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1. 发明申请

WO2010136000A4 STEROIDE ANIONIC COMPOUNDS, METHOD OF THEIR PRODUCTION, USAGE AND PHARMACEUTICAL PREPARATION INVOLVING THEM 审中-公开
标题翻译： ST系阴离子化合物，其生产方法，使用方法和药物制备方法涉及它们
公开(公告)号：WO2010136000A4
公开(公告)日：2011-05-19
申请号：PCT/CZ2010000065
申请日：2010-05-28
申请人： USTAV ORGANICKE CHEMIE BIOCHEMIE AKADEMIE VED CESKE REPUBLIKY V V I , FYZIOLOGICKY USTAV AKADEMIE VED CESKE REPUBLIKY V V I , PSYCHIATRICKE CT PRAHA , CHODOUNSKA HANA , STASTNA EVA , KAPRAS VOJTECH , KOHOUT LADISLAV , BOROVSKA JIRNA , VYKLICKY LADISLAV , VALES KAREL , CAIS ONDREJ , RAMBOUSEK LUKAS , STUCHLIK ALES , VALESOVA VERA
发明人： CHODOUNSKA HANA , STASTNA EVA , KAPRAS VOJTECH , KOHOUT LADISLAV , BOROVSKA JIRNA , VYKLICKY LADISLAV , VALES KAREL , CAIS ONDREJ , RAMBOUSEK LUKAS , STUCHLIK ALES , VALESOVA VERA
IPC分类号： C07J7/00 , A61K31/57 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/24 , A61P25/28 , A61P25/30 , A61P35/00 , C07J41/00
CPC分类号： C07J41/005 , C07J7/002
摘要： The presented invention applies to the compounds with general formula (I), where R1 stands for as mentioned previously in the compound specifications, the production process of the compounds with general formula (I), where R1 stands for as mentioned previously in the compound specifications, application of the compounds with general formula (I) 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) used for production of veterinary and human pharmaceutical preparations used in treatment of above mentioned diseases as well as in production of substances used in experimental research, analytic chemistry, dietary supplements or cosmetic preparations.
摘要翻译：本发明适用于具有通式（I）的化合物，其中R 1代表如前述化合物说明书中所述，通式（I）化合物的制备方法，其中R 1代表如前所述的化合物规格，具有通式（I）的化合物在治疗中枢神经系统的各种疾病，治疗与谷氨酸能神经递质系统失衡，中枢神经系统缺血性损伤，中枢神经系统的神经退行性改变和病症，情感障碍，抑郁症有关的神经精神障碍，PTSD和其他与压力，焦虑，精神分裂症和精神障碍，疼痛，成瘾，多发性硬化症，癫痫和神经胶质瘤有关的疾病。本发明进一步适用于具有通式（I）的化合物，其用于制备用于治疗上述疾病以及用于实验研究，分析化学，膳食补充剂或化妆品制剂中的物质的生产的兽药和人药物制剂。

2. 发明申请

WO2010003391A3 ANIONIC PREGNANE COMPOUNDS, METHOD FOR THEIR PRODUCING AND USE OF THEM 审中-公开
公开(公告)号：WO2010003391A3
公开(公告)日：2010-01-14
申请号：PCT/CZ2009/000091
申请日：2009-07-09
申请人： USTAV ORSANICKE CHEMIE A BIOCHEMIE AKADEMIE VED CESKE REPUBLIKY, V.V.I. , FYZIOLQGICKY USTAV AKADEMIE VED CESKE REPUBLIKY V.V.I. , STASTNA, Eva , CHODOUNSKA, Hana , POUZAR, Vladimir , KAPRAS, Vojtech , CAIS, Ondrej , VYKLICKY, Ladislav , KOHOUT, Ladislav
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
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.

3. 发明申请

WO2010136000A3 STEROIDE ANIONIC COMPOUNDS, METHOD OF THEIR PRODUCTION, USAGE AND PHARMACEUTICAL PREPARATION INVOLVING THEM 审中-公开
标题翻译：甾族化合物，涉及其生产，使用和药物制备的方法
公开(公告)号：WO2010136000A3
公开(公告)日：2011-03-24
申请号：PCT/CZ2010000065
申请日：2010-05-28
申请人： USTAV ORGANICKE CHEMIE BIOCHEMIE AKADEMIE VED CESKE REPUBLIKY V V I , FYZIOLOGICKY USTAV AKADEMIE VED CESKE REPUBLIKY V V I , PSYCHIATRICKE CT PRAHA , CHODOUNSKA HANA , STASTNA EVA , KAPRAS VOJTECH , KOHOUT LADISLAV , BOROVSKA JIRNA , VYKLICKY LADISLAV , VALES KAREL , CAIS ONDREJ , RAMBOUSEK LUKAS , STUCHLIK ALES , VALESOVA VERA
发明人： CHODOUNSKA HANA , STASTNA EVA , KAPRAS VOJTECH , KOHOUT LADISLAV , BOROVSKA JIRNA , VYKLICKY LADISLAV , VALES KAREL , CAIS ONDREJ , RAMBOUSEK LUKAS , STUCHLIK ALES , VALESOVA VERA
IPC分类号： C07J7/00 , A61K31/57 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/24 , A61P25/28 , A61P25/30 , A61P35/00 , C07J41/00
CPC分类号： C07J41/005 , C07J7/002
摘要： The presented invention applies to the compounds with general formula (I), where R1 stands for as mentioned previously in the compound specifications, the production process of the compounds with general formula (I), where R1 stands for as mentioned previously in the compound specifications, application of the compounds with general formula (I) 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) used for production of veterinary and human pharmaceutical preparations used in treatment of above mentioned diseases as well as in production of substances used in experimental research, analytic chemistry, dietary supplements or cosmetic preparations.
摘要翻译：本发明适用于具有通式（I）的化合物，其中R1代表化合物说明书中先前提及的具有通式（I）的化合物的制备方法，其中R 1如前面在化合物规格中所述（I）化合物在治疗各种中枢神经系统疾病中的应用，用于治疗与谷氨酸能神经递质系统不平衡相关的神经精神障碍，CNS缺血性损伤，神经退行性变化和中枢神经系统疾病，情感障碍，抑郁症，PTSD等与压力，焦虑，精神分裂症和精神病，疼痛，成瘾，多发性硬化，癫痫和神经胶质瘤有关的疾病。本发明还适用于用于生产用于治疗上述疾病的兽医和人类药物制剂的通式（I）化合物，以及用于实验研究，分析化学，膳食补充剂或化妆品制剂中使用的物质的制备。

4. 发明申请

WO2010003391A2 ANIONIC PREGNANE COMPOUNDS, METHOD FOR THEIR PRODUCING AND USE OF THEM 审中-公开
标题翻译： ANIONIC PREGNANE化合物，其生产和使用方法
公开(公告)号：WO2010003391A2
公开(公告)日：2010-01-14
申请号：PCT/CZ2009000091
申请日：2009-07-09
申请人： USTAV ORSANICKE CHEMIE A BIOCH , FYZIOLQGICKY USTAV , STASTNA EVA , CHODOUNSKA HANA , POUZAR VLADIMIR , KAPRAS VOJTECH , CAIS ONDREJ , VYKLICKY LADISLAV , KOHOUT LADISLAV
发明人： STASTNA EVA , CHODOUNSKA HANA , POUZAR VLADIMIR , KAPRAS VOJTECH , CAIS ONDREJ , VYKLICKY LADISLAV , KOHOUT LADISLAV
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 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.
摘要翻译：本发明涉及通式Ⅰ的孕烷阴离子化合物，其中R1为酯基，能够形成硫酸根离子，硫酸吡啶硫酸盐，半琥珀酸盐等，R2为α或β构型的氢原子，R3为酯基，如乙酰氧基，烟酰氧基等，及其药学上可接受的盐。通式I的化合物优选由式II的二醇或根据所述反应顺序转化的式VIII的二醇制备成通式I的化合物，其中R1是酯基，其能够形成离子如硫酸盐，硫酸吡啶鎓，半琥珀酸盐等，R2是α或β构型的氢原子，R3是酯基。通式I的化合物可用作生产用于治疗神经和精神疾病的药物的活性成分，以及与NMDA受体过度激活相关的病症，例如针对中枢神经系统（CNS）的兴奋性毒性损伤的神经保护剂，与之相关的病症 NMDA亚型谷氨酸受体过度激活，或者这种类型的受体涉及创造或某些精神和神经疾病时，特别是关于中枢神经系统疾病中的神经组织的创伤性和缺氧性损伤，例如老年痴呆症，亨廷顿病和帕金森病，也在老龄化认知障碍中; 其他适应症可能是迟发性运动障碍，肌萎缩性侧索硬化，橄榄体小脑变性，与艾滋病感染相关的神经问题1，过敏性脑脊髓炎，以及用于癫痫，焦虑，抑郁，精神分裂症，慢性疼痛和药物成瘾的药物。

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