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

0388664 - ÚMG 2013 RIV eng P - Patent Document
Novák, P. - Sedlák, David - Bartůněk, Petr - Kotora, Martin
Ligands of estrogen receptors α and β, method of their preparation, and pharmaceuticals comprising them.
2012. Owner: Ústav molekulární genetiky AV ČR, v. v. i. - Ústav organické chemie a biochemie AV ČR, v. v. i. - Přírodovědecká fakulta UK v Praze. Date of the patent acceptance: 18.12.2012. Patent Number: US8334280
Institutional research plan: CEZ:AV0Z50520514; CEZ:AV0Z40550506
Keywords : estrogen receptor ligand * hormone therapy * cancer therapy
Subject RIV: EB - Genetics ; Molecular Biology; CE - Biochemistry (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.
Permanent Link: http://hdl.handle.net/11104/0217584