Ligands of estrogen receptors α and β, method of their preparation, and pharmaceuticals comprising them

0388664 - ÚMG 2013 RIV eng P - Patentový dokument
Novák, P. - Sedlák, David - Bartůněk, Petr - Kotora, Martin
Ligands of estrogen receptors α and β, method of their preparation, and pharmaceuticals comprising them.
2012. Vlastník: Ústav molekulární genetiky AV ČR, v. v. i. - Ústav organické chemie a biochemie AV ČR, v. v. i. - Přírodovědecká fakulta UK v Praze. Datum udělení patentu: 18.12.2012. Číslo patentu: US8334280
Výzkumný záměr: CEZ:AV0Z50520514; CEZ:AV0Z40550506
Klíčová slova: estrogen receptor ligand * hormone therapy * cancer therapy
Kód oboru RIV: EB - Genetika a molekulární biologie; CE - Biochemie (UOCHB-X)
http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&r=1&f=G&l=50&s1=8334280.PN.&OS=PN/8334280&RS=PN/8334280

The invention relates to novel ligands of the estrogen receptors α and β of general formula II, which are useful as an active substance of pharmaceuticals, for example pharmaceutical compositions useful for hormone replacement therapy, as well as for the treatment of tumors and inflammatory diseases. The invention also relates to a novel preparation method of these ligands comprising cyclotrimerization of ethynylestradiol with the appropriate diyne in an organic solvent. Further, the invention relates to pharmaceuticals comprising the novel compounds according to the invention.
Trvalý link: http://hdl.handle.net/11104/0217584