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1. 发明申请

WO2011092226A8 SYNTHESIS OF SUBSTITUTED PYRAZOLINE CARBOXAMIDINE DERIVATIVES 审中-公开
标题翻译：取代的吡唑啉甲酰胺衍生物的合成
公开(公告)号：WO2011092226A8
公开(公告)日：2011-08-04
申请号：PCT/EP2011/051100
申请日：2011-01-27
申请人： ABBOTT HEALTHCARE PRODUCTS B.V. , VAN LOEVEZIJN, Arnold , LANGE, Josephus H.M. , BARF, Gerrit A. , DEN HARTOG, Arnold P.
发明人： VAN LOEVEZIJN, Arnold , LANGE, Josephus H.M. , BARF, Gerrit A. , DEN HARTOG, Arnold P.
IPC分类号： C07D231/06 , C07D231/54 , C07D409/04 , C07D409/12 , C07D513/10 , C07D491/107
摘要： This invention relates to organic chemistry, in particular to processes for the preparation of pyrazoline carboxamidine derivatives of formula (I), known as potent 5-HT6 antagonists. The invention also relates to novel intermediates of these compounds. wherein the symbols have the meanings given in the description.
摘要翻译：本发明涉及有机化学，具体涉及制备式（I）的吡唑啉甲脒衍生物的方法，称为有效的5-HT 6拮抗剂。本发明还涉及这些化合物的新中间体。其中符号具有说明书中给出的含义。

2. 发明申请

WO2009090177A1 BIFEPRUNOX DERIVATIVES 审中-公开
标题翻译： BIFEPRUNOX衍生物
公开(公告)号：WO2009090177A1
公开(公告)日：2009-07-23
申请号：PCT/EP2009/050336
申请日：2009-01-14
申请人： SOLVAY PHARMACEUTICALS B.V. , VAN STUIVENBERG, Herman H. , BARF, Gerrit A.
发明人： VAN STUIVENBERG, Herman H. , BARF, Gerrit A.
IPC分类号： C07D263/58 , A61K31/496 , A61P25/00 , A61P25/16
CPC分类号： C07D263/58
摘要： The present invention relates to bifeprunox derivatives of the formula (I) wherein R1 is one substituent selected from 3-OH, 4-OH, 3-OSO3H and 4-OSO3H; R2 is H; or an N-oxide or a pharmaceutically acceptable salt, a solvate or hydrate thereof, which are potent ligands for the dopamine D 2 receptor, exhibiting strong partial dopamine D 2 agonistic effects with a percentage agonism significantly higher than bifeprunox. The compounds of the invention may be used in the treatment, alleviation or prevention of dopamine D 2 receptor mediated diseases and conditions requiring dopamine D 2 agonistic effects.
摘要翻译：本发明涉及式（I）的二不饱和衍生物，其中R 1是选自3-OH，4-OH，3-OSO 3 H和4 -OSO 3 H的一个取代基; R2为H; 或作为多巴胺D2受体的有效配体的N-氧化物或其药学上可接受的盐，其溶剂合物或水合物，显示出比双歧杆菌明显高的百分比激动作用的强烈部分多巴胺D2激动作用。本发明的化合物可用于治疗，缓解或预防多巴胺D2受体介导的疾病和需要多巴胺D2激动作用的病症。

3. 发明申请

WO2007128694A1 N-OXIDES OF PYRIDYLMETHYLPIPERAZINE AND -PIPERIDINE DERIVATIVES 审中-公开
标题翻译：吡啶基甲基哌嗪和哌啶衍生物的N-氧化物
公开(公告)号：WO2007128694A1
公开(公告)日：2007-11-15
申请号：PCT/EP2007/054048
申请日：2007-04-25
申请人： SOLVAY PHARMACEUTICALS B.V. , VAN AAR, Marcel P.M. , VAN AMSTERDAM, Peter H. , BARF, Gerrit A. , BAKKER, Johan Antoine , DEN BESTEN, Cathaline , HERREMANS, Arnoldus H.J. , ZORGDRAGER, Jan
发明人： VAN AAR, Marcel P.M. , VAN AMSTERDAM, Peter H. , BARF, Gerrit A. , BAKKER, Johan Antoine , DEN BESTEN, Cathaline , HERREMANS, Arnoldus H.J. , ZORGDRAGER, Jan
IPC分类号： C07D405/12 , A61K31/444 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24
CPC分类号： C07D405/12
摘要： The invention concerns N-oxides of certain pyridylmethylpiperazine and -piperidine derivatives as alternatives or as `prodrugs' of their respective parent compounds, to pharmaceutical compositions containing these N-oxides, to methods for preparing them, and methods for preparing compositions. The invention relates to N-oxides of compounds having formula (a), wherein the symbols have the meanings given in the description, and wherein the oxidized nitrogen atom may be the nitrogen atom in the pyridyl ring of R 5 , or the nitrogen atom in the piperidine ring (when Z is carbon) or either one of the nitrogen atoms in the piperazine ring (when Z is nitrogen), or bóth the nitrogen atom connected to R 5 via a methylene group, ánd the nitrogen atom in the pyridyl ring of R 5 , and tautomers, stereoisomers, pharmacologically acceptable salts, hydrates and solvates thereof. The invention also relates to the uses of such N-oxides and compositions, particularly for the manufacture of a medicament useful in the treatment of affections or diseases of the central nervous system caused by disturbances in either the dopaminergic or serotinergic systems, for example Parkinson's disease, aggression, anxiety disorders, autism, vertigo, depression, disturbances of cognition or memory and in particular schizophrenia and other psychotic disorders.
摘要翻译：本发明涉及作为其各自母体化合物的替代物或“前药”的某些吡啶基甲基哌嗪和哌啶衍生物的N-氧化物，含有这些N-氧化物的药物组合物，其制备方法和制备组合物的方法。本发明涉及具有式（a）的化合物的N-氧化物，其中符号具有说明书中给出的含义，其中氧化的氮原子可以是R 5的吡啶环中的氮原子或哌啶环中的氮原子（当Z为碳时）或哌嗪环中的氮原子之一（当Z为氮时），或b连接至R 5的氮原子通过亚甲基和R 5的吡啶环中的氮原子，以及互变异构体，立体异构体，其药理学上可接受的盐，水合物和溶剂化物。本发明还涉及这种N-氧化物和组合物的用途，特别是用于制备用于治疗由多巴胺能或血清素能系统中的紊乱引起的中枢神经系统的感觉或疾病的药物，例如帕金森病，侵略，焦虑症，自闭症，眩晕，抑郁症，认知障碍或记忆障碍，特别是精神分裂症和其他精神障碍。

4. 发明公开

EP2234990A1 BIFEPRUNOX DERIVATIVES 审中-公开
标题翻译：联苯芦诺衍
公开(公告)号：EP2234990A1
公开(公告)日：2010-10-06
申请号：EP09702277.6
申请日：2009-01-14
申请人： Abbott Healthcare Products B.V.
发明人： VAN STUIVENBERG, Herman H. , BARF, Gerrit A.
IPC分类号： C07D263/58 , A61K31/496 , A61P25/00 , A61P25/16
CPC分类号： C07D263/58
摘要： The present invention relates to bifeprunox derivatives of the formula (I) wherein R1 is one substituent selected from 3-OH, 4-OH, 3-OSO3H and 4-OSO3H; R2 is H; or an N-oxide or a pharmaceutically acceptable salt, a solvate or hydrate thereof, which are potent ligands for the dopamine D2 receptor, exhibiting strong partial dopamine D2 agonistic effects with a percentage agonism significantly higher than bifeprunox. The compounds of the invention may be used in the treatment, alleviation or prevention of dopamine D2 receptor mediated diseases and conditions requiring dopamine D2 agonistic effects.

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