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1. 发明授权

US6046201A Pyridinecarboxamide derivatives 失效
标题翻译：吡啶甲酰胺衍生物
公开(公告)号：US6046201A
公开(公告)日：2000-04-04
申请号：US101441
申请日：1998-07-15
申请人： Norio Oshida , Yoji Mimaki , Hiroaki Satoh , Shinji Yokoyama , Yukiko Muraki , Kazumi Nishimura , Tamiko Hamada , Einosuke Sakurai , Hiroshi Sakai , Toshiji Sugai , Tomomi Tonoike , Koichi Itoh
发明人： Norio Oshida , Yoji Mimaki , Hiroaki Satoh , Shinji Yokoyama , Yukiko Muraki , Kazumi Nishimura , Tamiko Hamada , Einosuke Sakurai , Hiroshi Sakai , Toshiji Sugai , Tomomi Tonoike , Koichi Itoh
IPC分类号： C07D213/80 , C07D213/82 , A61K31/495 , C07D401/04
CPC分类号： C07D213/80 , C07D213/82
摘要： N-(12-Nitroxydodecyl)-6-(4-ethyl or isopropyl-1-piperazinyl)pyridine-3-carboxamide or physiologically acceptable salts thereof. The said compounds have excellent inhibiting activity of cerebral edema, especially ischemic cerebral edema, and inhibiting activity of delayed neuronal death (an inhibiting activity of Ca-influx in neuronal cells). Cerebral edema is a pathologic condition accompanying cerebrovascular disorders, especially the acute stage cerebrovascular disorders and then the compounds are useful as an inhibiting agent for cerebral edema or a therapeutic agent for cerebrovascular disorders. Moreover, because the compounds do hardly show a behavior suppressing action, which is considered to be side effect in treating cerebrovascular disorders at the acute stage, they are an excellent therapeutic agent for, in particular, the acute stage cerebrovascular disorders. Moreover, the compounds show a cerebral protective activity (an anti-anoxic activity), an activity of increasing cerebral blood flow, and an activity of inhibiting lipid peroxidation, and these activities may lead to the increased utility as a therapeutic agent for cerebrovascular disorders.
摘要翻译： PCT No.PCT / JP97 / 04208 Sec。 371日期：1998年7月15日 102（e）日期1998年7月15日PCT 1997年11月19日PCT PCT。出版物WO98 / 22440 日期1998年5月28日N-（12-硝基十二烷基）-6-（4-乙基或异丙基-1-哌嗪基）吡啶-3-甲酰胺或其生理上可接受的盐。所述化合物具有优异的脑水肿抑制活性，特别是缺血性脑水肿，抑制延迟性神经元死亡的活性（神经细胞内Ca流入的抑制活性）。脑水肿是伴随脑血管障碍，特别是急性期脑血管障碍的病理状况，然后该化合物可用作脑水肿的抑制剂或脑血管障碍的治疗剂。此外，由于化合物几乎不表现出在急性期治疗脑血管障碍中被认为是副作用的行为抑制作用，所以它们是特别是急性期脑血管障碍的优良治疗剂。此外，化合物显示脑保护活性（抗缺氧活性），增加脑血流量的活性和抑制脂质过氧化的活性，并且这些活性可导致作为脑血管障碍治疗剂的效用增加。

2. 发明授权

US5972943A Pyridinecarboxamide derivatives 失效
标题翻译：吡啶甲酰胺衍生物
公开(公告)号：US5972943A
公开(公告)日：1999-10-26
申请号：US101760
申请日：1998-07-20
申请人： Norio Oshida , Yoji Mimaki , Hiroaki Satoh , Shinji Yokoyama , Yukiko Muraki , Kazumi Nishimura , Tamiko Hamada , Einosuke Sakurai , Hiroshi Sakai , Toshiji Sugai , Tomomi Tonoike , Koichi Itoh
发明人： Norio Oshida , Yoji Mimaki , Hiroaki Satoh , Shinji Yokoyama , Yukiko Muraki , Kazumi Nishimura , Tamiko Hamada , Einosuke Sakurai , Hiroshi Sakai , Toshiji Sugai , Tomomi Tonoike , Koichi Itoh
IPC分类号： C07D213/80 , C07D213/82 , A61K31/495 , C07D401/04
CPC分类号： C07D213/80 , C07D213/82
摘要： Pyridinecarboxamide derivatives of the formula ##STR1## (wherein n represents an integer of 14-18, and R represents a hydrogen atom or a straight or branched C.sub.1 -C.sub.4 alkyl group) or physiologically acceptable salts thereof. The compounds have excellent inhibiting activity of cerebral edema, especially ischemic cerebral edema, and inhibiting activity of delayed death of neuronal cells (an inhibiting activity of Ca-influx in neuronal cells). Cerebral edema is a pathologic condition accompanying cerebrovascular disorders, especially the acute stage of cerebrovascular disorders and then the compounds are useful as an agent for inhibiting cerebral edema or a therapeutic agent for cerebrovascular disorders. Moreover, the compounds have no hypotensive action which is considered to be side-effect in treating the acute stage cerebrovascular disorders and hardly show a behavior suppressing action so that they are an excellent therapeutic agent for, in particular, the acute stage cerebrovascular disorders. Moreover, the compounds show a cerebral protective activity (an anti-anoxic activity), an increasing activity of cerebral blood flow, and an inhibiting activity of lipid peroxidation and these activities may lead to the increased utility as a therapeutic agent for cerebrovascular disorders.
摘要翻译： PCT No.PCT / JP97 / 04207 Sec。 371日期：1998年7月20日 102（e）1998年7月20日PCT PCT 1997年11月19日PCT公布。出版物WO98 / 22439 日期：1998年5月28日下式的吡啶甲酰胺衍生物（其中n表示14-18的整数，R表示氢原子或直链或支链的C 1 -C 4烷基）或其生理学上可接受的盐。该化合物具有优异的脑水肿抑制活性，特别是缺血性脑水肿，抑制神经元细胞延迟死亡的活性（神经细胞内Ca流入的抑制活性）。脑水肿是伴随脑血管障碍，特别是脑血管障碍的急性期的病理状况，然后该化合物可用作抑制脑水肿的药剂或脑血管障碍治疗剂。此外，化合物没有降压作用，被认为在治疗急性期脑血管障碍中具有副作用，并且几乎不显示行为抑制作用，因此它们是特别是急性期脑血管障碍的优良治疗剂。此外，化合物显示脑保护活性（抗缺氧活性），脑血流量的增加的活性和脂质过氧化的抑制活性，并且这些活性可能导致作为脑血管障碍治疗剂的效用增加。

3. 发明授权

US4994456A Pyridinecarboxylic acid amide derivatives and pharmaceutical compositions comprising same 失效
标题翻译：吡啶羧酸酰胺衍生物和包含其的药物组合物
公开(公告)号：US4994456A
公开(公告)日：1991-02-19
申请号：US483532
申请日：1990-02-22
申请人： Katsutoshi Miura , Hiroyasu Koyama , Toshiji Sugai , Hiroaki Yamada , Einosuke Sakurai , Masato Horigome
发明人： Katsutoshi Miura , Hiroyasu Koyama , Toshiji Sugai , Hiroaki Yamada , Einosuke Sakurai , Masato Horigome
IPC分类号： C07D213/81 , C07D213/82 , C07D401/04 , C07D401/06 , C07D401/14
CPC分类号： C07D213/81 , C07D213/82 , C07D401/04 , C07D401/06 , C07D401/14
摘要： Compounds are disclosed of the formula ##STR1## wherein R.sub.1 is hydrogen; C.sub.1 -C.sub.6 alkyl; C.sub.3 -C.sub.6 cycloalkyl or diphenylmethyl;Y is --NH(CH.sub.2).sub.n --R.sub.2 or ##STR2## R.sub.2 is OH or --ONO.sub.2 ; l is 2 or 3; m is 0 or 1; and n is 2 to 8; andphysiologically acceptable acid addition salts thereof. The compounds of formula (I) are of a blood flow-increasing and hypotensive actions and can be used for the therapy or prevention of diseases in the cardiovascular system.

4. 发明授权

US5250526A Pyridinecarboxylic acid amide derivatives and pharmaceutical compositions comprising same 失效
标题翻译：吡啶羧酸酰胺衍生物和包含其的药物组合物
公开(公告)号：US5250526A
公开(公告)日：1993-10-05
申请号：US746636
申请日：1991-08-19
申请人： Katsutoshi Miura , Hiroyasu Koyama , Toshiji Sugai , Hiroaki Yamada , Einosuke Sakurai , Masato Horigome
发明人： Katsutoshi Miura , Hiroyasu Koyama , Toshiji Sugai , Hiroaki Yamada , Einosuke Sakurai , Masato Horigome
IPC分类号： C07D213/82 , C07D401/04 , A61K31/495 , A61K31/55 , C07D401/06
CPC分类号： C07D213/82
摘要： Compounds are disclosed of the formula ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.3 alkyl or diphenylmethyl; Y is --NH(CH.sub.2).sub.n --R.sub.2 ; R.sub.2 is OH or --ONO.sub.2 ; m is 2 or 3; and n is 9 to 13 or physiologically acceptable acid addition salts thereof. The compounds of formula (I) are of a blood flow-increasing and hypotensive actions and can be used for the therapy or prevention of diseases in the cardiovascular system.

5. 发明授权

US5025012A Nicotinic acid derivatives and pharmaceutical compositions comprising same 失效
标题翻译：烟酸衍生物和包含其的药物组合物
公开(公告)号：US5025012A
公开(公告)日：1991-06-18
申请号：US484130
申请日：1990-02-22
申请人： Katsutoshi Miura , Hiroyasu Koyama , Toshiji Sugai , Hiroaki Yamada , Einosuke Sakurai
发明人： Katsutoshi Miura , Hiroyasu Koyama , Toshiji Sugai , Hiroaki Yamada , Einosuke Sakurai
IPC分类号： A61K31/44 , A61K31/4418 , A61K31/455 , A61K31/495 , A61K31/535 , A61K31/55 , A61P9/00 , A61P9/10 , A61P9/12 , C07D213/80 , C07D401/04 , C07D401/06 , C07D405/12 , C07D413/04 , C07D413/06
CPC分类号： C07D213/80 , C07D401/04 , C07D401/06 , C07D405/12 , C07D413/04 , C07D413/06
摘要： Compounds are disclosed of the formula ##STR1## wherein R.sub.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;Y is --CH.sub.2 --, --O--, ##STR2## R.sub.2 is C.sub.1 -C.sub.6 alkyl; C.sub.2 -C.sub.6 alkenyl; C.sub.3 -C.sub.6 cycloalkyl; phenyl which may be mono- or di-substituted on the phenyl ring with C.sub.1 -C.sub.6 alkoxy; aralkyl which may be mono- or di-substituted on the aromatic ring with C.sub.1 -C.sub.6 alkoxy; diphenylmethyl; carboalkoxy; or an O- or N-heterocyclic radical which is linked to the nitrogen atom via carbonyl or carbonylmethylene;m is 2 or 3;and n is 0 or 1, and physiologically acceptable acid addition salts thereof. The compounds of formula (I) are of a blood flow-increasing action and can be used for the therapy or prevention of diseases in the cardiovascular system.

6. 发明授权

US5227395A Anti-platelet aggregating agent 失效
标题翻译：抗药剂聚集剂
公开(公告)号：US5227395A
公开(公告)日：1993-07-13
申请号：US854904
申请日：1992-03-20
申请人： Hirohiko Komatsu , Einosuke Sakurai , Fumiko Hamaguchi , Tatsuo Nagasaka
发明人： Hirohiko Komatsu , Einosuke Sakurai , Fumiko Hamaguchi , Tatsuo Nagasaka
IPC分类号： A61K31/40 , A61K31/4015 , A61P7/02 , C07D207/27
CPC分类号： A61K31/40 , Y10S514/822
摘要： The use of 1-phenoxycarbonyl-2-pyrrolidinone derivatives as an anti-platelet aggregating agent. The derivatives are of the formula ##STR1## wherein R is a C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, a nitro group or a halogen atom and n is 0, 1 or 2.

7. 发明授权

US5110823A Pyrrolidine derivatives as nootropic agents 失效
标题翻译：吡咯烷衍生物作为诱导剂
公开(公告)号：US5110823A
公开(公告)日：1992-05-05
申请号：US660950
申请日：1991-02-26
申请人： Fumiko Hamaguchi , Tatsuo Nagasaka , Rie Hakamada , Einosuke Sakurai
发明人： Fumiko Hamaguchi , Tatsuo Nagasaka , Rie Hakamada , Einosuke Sakurai
IPC分类号： A61K31/415 , A61K31/42 , A61K31/495 , A61P25/28 , C07D487/04 , C07D487/14 , C07D498/04 , C07D498/14
CPC分类号： C07D487/04 , C07D487/14
摘要： Pyrrolidine derivatives of formula (I) are disclosed. ##STR1## wherein the ring A represents the following heterocyclic ring ##STR2## The compounds of formula (I) are useful as nootropic agents.
摘要翻译：公开了式（I）的吡咯烷衍生物。其中环A表示以下杂环。式（I）化合物可用作促智剂。

8. 发明授权

US5140041A 1-phenoxycarbonyl-2-pyrrolidinone derivatives and nootropic agents 失效
标题翻译： 1-苯氧羰基-2-吡咯烷酮衍生物和异构体
公开(公告)号：US5140041A
公开(公告)日：1992-08-18
申请号：US658300
申请日：1991-02-20
申请人： Fumiko Hamaguchi , Tatsuo Nagasaka , Einosuke Sakurai
发明人： Fumiko Hamaguchi , Tatsuo Nagasaka , Einosuke Sakurai
IPC分类号： C07D207/27 , A61K31/40 , A61K31/4015 , A61P25/28 , C07D207/26 , C07D207/263
CPC分类号： C07D207/27
摘要： 1-Phenoxycarbonyl-2-pyrrolidinone derivatives of formula (I) or (I') are disclosed. ##STR1## wherein R is a C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, a nitro group or a halogen atom and n is 1 or 2, and R' is the same as R, but including further a hydrogen atom. The compounds of formula (I') are useful as nootropic agents.

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