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    • 36. 发明公开
    • Prostaglandins
    • 前列腺素。
    • EP0043292A2
    • 1982-01-06
    • EP81303000.4
    • 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。
    • 37. 发明公开
    • Pesticidal tetrazines, their use and compositions, processes for their preparation and preparation intermediates
    • 四嗪杀虫剂,它们的用途和组合物,它们的制备方法和中间体及其制备方法。
    • EP0029657A2
    • 1981-06-03
    • EP80303728.2
    • 1980-10-22
    • FBC LIMITED
    • Parsons, John HenryWest, Peter John
    • C07D257/08C07C109/04C07C109/10C07C109/16C07D285/12A01N43/64
    • C07D285/12A01N43/713C07C243/36C07C243/38C07C251/72C07C2601/14C07C2601/16C07D257/08
    • The tetrazines and dihydrotetrazines of the formula:
      oroftheformula:
      wherein R 1 , R 2 and R', which may be the same or different, each represent hydrogen, phenyl, alkyl of 1 to 6 carbon atoms, or alkenyl or alkynyl of 3 to 6 carbon atoms, each of which may be unsubstituted or substituted by one or more halogen atoms, hydroxy groups, cyano groups, carboxy groups, alkoxycarbonyl groups of 2 to 5 carbon atoms or alkoxy groups of 1 to 4 carbon atoms; or R' and R' together represent a single bond; Hal represents fluorine, chlorine, bromine or iodine; and R 3 represents 2-iodophenyl, 2,5-dihalophenyl, 2-methylthiophenyl, cyclohexyl, cyclohexylalkyl, cyclohexenyl, cyclohexadienyl, 1-naphthyl, 2-naphthyl or biphenylyl, each of the cyclohexyl, cyclohexenyl, cyclohexadienyl, naphthyl or biphenylyl moieties of which may be unsubstituted to substituted by one or more alkyl, alkoxy or alkylthio groups of 1 to 6 carbon atoms, hydroxy, mercapto or cyano groups, halogen atoms, alkanoyloxy groups of 2 to 6 carbon atoms, amino or phenylamino groups, or alkylamino or dialkylamino groups, each alkyl moiety of which is of 1 to 6 carbon atoms, are effective to combat pests, particularly acarids and their eggs.
      The compounds are new and processes for their preparation are described.
    • 式的四嗪和dihydrotetrazines: worin - [R <1>,R <2>和R <4>,其可以是相同或不同的,各自代表氢,苯基,1至6个碳原子的烷基,或 链烯基或3-6个碳原子的炔基,其中的每一个可以是unsubstituiertem或由一个或多个卤素原子,羟基基团,氰基,羧基,烷氧基羰基的2-5个碳原子或1至4碳烷氧基的基团取代 原子; 或R <1>和R <2>一起代表单键; 哈尔darstellt氟,氯,溴或碘; 且R <3> darstellt 2-碘苯基,2,5-二卤代苯基,2-甲硫基苯基,环己基,亚环己基,环己环己二烯基,1- napnthyl,2-萘基或联苯基,每个环己基,环己烯基,环己二烯基,萘基或联苯基的 其中的部分可以是unsubstituiertem被一个或多个烷基,烷氧基或1〜6个碳原子,羟基,巯基或氰基,卤原子,2〜6个碳原子,氨基或苯基氨基,或烷酰氧基烷硫基到substituiertem 烷基氨基或二烷基氨基,所有的每个烷基部分是1〜6个碳原子,是有效对抗害虫,特别是螨和它们的卵。 化合物是新的和它们的制备方法进行说明。