Ohio State Innovation Foundation

Ustav Organicke Chemie a Biochemie Av Cr, V.v.i.

Institute of Molecular Genetics As Cr, V.v.i.

Univerzita Palackeho V Olomouci

Helmholtz Zentrum Munchen

Ustav Molekularni Genetiky Akademie Ved Cr, V.v.i.

Ustav Molekularni Genetikv Av Cr, V.v.i.

Univerzita Karlova V Praze, Prirodovedecka Fukulta UK

David Sedlak

Petr Bartunek

Werner Tjarks

Martin Kotora

Marian Hajduch

Petr Dzubak

Jerzy Adamski

Gabriele Moeller

Ondrej Stepanek

Petr Novak

Eva Prchalova

Disclosed herein are compounds comprising dicarba-closo-dodecaborane. The compounds can be, for example, estrogen receptor beta (ER&#x3b2;) agonists. In some examples, the compounds can be selective ER&#x3b2; agonists. Also provided herein are methods of treating, preventing, or ameliorating cancer in a subject, suppressing tumor growth in a subject, treating an inflammatory disease in a subject, treating a neurodegenerative disease in a subject, treating a psychotropic disorder in a subject, or a combination thereof, by administering to a subject a therapeutically effective amount of one or more of the compounds or compositions described herein, or a pharmaceutically acceptable salt thereof.

Carborane compounds and methods of use thereof

Disclosed herein are compounds comprising dicarba-closo-dodecaborane. The compounds can be, for example, estrogen receptor beta (ER&#x3b2;) agonists. In some examples, the compounds can be selective ER&#x3b2; agonists. Also provided herein are methods of treating, preventing, or ameliorating cancer in a subject, suppressing tumor growth in a subject, treating an inflammatory disease in a subject, treating a neurodegenerative disease in a subject, treating a psychotropic disorder in a subject, or a combination thereof by administering to a subject a therapeutically effective amount of one or more of the compounds or compositions described herein, or a pharmaceutically acceptable salt thereof.

15&#x3b2;-substituted derivatives of estrone of general formula I wherein R, R, R, R, Rare independently selected from the group consisting of: C-Calkyl, C-Calkoxy, C-Chalogenalkyl, halogen, COORwherein Ris C-Calkyl; H, OH; optionally, R, Rand Rare each formed by a hydrogen atom, while Rand Rtogether 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 R-R. Compounds of the invention may be used for diagnosis and possibly also for the treatment of estrogen-dependent diseases.

15&#x3b2;-substituted estrone derivatives as selective inhibitors of 17&#x3b2;-hydroxysteroid-dehydrogenases, method of preparation and use thereof

The invention relates to novel ligands of the estrogen receptors &#x3b1; and &#x3b2; 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. 

Ligands of estrogen receptors &#x3b1; and &#x3b2;, method of their preparation, and pharmaceuticals comprising them

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Prague, Czechia

David Sedlak