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39 条记录 (耗时 0.016 秒)

    4-Aralkyl-5-substituted-1,2,4-triazole-5-thiols
    13.
    发明公开
    4-Aralkyl-5-substituted-1,2,4-triazole-5-thiols 失效
    4-芳烷基-5-取代物1,2,4-三唑-5-硫醚。

    公开(公告)号：EP0323737A1

    公开(公告)日：1989-07-12

    申请号：EP88312197.2

    申请日：1988-12-22

    申请人： SMITHKLINE BECKMAN CORPORATION

    发明人： Kruse, Lawrence Ivan ,  Finkelstein, Joseph Alan

    IPC分类号： C07D249/12 ,  C07C159/00 ,  A61K31/41

    CPC分类号： C07D249/12 ,  C07C335/40

    摘要： Compounds of formula (I)
    and pharmaceutically acceptable salts thereof are described in which, n is 0 to 5; X¹ to X⁵ are any accessible combination of hydrogen, halogen, C₁₋₆alkyl, C₁₋₆alkoxy, cyano, nitro, SONH₂, SO₂NH₂, SO₂CH₃, SO₂CH₂F, SO₂CHF₂, SO₂CF₃, CF₃, CHO, OH, CH₂OH, CO₂H, or CO₂C p H 2p+1 wherein p is 1 to 4; R¹ is phenyl substituted by X¹ to X⁵, C₁₋₄alkyl, C₃₋₆cycloalkyl, or an arylC₁₋₄alkyl group substituted by X¹ to X⁵; R² is hydrogen, C₁₋₄alkyl or (CH₂) m -CO₂R³; m is 0 to 5; and R³ is H or C₁₋₄alkyl.
    These compounds are dopamine-β-hydroxylase inhibitors. Pharmaceutical compositions are described as are methods of use. Processes for the preparation of these compounds are described.

    摘要翻译： 描述式（I）化合物及其药学上可接受的盐，其中n为0至5; X 1〜X 5是氢，卤素，C 1-6烷基，C 1-6烷氧基，氰基，硝基，SONH 2，SO 2 NH 2，SO 2 CH 3，SO 2 CH 2 F，SO 2 CHF 2，SO 2 CF 3，CF 3，CHO，OH，CH 2 OH， CO2H或CO2CpH2p + 1，其中p为1至4; R 1是被X 1取代的苯基，X 5，C 1-4烷基，C 3-6环烷基或被X 1至X 5取代的芳基C 1-4烷基; R 2是氢，C 1-4烷基或（CH 2）m -CO 2 R 3; m为0〜5; 且R 3为H或C 1-4烷基。 这些化合物是多巴胺-β-羟化酶抑制剂。 药物组合物被描述为使用的方法。 描述了这些化合物的制备方法。

    Dopamine-beta-hydroxylase inhibitors
    14.
    发明公开
    Dopamine-beta-hydroxylase inhibitors 失效
    多巴胺-β-羟化酶抑制剂

    公开(公告)号：EP0246888A3

    公开(公告)日：1988-09-28

    申请号：EP87304504

    申请日：1987-05-20

    申请人： SMITHKLINE BECKMAN CORPORATION

    发明人： Finkelstein, Joseph Alan ,  Kruse, Lawrence Ivan

    IPC分类号： C07D249/12 ,  A61K31/41 ,  C07C133/02 ,  C07C159/00

    CPC分类号： C07D249/12

    摘要： Compounds of Formula :
    in which n is 0 to 5, R is hydrogen or C 1-4 alkyl and X is hydrogen, halo, C 1-4 alkyl, CN, NO₂, SO₂NH₂, COOH, CHO, OH, CH₂OH, C 1-4 alkoxy, CF₃, SO₂CH₃, SO₂CF₃ or CO₂C a H 2a+1 wherein a is 1 to 5 or any synthetically accessible combination thereof of up to 5 substituents or any pharmaceutically acceptable salt or hydrate thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy as dopamine β-hydroxylase inhibitors.

    摘要翻译： 式中n为0-5，R为氢或C1-4烷基，X为氢，卤素，C1-4烷基，CN，NO2，SO2NH2，COOH，CHO，OH，CH2OH，C1-4烷氧基，CF3， SO 2 CH 3，SO 2 CF 3或CO 2 CaH 2 a + 1，其中a为1至5或至多5个取代基的任何可合成获得的组合，或其任何药学上可接受的盐或水合物，其制备方法，含有它们的药物组合物以及它们作为多巴胺β - 羟化酶抑制剂。

    Dopamine-beta-hydroxylase inhibitors
    15.
    发明公开
    Dopamine-beta-hydroxylase inhibitors 失效
    β-羟化酶 - 阴离子多巴胺。

    公开(公告)号：EP0246888A2

    公开(公告)日：1987-11-25

    申请号：EP87304504.1

    申请日：1987-05-20

    申请人： SMITHKLINE BECKMAN CORPORATION

    发明人： Finkelstein, Joseph Alan ,  Kruse, Lawrence Ivan

    IPC分类号： C07D249/12 ,  A61K31/41 ,  C07C133/02 ,  C07C159/00

    CPC分类号： C07D249/12

    摘要： Compounds of Formula :
    in which n is 0 to 5, R is hydrogen or C 1-4 alkyl and X is hydrogen, halo, C 1-4 alkyl, CN, NO₂, SO₂NH₂, COOH, CHO, OH, CH₂OH, C 1-4 alkoxy, CF₃, SO₂CH₃, SO₂CF₃ or CO₂C a H 2a+1 wherein a is 1 to 5 or any synthetically accessible combination thereof of up to 5 substituents or any pharmaceutically acceptable salt or hydrate thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy as dopamine β-hydroxylase inhibitors.

    摘要翻译： 化合物：其中n为0至5，R为氢或C 1-4烷基，X为氢，卤素，C 1-4烷基，CN，NO 2，SO 2 NH 2，COOH，CHO，OH，CH 2 OH，C 1-4烷氧基 ，CF3，SO2CH3，SO2CF3或CO2CaH2a + 1，其中a为1-5或其最多5个取代基的任何合成可及的组合或其任何药学上可接受的盐或水合物，其制备方法，含有它们的药物组合物及其在治疗中的用途 作为多巴胺β-羟化酶抑制剂。

    Prostaglandins
    18.
    发明公开
    Prostaglandins 失效
    前列腺素。

    公开(公告)号：EP0043292A2

    公开(公告)日：1982-01-06

    申请号：EP81303000.4

    申请日：1981-07-01

    申请人： NATIONAL RESEARCH DEVELOPMENT CORPORATION

    发明人： Jones, Robert Leslie ,  Wilson, Norman Happer

    IPC分类号： C07C177/00 ,  C07D493/08 ,  C07C175/00 ,  C07C109/12 ,  C07C109/14 ,  C07C109/16 ,  C07C133/02 ,  C07C159/00 ,  C07C143/825 ,  C07C131/00 ,  A61K31/557

    CPC分类号： C07D493/08 ,  C07C45/305 ,  C07C45/44 ,  C07C47/225 ,  C07C47/47 ,  C07C57/26 ,  C07C251/72 ,  C07C403/20 ,  C07C405/0041 ,  C07C405/0066 ,  C07C405/0091 ,  C07C2601/16 ,  C07C47/198

    摘要： Novel compounds have a formula (I)
    wherein
    represents a bicyclo (2,2,1) hept-2Z-ene, bicyclo (2,2,1) heptane, 7-oxabicyclo (2,2,1) hept-2Z-ene, 7-oxabicyclo (2,2,1) heptane, bicyclo (2,2,2) oct-2Z-ene or bicyclo (2,2,2) octane substituted at the 5-position by the group R 1 and at the 6-position by the group C(R 2 )=NR, a 6,6-dimethyl-bicyclo (3,1,1) heptane substituted at the 5- position by the group R' and at the 6-position by the group C(R 2 )=NR or at the 5-position by the group C(R 2 )=NR and at the 6-position by the group R 1 , a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R 1 and at the 5-position by the group C(R 2 )=NR, or a 1-hydroxycyclopentane substituted at the 2-position by the group R 1 and at the 2-position by the group C(R 2 )=NR, R 1 is a 6-carboxyhex-2-enyl group or a modification thereof as defined herein, R 2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, and R is a group -OR 3 , -OR 4 , -A-R 3 or -N=R 5 in which A is -NH-, -NH.CO-, -NH.CO.CH 2 N(R 6 )-, -NH.SO 2 -, -NH.CO.NH or -NH.CS.NH- and wherein R 3 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, R 4 is an aliphatic hydrocarbon group which is substituted through an oxygen atom by an aliphatic hydrocarbon group which is itself substituted by an aromatic group, R 5 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, and R 6 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, with the proviso that when R is a group -OR 3 , -NH.COR 3 or-NH.CO.NHR3 then
    excludes bicyclo (2,2,1) hept-2Z-enes and bicyclo (2,2,1) heptanes. The compounds are of value for use in phar. maceutical compositions particularly in the context of the inhibition of thromboxane activity.

    摘要翻译： 新化合物具有式（I）表示双环[2,2,1]庚-2Z-烯，双环[2,2,1]庚烷，7-氧杂双环[2,2,1]庚-2 - 烯基，7-氧杂二环[2,2,1]庚烷，双环[2,2,2]辛-2Z-烯或在5位被基团R 1取代的双环[2,2,2]辛烷 并且在C（R 2）= NR基团的6位上，在5位被基团R 1取代的6,6-二甲基 - 双环[3,1,1]庚烷和 在C（R 2）= NR的6位上或在C（R 2）= NR的5位，在6位被基团R 1取代， 环己-1-烯或环基在4-位上被基团R 1取代，在5-位被C（R 2）= NR取代，或在2-位取代的1-羟基环戊烷 通过基团R 1和基团C（R 2）= NR的2-位，R 1是如本文所定义的6-羧基己-2-烯基或其修饰， 2>是氢，脂族烃基或直接取代或通过氧或者-SO取代的脂族烃基 R为-OR 3，-OR 4，-AR 3或-N = R 5的基团，其中A为-NH-，-CH .CO- ，-NH.CO.CH 2 N（R 6） - ， - NHSO 2 - ， - NH.CO.NH或-NH.CS.NH-，并且其中R 3是脂族烃基，芳族基团 或通过芳族基团直接或通过氧或硫原子取代的脂族烃基，R 4是被本身被芳基取代的脂族烃基通过氧原子取代的脂族烃基，R 5是由芳基直接取代或通过氧或硫原子取代的脂肪族烃基，芳香族基团或脂肪族烃基，R 6是氢，脂肪族烃基，芳香族基团或脂肪族烃基 烃基直接或通过芳族基团通过氧或硫原子取代，条件是当R为基团-OR 3，-NHCOR 3或-NH.CO.NHR 3时， CHEM>不包括双环[2,2,1]庚-2Z-en es和双环[2,2,1]庚烷。 这些化合物在药物组合物中是有用的，特别是在抑制血栓素活性的情况下。