专利检索 ap:("USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I." OR "USTAV MOLEKULARNI GENETIKY AKADEMIE VED CR, V.V.I." OR "UNIVERZITA PALACKEHO V OLOMOUCI" OR "HELMHOLTZ ZENTRUM MUNCHEN") AND inv:"Ondrej Stepanek" 第 1 页

1.

发明授权
15β-substituted estrone derivatives as selective inhibitors of 17β-hydroxysteroid-dehydrogenases, method of preparation and use thereof 有权

公开(公告)号：US10759826B2

公开(公告)日：2020-09-01

申请号：US16305829

申请日：2017-06-07

申请人： 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

IPC分类号： A61K31/566 , C07J1/00

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.