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

0539089 - ÚOCHB 2021 RIV eng P - Patent Document
Kotora, Martin - Prchalová, Eva - Adamski, J. - Möller, G. - Štěpánek, Ondřej - Bartůněk, Petr - Sedlák, David - Hajdúch, M. - Džubák, P.
15β-substituted estrone derivatives as selective inhibitors of 17β-hydroxysteroid-dehydrogenases, method of preparation and use thereof.
2020. Owner: Ústav organické chemie a biochemie AV ČR, v. v. i. - Ústav molekulární genetiky AV ČR, v. v. i. - Univerzita Palackého v Olomouci - Helmholtz Zentrum München GmbH. Date of the patent acceptance: 01.09.2020. Patent Number: US10579826
R&D Projects: GA MŠMT LO1220
Institutional support: RVO:61388963 ; RVO:68378050
Keywords : 17β-hydroxysteroid dehydrogenase type 1 * 17βHSD1 * inhibitor
OECD category: Organic chemistry
https://worldwide.espacenet.com/publicationDetails/originalDocument?CC=US&NR=10759826B2&KC=B2&FT=D&ND=4&date=20200901&DB=&locale=en_EP

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.
Permanent Link: http://hdl.handle.net/11104/0317085