公开(公告)号：EP2313424A2

公开(公告)日：2011-04-27

申请号：EP09775815.5

申请日：2009-07-09

申请人： Ustav Organicke Chemie A Biochemie Akademie Ved Ceske Republiky ,  Fyziolqgicky Ustavakademie Ved Ceske Republiky V.v

发明人： STASTNA, Eva ,  CHODOUNSKA, Hana ,  POUZAR, Vladimir ,  KAPRAS, Vojtech ,  CAIS, Ondrej ,  VYKLICKY, Ladislav ,  KOHOUT, Ladislav

IPC分类号： C07J7/00 ,  C07J31/00 ,  A61K31/58 ,  A61K31/57

CPC分类号： C07J41/0077 ,  C07J7/002 ,  C07J31/006

摘要： This invention relates to pregnane anionic compounds of general formula I in which R
1 is ester group, which is able to form ion such as sulfate, pyridinium sulfate, hemisuccinate etc., R
2 is hydrogen atom in alpha or beta configuration, and R
3 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 R
1 is ester group, which is able to form ion such as sulfate, pyridinium sulfate, hemisuccinate etc., R
2 is hydrogen atom in alpha or beta configuration, and R
3 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.

公开(公告)号：EP2435463A2

公开(公告)日：2012-04-04

申请号：EP10744655.1

申请日：2010-05-28

申请人： Ustav Organicke Chemie A Biochemie Akademie Ved Ceske Republiky ,  Fyziologický Ústav Akademie VÊD Ceské Republiky V.V.I. ,  Psychiatrické Centrum Praha

发明人： CHODOUNSKÁ, Hana ,  STASTNÁ, Eva ,  KAPRAS, Vojtech ,  KOHOUT, Ladislav ,  BOROVSKÁ, Jirna ,  VYKLICKY, Ladislav ,  VALEs, Karel ,  CAIS, Ondrej ,  RAMBOUSEK, Lukás ,  STUCHLÍK, Ales ,  BUBENÍKOVÁ VALESOVÁ, Vera

IPC分类号： C07J7/00 ,  C07J41/00 ,  A61K31/57 ,  A61P25/02 ,  A61P25/08 ,  A61P25/24 ,  A61P25/18 ,  A61P25/04 ,  A61P25/30 ,  A61P25/28 ,  A61P35/00

CPC分类号： C07J41/005 ,  C07J7/002 ,  Y02P20/55

摘要： The presented invention applies to the compounds with general formula I, where R 1 stands for a group of the general formula R 3 OOC-R 2- C (R 4 )-R 5 -, where R 2 stands for alkyl or alkenyl group with 1 to 18 carbon in a straight or a branching carbon chain, which may be substituted by one or more halogen atoms; R 3 represents either a hydrogen atom or a protecting group of carboxyl groups, preferably benzyl group; R 4 represents oxygen atom, nitrogen atom or a sulfur atom bound by a double bond or R 4 represents two hydrogen atoms; R 5 represents any at least bivalent atom, preferably an oxygen atom, nitrogen, or carbon atom, except when R 2 represents the group -(CH 2 ) n - where n = 0-3 and simultaneously R 3 represents a hydrogen atom and R 4 and R 5 represent an oxygen atom. The present invention also relates to the production process of the compounds with general formula I, where R 1 stands for as mentioned previously, the compounds with general formula I for use in treatment of various diseases of central nervous system, in treatment of neuropsychiatric disorders related to imbalance of glutamatergic neurotransmitter system, ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, PTSD and other diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addictions, multiple sclerosis, epilepsy and gliomas. This invention further applies to the compounds with general formula I for use in the production of veterinary and human pharmaceutical preparations for use in treatment of above mentioned diseases as well as in production of substances used in experimental research, analytic chemistry, dietary supplements or cosmetic preparations.