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    ARTHROPODICIDES AND PROCESS FOR THEIR PREPARATION
    2.
    发明申请
    ARTHROPODICIDES AND PROCESS FOR THEIR PREPARATION 审中-公开
    抗坏血酸及其制备方法

    公开(公告)号：WO1998018329A1

    公开(公告)日：1998-05-07

    申请号：PCT/HU1997000071

    申请日：1997-10-30

    Applicant: CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT. ,  ARVAI, Géza ,  BERTOK, Béla ,  BLEICHER, Edit ,  CSIZ, László ,  CZUDOR, Irén ,  HEGEDÜS, Agnes ,  PAP, László ,  SZÉKELY, István

    Inventor： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT.

    IPC: A01N53/00

    CPC classification number: C07C67/14 ,  A01N53/00 ,  C07C69/743

    Abstract: The invention relates to an arthropodicidal ectoparasiticidal composition, characterized in that, it contains one or more representative(s) of 1S-trans, (1S-trans) alpha S or (1S-trans) alpha (R, S) isomers or a racemic (1S-trans) alpha S(1R-trans) alpha R isomer mixtrure of one or more cyclopropan carboxylic acid ester type compound(s) containing two asymmetric centers in the cyclopropane ring and optionally one or more further asymmetric center(s) in other part of the molecule in an amount of from 0,001-99 % by weight optionally in admixture with an amount of up to 100 % by weight of one or more auxiliary agent(s) particularly antioxidants, stabilising agents, wetting agents, emulsifying agents, dispersing agents, antifoam agents, diluents and/or fillers.

    Abstract translation: 本发明涉及一种节肢针刺杀螨杀虫剂组合物，其特征在于其含有一个或多个代表性的1S-反式，（1S-反式）αS或（1S-反式）α（R，S）异构体或外消旋 在环丙烷环中含有两个不对称中心的一种或多种环丙烷羧酸酯型化合物的（1S-反式）αS（1R-反式）αR异构体混合物和任选的一种或多种其它不对称中心 0.001-99重量％的一部分分子，任选地与至多100重量％的一种或多种助剂，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。

    QUINOXALINE COMPOUNDS, PHARMACEUTICAL PREPARATIONS CONTAINING THEM AND A PROCESS FOR THE PREPARATION THEREOF
    3.
    发明申请
    QUINOXALINE COMPOUNDS, PHARMACEUTICAL PREPARATIONS CONTAINING THEM AND A PROCESS FOR THE PREPARATION THEREOF 审中-公开
    喹啉化合物，含有它们的药物制剂及其制备方法

    公开(公告)号：WO1997019934A1

    公开(公告)日：1997-06-05

    申请号：PCT/HU1996000072

    申请日：1996-11-28

    Applicant: CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT. ,  BATA, Imre ,  BATORI, Sándor ,  BENCE, Judit ,  BÖCSKEI, Zsolt ,  CSIKOS, Éva ,  ERDO"e;, Sándor ,  GÖNCZI, Csaba ,  HERMECZ, István ,  HÉJA, Gergely ,  LAKICS, Viktor ,  MAJLATH, Csilla ,  MOLNAR, Péter ,  PODANYI, Benjamin ,  RITZ, Imola ,  SANTANÉ, Csutor, Andrea ,  SZO"e;KÉNÉ, Szappanos, Andrea ,  SZVOBODA, Györgyné

    Inventor： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT.

    IPC: C07D241/44

    CPC classification number: C07D241/54 ,  C07D241/44

    Abstract: The invention relates to compounds of general formula (I) and salts, tautomeric forms and N-oxides thereof in which formula: Z means hydrogen, hydroxy, C1-4 alkyl, C7-9 phenylalkyl, optionally substituted phenyl, COOC1-4 alkyl, C2-14 acyl, C1-4 alkylsulphonyl, trifluoromethyl-sulphonyl, optionally substituted benzoyl, optionally substituted phenyl-sulphonyl group; Y means hydrogen, or optionally substituted amino group, or Y and Z form together a -CO-O- group, where Y and Z mean together a valency bond, or Y and Y mean together a valency bond, and at the same time Z means hydrogen, hydroxy, C1-4 alkyl, C7-9 phenylalkyl, optionally substituted phenyl, COOC1-4 alkyl, C2-14 acyl, C1-4 alkylsulphonyl, trifluoromethyl-sulphonyl, optionally substituted benzoyl, optionally substituted phenyl-sulphonyl group; X and X mean together =O, or =S, or X means hydrogen, -NHR or -WR groups, and at the same time X means hydrogen, or X and X together form a valency bond, X means hydrogen, C1-4 alkyl, C7-9 phenylalkyl, optionally substituted phenyl, R and R mean hydrogen, halogen, C1-4 alkyl, trifluoromethyl, ciano, mercapto or sulphonylamido group, R means hydrogen or nitro group, R means hydrogen or hydroxy group, R means hydrogen, C1-4 alkyl, C7-9 phenylalkyl group, W means oxygen or sulfur with the proviso, that a) if at least one of the substituents of R , R and R is different from hydrogen or b) if the meaning of Z and Z is hydrogen and R means 6-chloro, R means hydrogen, R has a different meaning from 7-chloro, or R means 6-methyl, R means hydrogen, R has a different meaning from 7-methyl; compounds of general formula (I) show a significant activity at the glycine binding site of the NMDA-receptor, therefore they can be used as active ingredients of pharmaceutical compositions.

    Abstract translation: 本发明涉及通式（I）的化合物及其盐，互变异构形式和N-氧化物，其中式：Z 1表示氢，羟基，C 1-4烷基，C 7-9苯基烷基，任选取代的苯基，COOC1- C 1-4烷基磺酰基，三氟甲磺酰基，任选取代的苯甲酰基，任选取代的苯基磺酰基; Y 1表示氢或任选取代的氨基，或Y 1和Z 1一起形成-CO-O-基团，其中Y 2和Z 2表示价键，或 Y 1和Y 2均表示价键，同时Z 2表示氢，羟基，C 1-4烷基，C 7-9苯基烷基，任选取代的苯基，COOC 1-4烷基， 14酰基，C 1-4烷基磺酰基，三氟甲基磺酰基，任选取代的苯甲酰基，任选取代的苯基磺酰基; X 1和X 2均表示= O或= S或X 1表示氢，-NHR 4或-WR 5基团，同时X 2表示氢 或X 2和X 3一起形成价键，X 3表示氢，C 1-4烷基，C 7-9苯基烷基，任选取代的苯基，R 1和R 2表示氢， 卤素，C 1-4烷基，三氟甲基，碳原子，巯基或磺酰氨基，R 3表示氢或硝基，R 4表示氢或羟基，R 5表示氢，C 1-4烷基， 9苯基烷基，W表示氧或硫，条件是a）如果R 1，R 2和R 3的至少一个取代基不同于氢或b）如果Z的含义 1和Z 2是氢，R 1表示6-氯，R 3表示氢，R 2与7-氯不同，或者R 1表示6-甲基， R 3表示氢，R 2与7-甲基具有不同的含义; 通式（I）的化合物在NMDA受体的甘氨酸结合位点显示出显着的活性，因此它们可以用作药物组合物的活性成分。

    PROCESS FOR THE PREPARATION OF QUINOLINE-CARBOXYLIC ACID DERIVATIVES
    5.
    发明申请
    PROCESS FOR THE PREPARATION OF QUINOLINE-CARBOXYLIC ACID DERIVATIVES 审中-公开
    制备喹喔啉羧酸衍生物的方法

    公开(公告)号：WO1988002748A1

    公开(公告)日：1988-04-21

    申请号：PCT/HU1987000044

    申请日：1987-10-14

    Applicant: CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT ,  FRANK, Judit ,  BÉRES, József, Károlyné ,  KULCSAR, Gábor

    Inventor： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT

    IPC: C07D215/56

    CPC classification number: C07D215/56

    Abstract: New and simple process for the preparation of quinoline-carboxylic acid derivatives of general formula (I) as well as hydrates and therapeutically acceptable salts thereof. In the formula the meaning of the substituents is as follows: R is a hydrogen atom or a formyl group, R is a hydrogen atom or a straight or branched chain alkyl group having 1 to 4 carbon atoms, which may be substituted by a hydroxyl group, a halogen atom or an amino group; or a CH3-NH-group, R is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms. According to the invention the compound of general formula (II) or an acid addition salt thereof is reacted with piperazine in dimethylformamide and - if desired - the compound of general formula (III) thus obtained is subjected to an acidic or alkaline treatment, or is reacted advantageously with hydrazine or preferably with hydrazine-hydrate.

    Abstract translation: 用于制备通式（I）的喹啉羧酸衍生物的新的和简单的方法以及其水合物及其治疗上可接受的盐。 在该式中，取代基的含义如下：R是氢原子或甲酰基，R 1是氢原子或具有1至4个碳原子的直链或支链烷基，其可以被 羟基，卤素原子或氨基; 或CH 3 -NH基，R 2是氢原子或具有1至4个碳原子的烷基。 根据本发明，将通式（II）的化合物或其酸加成盐与二甲基甲酰胺中的哌嗪反应，如果需要，将所得通式（III）的化合物进行酸或碱处理，或 有利地与肼反应或优选与肼水合物反应。

    PROCESS FOR THE PREPARATION OF BENZYL-ETHERS BY USE OF PHASE TRANSFER
    7.
    发明申请
    PROCESS FOR THE PREPARATION OF BENZYL-ETHERS BY USE OF PHASE TRANSFER 审中-公开
    通过使用相转移制备苯甲醚的方法

    公开(公告)号：WO1998022417A1

    公开(公告)日：1998-05-28

    申请号：PCT/HU1997000074

    申请日：1997-11-12

    Applicant: CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT. ,  ARVAI, Géza ,  BERTOK, Béla ,  KURUCZNÉ RIBAI, Zsuzsanna ,  PAP, László ,  SZÉKELY, István

    Inventor： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT.

    IPC: C07C41/16

    CPC classification number: C07C41/16 ,  C07D317/54 ,  C07C43/215 ,  C07C43/225 ,  C07C43/2055

    Abstract: The subject of the invention is the process for the preparation of mixed ethers of general formula (I), wherein Ar represents an alicyclic, aromatic or one or more heteroatom-containing heterocyclic moiety, optionally substituted by one or more C1-4 alkoxy, methylenedioxy, C1-4alkyl, halogen, C1-4haloalkyl or nitro-group, and/or condensed with a benzene ring; R means hydrogen, C1-4 alkyl, C1-4 haloalkyl, C2-4 alkenyl, phenyl, substituted phenyl, C3-6cycloalkyl group; R means C1-6alkyl, C3-6alkenyl, or C3-6alkinyl group, optionally mono- or poly-substituted by C1-6alkyl, C1-6alkoxy, C3-6alkenyl, C3-6alkinyl, C1-6haloalkyl group or by halogen atom; or a C1-4 alkyloxy-C1-4alkyl-oxy-C1-4alkyl group. n = 1,2 by the reaction of compounds of general formula (II), wherein R and n have the same meaning as above; X means hydroxy, halogen or sulfonester leaving group, with the compounds of the general formula (III): R2-Y, wherein R has the same meaning as above; Y means hydroxy, halogen or sulfonester leaving group, with the proviso that one of the reaction partners of general formulae (II) and (III) is an alcohol, characterized by, that the reaction is performed under heterogenous conditions in presence of an aqueous base and a phase transfer catalyst, and the resulting product is optionally stabilized by the addition of a base and/or anti-oxidant.

    Abstract translation: 本发明的主题是制备通式（I）的混合醚的方法，其中Ar表示脂环族，芳族或一个或多个含杂原子的杂环部分，任选被一个或多个C 1-4烷氧基亚甲二氧基 ，C 1-4烷基，卤素，C 1-4卤代烷基或硝基，和/或与苯环稠合; R 1表示氢，C 1-4烷基，C 1-4卤代烷基，C 2-4烯基，苯基，取代的苯基，C 3-6环烷基; R 2表示C 1-6烷基，C 3-6烯基或C 3-6炔基，任选被C 1-6烷基，C 1-6烷氧基，C 3-6烯基，C 3-6烯基，C 1-6卤代烷基或卤素单取代或多取代 原子; 或C 1-4烷氧基-C 1-4烷基 - 氧基-C 1-4烷基。 通过通式（II）的化合物（其中R 1和n具有与上述相同的含义）的反应，n = 1,2; X表示羟基，卤素或砜类离去基团，与通式（III）的化合物：R2-Y，其中R 2具有与上述相同的含义; Y表示羟基，卤素或砜类离去基团，条件是通式（II）和（III）的反应伴侣之一是醇，其特征在于反应在异质条件下在碱水溶液 和相转移催化剂，并且所得产物任选地通过加入碱和/或抗氧化剂来稳定。

    LIPOSOME COMPOSITION CONTAINING SELEGILIN
    8.
    发明申请
    LIPOSOME COMPOSITION CONTAINING SELEGILIN 审中-公开
    含有塞来吉林的脂肪组合物

    公开(公告)号：WO1996012472A1

    公开(公告)日：1996-05-02

    申请号：PCT/HU1995000052

    申请日：1995-10-20

    Applicant: CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT ,  MEZEI, Michael ,  GAAL, József ,  SZÉKACS, Gábor ,  SZEBENI, Gyula ,  MARMAROSI, Tamásné ,  MAGYAR, Kálmán ,  LENGYEL, József ,  SZATMARI, István ,  TURI, Agnes

    Inventor： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT

    IPC: A61K09/127

    CPC classification number: A61K31/137 ,  A61K9/127

    Abstract: This invention provides liposomic composition, containing as active ingredient (-)-N- alpha -dimethyl-N-(2-propynylphenylethylamine) (selegilin) and/or salt thereof. This composition contains: 0.1-40 % by weight of selegilin and/or a salt thereof, 2 to 40 % by weight of lipids, preferably phospholipids, 0 to 10 % by weight of cholesterol, 0 to 20 % by weight of an alcohol, 0 to 25 % by weight of a glycol, 0 to 3 % by weight of an antioxidant, 0 to 3 % by weight of a preserving agent, 0 to 2 % by weight of a viscosity influencing agent, 0 to 50 % by weight of cyclodextrin or a cyclodextrin derivative and 30 to 90 % by weight of water. This invention relates to pharmaceutical composition, containin the liposomic composition described and if desired, usual filling and diluting agents and other auxiliaries, preferably in oral, parenteral or transdermal form. This invention provides the process for the preparation of liposomic compositions containing selegilin and/or salt thereof. Accordingly liposomic composition of this invention may be administered for the treatment of Alzheimer's disease, Parkinson's disease, depression, stroke, motion sickness or myelitis.

    Abstract translation: 本发明提供含有作为（ - ） - N-α-二甲基-N-（2-丙炔基苯乙胺）（selegilin）和/或其盐的活性成分的脂质体组合物。 该组合物包含：0.1-40重量％的赛莱格林和/或其盐，2至40重量％的脂质，优选磷脂，0至10重量％的胆固醇，0至20重量％的醇， 0〜25重量％的二醇，0〜3重量％的抗氧化剂，0〜3重量％的防腐剂，0〜2重量％的粘度影响剂，0〜50重量％ 环糊精或环糊精衍生物和30〜90重量％的水。 本发明涉及药物组合物，所述药物组合物包含所述的脂质体组合物，如果需要，含有通常的填充和稀释剂和其它助剂，优选口服，肠胃外或透皮形式。 本发明提供了制备含有塞来林和/或其盐的脂质体组合物的方法。 因此，本发明的脂质体组合物可以用于治疗阿尔茨海默氏病，帕金森病，抑郁症，中风，运动病或脊髓炎。

    IMPROVED PROCESS FOR THE PREPARATION OF AMIDOXIME DERIVATIVES
    10.
    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

    Applicant: CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT ,  BERTOK, Béla ,  SZÉKELY, István ,  THURNER, Angelika ,  SOMFAI, Éva ,  BOTAR, Sándor ,  GAJARY, Antal ,  TAKACS, Kálmán ,  NAGY, Lajos

    Inventor： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT

    IPC: C07C251/58

    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。

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