Anionic pregnane compounds, method for their producing and use of them

0435943 - ÚOCHB 2015 RIV eng P - Patent Document
Šťastná, Eva - Chodounská, Hana - Pouzar, Vladimír - Kapras, Vojtěch - Cais, Ondřej - Vyklický ml., Ladislav - Kohout, Ladislav
Anionic pregnane compounds, method for their producing and use of them.
2014. Owner: Ústav organické chemie a biochemie AV ČR, v. v. i. - Fyziologický ústav AV ČR, v. v. i. Date of the patent acceptance: 23.04.2014. Patent Number: EP2313424
R&D Projects: GA ČR(CZ) GAP303/12/1464
Institutional support: RVO:61388963 ; RVO:67985823
Keywords : NMDA * neurosteroid * neuroprotection
Subject RIV: CC - Organic Chemistry
http://worldwide.espacenet.com/publicationDetails/biblio?CC=EP&NR=2313424B1&KC=B1&FT=D&ND=5&date=20140423&DB=EPODOC&locale=en_EP

This invention relates to pregnane anionic compounds of general formula I in which R1 is ester group, which is able to form ion such as sulfate, pyridinium sulfate, hemisuccinate etc., R2 is hydrogen atom in alpha or beta configuration, and R3 is ester group, as is acetoxy group, nicotinoyloxy group etc., and their pharmaceutically acceptable salts. Compounds of general formula I are preferably produced from the diol of formula II or diol of formula VIII, which are converted according to described sequence of reactions, to compounds of general formula I, in which R1 is ester group, which is able to form ion such as sulfate, pyridinium sulfate, hemisuccinate etc., R2 is hydrogen atom in alpha or beta configuration, and R3 is ester group. The compounds of general formula I are useful as active ingredients for production of pharmaceuticals for the treatment of neurological and psychiatric diseases and conditions associated with excessive activation of NMDA receptors such as neuroprotective agents against excitotoxic damage of the central nervous system (CNS), conditions associated with excessive activation of NMDA-subtype glutamate receptors or, where this type of receptor is involved in the creation or during the certain mental and neurological diseases, in particular concerning the traumatic and hypoxic damage Io nervous tissue in the central nervous system diseases, such as Alzheimer's, Huntington's and Parkinson's disease, also in cognitive disorders in aging; the other indications could be tardive dyskinesia, amyotrophic lateral sclerosis, olivopontocerebellar degeneration, neurological problems1 associated with AIDS infection, allergic encephalomyelitis, and for medication of epilepsy, anxiety, depression, schizophrenia, chronic pain and drug addiction.
Permanent Link: http://hdl.handle.net/11104/0239749