriele Moeller,Ondrej Stepanek,Petr Bartunek,David Sedlak,Marian Hajduch,Petr Dzubak
申请号:
US16305829
公开号:
US10759826B2
申请日:
2017.06.07
申请国别(地区):
US
年份:
2020
代理人:
摘要:
15β-substituted derivatives of estrone of general formula I wherein R1, R2, R3, R4, R5 are independently selected from the group consisting of: C1-C4 alkyl, C1-C4 alkoxy, C1-C4 halogenalkyl, halogen, COOR6 wherein R6 is C1-C4 alkyl; H, OH; optionally, R3, R4 and R5 are each formed by a hydrogen atom, while R1 and R2 together form an aryl group, preferably naphthyl, in which the aromatic ring in position C-15 can be mono-, di-, tri-, tetra- and penta-substituted with substituents R1-R5. Compounds of the invention may be used for diagnosis and possibly also for the treatment of estrogen-dependent diseases.
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