公开(公告)号：EP3243829A1

公开(公告)日：2017-11-15

申请号：EP16001932.9

申请日：2010-05-28

申请人： Ústav Organické Chemie A Biochemie Akademie Ved Ceské Republiky, v.v.i. ,  Fyziologický Ústav Akademie VÊD Ceské Republiky V.V.I. ,  Národní ústav dusevního zdraví

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.

摘要翻译： 本发明适用于具有通式I的化合物，其中R 1代表通式R 3 OOC-R 2 -C（R 4）-R 5 - 的基团，其中R 2代表烷基或烯基，其中1-18碳 直链或支链碳链，其可以被一个或多个卤素原子取代; R 3表示氢原子或羧基的保护基，优选苄基; R4表示氧原子，氮原子或通过双键结合的硫原子或R4表示两个氢原子; 除了当R 2代表基团 - （CH 2）n - 时，其中n = 0〜3，同时R 3代表氢原子，R 4和R 5代表一个至少是二价原子，优选氧原子，氮或碳原子 氧原子。 本发明还涉及具有通式I的化合物的制备方法，其中R1如前所述，具有通式I的化合物用于治疗各种中枢神经系统疾病，用于治疗与神经精神病相关的神经精神障碍 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障碍，情感障碍，抑郁症，创伤后应激障碍和其他与压力，焦虑，精神分裂症和精神病性障碍，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，用于生产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的物质的生产的兽药和人药物制剂 。

公开(公告)号：EP2435463B1

公开(公告)日：2016-10-12

申请号：EP10744655.1

申请日：2010-05-28

申请人： Ústav Organické Chemie Biochemie Akademie Ved Ceské Republiky, V.V.I. ,  Fyziologický Ústav Akademie VÊD Ceské Republiky V.V.I. ,  Národní ústav dusevního zdraví

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.