4-AMINO-1,5-SUBSTITUTED 1,5-DIHYDRO-IMIDAZOL-2-ONES
    4.
    发明公开
    4-AMINO-1,5-SUBSTITUTED 1,5-DIHYDRO-IMIDAZOL-2-ONES 审中-公开
    4-氨基-1,5-取代的1,5-二氢 - 咪唑-2-酮

    公开(公告)号:EP1994009A1

    公开(公告)日:2008-11-26

    申请号:EP07726523.9

    申请日:2007-02-27

    CPC分类号: C07D233/92

    摘要: The present invention relates to compounds of the general formula wherein R1 is -(CH2)n-aryl or -(CH2)n-heteroaryl, wherein such groups are unsubstituted or substituted by one or more substituents, selected from the group consisting of halogen, lower alkyl substituted by halogen, lower alkoxy, lower alkyl, cyano, nitro, -O-lower alkyl substituted by halogen or morpholinyl; R2 is -(CH2)n-aryl or -(CH2)n-heteroaryl, wherein such groups are unsubstituted or substituted by one or more substituents, selected from the group consisting of lower alkyl, lower alkoxy, halogen or -N(lower alkyl)2; R3 is hydrogen or lower alkyl; R4 is -(CH2)n-aryl or -(CH2)n-heteroaryl, wherein such groups are unsubstituted or substituted by one or more substituents, selected from the group consisting of halogen or lower alkoxy, or is lower alkyl, -(CH2)n-cycloalkyl; or R3 and R4 form together with the N-atom a heterocyclic ring; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been found that the compounds of general formula I or their tautomeric forms are good inhibitors of the glycine transporter 1 (GIyT-1), and that they have a good selectivity to glycine transporter 2 (GIyT-2) inhibitors, useful for the treatment of schizophrenia.

    METHOD FOR PRODUCING 4-NITROIMIDAZOLE COMPOUND
    5.
    发明授权
    METHOD FOR PRODUCING 4-NITROIMIDAZOLE COMPOUND 有权
    制造方法4-硝基咪唑

    公开(公告)号:EP1720838B1

    公开(公告)日:2007-07-04

    申请号:EP05710450.7

    申请日:2005-02-15

    发明人: SHINHAMA, Koichi

    IPC分类号: C07D233/92

    CPC分类号: C07D233/92

    摘要: The present invention provides a method for producing a 4-nitroimidazole compound represented by general formula (1) at high yield and at high purity by a safe method causing few dangers such as explosion. The production method of the present invention comprises iodinating a 4-nitroimidazole compound represented by general formula (2): wherein each of X1 and X2 represents a chlorine atom or bromine atom, and then reducing the obtained 5-iodo-4-nitroimidazole compound represented by general formula (3): wherein X2 is the same as defined above.

    Imidazoles and their compositions for plant growth regulation
    9.
    发明公开
    Imidazoles and their compositions for plant growth regulation 失效
    咪唑和ren ren Zusammensetzungen zur Regelung des Pflanzenwachstums。

    公开(公告)号:EP0269238A1

    公开(公告)日:1988-06-01

    申请号:EP87309141.7

    申请日:1987-10-15

    CPC分类号: C07D233/90 A01N43/50

    摘要: The invention provides a method of regulating the growth of a plant using a compound of the formula:
    wherein R¹ represents alkyl or phenyl optionally substituted by halogen, alkyl, alkoxy, alkylthio, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, nitro, cyano, amino, carboxy, phenoxy, benzyloxy, alkoxycarbonyl, alkylamino, dialkylamino, alkanoylamino, R² represents nitro, cyano, carbamoyl or -CONR⁵R⁶ or -NR⁶COR⁵ (wherein R⁵ is as hereinbefore defined for R¹ and R⁶ represents hydrogen or alkyl), R³ represents halogen, nitro, cyano, amino, carbamoyl, -CONR⁷R⁸ (wherein R⁷ is as hereinbefore defined for R¹ and R⁸ represents hydrogen or alkyl), and R⁴ represents hydrogen or alkyl, or salts thereof with the exclusion of compounds in which R² and R³ simultaneously represent cyano groups; plant-growth regulating compositions, novel compounds and their preparation are described.

    摘要翻译: 本发明提供了使用下式化合物调节植物生长的方法:其中R 1表示任选被卤素,烷基,烷氧基,烷硫基,三氟甲基,三氟甲氧基,三氟甲硫基,硝基, 氰基,氨基,羧基,苯氧基,苄氧基,烷氧基羰基,烷基氨基,二烷基氨基,烷酰基氨基,R 2表示硝基,氰基,氨基甲酰基或-CONR 5 R 6或-NR 6 COR 5 R 5如上文定义,R 1和R 6代表氢或烷基),R 3表示卤素,硝基,氰基,氨基,氨基甲酰基,-CONR 7 R 8(其中 R 7如上文定义,R 1和R 8表示氢或烷基),R 4表示氢或烷基,或其盐,排除其中R 2和R 2的化合物 3同时表示氰基; 描述了植物生长调节组合物,新化合物及其制备方法。

    Procédé de préparation du méthylnitroimidazole
    10.
    发明公开
    Procédé de préparation du méthylnitroimidazole 失效
    Verfahren zur Herstellung von Methylnitro咪唑。

    公开(公告)号:EP0247954A1

    公开(公告)日:1987-12-02

    申请号:EP87420139.5

    申请日:1987-05-20

    发明人: Desbois, Michel

    IPC分类号: C07D233/92

    CPC分类号: C07D233/92

    摘要: La présente invention concerne un nouveau procédé de préparation de méthylnitroimidazole par mise en contact au sein de l'acide flurohydrique de méthylimidazole et d'un agent nitrant.

    摘要翻译: 通过使甲基咪唑与氢氟酸中的硝化剂接触来制备甲基硝基咪唑。