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ANIONIC PREGNANE COMPOUNDS, METHOD FOR THEIR PRODUCING AND USE OF THEM
专利权人:
发明人:
申请号:
EP09775815.5
公开号:
EP2313424B1
申请日:
2009.07.09
申请国别(地区):
EP
年份:
2014
代理人:
摘要:
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 Alzheimers, Huntingtons and Parkinsons 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.La présente invention concerne des composés anioniques de prégnane de formule générale I où R1 représente un groupe ester capable de former un ion tel que le sulfate, le sulfate de pyridinium, lhémisuccinate, etc., R2
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