Anticonvulsive compounds
    13.
    发明公开
    Anticonvulsive compounds 失效
    抗惊厥药

    公开(公告)号:EP0162669A2

    公开(公告)日:1985-11-27

    申请号:EP85303451.0

    申请日:1985-05-16

    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.

    摘要翻译: 使用抗惊厥药:下式的二氢尿嘧啶化合物:其中A和B之一为... ...(其中Y1 Y2和Y3各自为H,C1-C4直链或支链烷基,卤素 ,硝基,氨基,羧基,2-7个碳原子的烷氧基羰基或-CF 3),萘基或二苯基甲基,另一个是H,C 1 -C 6直链或支链烷基,C 2 -C 6烯基,环戊基,环己基或 CHEM> ...(其中Z 1,Z 2和Z 3各自为H,C 1 -C 4直链或支链烷基,卤素或-CF 3); X为O或S; 和R 1,R 2和R 3各自为H或C 1 -C 3直链或支链烷基。

    Phosphorus-containing peptide derivative
    14.
    发明公开
    Phosphorus-containing peptide derivative 失效
    磷光体吸附剂Peptidderivat。

    公开(公告)号:EP0103867A1

    公开(公告)日:1984-03-28

    申请号:EP83109190.5

    申请日:1983-09-16

    摘要: A phosphorus-containing peptide derivative represented by the general formula [I]:
    {wherein R, is hydrogen, lower alkyl, lower alkoxycarbonyl, aralkyloxycarbonyl or
    [wherein R e is hydrogen, alkyl having 1 to 17 carbon atoms, unsubstituted or substituted aryl (wherein the substituent is selected from lower alkyl, lower alkoxy and halogen), unsubstituted or substituted aralkyl (wherein the substituent is selected from lower alkyl, lower alkoxy and halogen), or cycloalkyl having 5 or 6 carbon atoms]; R 2 is hydrogen, unsubstituted or substituted lower alkyl (wherein the substituent is selected from amino, mercapto, lower alkylthio, carboxyl, hydroxyl, guanidino and imidazolyl), unsubstituted or substituted aryl (wherein the substituent is selected from amino, hydroxyl, lower alkoxy, aralkyloxy, lower alkyl, halogen and nitro), unsubstituted or substituted aralkyl (wherein the substituent is seiected from amino, lower alkyl halogen and nitro) or

    (wherein R 7 has the same meaning as R 3 ); R 3 is hydrogen, lower alkyl, unsubstituted or substituted aralkyl (wherein the substituent has the same meaning as in R e ), R 8 -CO-(wherein R 8 has the same meaning as R e ), R 9 -O-CO-[wherein R 9 is lower alkyl, unsubstituted or substituted aryl (wherein the substituent has the same meaning as in R e ), unsubstituted or substituted aralkyl (wherein the substituent has the same meaning as in R 8 )], or R 9 NHCO- (wherein R 9 has the same meaning as defined above); and R 4 and R 5 are the same or different, and are hydrogens, alkyls having 1 to 18 carbon atoms, unsubstituted or substituted aryl (wherein the substituent has the same meaning as in R e ), unsubstituted or substituted aralkyl (wherein the substituent has the same meaning as in R 6 ), -(CH 2 CH 2 O) m CH 3 (wherein m is an integer of 1 - 4), or -CH[CH 2 OCO(CH 2 ) n CH 3 ] 2 (wherein n is 0 or an integer of 1 - 10) }, and pharmacologically acceptable salts thereof is prepared. Said compounds have an angiotensin converting enzyme-inhibiting action and as the result an anti-hypertensive action.

    摘要翻译: 由通式[I]表示的含磷肽衍生物:... ... {其中R1是氢,低级烷基,低级烷氧基羰基,芳烷氧基羰基或...... R6- [... [其中R6是氢,具有1 至17个碳原子,未取代或取代的芳基(其中取代基选自低级烷基,低级烷氧基和卤素),未取代或取代的芳烷基(其中取代基选自低级烷基,低级烷氧基和卤素)或具有5或 6个碳原子]; R2是氢,未取代或取代的低级烷基(其中取代基选自氨基,巯基,低级烷硫基,羧基,羟基,胍基和咪唑基),未取代或取代的芳基(其中取代基选自氨基,羟基,低级烷氧基, 芳烷氧基,低级烷基,卤素和硝基),未取代或取代的芳烷基(其中取代基选自氨基,低级烷基,卤素和硝基)或...(其中R7具有与R3相同的含义)。 R3是氢,低级烷基,未取代或取代的芳烷基(其中取代基与R6相同),R8-CO-(其中R8与R6相同),R9-O-CO- [其中R9较低 烷基,未取代或取代的芳基(其中取代基具有与R6相同的含义),未取代或取代的芳烷基(其中取代基具有与R 6相同的含义)]或R9NHCO-(其中R9具有与上述相同的含义 ); 并且R 4和R 5相同或不同,并且是氢,具有1至18个碳原子的烷基,未取代或取代的芳基(其中取代基具有与R 6相同的含义),未取代或取代的芳烷基(其中取代基具有相同 意义如R6)中, - (CH2CH2O)m CH3(其中m为1-4的整数)或CH [CH 2 OCO(CH 2)n CH 3] 2(其中n为0或1-10的整数)}, 并制备其药理学上可接受的盐。 所述化合物具有血管紧张素转化酶抑制作用,结果是抗高血压作用。

    Novel piperidine derivatives, processes for preparation thereof and pharmaceutical compositions containing same
    15.
    发明公开
    Novel piperidine derivatives, processes for preparation thereof and pharmaceutical compositions containing same 失效
    新的哌啶衍生物,涉及它们的制备方法和含有它们的药物制剂。

    公开(公告)号:EP0070171A1

    公开(公告)日:1983-01-19

    申请号:EP82303623.1

    申请日:1982-07-09

    摘要: New piperidine derivatives are disclosed having the following general formula:
    wherein Y is a group represented by R 10 or
    R 10 is hydrogen, alkyl having 1 - 3 carbon atoms, or substituted or unsubstituted benzyl, and when Y is
    Q is H; m is 0 or an integer of 1 - 5; A is hydroxyl, halogen, C 1 -C 5 alkyl, C 1 -C 5 alkoxy, C 2 -C 5 alkenyloxy, C 2 -C 5 alkinyloxy, C 1 -C 5 alkylthio, carboxyl, C 1 -C 5 alkoxycarbonyl, nitro, amino, C 1 -C 5 alkylamino, C 1 -C 5 alkanoylamino, sulfamoyl, mono or di-(C I -C 5 alkyl) aminosulfonyl, C 1 -C 5 alkylsulfonyl, carbamoyl, cyano or trifluoromethyl; when m is 2 or more, the A groups may be the same or different, or two A groups may be combined to form a C 1 -C 5 alkylenedioxy group; X is oxygen, sulfur, carbonyl, hydroxymethylene or methylene; R is straight-chain alkylene having 1 - 4 carbon atoms, or straight-chain alkylene having 1 - 4 carbon atoms and having a C 1 -C 5 alkyl substituent; Q is hydrogen, C 1 -C 5 alkyl, halogen, hydroxyl or C 1 -C 5 alkanoyloxy; n is 0 or an integer of 1 - 4; R 2 is hydroxyl, C 1 -C 5 alkoxy, halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, nitro or amino; when n is 2 or more, the R 2 groups may be the same or different, or two R 2 groups may by combined to form a C 1 -C 5 alkylenedioxy; B is -NH-, -N(R)- (wherein R is C 1 -C 5 alkyl, or substituted or unsubstituted phenyl) or -0-; and acid addition salts thereof.
    The new piperidine derivatives wherein Y is
    have a hypotensive activity.

    摘要翻译: 新的哌啶衍生物是圆盘游离缺失具有以下通式: worin Y为R10或表示的基团 R10是具有1至3个碳原子的氢,烷基,或substituiertem奥德unsubstituiertem苄基,和当Y是 Q是H; m为0或在1至5的整数; A是羟基,卤素,C1-C5烷基,C1-C5烷氧基,C2-C5链烯氧基,C2-C5炔氧基,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,单或二 - (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基团可以相同或不同,或者两个A基团可以结合以形成C1-C5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1-4个碳原子,或具有1-4个碳原子和具有C 1 -C 5烷基取代基的亚烷基的直链; Q是氢,C1-C5烷基,卤素,羟基或C1-C5烷酰氧基; n是0或1-4整数; R 2是羟基,C1-C5烷氧基,卤素,三氟甲基,三氟甲氧基,三氟甲硫基,硝基或氨基; 当n为2或更大时,R 2基团可以是相同或不同的,或