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    Anticonvulsive compounds
    2.
    发明公开
    Anticonvulsive compounds 失效
    有毒化合物

    公开(公告)号：EP0162669A3

    公开(公告)日：1986-11-20

    申请号：EP85303451

    申请日：1985-05-16

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Teranishi, Masayuki ,  Murakata, Chikara ,  Matsukuma, Ikuo ,  Shuto, Katsuichi ,  Ichikawa, Shunji

    IPC分类号： A61K31/505 ,  C07D239/22

    CPC分类号： C07D239/22 ,  A61K31/505

    摘要： For use an an anticonvulsive: dihydrouracil compounds of the formula
    where one of A and B is
    (where Y, Y 2 and Y 3 are each H, C 1 -C 4 straight- or branched-chain alkyl, halogen, nitro, amino. carboxyl, alkoxycarbonyl of 2-7 carbon atoms or -CF 3 ), naphthyl or diphenylmethyl and the other is H, C 1 -C 6 straight- or branched-chain alkyl, C 1 -C 6 alkenyl, cyclopentyl, cyclohexyl or
    (where Z 1 , Z 2 and Z 3 are each H, C 1 -C 4 straight- or branched-chain alkyl, halogen or -CF 3 ); X is 0 or S; and R 1 , R 2 and R 3 are each H or C 1 -C 3 straight- or branched-chain alkyl.

    Novel piperidine derivatives and pharmaceutical compositions containing same
    3.
    发明公开
    Novel piperidine derivatives and pharmaceutical compositions containing same 失效
    新型哌啶衍生物和含有其的药物组合物

    公开(公告)号：EP0092391A3

    公开(公告)日：1984-09-26

    申请号：EP83302123

    申请日：1983-04-14

    申请人： KYOWA HAKKO KOGYO CO., LTD

    发明人： Teranishi, Masayuki ,  Obase, Hiroyuki ,  Nomoto, Yuji ,  Shuto, Katsuichi ,  Karasawa, Akira ,  Kasuya, Yutaka

    IPC分类号： C07D401/06 ,  C07D401/04 ,  A61K31/445 ,  C07D211/58 ,  C07D211/26

    CPC分类号： C07D401/04 ,  C07D211/26 ,  C07D211/58 ,  C07D401/06

    摘要： Novel piperidine derivatives are disclosed having hypotensive activity, as well as pharmaceutical preparations containing them. The novel compounds are of the formula
    wherein A is a hydroxyl group, a halogen atom, a C,-C 5 alkyl group, a C 1 -C 5 alkoxy group, a C 2 -C 5 alkenyloxy group, a C 1 -C 5 alkinyloxy group, a C 1 -C 5 alkylthio group, a carboxyl group, a C 1 -C 5 alkoxycarbonyl group, a nitro group, an amino group, a C 1 -C 5 alkylamino group, a C,-C 5 alkanoylamino group, a sulfamoyl group, a mono- or di- (C 1 -C 5 alkyl) aminosulfonyl group, a C 1 -C 5 alkylsulfonyl group, a carbamoyl group, a cyano group or a trifluoromethyl group; when m is 2 or more, A may be the same or different groups, or two A groups may combine to form a C,-C 5 alkylenedioxy group; m is 0 or an integer of 1-5; Q is a carbonyl group or a hydroxymethylene group; R is a hydrogen atom or an alkyl group having 1-4 carbon atoms; X and Y are defined as follows: i) when Y = H, X represents
    ii) when Y = CH 3 , X represents
    and when
    X represents a hydrogen atom and their pharmacologically acceptable acid addition salts.

    摘要翻译： 公开了具有降血压活性的新型哌啶衍生物，以及含有它们的药物制剂。 该新化合物具有式CHEM，其中A为羟基，卤原子，C1-C5烷基，C1-C5烷氧基，C7-C5链烯氧基，C1-C5烷氧基， C1-C5烷硫基，羧基，C1-C5烷氧基羰基，硝基，氨基，C1-C5烷基氨基，C1-C5烷酰基氨基，氨磺酰基，一或二（ C1-C5烷基）氨基磺酰基，C1-C5烷基磺酰基，氨基甲酰基，氰基或三氟甲基; 当m为2以上时，A可以相同或不同，或两个A基团可以结合形成C1-C5亚烷基二氧基; m为0或1-5的整数; Q是羰基或羟基亚甲基; R是氢原子或具有1-4个碳原子的醇酸基; X和Y定义如下：i）当Y = H时，X表示 ii）当Y = CH 3时，X表示，当Y = CHEM时，X表示氢原子及其药理学上可接受的酸加成盐 。

    Novel piperidine derivatives, method for the preparation thereof and pharmaceutical compositions containing them
    4.
    发明公开
    Novel piperidine derivatives, method for the preparation thereof and pharmaceutical compositions containing them 失效
    哌啶衍生物，涉及它们的制备方法和含有它们的药物组合物。

    公开(公告)号：EP0029707A1

    公开(公告)日：1981-06-03

    申请号：EP80304147.4

    申请日：1980-11-19

    申请人： KYOWA HAKKO KOGYO CO., LTD

    发明人： Teranishi, Masayuki ,  Nakamizo, Nobuhiro ,  Obase, Hiroyuki ,  Kubo, Kazuhiro ,  Takai, Haruki ,  Kasuya, Yutaka

    IPC分类号： C07D401/04 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  A61K31/445 ,  A61K31/505 ,  A61K31/54 ,  A61K31/535

    CPC分类号： C07D211/58

    摘要： New piperidine derivatives which have a useful pharmacological activity such as a hypotensive activity are disclosed. The novel compounds are of the formula


    wherein A is hydroxy, halogen, lower alkyl, lower alkoxy, lower alkenyloxy, lower alkenyloxy, lower alkylthio, carboxy, lower alkoxycarbonyl, nitro, amino, lower alkylamino, lower alkanoylamino, sulfamoyl, mono- or di-lower alkylaminosulfonyl, lower alkylsulfonyl, carbamoyl, cyano or trifluoromethyl;
    m is 0 or an integer of 1-5, and when m is 2 or more, the A groups may be the same of different and any two A's may together form a lower alkylenedioxy group;
    X is oxygen, sulfur, carbonyl, hydroxymethylene or methylene;
    R 1 is straight-chain alkylene having 1-4 carbon atoms with or without lower alkyl substituent(s); R 2 is hydrogen or lower alkyl; and
    Y is a monovalent or divalent group of the formula 1,2 or 3:
    wherein p and q are each 0 or 1 provided that p and q are not both 1 at the same time: and when p and q are both 0, B is -N=N-.

    p is 1 and q is 0, B is -CONH-, -COO-,
    and when
    p is 0 and q is 1, B is -CONH or -S0 2 NH-;
    and R 3 is hydroxy, lower alkoxy, halogen, trifluoromethyl, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, nitro or amino;
    n is 0 or an integer of 1-4, and when n is 2 or more, the R 3 groups may be the same or different and any two R 3 groups maytogetherform a lower alkylenedioxv group;
    wherein R 3 and n are as defined above, and
    wherein R 3 and n are as defined above.

    Also disclosed are acid addition salts of the above compounds, pharmaceutical compositions containing them and a method for their preparation.

    摘要翻译： 其中有一个有用的药理活性的新哌啶衍生物：如降压作用是游离缺失盘。 新化合物是下式的 worin A是羟基，卤素，低级烷基，低级烷氧基，低级链烯氧基，低级链烯氧基，低级烷硫基，羧基，低级烷氧羰基，硝基，氨基，低级烷基氨基，低级烷酰基氨基，氨磺酰基，单 - 或二 - 低级烷基氨基磺酰，低级烷基磺酰基，氨基甲酰基，氰基或三氟甲基; m为0或在1至5的整数，当m为2以上时，A基团可以是相同的不同的，并且任何两个A可以一起形成低级亚烷基二氧基; X是氧，硫，羰基，羟基亚甲基或亚甲基; R 1为直链亚烷基具有带或不带低级烷基取代基（一个或多个）1-4个碳原子; R 2是氢或低级烷基; 和Y是下式的一价或二价基团1,2或3： worin p和q各自是0或1提供p和q不同时为1的同时; 并且当p和q均为0，B为-N = N， p是1和q是0，B是-CONH-，-COO- 和当p是0且q是1，B 为-CONH-或-SO 2 NH-; 且R 3是羟基，低级烷氧基，卤素，三氟甲基，三氟甲基，三氟甲氧基，三氟甲硫基，硝基和氨基; n是0或1-4的整数，并且当n为2或更大时，R 3基团可以相同或不同，并且任何两个R 3基团可以一起形成低级亚烷基二氧基; worin R 3和n如上所定义，和 worin R3和n如上述所定义。 所以圆盘游离缺失是上述化合物的酸加成盐，包含它们的药物组合物和方法对于它们的制备方法。

    Quinoline-n-oxide derivative and pharmaceutical composition
    6.
    发明公开
    Quinoline-n-oxide derivative and pharmaceutical composition 失效
    喹啉N-氧化物衍生物和药物制剂。

    公开(公告)号：EP0177764A1

    公开(公告)日：1986-04-16

    申请号：EP85111243.3

    申请日：1985-09-05

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Teranishi, Masayuki ,  Suzuki, Koji ,  Kase, Hiroshi ,  Kitamura, Shigeto ,  Shuto, Katsuichi ,  Omori, Kenji

    IPC分类号： C07D215/60 ,  C07D405/12 ,  A61K31/47

    CPC分类号： C07D405/12 ,  C07D215/60

    摘要： A quinoline-N-oxide derivative represented by the formula:
    [wherein X is hydroxy, lower alkoxy, lower alkylthio, unsubstituted or substituted aralkyloxy, or unsubstituted or substituted aralkylthio; Y is a hydrogen atom or halogen atom; R, is alkylene or alkenylene having 3 to 15 carbon atoms; Z is hydroxymethyl, lower alkoxymethyl, unsubstituted or substituted aryloxymethyl, tetrahydropyranyloxymethyl, tetrahydrofuranyloxymethyl, unsubstituted or substituted arylsulfonyloxymethyl, lower alkylthiomethyl, unsubstituted or substituted arylthiomethyl, lower alkylsulfinylmethyl, unsubstituted or substituted arylsulfinylmethyl, lower alkylsulfonylmethyl, unsubstituted or substituted arylsulfonylmethyl, aminomethyl, -CH 2 NHR 2 (wherein R 2 is lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), -CH 2 NR 3 R 4 , (wherein R 3 and R 4 are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), -CH 2 N + R 5 R 6 R 7 (wherein R 5 , R 6 , and R 7 are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl, where the counterion is an anion of acid or a hydroxyl ion), -COR 8 (wherein R. is a hydrogen atom, lower alkyl or hydroxy), -CH(OR 9 ) 2 (wherein R. is lower alkyl), iminomethyl, hydroxyiminomethyl, or a halogen atom] and its salts, can very strongly inhibit the lipoxygenase and considerably suppress production and release of its metabolites, and thus are useful as preventive and healing agents for the diseases caused by the lipoxygenase metabolites.

    Novel piperidine derivatives and pharmaceutical compositions containing same
    7.
    发明公开
    Novel piperidine derivatives and pharmaceutical compositions containing same 失效
    哌啶 - 衍生物和药物制剂Zusammensetzungen。

    公开(公告)号：EP0092391A2

    公开(公告)日：1983-10-26

    申请号：EP83302123.1

    申请日：1983-04-14

    申请人： KYOWA HAKKO KOGYO CO., LTD

    发明人： Teranishi, Masayuki ,  Obase, Hiroyuki ,  Nomoto, Yuji ,  Shuto, Katsuichi ,  Karasawa, Akira ,  Kasuya, Yutaka

    IPC分类号： C07D401/06 ,  C07D401/04 ,  A61K31/445

    CPC分类号： C07D401/04 ,  C07D211/26 ,  C07D211/58 ,  C07D401/06

    摘要： Novel piperidine derivatives are disclosed having hypotensive activity, as well as pharmaceutical preparations containing them. The novel compounds are of the formula
    wherein A is a hydroxyl group, a halogen atom, a C,-C 5 alkyl group, a C 1 -C 5 alkoxy group, a C 2 -C 5 alkenyloxy group, a C 1 -C 5 alkinyloxy group, a C 1 -C 5 alkylthio group, a carboxyl group, a C 1 -C 5 alkoxycarbonyl group, a nitro group, an amino group, a C 1 -C 5 alkylamino group, a C,-C 5 alkanoylamino group, a sulfamoyl group, a mono- or di- (C 1 -C 5 alkyl) aminosulfonyl group, a C 1 -C 5 alkylsulfonyl group, a carbamoyl group, a cyano group or a trifluoromethyl group; when m is 2 or more, A may be the same or different groups, or two A groups may combine to form a C,-C 5 alkylenedioxy group; m is 0 or an integer of 1-5; Q is a carbonyl group or a hydroxymethylene group; R is a hydrogen atom or an alkyl group having 1-4 carbon atoms; X and Y are defined as follows: i) when Y = H, X represents
    ii) when Y = CH 3 , X represents
    and when
    X represents a hydrogen atom and their pharmacologically acceptable acid addition salts.

    摘要翻译： 公开了具有降血压活性的新型哌啶衍生物，以及含有它们的药物制剂。 该新化合物具有式CHEM，其中A为羟基，卤原子，C1-C5烷基，C1-C5烷氧基，C7-C5链烯氧基，C1-C5烷氧基， C1-C5烷硫基，羧基，C1-C5烷氧基羰基，硝基，氨基，C1-C5烷基氨基，C1-C5烷酰基氨基，氨磺酰基，一或二（ C1-C5烷基）氨基磺酰基，C1-C5烷基磺酰基，氨基甲酰基，氰基或三氟甲基; 当m为2以上时，A可以相同或不同，或两个A基团可以结合形成C1-C5亚烷基二氧基; m为0或1-5的整数; Q是羰基或羟基亚甲基; R是氢原子或具有1-4个碳原子的醇酸基; X和Y定义如下：i）当Y = H时，X表示 ii）当Y = CH 3时，X表示，当Y = CHEM时，X表示氢原子及其药理学上可接受的酸加成盐 。