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175 条记录 (耗时 0.014 秒)

    Preparation of bicyclohexane derivative
    51.
    发明公开
    Preparation of bicyclohexane derivative 失效
    Verfahren zur Herstellung von einem Bicyclohexanderivat

    公开(公告)号：EP0751117A1

    公开(公告)日：1997-01-02

    申请号：EP96304718.8

    申请日：1996-06-26

    申请人： ELI LILLY AND COMPANY

    发明人： Robey, Roger Lewis

    IPC分类号： C07C229/50 ,  C07D233/78 ,  C07C227/24 ,  C07C62/24

    CPC分类号： C07D235/02 ,  C07C62/24 ,  C07C227/24 ,  C07C229/50 ,  C07C2602/18

    摘要： A process for the preparation of (+)-2-amino-bicyclo[3.1.0]-hexane-2-6-dicarboxylic acid, or a pharmaceutically acceptable salt thereof, which comprises hydrolysing (-)-2-spiro-5'-hydantoinbicyclo[3.1.0]hexane-6-carboxylic acid or a salt thereof, and optionally forming a pharmaceutically acceptable salt. Also disclosed are novel intermediates useful in the process.

    摘要翻译： 制备（+） - 2-氨基 - 二环己基-2,6-二羧酸或其药学上可接受的盐的方法，其包括水解（ - ） - 2-螺-5'-乙内酰脲双环[ .1.0己烷-6-羧酸或其盐，并任选地形成药学上可接受的盐。 还公开了在该方法中有用的新型中间体。

    Process for preparing 5-arylhydantoin
    53.
    发明公开
    Process for preparing 5-arylhydantoin 失效
    Verfahren zur Herstellung von 5-Arylhydantoin。

    公开(公告)号：EP0474112A1

    公开(公告)日：1992-03-11

    申请号：EP91114490.5

    申请日：1991-08-29

    申请人： KANEGAFUCHI KAGAKU KOGYO KABUSHIKI KAISHA

    发明人： Yamada, Masahiko ,  Takahashi, Satomi

    IPC分类号： C07D233/78

    CPC分类号： C07D233/78 ,  C07D233/76

    摘要： A process for preparing a 5-arylhydantoin having the formula (II):

    which comprises:
    reacting methyl 2-hydroxy-2-methoxyacetate, urea and an aryl compound having the formula (I):

    in the presence of an acid. According to the process, the 5-arylhydantoin which is a very effective intermediate for preparing D-arylglycines can be easily prepared from the unexpensive raw materials in a high purity.

    摘要翻译： 制备具有式（II）的5-芳基乙内酰脲的方法：，其包括：使2-羟基-2-甲氧基乙酸甲酯，脲和具有式（I）的芳基化合物：在 酸。 根据该方法，作为制备D-芳基甘氨酸的非常有效的中间体的5-芳基乙内酰脲可以以高纯度的廉价原料容易地制备。

    Leukotriene antagonists, their production, and compositions containing them
    57.
    发明公开
    Leukotriene antagonists, their production, and compositions containing them 失效
    Leukotrienantagonisten，deren Herstellung und diese enthaltende Zusammensetzungen。

    公开(公告)号：EP0104885A1

    公开(公告)日：1984-04-04

    申请号：EP83305588.2

    申请日：1983-09-21

    申请人： MERCK FROSST CANADA INC.

    发明人： Belanger, Patrice C. ,  Fortin, Rejean ,  Guindon, Yvan ,  Rokach, Joshua ,  Yoakim, Christiane

    IPC分类号： C07C149/40 ,  C07C147/14 ,  C07C147/107 ,  C07D317/14 ,  C07D233/78 ,  C07D207/404 ,  C07D303/02 ,  C07C59/90 ,  A61K31/19 ,  C07C59/64 ,  C07C51/347

    CPC分类号： C07D207/26 ,  C07C45/71 ,  C07C59/90 ,  C07C317/00 ,  C07C323/00 ,  C07D207/33 ,  C07D233/74 ,  C07D257/04 ,  C07D307/58 ,  C07D317/34 ,  C07C49/84

    摘要： Compounds of the formulae:

    and their pharmaceutically acceptable (including acid- addition) salts, which are novel, are antagonists of leukotrienes of C 4 , D 4 and E 4 , the slow reacting substance of anaphylaxis. They can be made into pharmaceutical compositions by incorporating them in a pharmaceutical carrier.
    In the formulae, each R is H, OH, SH, C 1-8 alkyl, C 2-8 alkenyl, CF 3 , C 1-8 alkoxy, C 1-8 alkylthio, phenyl, phenyl having C 1-3 alkyl or halogen substitution, phen (C 2-4 alkyl), halogen, amino, N(R 4 ) 2 , COOR 4 or CH 2 OR 4 where R 4 is H or C 1-8 alkyl, formyl, CN, CF 3 S or NO 2 ;
    each R' is R 4 ; OR 4 ; COOR 4 ; N(R 4 ) 2 ; SR 4 ; CH 2 OR 4 orCHO; , or together R' and R' are 0, CH 2 or
    Y is oxyge, sulfur, sulfoxide, sulfone,
    = NR 12 , = N - CO - R 13 or - N - CN, where R 11 is C 1-4 alkyl, R 12 is H or C 1-4 atkyl and R 13 is C 1-4 alkyl or C 1-4 alkoxy;

    Y' is Y,
    each R 1 is hydrogen or C 1-3 alkyl; each m is an integer from 0 to 6;
    R 2 is
    where Z is O. S, CH 2 , H and OH, C 1-4 alkenyl, or = N - R 14 , where R 14 is OH, CN, COOH, halogen, formyl, C 1-8 acyl, C 1-8 alkyl, C 1-8 alkoxy, C 1-8 halogenated alkyl, phenyl, or phenyl having C 1-3 alkyl or C 1-3 alkoxy substitution; each R e is H or C 1-4 alkyl; each R 7 is H, OH or C 1-4 alkyl; each R 8 is H or C 1-4 alkyl and is absent when the two indicated carbons are triply bonded;
    R 5 is COOR 4 ; CH 2 OH; CHO; tetrazole; NHSO 2 R 14 ; CON-HSO 2 R 14 hydroxymethylketone; CN; CON(R 7 ) 2 ; a monocyclic or bicyclic heterocyclic ring containing an acidic hydroxyl group; or COOR 15 where R 15 is:
    where each s is independently 0-3, R 6 is as defined above and R 16 is

    (A) a monocyclic or bicyclic heterocyclic radical containing from 3 to 12 nuclear carbon atoms and 1 or 2 N heteroatoms or one N and one S heteratom, each ring in the heterocyclic radical being formed of 5 or 6 atoms, or
    (B) W-R 17 where W is O, S or NH and R 17 contains up to 21 carbon atoms and is (1) a hydrocarbon radical or (2) an acyl radical or an organic acyclic or monocyclic carboxylic acid containing not more than 1 heteroatom in the ring;

    each of r and q is 0-20 but r + q does not exceed 20; and
    p is 0 or 1;
    R 3 is C 1-6 alkyl or C 3-8 alkenyl;
    R 9 is C 1-8 alkyl, C 1-8 alkoxy or (CH 2 ) r R 5 , where r and R s are as defined above: and
    R 10 is H, C 1-8 alkyl; R 4 CO- or R 4 OCH 2 , where R 4 is as defined above.

    The compounds are prepared by condensing together two compounds having appropriately substituted benzene rings, one of which contains a halogen atom in the chain containing Y and Y', which removes a hydrogen atom from the ring of the other compound.

    摘要翻译： 下列化合物：及其药学上可接受的（包括酸加成）盐，它们是C4，D4和E4的白三烯拮抗剂，其是过敏反应的缓慢反应物质。 它们可以通过将其并入药物载体中而制成药物组合物。 式中，R为H，OH，SH，C 1-6烷基，C 2-6烯基，CF 3，C 1-6烷氧基，C 1-6链炔基，苯基，具有C1-3烷基或卤素取代基的苯基，苯基（C2 -4烷基），卤素，氨基，N（R4）2，COOR4或CH2OR4，其中R4是H或C1-6烷基，甲酰基，CN，CF3S或NO2; 每个R 1是R 4; OR 4; COOR4; N（R 4）2; SR4; CH2OR4或CHO; 或R 1和R 2分别为O，CH 2或CH 2 Y，是氧，硫，亚砜，砜，= NR 11，= NR 12，= N-CO-R 13或-N-CN，其中R 11为C 1-4 烷基，R 12为H或C 1-4烷基，R 13为C 1-4烷基或C 1-4烷氧基; Y min为Y，-CH 2 - 或 - 每个R 1是氢或C 1-3烷基; 每个m是0至6的整数; 其中Z是O，S，CH2，H和OH，C1-4链烯基或= N-R14，其中R14是OH，CN，COOH，卤素，甲酰基，C1-6酰基，C1-6烷基， C 1-6烷氧基，C 1-6卤代烷基，苯基或具有C 1-3烷基或C 1-3烷氧基取代基的苯基; 每个R 6是H或C 1-4烷基; 每个R 7是H，OH或C 1-4烷基; 每个R 8为H或C 1-4烷基，当两个表示的碳原子键合时不存在; R5为COOR4; CH2OH; CHO; 四唑; NHSO2R14; CONHSO2R14羟甲基酮; CN; CON（R7）2; 含有酸性羟基的单环或双环杂环; 或COOR 15，其中R 15为：其中各s独立地为0-3，R 6如上所定义，R 16为（A）含有3至12个核碳原子和1或2个N杂原子的单环或双环杂环基，或 一个N和一个S杂原子，杂环基中的每个环由5或6个原子形成，或（B）W-R 17，其中W是O，S或NH，R 17含有最多21个碳原子，并且是（1）a 烃基或（2）环中含有不超过1个杂原子的酰基或有机酰基或单环羧酸; r和q各自为0-20，但r + q不超过20; p为0或1; R3是C1-6烷基或C3-6烯基; R 9是C 1-6烷基，C 1-6烷氧基或（CH 2）r R 5，其中r和R 5如上所定义; R 10为H，C 1-6烷基; R4CO-或R4OCH2，其中R4如上所定义。 通过将具有适当取代的苯边缘的两种化合物冷凝在一起制备化合物，其中一个在含有Y和Ymin的链中含有卤素原子，其从另一种化合物的环除去氢原子。

    Therapeutic use of allantoin-formaldehyde condensation products
    59.
    发明公开
    Therapeutic use of allantoin-formaldehyde condensation products 失效
    治疗安息托 - 甲醛。

    公开(公告)号：EP0080281A1

    公开(公告)日：1983-06-01

    申请号：EP82305875.5

    申请日：1982-11-04

    申请人： WIGGLESWORTH LIMITED

    发明人： Harrison, Anthony Ralph ,  Morrison, Alexander McKenzie

    IPC分类号： C07D233/78 ,  C07D233/72 ,  A61K31/415

    CPC分类号： C07D233/88

    摘要： Monomeric, dimeric and polymeric allantoinformal- dehyde condensation products, especially imidazolidinyl urea and diazolidinyl urea, have been found to be therapeutically effective in the treatment of humans and animals, especially in the treatment of diseases and malconditions of the skin and other membranes. The compounds have the advantages of water-solubility, low toxicity, low irritancy and broad action, which is a combination of properties not found in many drugs. The compounds may be used in a wide variety of compositions and formulations.

    摘要翻译： 已经发现单体，二聚和聚合的尿囊素甲醛缩合产物，特别是咪唑烷基脲和重氮烷基脲，对治疗人和动物具有治疗上的有效性，特别是在治疗皮肤和其它膜的疾病和病症方面。 该化合物具有水溶性，低毒性，低刺激性和广泛作用的优点，这是许多药物中未见的性质的组合。 所述化合物可以以各种各样的组合物和制剂使用。