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11.发明申请
公开(公告)号：WO1986004216A1
公开(公告)日：1986-07-31
申请号：PCT/HU1986000004
申请日：1986-01-16
Applicant: CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA ... , HIDASI, György , SZÉKELY, István , BERTOK, Béla , ZOLTAN, Sándor , NAGY, Lajos , GAJARI, Antal , SOMFAI, Éva , HEGEDÜS, Agnes , PAP, László , SOOS, Rudolf , RADVANY, Erzsébet , BOTAR, Sándor , SZABOLCSI, Tamás
IPC: A01N53/00
CPC classification number: A01N53/00 , A01N2300/00
Abstract: A synergistic insecticidal composition containing more than one active ingredients and being harmless to environment characterized by comprising in an amount of from 0.001 to 99% by weight a synthetic pyrethroide of the formula (I) - namely substantially only the 1RtransS and 1StransR enantiomer-pair (Ib) out from the possible eight isomers - optionally in admixture with an amount of up to 100% by weight of one or more activator(s) and auxiliary agent(s), particularly antioxidants, stabilising agents, wetting agents, emulsifying agents, dispersing agents, antifoam agents, diluents and/or fillers. The enantiomer-pair Ib consisting of the 1RtransS and 1StransR isomers is new and the invention also relates to the said new enantiomer-pair and a process for the preparation thereof. The advantage of the insecticidal composition of the present invention is that it is less toxical towards warm-blooded animals and useful parasites and is therefore much less harmful to the environment.
Abstract translation: 一种含有多于一种活性成分并且对环境无害的协同杀虫组合物，其特征在于其含量为0.001至99重量％的式（I）的合成拟除虫菊酯，即基本上仅为1RtransS和1StransR对映异构体对（ Ib）可能的八种异构体 - 任选地与至多100重量％的一种或多种活化剂和辅助剂，特别是抗氧化剂，稳定剂，润湿剂，乳化剂，分散剂 试剂，消泡剂，稀释剂和/或填料。 由1RtransS和1StransR异构体组成的对映体对1b是新的，本发明还涉及所述新的对映异构体对及其制备方法。 本发明的杀虫组合物的优点在于对温血动物和有用寄生虫的毒性较小，因此对环境的危害较小。
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Patent Agency Ranking12.发明申请AN IMPROVED PROCESS FOR THE PREPARATION OF SUBSTITUTED ISOFLAVONE DERIVATIVES 审中-公开制备取代的异佛尔酮衍生物的改进方法
公开(公告)号：WO1991015483A1
公开(公告)日：1991-10-17
申请号：PCT/HU1990000023
申请日：1990-04-06
Applicant: CHINOIN GYOGYSZER- ÉS VEGYÉSZETI TERMÉKEK GYARA ... , KALLAY, Tamás , LANYI, György , LEDNICZKY, László , IMREI, Lajos , HOFFMANN, György , SZILADI, Mária , SOMFAI, Éva , MONTAY, Tibor
IPC: C07D311/36
CPC classification number: C07D311/36
Abstract: The invention relates to a process for the preparation of pure isoflavone derivatives of general formula (I), wherein R stands for hydrogen or isopropyl, R and R stand for hydrogen or C1-2 alkoxy by reacting a rezorcinol-derivative of general formula (III) wherein R and R are as given above with ethyl-orthoformiate of the formula (IV): (C2H5O)3CH in the presence of a base and optionally by alkylating the product. The process is carried out by subjecting the compounds of general formula (III) and (IV), wherein R and R are as given above, to ring-closure at 70-100 DEG C in the presence of an organic solvent, preferably dimethyl-formamide and/or isopropanol in a 0.3-2-fold volume calculated to the volume of the rezorcinol derivatives and/or in the presence of excess of the ester of formula (IV) in order to produce a 20-70 % by weight solution (supersaturated) of the product of general formula (VII) wherein R and R are as given above, and whereby the product of general formula (VII), wherein R and R are as given above, continuously precipitates from the mixture and filtering the product of general formula (VII) after cooling from the reaction mixture and/or adding a polar or apolar solvent to the reaction mixture and selectively dissolving thus the side product and filtering the product of general formula (VII), wherein R and R are as given above, and/or adding to the reaction mixture an almost equivalent amount of anhydrous potassium carbonate and isolating the crystallized double salt of general formula (V) wherein R and R are as given above, whereafter the products of general formula (V) or (VII) are reacted with isopropil-halide and optionally separating the pure product containing at most 0.5 % by weight of contaminating compound of general formula (VI).
Abstract translation: 本发明涉及一种制备通式（I）的纯异黄酮衍生物的方法，其中R代表氢或异丙基，R 2和R 3代表氢或C 1-2烷氧基，通过使间苯二酚 - 其中R 2和R 3如上文所给出的通式（III）的衍生物与式（IV）的原甲酸乙酯：（C 2 H 5 O）3 CH在碱的存在下，任选地通过烷基化产物。 该方法通过使式（III）和（IV）的化合物（其中R 2和R 3如上所述）在70-100℃下在存在下进行闭环来进行 有机溶剂，优选二甲基甲酰胺和/或异丙醇，其计算方法为以间苯二酚衍生物的体积计算为0.3-2倍，和/或在过量的式（IV）的酯存在下，以产生20- 通式（VII）的产物（其中R 2和R 3如上所述）的70重量％溶液（过饱和的），其中通式（Ⅶ）的产物，其中R 2和R 如上所述，从反应混合物冷却后，从混合物中连续沉淀并过滤通式（VII）的产物，和/或向反应混合物中加入极性或非极性溶剂，并选择性地将副产物溶解， 过滤通式（VII）的产物，其中R 2和R 3如上所定义，和/或向反应物 在混合物中几乎相当量的无水碳酸钾并分离出其中R 2和R 3如上所述的通式（Ⅴ）的结晶双盐，之后通式（Ⅴ）或（Ⅶ）的产物 与异丙烯卤化物反应，并任选分离含有至多0.5重量％的通式（VI）的污染化合物的纯产物。
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公开(公告)号：WO1989009541A1
公开(公告)日：1989-10-19
申请号：PCT/HU1989000012
申请日：1989-04-07
Applicant: CHINOIN GYOGYSZER- ÉS VEGYÉSZETI TERMÉKEK GYARA ... , SZEGO, András , PAP, László , NAGY, Lajos , SOMFAI, Éva , SZUCSANY, György , SZÉKELY, István , DEAKNÉ, Molnár, Anikó , HEGEDÜS, Agnes
IPC: A01N25/24
CPC classification number: A01N25/02
Abstract: The invention relates to ULV plant protecting arthropodicidal formulation comprising alkyl aryl polyglycol ether as further additives in addition to the active ingredient(s) dissolved in the mixture of aliphatic hydrocarbons and sunflower oil. The formulation according to the invention has an initial contact angle on the plant surface of > 13°, after 20 minutes of > 6° and it is after 120 minutes still at least 2°.
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公开(公告)号：WO1988002254A1
公开(公告)日：1988-04-07
申请号：PCT/HU1987000040
申请日：1987-09-25
Applicant: CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT , KNOLL, József , SIMAY, Antal , SZINNYEI, Éva , SOMFAI, Éva , TÖRÖK, Zoltán , MOZSOLITS, Károly , BERGMANN, János
IPC: A61K31/135
CPC classification number: A61K31/135
Abstract: Pharmaceutical composition comprising as active ingredient a compound of general Formula (I), wherein R stands for straight or branched chain alkyl comprising 1 to 8 carbon atoms; phenyl alkyl having 7 to 10 carbon atoms; phenyl; or cycloalkyl comprising 3 to 8 carbon atoms; R stands for straight or branched chain alkyl comprising 1 to 8 carbon atoms, alkyl comprising 1 to 8 carbon atoms substituted by halogen, hydroxy, alkoxy having 1 to 4 carbon atoms or by one or two phenyl groups; phenyl; or cycloalkyl having 3 to 8 carbon atoms, with the proviso that groups R and R together contain at least three carbon atoms. The invention also relates to a process for the preparation of compounds of the general Formula (I) by methods known per se. The compounds of the general Formula (I) are psychostimulants having a new spectrum of effect which can be used in therapy for increasing psychical activity (learning and retention) and for treating clinical patterns of depression and deficites of learning and retention like in Alzheimer's disease, and are void of side effects (e.g. due to catecholamine release) of known stimulants.
Abstract translation: 药物组合物，其包含作为活性成分的通式（I）的化合物，其中R 1代表包含1至8个碳原子的直链或支链烷基; 具有7至10个碳原子的苯基烷基; 苯基; 或包含3至8个碳原子的环烷基; R 2代表包含1至8个碳原子的直链或支链烷基，由卤素，羟基，具有1至4个碳原子的烷氧基或1或2个苯基取代的1至8个碳原子的烷基; 苯基; 或具有3至8个碳原子的环烷基，条件是基团R 1和R 2一起含有至少三个碳原子。 本发明还涉及通过本身已知的方法制备通式（I）的化合物的方法。 通式（I）的化合物是具有新的效应谱系的精神兴奋剂，其可用于治疗增加心理活动（学习和保留）和用于治疗抑郁症的学习和保留的临床模式，如阿尔茨海默病， 并且没有已知的兴奋剂的副作用（例如由于儿茶酚胺释放）。
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15.发明申请
公开(公告)号：WO1986004215A1
公开(公告)日：1986-07-31
申请号：PCT/HU1986000003
申请日：1986-01-16
Applicant: CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA ... , HIDASI, György , SZÉKELY, István , BERTOK, Béla , ZOLTAN, Sándor , NAGY, Lajos , GAJARI, Antal , SOMFAI, Éva , HEGEDÜS, Agnes , PAP, László , SOOS, Rudolf , RADVANY, Erzsébet , BOTAR, Sándor , SZALBOLCSI, Tamás
IPC: A01N53/00
CPC classification number: A01N53/00 , A01N2300/00
Abstract: An insecticidal composition containing more than one active ingredients which comprises as active ingredient in an amount of 0.001-99% by weight a synthetic pyrethroide of general Formula (I), (wherein X stands for chlorine or bromine) - namely out of the eight possible isomers at least 95% of a 55:45 - 25:75 mixture of the enantiomer-pairs Ia:Ib, wherein Ia is 1RcisS + 1ScisR and Ib is 1RtransS + 1StransR - if desired, in admixture with an activator and/or with an amount of up to 100% of an auxiliary agent, preferably an antioxidant, stabilizer, wetting agent, emulsifiying agent, dispersing agent, antifoam agent, diluent, carrier, and/or filler. The advantage of the insecticidal composition of the present invention is that it is less toxical towards warm-blooded animals and useful parasites and is therefore much less harmful to the environment.
Abstract translation: 含有多于一种活性成分的杀虫组合物，其包含作为通式（I）的合成除虫菊酯（其中X表示氯或溴）的0.001-99重量％的活性成分，即8个可能的 异构体至少95％的对映体对Ia：Ib的55:45-25:75的混合物，其中Ia是1RcisS + 1ScisR和Ib是1RtransS + 1StransR，如果需要，与活化剂和/或与 助剂，优选抗氧化剂，稳定剂，润湿剂，乳化剂，分散剂，消泡剂，稀释剂，载体和/或填料的量高达100％。 本发明的杀虫组合物的优点在于对温血动物和有用寄生虫的毒性较小，因此对环境的危害较小。
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公开(公告)号：WO1986003202A1
公开(公告)日：1986-06-05
申请号：PCT/HU1985000068
申请日：1985-11-15
Applicant: CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA ... , LANYI, György , NAGY, Lajos , DÉNES, Valéria , SOMFAI, Éva , RADVANY, Erzsébet , PAP, László , VISNYOVSZKY, Mária , DETRE, Tamás , SZEGO, András
IPC: C07D307/79
CPC classification number: A01N47/22 , C07D307/86
Abstract: New compounds of general formula (I) wherein R stands for hydrogen or C1-4 alkyl; and R represents C1-4 alkyl or C2-8 dialkylamino, or a group of general formula R -(CH2)n- wherein n is an integral number 1 or 2; R represents -COOR , wherein R is C1-4 alkyl or a group of general formula (II), and R and R stand for hydrogen or C1-4 alkoxy; or R and R together may form a group of formula -(CH2)2-O-(CH2)2- and salts thereof and a process for the preparation of the same. The compounds of general formula (I) exhibit useful pesticidal - particularly insecticidal, akaricidal and/or nematocidal - effect and the invention also relates to pesticidal compositions comprising as active ingredient at least one compound of general formula (I) or a salt thereof.
Abstract translation: 通式（I）的新化合物，其中R 2代表氢或C 1-4烷基; 和R 3表示C 1-4烷基或C 2-8二烷基氨基，或通式R 4 - （CH 2）n - 的基团，其中n是整数1或2; R 4表示-COOR 5，其中R 5是C 1-4烷基或通式（II）的基团，R 6和R 7代表氢或C 1-4烷氧基; 或R 2和R 3一起可以形成式 - （CH 2）2 -O - （CH 2）2 - 的基团及其盐及其制备方法。 通式（I）的化合物表现出有用的杀虫 - 特别是杀虫，杀螨和/或杀线虫作用，并且本发明还涉及包含至少一种通式（I）化合物或其盐作为活性成分的杀虫组合物。
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