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    • 71. 发明公开
    • Prostaglandins
    • 前列腺素
    • EP0043292A3
    • 1982-12-15
    • EP81303000
    • 1981-07-01
    • NATIONAL RESEARCH DEVELOPMENT CORPORATION
    • Jones, Robert LeslieWilson, Norman Happer
    • C07C177/00C07D493/08C07C175/00C07C109/12C07C109/14C07C109/16C07C133/02C07C159/00C07C143/825C07C131/00A61K31/557
    • C07D493/08C07C45/305C07C45/44C07C47/225C07C47/47C07C57/26C07C251/72C07C403/20C07C405/0041C07C405/0066C07C405/0091C07C2601/16C07C47/198
    • 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.
    • 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基的6-位上或在C(R 2)= NR基的5位,在6位由基团R 1取代,a 环己-1-烯或环己基在4-位被基团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,脂族烃基或脂族烃基直接或通过氧或磺取代 R 1是-OR 3,-OR 4,-AR 3或-N = R 5,其中A是-NH-,-CH.CO- ,-NH.CO.CH 2 N(R 6) - , - NHS 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是脂族烃基,其被本身被芳基取代的脂族烃基经氧原子取代,R 5是脂肪族烃基,芳香族基团或脂肪族烃基,其被芳基直接或者被氧原子或硫原子取代,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。