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1.发明授权Derivatives of acyl-piperazinyl-pyrimidines, preparation thereof and application as medicaments 失效酰基 - 哌嗪基 - 嘧啶的衍生物，其制备和作为药物的应用公开(公告)号：US06372746B1
公开(公告)日：2002-04-16
申请号：US09462880
申请日：2000-02-24
IPC分类号： C07D40304
CPC分类号： C07D405/12 , C07D239/42 , C07D401/12 , C07D403/12 , C07D409/12 , C07D417/12
摘要： The derivatives of acyl-piperazinyl-pyrimidines of general formula (I), where X is O or S; R1 is alkoxy or trifluoromethyl; R2 is alkyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl, show activity in the central nervous system. Compounds of general formula (I) in which X is O can be obtained by reacting a derivative of pyrimidine with a derivative of piperazine or by reacting a derivative of piperazinyl-pyrimidine with a carboxylic acid or a salt or derivative thereof. Compounds of general formula (I) in which X is S can be obtained by reacting (I) in which X is O with Lawesson's reagent or with phosphorous pentasulphide. The compounds (I) show sedative activity, anticonvulsant, sleep-inducing or general anaesthetic activity and can be applied in human or veterinary medicine
摘要翻译： 通式（I）的酰基哌嗪基 - 嘧啶衍生物，其中X为O或S; R1是烷氧基或三氟甲基; R2是烷基，环烷基，杂环烷基，芳基，芳基烷基，杂芳基或杂芳基烷基，在中枢神经系统中显示活性。 其中X为O的通式（I）化合物可以通过使嘧啶衍生物与哌嗪的衍生物反应或通过使哌嗪基 - 嘧啶的衍生物与羧酸或其盐或衍生物反应来获得。 其中X为S的通式（I）的化合物可以通过（I）其中X为O与Lawesson's试剂或五硫化磷反应而获得。 化合物（I）显示镇静活性，抗惊厥，睡眠诱导或全身麻醉活性，可应用于人或兽药
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公开(公告)号：US07829559B2
公开(公告)日：2010-11-09
申请号：US11574364
申请日：2005-08-29
申请人： Jordi Corbera Arjona , Maria Rosa Cuberes-Altisent , Joerg Holenz , Daniel Martínez-Olmo , David Vaño-Domenech
发明人： Jordi Corbera Arjona , Maria Rosa Cuberes-Altisent , Joerg Holenz , Daniel Martínez-Olmo , David Vaño-Domenech
IPC分类号： A61K31/535
CPC分类号： C07D491/10 , C07D231/56 , C07D401/06 , C07D403/06
摘要： The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to pyrazole derivatives of formula (I) and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use therapy and prophylaxis, in particular for the treatment of psychosis or pain.
摘要翻译： 本发明涉及具有对σ受体的药理学活性的化合物，更具体地说，涉及式（I）的吡唑衍生物及其制备方法，包括它们的药物组合物，以及它们的用途治疗和预防，特别是 治疗精神病或疼痛。
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公开(公告)号：US08394797B2
公开(公告)日：2013-03-12
申请号：US12893256
申请日：2010-09-29
申请人： Jordi Corbera Arjona , Maria Rosa Cuberes-Altisent , Joerg Holenz , Daniel Martínez-Olmo , David Vaño-Domenech
发明人： Jordi Corbera Arjona , Maria Rosa Cuberes-Altisent , Joerg Holenz , Daniel Martínez-Olmo , David Vaño-Domenech
IPC分类号： A61K31/535
CPC分类号： A61K31/55 , A61K31/416 , A61K31/4178 , A61K31/438 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D231/56 , C07D401/06 , C07D403/06 , C07D491/10
摘要： The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to pyrazole derivatives of formula I and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use therapy and prophylaxis, in particular for the treatment of psychosis or pain.
摘要翻译： 本发明涉及对σ受体具有药理活性的化合物，更具体地说，涉及式I的吡唑衍生物，以及这些化合物的制备方法，包含它们的药物组合物，以及它们的用途治疗和预防，特别是用于治疗 的精神病或疼痛。
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公开(公告)号：US07282499B2
公开(公告)日：2007-10-16
申请号：US10977738
申请日：2004-10-29
IPC分类号： A61K31/5375 , A61K31/5377 , C07D413/02
CPC分类号： C07D491/10 , C07D231/56 , C07D401/06 , C07D403/06
摘要： The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to some pyrazole derivatives, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use therapy and prophylaxis, in particular for the treatment of psychosis or pain.
摘要翻译： 本发明涉及对σ受体具有药理活性的化合物，更具体地说，涉及一些吡唑衍生物，制备这些化合物的方法，包含它们的药物组合物，以及它们的用途治疗和预防，特别是用于治疗精神病 或疼痛。
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