Patents Assigned to USTAV MOLEKULARNI GENETIKY AKADEMIE VED CR, V.V.I.
  • 15?-substituted estrone derivatives as selective inhibitors of 17?-hydroxysteroid-dehydrogenases, method of preparation and use thereof
    Patent number: 10759826
    Abstract: 15?-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.
    Type: Grant
    Filed: June 7, 2017
    Date of Patent: September 1, 2020
    Assignees: 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
    Inventors: Martin Kotora, Eva Prchalova, Jerzy Adamski, Gabriele Moeller, Ondrej Stepanek, Petr Bartunek, David Sedlak, Marian Hajduch, Petr Dzubak
  • 15beta-substituted estrone derivatives as selective inhibitors of 17beta-hydroxysteoid-dehydrogenases, method of preparation and use thereof
    Publication number: 20190330258
    Abstract: 15?-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.
    Type: Application
    Filed: June 7, 2017
    Publication date: October 31, 2019
    Applicants: 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
    Inventors: Martin KOTORA, Eva PRCHALOVA, Jerzy ADAMSKI, Gabriele MOELLER, Ondrej STEPANEK, Petr BARTUNEK, David SEDLAK, Marian HAJDUCH, Petr DZUBAK