PHENYL-GLYCINE DERIVATIVES
    1.
    发明申请
    PHENYL-GLYCINE DERIVATIVES 审中-公开
    苯乙酸衍生物

    公开(公告)号:WO1991001969A1

    公开(公告)日:1991-02-21

    申请号:PCT/HU1990000052

    申请日:1990-07-25

    CPC classification number: C07D307/58 C07C227/18 C07C309/00

    Abstract: Process for the preparation of compounds (I), wherein A and R are defined as in Claim 1, by reaction of phenyl-glycine (VII) in the presence of alkanol with 1.05-1.3 moles of alkali hydroxide and reacting the mixture with an acid with a higher pH value than 4.3, or by reaction of (VII) with an equivalent amount of alkali salts of acids possessing a higher pH value than 4.3, and condensing the obtained amino acid salt in the presence of alkanol with a compound (VIII) -R is defined as in Claim 1- at the boiling point of the reaction mixture, removing water continuously from the reaction mixture by a binary or ternary azeotropic distillation. The thus obtained compound is optionally reacted with a reactive trifluoro-methane sulphonic acid derivative.

    Abstract translation: 制备化合物(I)的方法,其中A和R 2如权利要求1所定义,通过苯基 - 甘氨酸(VII)在烷醇存在下与1.05-1.3摩尔碱金属氢氧化物反应,并使混合物 具有比4.3高的pH值的酸,或通过(VII)与等量的pH值大于4.3的酸的碱金属盐的反应,并将所得到的烷基醇存在下的氨基酸盐与化合物 (VIII)-R 1如权利要求1中所定义,在反应混合物的沸点下,通过二元或三元共沸蒸馏从反应混合物中连续除去水。 由此得到的化合物任选与反应性三氟甲烷磺酸衍生物反应。

    IMPROVED PROCESS FOR THE PREPARATION OF AMIDOXIME DERIVATIVES
    3.
    发明申请
    IMPROVED PROCESS FOR THE PREPARATION OF AMIDOXIME DERIVATIVES 审中-公开
    改进酰胺衍生物的制备方法

    公开(公告)号:WO1990008131A1

    公开(公告)日:1990-07-26

    申请号:PCT/HU1990000003

    申请日:1990-01-10

    CPC classification number: C07D213/78 C07C259/12 C07D295/088

    Abstract: The invention relates to an improved process for preparing amidoxime derivatives of general formula (I), wherein R means a C2-15 group, which may be unsaturated and/or cyclic alkyl, aralkyl group or optionally substituted and/or condensed aromatic and/or heteroaromatic group; R stands for hydrogen or an optionally substituted straight or branched chain or cyclic and/or unsaturated C1-7 alkyl or aromatic group; R represents an optionally substituted straight or branched chain or cylic and/or unsaturated C1-7 alkyl or aromatic group; or R and R together with the adjacent nitrogen atom may form a 5- to 8-membered ring optionally containing other heteroatom(s); and X stands for halogen and their salts by reacting an amidoxime of general formula (II), wherein R is as defined above, in the presence of an alkaline substance, transforming the product to a salt with an acid or transforming the salt to the base, which comprises reacting the amidoxime with an alkaline metal hydroxide or alkaline metal alkoxide and dimethylformamide or 1,3-dimethyl-2-imidazolidinone, preferably in the presence of a proton source, reacting the amidoxime complex thus obtained preferably without isolation with an amine of general formula (III). The invention relates further to pure O-(2-hydroxy-piperidino-1-propil)nicotinic acid amidoxime hydrochloride and hydrobromide and O-(2-hydroxy-3-piperidino-1-propyl)nicotinic acid amidoxime base.

    Abstract translation: 本发明涉及一种制备通式(I)的偕胺肟衍生物的改进方法,其中R 1表示C2-15基团,其可以是不饱和和/或环状烷基,芳烷基或任选取代的和/或稠合的芳族 和/或杂芳族基团; R 2代表氢或任选取代的直链或支链或环状和/或不饱和的C 1-7烷基或芳基; R 3表示任选取代的直链或支链或环状和/或不饱和的C 1-7烷基或芳基; 或R 2和R 3与相邻的氮原子一起可以形成任选含有其它杂原子的5-至8-元环; X代表卤素及其盐,通过在碱存在下使通式(II)的偕胺肟(其中R 1如上述定义)在酸存在下反应,将产物转化为酸或转化盐 包括使偕胺肟与碱金属氢氧化物或碱金属醇盐和二甲基甲酰胺或1,3-二甲基-2-咪唑啉酮反应,优选在质子源存在下,使得到的偕胺肟配合物优选不与其分离而与 通式(III)的胺。 本发明还涉及纯O-(2-羟基 - 哌啶子基-1-丙基)烟酸偕胺肟盐酸盐和氢溴酸盐和O-(2-羟基-3-哌啶子基-1-丙基)烟酸偕胺肟碱。

    PHENYL-GLYCINE DERIVATIVES
    5.
    发明申请
    PHENYL-GLYCINE DERIVATIVES 审中-公开
    苯乙酸衍生物

    公开(公告)号:WO1991001968A1

    公开(公告)日:1991-02-21

    申请号:PCT/HU1990000051

    申请日:1990-07-25

    CPC classification number: C07D307/58 C07C227/18 C07C229/36 C07C309/00

    Abstract: Process for the preparation of compounds (I), wherein X, Y, A and R are defined as in Claim 1, by reaction of a substituted phenyl-glycine (VII) in the presence of alkanol with 1.05-1.3 moles of alkali-hydroxide and reacting the reaction mixture with an acid, the pH-value of which is higher than 4.3, or by reaction of (VII) with an equivalent amount of alkali salts derived from acids having a pH value higher than 4.3, and condensing the obtained amine acid salt in the presence of alkanol with a compound (VIII) -R is defined as in Claim 1- at the boiling point of the reaction mixture, removing water continuously from the reaction mixture by a binary or ternary azeotropic distillation. The thus obtained compound is optionally reacted with a reactive derivative of trifluoro-methane-sulphonic acid.

    Abstract translation: 化合物(I)的制备方法,其中X,Y,A和R 2如权利要求1所定义,通过在烷醇存在下取代的苯基 - 甘氨酸(VII)与1.05-1.3摩尔 碱金属氢氧化物,并使反应混合物与其pH值高于4.3的酸反应,或通过(Ⅶ)与等于pH值大于4.3的酸等量的碱金属盐反应,并使 在烷醇与化合物(VIII)-R 1的存在下,所得的胺酸盐在反应混合物的沸点下定义,如权利要求1所述,通过二元或三元共沸从反应混合物中连续除去水 蒸馏。 由此获得的化合物任选地与三氟甲烷磺酸的反应性衍生物反应。

    NOVEL COMBINED COMPOSITIONS FOR COMBATTING PESTS
    6.
    发明申请
    NOVEL COMBINED COMPOSITIONS FOR COMBATTING PESTS 审中-公开
    用于组合PESTS的新型组合物

    公开(公告)号:WO1991001640A1

    公开(公告)日:1991-02-21

    申请号:PCT/HU1990000055

    申请日:1990-07-30

    CPC classification number: A01N53/00 A01N47/38 A01N43/54 A01N43/653 A01N2300/00

    Abstract: The invention relates to novel combined compositions for combatting plant, animal and sanitarian as well as forestry, horticultural and warehouse pests. These compositions contain a pyrethroid-type insecticide as an insecticidally active ingredient and at least one fungicide inhibiting the ergosterol biosynthesis as activity-strengthening agent as well as optionally piperonylbutoxide and other additives. The advantages of the compositions according to the invention consist therein that the activity-strengthening substances used are fungicidal agents widely used and have an advantageous toxicology. The activity-strengthening agent exerts a synergistic effect together with the pyrethroid-type insecticide. The combinations according to the invention bear an outstanding importance in the protection of stored crops.

    Abstract translation: 本发明涉及用于对抗植物,动物和卫生以及林业,园艺和仓库害虫的新型组合组合物。 这些组合物含有拟除虫菊酯型杀虫剂作为杀虫活性成分和至少一种抑制麦角甾醇生物合成作为活性增强剂以及任选的胡椒基丁醚和其它添加剂的杀真菌剂。 根据本发明的组合物的优点在于其中使用的活性增强物质是广泛使用的杀真菌剂并且具有有利的毒理学。 活性增强剂与拟除虫菊酯类杀虫剂一起发挥协同作用。 根据本发明的组合在保护作物方面具有突出的重要性。

    COMPOSITION TO PREVENT SEASICKNESS
    8.
    发明申请
    COMPOSITION TO PREVENT SEASICKNESS 审中-公开
    组合物以防止食欲

    公开(公告)号:WO1988004552A1

    公开(公告)日:1988-06-30

    申请号:PCT/HU1987000058

    申请日:1987-12-18

    CPC classification number: A61K31/135

    Abstract: The compounds of general Formula I (wherein R is hydrogen or halogen) and pharmaceutically acceptable acid addition salts thereof are suitable for the prophylaxis of undesired and unfavourable symptoms (e.g. perspiration, nausea, vomiting, dizziness, etc.)which occur when healthy humans or mammal animals are subjected to unusual moving (e.g. during transportation on aeroplane, or vehicles, ships, etc.). The invention relates to the above pharmaceutical compositions and a process for the preparation thereof.

    Abstract translation: 通式I(其中R是氢或卤素)的化合物及其药学上可接受的酸加成盐适用于预防健康人或其他疾病时发生的不良和不利症状(例如出汗,恶心,呕吐,眩晕等) 哺乳动物受到异常移动(例如在飞机上运输,或车辆,船舶等)。 本发明涉及上述药物组合物及其制备方法。

    DECOLOURIZED PREPARATIONS CONTAINING FORMED ELEMENTS OF BLOOD, PROCESS FOR THEIR PREPARATION AS WELL AS FOOD- AND FEED-ADDITIVES CONTAINING THE SAME AND PROCESSES FOR PREPARATION OF THE LATTER
    10.
    发明申请
    DECOLOURIZED PREPARATIONS CONTAINING FORMED ELEMENTS OF BLOOD, PROCESS FOR THEIR PREPARATION AS WELL AS FOOD- AND FEED-ADDITIVES CONTAINING THE SAME AND PROCESSES FOR PREPARATION OF THE LATTER 审中-公开
    包含形成的血液元素的分解制剂,其制备方法以及含有该组合物的食品和饲料添加剂以及其制备方法

    公开(公告)号:WO1986005361A1

    公开(公告)日:1986-09-25

    申请号:PCT/HU1986000017

    申请日:1986-03-19

    CPC classification number: A23J3/12 A23J1/06 A23K10/24

    Abstract: A process for the preparation of decolourized products containing formed elements of blood such as full blood powder, hemoglobin powder, blood concentrates and processes to prepare food additives and foods of the same, from solutions, suspensions or emulsions containing formed elements of blood, by adding anticoagulants, opening the formed elements of blood containing hemoglobin by known methods, and if desired concentrating the compositions thus obtained and/or freeze drying the same. The invention is performed by adjusting the pH value of the mixture containing the open formed elements and the hemoglobin to pH = 1-2, treating the mixture with an oxidizing agent in the presence of a carbohydrate derivative containing a dienol-group, if desired dialyzing the solution thus obtained to eliminate the by-products, concentrating the solution until a dry substance content of 10-40 % w/v is obtained before or after adjusting the pH value to 7-7.5 and - if desired - freeze drying the product.

    Abstract translation: 一种制备包含血液成分元素的脱色产品的方法,例如全血,血红蛋白粉,血液浓缩物,以及制备食品添加剂及其食品的方法,由含血液形成元素的溶液,悬浮液或乳液中加入 抗凝剂,通过已知方法打开含血红蛋白的血液的形成元素,如果需要,浓缩由此获得的组合物和/或冷冻干燥该组合物。 本发明通过将含有开放形成元素和血红蛋白的混合物的pH值调节至pH = 1-2,在含有二烯醇基团的碳水化合物衍生物的存在下用氧化剂处理该混合物,如果需要透析 由此获得的溶液消除副产物,将溶液浓缩直到在将pH值调节至7-7.5之前或之后获得干物质含量为10-40%w / v,并且如果需要,冷冻干燥产物。

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