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    • 5. 发明授权
    • Method for production of pyrrolidinone derivatives
    • 吡咯烷酮衍生物的制备方法
    • US06207825B1
    • 2001-03-27
    • US09190297
    • 1998-11-13
    • Hajime IizukaHiroshi NagaseNaruyoshi Mita
    • Hajime IizukaHiroshi NagaseNaruyoshi Mita
    • C07D40106
    • C07D207/277
    • A compound represented by the following formula (12) useful as an intermediate for production of drug or agricultural chemical: (wherein R21 to R25 are each independently a hydrogen atom, a hydroxyl group, a halogen atom, an alkyl group of 1 to 4 carbon atoms, an alkoxy group of 1 to 4 carbon atoms, a perfluoroalkyl group of 1 to 4 carbon atoms, a cyano group, a nitro group, an amino group, a carboxyl group, a thiol group, an alkylthio group of 1 to 4 carbon atoms or a carbamoyl group) can be produced by reacting a compound represented by the formula (13): (wherein R21 to R25 have the same definitions as given above) with 1,1-cyclopropanedicarboxylic acid. The compound of the formula (12) is useful as a raw material for production of a pyrrolidinone compound useful as an active ingredient of drug.
    • 由下式(12)表示的化合物可用作药物或农药的生产中间体:(其中R21至R25各自独立地为氢原子,羟基,卤素原子,1-4个碳原子的烷基 1〜4个碳原子的烷氧基,1〜4个碳原子的全氟烷基,氰基,硝基,氨基,羧基,硫醇基,1〜4个碳的烷硫基 原子或氨基甲酰基)可以通过使式(13)表示的化合物(其中R21至R25具有与上述相同的定义)与1,1-环丙烷二羧酸反应来制备。 式(12)的化合物可用作生产用作药物活性成分的吡咯烷酮化合物的原料。
    • 8. 发明授权
    • Pyridazinone derivatives
    • 哒嗪酮衍生物
    • US4639451A
    • 1987-01-27
    • US504039
    • 1983-06-03
    • Tsutomu KatakamiNobuyuki FukazawaHajime IizukaTakashi NishinaJoji KamiyaYasuhito TanakaTakuo Nakano
    • Tsutomu KatakamiNobuyuki FukazawaHajime IizukaTakashi NishinaJoji KamiyaYasuhito TanakaTakuo Nakano
    • C07D237/04C07D401/12C07D403/12C07D405/12C07D409/12A61K31/50
    • C07D401/12C07D237/04C07D403/12C07D405/12C07D409/12
    • This invention relates to pyridazinone derivatives of the general formula: ##STR1## [wherein R.sup.1 stands for a hydrogen atom or a lower alkyl group; R.sup.2 for a hydrogen atom or a lower alkyl group; and A for (i) a ring selected from a benzene ring, a furan ring, a thiophene ring and a pyridine ring (on which ring 1-3 substituents or atoms selected from amino groups, nitro groups, lower alkanoylamino groups, hydroxyl groups, lower alkanoyloxy groups, sulfamoyl groups and halogen atoms may be present), or (ii) a grouping of the formula: ##STR2## (wherein R.sup.3 stands for a hydrogen atom, a lower alkyl group, a phenyl(lower)alkyl, a hydroxyphenyl(lower)alkyl group, a lower alkylmercapto(lower)alkyl group, a benzylmercapto(lower)alkyl group, a guanidino(lower)alkyl group, a nitroguanidino(lower)alkyl group, an indolyl(lower)alkyl group, a carbamoyl(lower)alkyl group or a carboxy(lower)alkyl group, R.sup.4 for a hydrogen atom or a lower alkyl group, R.sup.5 for a hydrogen atom, a lower alkyl group, a lower alkanoyl group, a benzoyl or a benzyloxycarbonyl group, and R.sup.3 and R.sup.4 may be combined to form a grouping of the formula: ##STR3## which forms a ring), or (iii) a grouping of the formula: ##STR4## (wherein R.sup.6, R.sup.7 and R.sup.8 each stand for a hydrogen atom or a lower alkyl group, B is an oxygen atom or a sulfur atom, R.sup.9 stands for a hydrogen atom or a lower alkanoyl group, and n is 0 or 1)].
    • PCT No.PCT / JP82 / 00415 Sec。 371日期:1983年6月3日 102(e)日期1983年6月3日PCT提交1982年10月20日PCT公布。 第WO83 / 01447号公报 日本1983年4月28日。本发明涉及以下通式的哒嗪酮衍生物:其中R1代表氢原子或低级烷基; R2为氢原子或低级烷基; A为(i)选自苯环,呋喃环,噻吩环和吡啶环的环(其中1-3个取代基或选自氨基,硝基,低级烷酰基氨基,羟基, 低级烷酰氧基,氨磺酰基和卤素原子可以存在),或(ii)下式的基团:其中R3代表氢原子,低级烷基,苯基(低级)烷基,羟基苯基 (低级)烷基,低级烷基巯基(低级)烷基,苄基巯基(低级)烷基,胍基(低级)烷基,硝基胍基(低级)烷基,吲哚基(低级)烷基,氨基甲酰基 低级)烷基或羧基(低级)烷基,R4表示氢原子或低级烷基,R5表示氢原子,低级烷基,低级链烷酰基,苯甲酰基或苄氧基羰基,R3和 R4可以组合以形成下式的分组:形成环的),或(iii)下式的分组:( 其中R6,R7和R8各自代表氢原子或低级烷基,B是氧原子或硫原子,R9代表氢原子或低级烷酰基,n是0或1)]。