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
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
Publication number: 20060009434
Abstract: The invention relates to new 2-substituted estra-1,3,5(10)-trien-17-ones of general formula I in which R2 means a saturated or unsaturated C1-C8-alkyl group, a C1-C5-alkyloxy group, an aralkyl radical or alkylaryl radical, a radical —O—CnFmHo, whereby n=1, 2, 3, 4, 5 or 6, m?1 and m+o=2n+1, or a group CH2XY, in which X stands for an oxygen atom and Y stands for an alkyl radical with 1 to 4 carbon atoms, as well as a halogen atom or a nitrile group, R13 means a hydrogen atom or a methyl group, R16 means a hydrogen atom or a fluorine atom, Z means an oxygen atom or a sulfur atom, R3 and R5, in each case independently of one another, mean an ?- or ?-position hydrogen atom, R4 and R6, in each case independently of one another, mean an ?- or ?-position hydrogen atom, a C1-C5-alkyl group, a C1-C5-alkyloxy group, a C1-C5-acyl group or a hydroxy group or an aralkyl radical or alkylaryl radical, R3 and R4 together mean an oxygen atom, R5 and R6 together mean an oxygen atom, R7 and R8 in each case mean a
Type:
Application
Filed:
June 17, 2005
Publication date:
January 12, 2006
Inventors:
Alexander Hillisch, Olaf Peters, Christian Gege, Wilko Regenhardt, Andrea Rosinus, Jerzy Adamski, Gabriele Moeller