利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

88 条记录 (耗时 0.017 秒)

    Bicyclo(2.2.1)heptane oximes used for plant growth regulating
    1.
    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。

    1,4;3,6-Dianhydro-2,5-diazido-2,5-dideoxy-hexitols
    4.
    发明授权
    1,4;3,6-Dianhydro-2,5-diazido-2,5-dideoxy-hexitols 失效
    1,4; 3,6-二氢-2,5-二叠氮基-2,5-二脱氧 - 己醇

    公开(公告)号：US4332818A

    公开(公告)日：1982-06-01

    申请号：US242709

    申请日：1981-03-11

    申请人： Janos Kuszmann ,  Gabor Medgyes ,  Ferenc Andrasy ,  Pal Berzsenyi

    发明人： Janos Kuszmann ,  Gabor Medgyes ,  Ferenc Andrasy ,  Pal Berzsenyi

    IPC分类号： A61K31/34 ,  A61K31/70 ,  A61P25/20 ,  C07D307/22 ,  C07D317/14 ,  C07D317/24 ,  C07D317/28 ,  C07D493/04

    CPC分类号： C07D493/04 ,  C07C247/00 ,  C07D317/14 ,  C07D317/24 ,  C07D317/28

    摘要： The invention relates to new stereoisomeric 1,4;3,6-dianhydro-2,5-diazido-2,5-dideoxy-hexitols of the Formula I.These compounds can be prepared by(a) reacting a hexitol derivative of the general Formula II /wherein R is a mesyl or tosyl group/ in an aqueous or anhydrous organic solvent with an alkali metal azide or ammonium azide; or(b) mesylating or tosylating a compound of the Formula III and treating the mixed ester of the general Formula IV thus obtained /wherein R is as stated above/ with a base; or(c) subjecting a compound of the Formula III to debenzoylation and subsequently to partial esterification and treating the compound of the general Formula V thus obtained /wherein R is as stated above/ with a base.The new compounds of the Formula I possess valuable hypnotic properties and can be used in therapy. ##STR1##

    摘要翻译： 本发明涉及式I的新的立体异构体1,4,3,6-二脱氢-2,5-二叠氮基-2,5-二脱氧 - 己醇。这些化合物可以通过以下步骤制备：（a）将一般的己糖醇衍生物 式II其中R是甲磺酰基或甲苯磺酰基，在含有碱金属叠氮化物或叠氮化铵的水性或无水有机溶剂中; 或（b）将式III化合物甲磺酰化或甲苯磺酸化，并将所得通式IV的混合酯/其中R如上所述/与碱反应; 或（c）使式III化合物进行脱苯甲酰化，然后将由此获得的通式V化合物进行部分酯化和处理，其中R如上所述/与碱反应。 式I的新化合物具有宝贵的催眠特性，可用于治疗。 公式 [I] [II]

    Process for the preparation of 1-[3-mercapto-(2S)-methylpropionyl]-pyrrolidine-(2S)-carboxylic acid
    5.
    发明授权
    Process for the preparation of 1-[3-mercapto-(2S)-methylpropionyl]-pyrrolidine-(2S)-carboxylic acid 失效
    制备1- [3-巯基 - （2S） - 甲基丙酰基] - 吡咯烷 - （2S） - 羧酸的方法

    公开(公告)号：US4332725A

    公开(公告)日：1982-06-01

    申请号：US218814

    申请日：1980-12-22

    申请人： Janos Fischer ,  Laszlo Rozsa ,  Pal Vago ,  Anna Bakonyi ,  Gabor Fazekas

    发明人： Janos Fischer ,  Laszlo Rozsa ,  Pal Vago ,  Anna Bakonyi ,  Gabor Fazekas

    IPC分类号： A61K31/40 ,  A61K31/401 ,  A61P9/12 ,  C07C53/19 ,  C07C53/50 ,  C07D207/16

    CPC分类号： C07D207/16 ,  C07C53/19 ,  C07C53/50

    摘要： The invention relates to a novel process for the preparation of 1-[3-mercapto-(2S)-methylpropionyl]-pyrrolidine-(2S)-carboxylic acid through the N-acylation of L-proline.According to the process of the invention L-proline is acylated with a 3-halogen-2-methylpropionyl chloride of the formula III ##STR1## wherein Hal is a halogen atom, preferably chlorine or bromine, the obtained 1-[3-halogen-(2S)-methylpropionyl]-pyrrolidine-(2S)-carboxylic acid, wherein Hal is as stated above, is reacted with an alkali thiosulfate or alkali trithiocarbonate and the reaction product is hydrolized with an acid.The process of the invention is very economical as compared with the known processes. The desired product is prepared from methacrylic acid in 4 reaction steps with a total yield of 25 percent and from L-proline in 2 reaction steps with a total yield of 30 percent.

    摘要翻译： 本发明涉及通过L-脯氨酸的N-酰化制备1- [3-巯基 - （2S） - 甲基丙酰基] - 吡咯烷 - （2S） - 羧酸的新方法。 根据本发明的方法，L-脯氨酸用式III III的3-卤素-2-甲基丙酰氯酰化，其中Hal是卤素原子，优选氯或溴，得到的1- [3-卤素 - （2S） - 甲基丙酰基] - 吡咯烷 - （2S） - 羧酸（其中Hal如上所述）与碱金属硫代硫酸盐或碱式三硫代碳酸酯反应，反应产物用酸水解。 与已知方法相比，本发明的方法是非常经济的。 所需产物由甲基丙烯酸在4个反应步骤中制备，总产率为25％，在2个反应步骤中由L-脯氨酸制备，总产率为30％。

    Pyrido[2,3-e]-as-triazine derivatives and pharmaceutical compositions
    6.
    发明授权
    Pyrido[2,3-e]-as-triazine derivatives and pharmaceutical compositions 失效
    吡啶并[2,3-e] -as-三嗪衍生物和药物组合物

    公开(公告)号：US4324786A

    公开(公告)日：1982-04-13

    申请号：US143778

    申请日：1980-04-25

    申请人： Andras Messmer ,  Pal Benko ,  Gyorgy Hajos ,  Lujza Petocz ,  Ibolya Kosoczky ,  Peter Gorog

    发明人： Andras Messmer ,  Pal Benko ,  Gyorgy Hajos ,  Lujza Petocz ,  Ibolya Kosoczky ,  Peter Gorog

    IPC分类号： A61K31/53 ,  A61K31/535 ,  A61P25/00 ,  A61P25/04 ,  A61P25/20 ,  A61P29/00 ,  C07D221/04 ,  C07D253/10 ,  C07D471/04 ,  C07D471/14

    CPC分类号： C07D471/04

    摘要： New pyrido[2,3-e]-as-triazine derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each stand for a C.sub.1-20 alkylcarbonyl, halogenated (C.sub.1-4 alkyl)-carbonyl, C.sub.1-4 alkoxycarbonyl, benzoyl, phenyl-(C.sub.1-4 alkyl)-carbonyl or phenyl-(C.sub.2-4 alkenyl)-carbonyl group or a 5-10-membered mono- or bicyclic nitrogen-containing heterocyclic acid residue (preferably a pyridylcarbonyl group) containing optionally one or more additional nitrogen, oxygen and/or sulfur atoms in the heterocyclic ring, and optionally one or more identical or different substituents selected from the group consisting of halogen, C.sub.1-4 alkoxy, nitro and hydroxy are attached to the aromatic or heterocyclic rings, furthermore one of R.sup.1 and R.sup.2 may also stand for hydrogen atom, orR.sup.1 and R.sup.2 may form, together with the adjacent nitrogen atoms, a pyrazole-2,4 ring having optionally a C.sub.1-6 alkyl substituent in position 3, andR.sup.3 stands for hydrogen, halogen, C.sub.1-4 alkoxy, amino, mono-(C.sub.1-6 alkyl)-amino, di-(C.sub.1-6 alkyl)-amino, hydroxy, alkylated or acylated hydroxy, morpholino, piperazino, N-(C.sub.1-6 alkyl)-piperazino, N-benzylpiperazino or N-pyridylpiperazino group,and pharmaceutically acceptable acid addition salts thereof are prepared by acylating the respective 1,2-unsubstituted 1,2-dihydro-pyrido[2,3-e]-as-triazine derivatives.The new compounds according to the invention act on the central nervous system and exert sedative, analgesic, narcosis potentiating, tetrabenazine antagonizing and antiphlogistic effects. The new compounds according to the invention can be applied to advantage in the therapy.

    摘要翻译： 通式（I）的新的吡啶并[2,3-e] -as-三嗪衍生物，其中R 1和R 2各自代表C 1-20烷基羰基，卤代（C 1-4烷基） - 羰基 ，C 1-4烷氧基羰基，苯甲酰基，苯基 - （C 1-4烷基） - 羰基或苯基 - （C 2-4烯基） - 羰基或5-10元单环或双环含氮杂环酸残基（优选 含有任选的一个或多个杂环中的一个或多个另外的氮，氧和/或硫原子，以及任选地一个或多个相同或不同的选自卤素，C 1-4烷氧基，硝基和羟基的取代基被连接到 芳族或杂环，此外，R 1和R 2中的一个也可以代表氢原子，或者R 1和R 2可以与相邻的氮原子一起形成具有任选地C 1-6烷基取代基的吡唑-2,4环的位置 3，R3代表氢，卤素，C1-4烷氧基，氨基，单 - （C1-6烷基） - 氨基，二 - （C1-6烷基） - 氨 羟基，烷基化或酰化羟基，吗啉代，哌嗪子基，N-（C 1-6烷基） - 哌嗪基，N-苄基哌嗪子基或N-吡啶基哌嗪子基及其药学上可接受的酸加成盐， 未取代的1,2-二氢 - 吡啶并[2,3-e] -as-三嗪衍生物。 根据本发明的新化合物作用于中枢神经系统，并施加镇静，止痛，麻醉增强，丁苯那嗪拮抗和消炎作用。 根据本发明的新化合物可以在治疗中有利地应用。

    1-Phenyl-2-amino-1,3-propanediol-N-aryloxyalkyl derivatives
    7.
    发明授权
    1-Phenyl-2-amino-1,3-propanediol-N-aryloxyalkyl derivatives 失效
    1-苯基-2-氨基-1,3-丙二醇-N-芳氧基烷基衍生物

    公开(公告)号：US4259257A

    公开(公告)日：1981-03-31

    申请号：US73563

    申请日：1979-09-07

    申请人： Laszlo Levai ,  Gabor Fazekas ,  Lujza Petocz ,  Katalin Grasser

    发明人： Laszlo Levai ,  Gabor Fazekas ,  Lujza Petocz ,  Katalin Grasser

    IPC分类号： A61K31/135 ,  A61K20060101 ,  A61K31/13 ,  A61K31/137 ,  A61P11/04 ,  A61P21/00 ,  A61P23/02 ,  A61P25/00 ,  A61P25/02 ,  A61P29/00 ,  B01J23/00 ,  B01J23/40 ,  B01J25/00 ,  C07B61/00 ,  C07C20060101 ,  C07C67/00 ,  C07C213/00 ,  C07C215/36 ,  C07C93/06

    CPC分类号： C07C51/353

    摘要： The invention relates to novel 1-phenyl-2-amino-1,3-propanediol-N-alkyl derivatives having the general formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl having from 1 to 8 carbon atoms or phenoxymethyl, andR.sub.2 is hydrogen, alkyl having from 1 to 8 carbon atoms or 2,2-diphenylethyl,with the proviso that if R.sub.1 is phenoxymethyl then R.sub.2 may stand only for methyl, and if R.sub.2 is 2,2-diphenylethyl then R.sub.1 may stand only for hydrogen, and its isomers and pharmaceutically acceptable salts. Furthermore, the invention relates to a process for preparing these compounds.The novel 1-phenyl-2-amino-1,3-propanediol-N-alkyl derivatives having the general formula I possess significant anti-anginose activity and show several other biological activities.

    摘要翻译： 本发明涉及具有通式I（I）的新颖的1-苯基-2-氨基-1,3-丙二醇-N-烷基衍生物，其中R 1是氢，具有1至8个碳原子的烷基或苯氧基甲基， 并且R 2是氢，具有1至8个碳原子的烷基或2,2-二苯基乙基，条件是如果R 1是苯氧基甲基，那么R 2可以仅仅是甲基，并且如果R 2是2,2-二苯基乙基，那么R 1可以仅仅是 氢及其异构体和药学上可接受的盐。 此外，本发明涉及一种制备这些化合物的方法。 具有通式I的新型1-苯基-2-氨基-1,3-丙二醇-N-烷基衍生物具有显着的抗焦虑作用，并显示出其它几种生物活性。

    Process of and equipment for the analysis of liquid samples by titration
    8.
    发明授权
    Process of and equipment for the analysis of liquid samples by titration 失效
    通过滴定分析液体样品的过程和设备

    公开(公告)号：US4120657A

    公开(公告)日：1978-10-17

    申请号：US788540

    申请日：1977-04-18

    申请人： Geza Nagy ,  Erno Pungor ,  Klara Toth ,  Jeno Havas ,  Zsofia Feher

    发明人： Geza Nagy ,  Erno Pungor ,  Klara Toth ,  Jeno Havas ,  Zsofia Feher

    IPC分类号： G01N27/26 ,  G01N27/44 ,  G01N31/16 ,  G01N33/18 ,  B01K3/00

    CPC分类号： G01N31/166 ,  Y10T436/117497 ,  Y10T436/193333 ,  Y10T436/203332

    摘要： The invention relates to a process of and equipment for a selective, quick and accurate analysis of liquid samples. According to the process of the invention a liquid or a gas sample absorbed by a liquid is allowed to flow at a constant volume rate and overtitrated with an amount of a reagent adequate to the measurement in a definite time. Then the flow of the reagent is decreased to zero in a definite time, meanwhile continuously following, in a known way, the changes occurring in the reaction mixture. The determination of the concentration is carried out by comparing the time elapsed between the appearances of the two chemical equivalence points with calibration curves prepared with standard solutions, said time having a well defined functional relationship with the concentration of the sample.The equipment according to the invention for carryinng out the process according to the invention contains an analysis channel in contact with a sample-storage tank or liquid storage tank or sampling device or liquid feeding device, said analysis channel comprising a gas-permeable membrane contacting a sample gas before the titration section if desired, said analysis channel being equipped with a pump, said analysis channel having a titration section comprising a small-volume flowthrough homogenizing space and a reagent feeder or reagent generator device coupled to a programming unit and joining said channel before the said homogenizing space. For the measurement and recording of changes occurring in time, said analysis channel has, in its section between said homogenizing space and the suitably shaped effluent section, a detector section containing one or more detectors and a recording and/or indicator unit; if desired, said analysis channel has an electronic signal processing unit coupled to the recording and/or indicator unit and to the programming unit.The accuracy of analyses carried out by the process and equipment according to the invention is identical with or higher than that of automatic titrators, and its velocity is identical with that of measurements carried out by flowthrough analysis channels, combining in this way all the advantages of both methods and measuring instruments.

    摘要翻译： 本发明涉及用于液体样品选择性，快速和准确分析的方法和设备。 根据本发明的方法，允许液体或气体样品被液体吸收，以恒定的体积速率流动，并在一定时间内用足够量的试剂进行过量滴定。 然后试剂的流动在一定时间内降至零，同时以已知的方式连续跟随反应混合物中发生的变化。 通过将两个化学当量点的出现时间与标准溶液制备的校准曲线进行比较，进行浓度测定，所述时间与样品浓度具有明确的功能关系。

    Novel oxime ethers
    9.
    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。