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    Bicyclo(2.2.1)heptane oximes
    15.
    发明授权
    Bicyclo(2.2.1)heptane oximes 失效
    双环（2.2.1）庚烷肟

    公开(公告)号：US4511737A

    公开(公告)日：1985-04-16

    申请号：US551941

    申请日：1983-11-15

    申请人： Zoltan Budai ,  Attila Kis-Tamas ,  Tibor Mezei ,  Aranka Lay ,  Zoltan Vigh ,  Agnes Sokorai

    发明人： Zoltan Budai ,  Attila Kis-Tamas ,  Tibor Mezei ,  Aranka Lay ,  Zoltan Vigh ,  Agnes Sokorai

    IPC分类号： A01N33/24 ,  A01N33/04 ,  A01N35/10 ,  A01P21/00 ,  C07C251/44 ,  C07C251/50 ,  C07C131/02

    CPC分类号： A01N35/10

    摘要： The invention relates to new bicyclo(2.2.1)heptane derivatives of the general formula I ##STR1## wherein R represents a C.sub.1-12 alkyl group optionally substituted by a lower alkoxy group, a C.sub.2-4 alkenyl group or a phenyl-(lower alkyl) group optionally substituted on (I), phenyl ring by one or more lower alkoxy groups or halogen atoms.The invention relates further to plant growth regulating compositions comprising as active agent 0.001 to 95% by weight of a racemic and/or optically active compound of the general formula I, wherein R has the above defined meanings, along with a conventional organic or inorganic, solid and/or liquid carrier and/or filler and/or diluent and/or surfactant.The invention encompasses also the preparation of the compounds of the general formula (I) which comprises reacting a racemic or optically active compound of the general formula (II) ##STR2## wherein Y is an oxygen or sulfur atom or an oxim group, with a compound of the general formula (III)R--XwhereinR is as defined above, andX represents a leaving group, preferably a halogen atom, a sulfonyloxy or an aminooxy group, with the proviso that when using a compound of the general formula (II), in which Y is an oxim group, X is other than aminooxy group,in the presence of a basic condensing agent, and optionally resolving the racemic compound of the general formula (I) obtained into its optically active antipodes.

    摘要翻译： 本发明涉及通式I（I）的新型双环（2.2.1）庚烷衍生物，其中R表示任选被低级烷氧基取代的C 1-12烷基，C 2-4链烯基或苯基 - （低级烷基）基团，其任选地在（I）上取代，苯基环由一个或多个低级烷氧基或卤素原子取代。 本发明进一步涉及植物生长调节组合物，其包含作为活性剂0.001至95重量％的通式I的外消旋和/或旋光活性化合物，其中R具有上述定义的含义，以及常规的有机或无机， 固体和/或液体载体和/或填料和/或稀释剂和/或表面活性剂。 本发明还包括通式（I）的化合物的制备，其包括使通式（II）的外消旋或光学活性化合物其中Y是氧或硫原子或肟基的（II） 与通式（III）RX的化合物，其中R如上定义，X​​表示离去基团，优选卤素原子，磺酰氧基或氨基氧基，条件是当使用通式 （II），其中Y是肟基，X不是氨基氧基，在碱性缩合剂的存在下，并且任选地将通式（I）的外消旋化合物拆分成其光学活性对映体。

    Process for the preparation of high purity perindopril and intermediates useful in the synthesis
    18.
    发明申请
    Process for the preparation of high purity perindopril and intermediates useful in the synthesis 有权
    制备高纯度培哚普利和合成中有用的中间体的方法

    公开(公告)号：US20050119492A1

    公开(公告)日：2005-06-02

    申请号：US10503272

    申请日：2003-01-29

    申请人： Guyla Simig ,  Tibor Mezei ,  Marta Porcs-Makkay ,  Attila Mandi

    发明人： Guyla Simig ,  Tibor Mezei ,  Marta Porcs-Makkay ,  Attila Mandi

    IPC分类号： A61K31/404 ,  A61P9/12 ,  A61P43/00 ,  C07D209/42 ,  A61K31/405

    CPC分类号： C07D209/42

    摘要： The invention relates to 1-{2(S)-[1(S)-(ethoxycarbonyl)butylamino]propionyl}-(3aS,7aS)octahydroindol-2(S)-carboxylic acid of the Formula I and the t-butylamine salt of the Formula I′ thereof free of contaminations derivable from dicyclohexyl carbodiimide, and a process for the preparation thereof. The invention also relates to new intermediates of the general Formula III (wherein R stands for lower alkyl or aryl lower alkyl). The compound of the Formula I—perindopril—is a known ACE inhibitor.

    摘要翻译： 本发明涉及式I的1- {2（S） - [1（S） - （乙氧基羰基）丁基氨基]丙酰基} - （3aS，7aS）八氢吲哚-2（S） - 羧酸和叔丁胺盐 式I'的化合物，其不含可衍生自二环己基碳二亚胺的污染物及其制备方法。 本发明还涉及通式III的新中间体（其中R代表低级烷基或芳基低级烷基）。 式I培哚普利的化合物是已知的ACE抑制剂。

    Bicyclo(2.2.1)heptane oximes used for plant growth regulating
    19.
    发明授权
    Bicyclo(2.2.1)heptane oximes used for plant growth regulating 失效
    用于植物生长调节的双环（2.2.1）庚烷肟

    公开(公告)号：US4425158A

    公开(公告)日：1984-01-10

    申请号：US322675

    申请日：1981-11-18

    申请人： Zoltan Budai ,  Attila Kis-Tamas ,  Tibor Mezei ,  Aranka Lay nee Konya ,  Zoltan Vigh ,  Agnes Sokorai nee Janki

    发明人： Zoltan Budai ,  Attila Kis-Tamas ,  Tibor Mezei ,  Aranka Lay nee Konya ,  Zoltan Vigh ,  Agnes Sokorai nee Janki

    IPC分类号： A01N33/24 ,  A01N33/04 ,  A01N35/10 ,  A01P21/00 ,  C07C251/44 ,  C07C251/50

    CPC分类号： A01N35/10

    摘要： The invention relates to new bicyclo(2.2.1)heptane derivatives of the general formula I ##STR1## wherein R represents a C.sub.1-12 alkyl group optionally substituted by a lower alkoxy group, a C.sub.2-4 alkenyl group or a phenyl-(lower alkyl) group optionally substituted on the phenyl ring by one or more lower alkoxy groups or halogen atoms.The invention relates further to plant growth regulating compositions comprising as active agent 0.001 to 95% by weight of a racemic and/or optically active compound of the general formula I, wherein R has the above defined meanings, along with a conventional organic or inorganic, solid and/or liquid carrier and/or filler and/or diluent and/or surfactant.The invention encompasses also the preparation of the compounds of the general formula I which comprises reacting a racemic or optically active compound of the general formula II ##STR2## wherein Y is an oxygen or sulfur atom or an oxim group, with a compund of the general formula IIIR - XwhereinR is as defined above, andX represents a leaving group, preferably a halogen atom, a sulfonyloxy or an aminooxy group, with the proviso that when using a compound of the general formula II, in which Y is an oxim group, X is other than aminooxy group,in the presence of a basic condensing agent, and optionally resolving the racemic compound of the general formula I obtained into its optically active antipodes.

    摘要翻译： 本发明涉及通式I的新的双环（2.2.1）庚烷衍生物，其中R表示任选被低级烷氧基，C 2-4链烯基或苯基 - （ 低级烷基）基团，其任选在苯环上被一个或多个低级烷氧基或卤素原子取代。 本发明进一步涉及植物生长调节组合物，其包含作为活性剂0.001至95重量％的通式I的外消旋和/或旋光活性化合物，其中R具有上述定义的含义，以及常规的有机或无机， 固体和/或液体载体和/或填料和/或稀释剂和/或表面活性剂。 本发明还包括通式I的化合物的制备，其包括使通式II的外消旋或旋光活性化合物其中Y是氧或硫原子或肟基，与下列化合物反应： 通式III R-X其中R如上定义，X​​表示离去基团，优选卤素原子，磺酰氧基或氨基氧基，条件是当使用通式II的化合物时，其中Y为 肟基，X不是氨基氧基，在碱性缩合剂的存在下，并且任选地将所得通式I的外消旋化合物拆分成其光学活性对映体。

    Novel oxime ethers
    20.
    发明授权
    Novel oxime ethers 失效
    新型肟醚

    公开(公告)号：US4077999A

    公开(公告)日：1978-03-07

    申请号：US749399

    申请日：1976-12-10

    申请人： Zoltan Budai ,  Aranka Lay nee Konya ,  Tibor Mezei ,  Katalin Grasser ,  Eniko Szirt nee Kiszelly ,  Ibolya Kosoczky ,  Lujza E. Petocz

    发明人： Zoltan Budai ,  Aranka Lay nee Konya ,  Tibor Mezei ,  Katalin Grasser ,  Eniko Szirt nee Kiszelly ,  Ibolya Kosoczky ,  Lujza E. Petocz

    IPC分类号： C07C251/58 ,  C07D295/088 ,  C07C131/02 ,  C07C131/04

    CPC分类号： C07D295/088 ,  C07C251/58 ,  C07C2101/08 ,  C07C2101/16 ,  C07C2101/18

    摘要： The invention relates to novel oxime ethers of the formula I ##STR1## wherein R stands for a phenyl group which may be substituted by a halogen atom or by one or more C.sub.1 -C.sub.4 alkoxy, hydroxyl, nitro or di(C.sub.1 -C.sub.3 alkyl)amino groups,R.sup.1 and R.sup.2 denote each a hydrogen atom or together a valence bond,A denotes a C.sub.2 -C.sub.4 straight or branched-chain alkylene group,N denotes an integer from 3 to 10, andR.sup.3 and R.sup.4 denote a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, furthermore to acid addition salts and quaternary ammonium salts thereof. These new compounds are biologically active, and possess primarily local analgesic, spasmolytic, nicotine-lethality inhibiting, tetrabenazine-antagonistic and tetra-cor-spasm inhibiting effects.

    摘要翻译： 本发明涉及式I（I）的新型肟醚，其中R代表可被卤素原子取代的苯基或一个或多个C 1 -C 4烷氧基，羟基，硝基或二（C1- C 3烷基）氨基，R 1和R 2各自表示氢原子或价键一起，A表示C 2 -C 4直链或支链亚烷基，N DENOTES AN INTEGER为3〜10，R 3和R 4表示氢 原子或C1-C4烷基，此外还涉及其酸加成盐和季铵盐。 这些新化合物具有生物活性，主要具有局部镇痛，解痉，尼古丁致死抑制，四苯并嗪拮抗和四痉挛抑制作用。