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    8-(Substituted N-phenylcarboxamidomethyl) pyrrolizidines and use thereof as antiarrhythmics
    3.
    发明授权
    8-(Substituted N-phenylcarboxamidomethyl) pyrrolizidines and use thereof as antiarrhythmics 失效
    8-（取代的N-苯基甲酰胺基甲基）吡咯烷酮及其作为抗心律失常药的用途

    公开(公告)号：US4564624A

    公开(公告)日：1986-01-14

    申请号：US473947

    申请日：1983-03-10

    申请人： Seiji Miyano ,  Kunihiro Sumoto ,  Minoru Morita ,  Fumio Sato

    发明人： Seiji Miyano ,  Kunihiro Sumoto ,  Minoru Morita ,  Fumio Sato

    IPC分类号： A61K31/40 ,  A61P9/06 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： An 8-substituted pyrrolizidine derivative representable by the formula: ##STR1## (wherein R.sup.1 stands for hydrogen or a lower alkyl group, R.sup.2 stands for hydrogen, a lower alkyl group, a lower alkoxy group or halogen, and R.sup.3 stand for a lower alkyl group, a lower alkoxy group, amino group or halogen), which can be produced by reacting a corresponding substituted anilin with 8-halocarbonylmethyl pyrrolizidine or reacting an alkali metal salt of the corresponding substituted anilin with 8-alcoxycarbonylmethyl pyrrolizidine. The derivative is useful as an antiarrhythmic agent.

    摘要翻译： 可由下式​​表示的8-取代的吡咯并吡啶衍生物：其中R1代表氢或低级烷基，R2代表氢，低级烷基，低级烷氧基或卤素，R3代表低级烷基 基团，低级烷氧基，氨基或卤素），其可以通过使相应的取代的苯胺基与8-卤代羰基甲基吡咯烷酮反应或使相应的取代的苯胺基的碱金属盐与8-烷氧羰基甲基吡咯嗪在反应中制备。 该衍生物可用作抗心律失常剂。

    Pyrrolizidine compounds, and their use as antiarrhythmic agents
    6.
    发明授权
    Pyrrolizidine compounds, and their use as antiarrhythmic agents 失效
    吡咯烷啶化合物及其作为抗心律不齐剂的用途

    公开(公告)号：US4831049A

    公开(公告)日：1989-05-16

    申请号：US751797

    申请日：1985-07-03

    申请人： Seiji Miyano ,  Kunihiro Sumoto ,  Fumio Satoh

    发明人： Seiji Miyano ,  Kunihiro Sumoto ,  Fumio Satoh

    IPC分类号： A61K31/40 ,  A61P9/06 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： A novel pyrrolizidine compound of the formula ##STR1## wherein R.sup.1 is an alkyl group of 1 to 4 carbon atoms or a phenyl group; and R.sup.2 and R.sup.3 are such that at least one of them is an alkyl group of 1 to 4 carbon atoms and the other, if not alkyl, being a hydrogen atom is produced by reacting .DELTA..sup.4(8) -dehydropyrrolizidine with a substituted malonic acid and the thus formed 2-substituted-8-pyrrolizidineacetic acid with a substituted aniline. The products are subjected to optical resolution and are potentantiarrhythmic agents.

    摘要翻译： 式（Ⅰ）的新型吡咯烷酮化合物，其中R 1为1至4个碳原子的烷基或苯基; 并且R2和R3使得它们中的至少一个是具有1至4个碳原子的烷基，而另一个（如果不是烷基）是氢原子，则通过使DELTA 4（8） - 溴丙啶与取代的丙二酸反应 和由此形成的2-取代-8-吡咯烷二酸乙酯与取代的苯胺。 产品经受光学拆分，是有效的抗心律失常药。

    Oxabicycloheptane derivatives
    7.
    发明授权
    Oxabicycloheptane derivatives 失效
    氧杂双环庚烷衍生物

    公开(公告)号：US4713453A

    公开(公告)日：1987-12-15

    申请号：US19973

    申请日：1987-02-27

    申请人： Toshio Tatsuoka ,  Kenji Suzuki ,  Kayoko Imao ,  Fumio Satoh ,  Seiji Miyano ,  Kunihiro Sumoto

    发明人： Toshio Tatsuoka ,  Kenji Suzuki ,  Kayoko Imao ,  Fumio Satoh ,  Seiji Miyano ,  Kunihiro Sumoto

    IPC分类号： C07D333/00 ,  A61K31/00 ,  A61K31/35 ,  A61K31/352 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/435 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  A61P9/00 ,  A61P25/18 ,  A61P25/28 ,  C07D311/94 ,  C07D405/04 ,  C07D405/12 ,  C07D407/04 ,  C07D409/04 ,  C07D487/04 ,  C07D417/00 ,  C07D401/00 ,  C07D405/00 ,  C07D413/00

    CPC分类号： C07D405/04 ,  C07D311/94 ,  C07D405/12 ,  C07D409/04 ,  C07D487/04

    摘要： The present invention relates to a novel oxabicycloheptane derivative of the following formula and a pharmaceutically acceptable salt thereof: ##STR1## where D is a hydrogen atom, a halogen atom, a hydroxyl group, an alkoxy group, an arylalkoxy group, an acyloxy group, a dialkylcarbamoyloxy group or an amidoalkyloxy group; B is a substituted or unsubstituted phenyl, thienyl or furyl group; A is the group ##STR2## (where l is 0 or 1; m and n are each 1 or more, provided that m+n is an interger of 2-8; R.sup.1 is an alkylamino group, a dialkylamino group, an arylalkylamino group, a morpholino group, a thiomorpholino group, a 1-pyrrolidinyl group, a piperidino group, an N-alkylpiperazinyl group, an N-hydroxyalkylpiperazinyl or a pyrrolizidinyl group; and R.sup.2 is a lower alkyl group or a hydroxl group), or the group ##STR3## (where l, m, n, R.sup.1 and R.sup.2 are each the same as defined above), or the group ##STR4## (where R.sup.3 and R.sup.4 which may be the same or different each represents a hydrogen atom, a lower alkyl group, an alkoxycarbonyl group or an acyl group), or the group ##STR5## (where m, l, n, R.sup.1 and R.sup.2 are each the same as defined above). The oxabicycloheptane derivative having the formula defined above and pharmaceutically acceptable salts thereof are effective in ameliorating or eliminating the symptoms that appear either as a result of organic disorders in the brain or on account of pathergasia. These compouds also have antidepressant effects and the useful as psychopharmaceuticals.

    摘要翻译： 本发明涉及下式的新型氧杂双环庚烷衍生物及其药学上可接受的盐：其中D是氢原子，卤素原子，羟基，烷氧基，芳基烷氧基，酰氧基， 二烷基氨基甲酰氧基或酰氨基烷氧基; B是取代或未取代的苯基，噻吩基或呋喃基; A是组（其中l是0或1; m和n各自为1或更多，条件是m + n是2-8的整数; R1是烷基氨基，二烷基氨基，芳基烷基氨基 吗啉基，硫代吗啉基，1-吡咯烷基，哌啶子基，N-烷基哌嗪基，N-羟基烷基哌嗪基或吡咯烷基; R2为低级烷基或羟基），或该基团 ＆lt; IMAGE＆gt;（其中l，m，n，R 1和R 2各自与上述相同）或基团（其中可以相同或不同的R 3和R 4各自表示氢原子，低级烷基 基团，烷氧基羰基或酰基）或基团（其中m，l，n，R 1和R 2各自与上述定义相同）。 具有上述定义的式的氧杂双环庚烷衍生物及其药学上可接受的盐在改善或消除由于脑中有机疾病或由于麻醉引起的症状而有效。 这些药物也具有抗抑郁作用，作为心理药物有用。

    8-substituted pyrrolizidine and quaternary ammonium salts thereof
    8.
    发明授权
    8-substituted pyrrolizidine and quaternary ammonium salts thereof 失效
    8-取代的吡咯烷啶及其季铵盐

    公开(公告)号：US4617401A

    公开(公告)日：1986-10-14

    申请号：US574932

    申请日：1984-01-27

    申请人： Seiji Miyano ,  Kunihiro Sumoto ,  Minoru Morita ,  Fumio Sato

    发明人： Seiji Miyano ,  Kunihiro Sumoto ,  Minoru Morita ,  Fumio Sato

    IPC分类号： A61K31/40 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  A61P43/00 ,  C07D487/04 ,  C07D209/52

    CPC分类号： C07D487/04

    摘要： Novel 8-substituted pyrrolizidines and quaternary ammonium salts thereof of the formula ##STR1## wherein R is a C.sub.4`-C.sub.10 alkyl, aralkyl or aryl group; a lower alkoxycarbonyl or a lower alkoxycarbonylmethyl group; a lower aliphatic carboxyl group amidated with pyridinylamine, aniline, cyclohexylamine, phenylbenzylamine or methoxyphenylbenzylamine; a lower hydroxyalkyl group which has one or two phenyl, a trihalomethylphenyl or a halophenyl group; a lower alkyl group which has a hydroxyl group esterified with acetic, benzoic, cinnamic, xanthene-carboxylic or methoxybenzoic acid, or etherified with a C.sub.2 -C.sub.13 alcohol; a lower alkyl group having a primary amino, a lower alkylamino, guanidino, benzylamino, hydroxylbenzylamino, methoxybenzylamino, aminobenzylamino, acetamino, benzoylamino, hydroxybenzoylamino, methoxybenzoylamino, or aminobenzoylamino group; or a lower alkyl group bearing benzoyl, methoxybenzoyl or halobenzoyl group; Y stands for an alkyl group quaternizing the nitrogen of the pyrrolizidine nucleus, which may optionally be substituted with halogen, an aryl, phenacyl or phenylphenacyl group; X stands for halogen. These compounds have various pharmacological activities such as atropine-like activity, papaverine-like activity, neuromuscular-blocking activity, etc.

    摘要翻译： 新颖的8-取代的吡咯并二唑及其季铵盐，其中R是C 4 -C 10烷基，芳烷基或芳基; 低级烷氧基羰基或低级烷氧羰基甲基; 与吡啶胺，苯胺，环己胺，苯基苄胺或甲氧基苯基苄胺酰胺化的低级脂族羧基; 具有一个或两个苯基，三卤代甲基苯基或卤代苯基的低级羟烷基; 具有用乙酸，苯甲酸，肉桂酸，呫吨 - 羧酸或甲氧基苯甲酸酯化的羟基的低级烷基，或用C 2 -C 13醇醚化; 具有伯氨基，低级烷基氨基，胍基，苄基氨基，羟基苄基氨基，甲氧基苄基氨基，氨基苄基氨基，乙酰氨基，苯甲酰基氨基，羟基苯甲酰氨基，甲氧基苯甲酰氨基或氨基苯甲酰氨基的低级烷基。 或具有苯甲酰基，甲氧基苯甲酰基或卤代苯甲酰基的低级烷基; Y表示可以任选被卤素，芳基，苯甲酰基或苯基苯甲酰基取代的吡咯烷子核的氮季铵化的烷基; X代表卤素。 这些化合物具有各种药理活性，如阿托品样活性，罂粟碱样活性，神经肌肉阻滞活性等。