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    BICYCLIC AMINE DERIVATIVES
    73.
    发明申请
    BICYCLIC AMINE DERIVATIVES 审中-公开
    双相胺衍生物

    公开(公告)号：WO98046600A1

    公开(公告)日：1998-10-22

    申请号：PCT/GB1998/000693

    申请日：1998-03-04

    IPC: A01N43/90 ,  C07D451/00 ,  C07D451/02 ,  A01N43/34 ,  A61K31/46

    CPC classification number: C07D451/02 ,  C07D451/00

    Abstract: The invention concerns a method of combating and controlling insect, acarine or nematode pests which comprises treating said pests, or the locus of said pests, with an effective amount of a compound of formula (I), wherein A is WXC-CYZ or XC=CY; R is hydrogen, formyl or cyano or a group selected from alkyl, aryl, heteroaryl, aralkyl, heteroarylalkyl, alkenyl, aralkenyl, alkynyl, alkoxycarbonyl, alkanesulfonyl, arenesulfonyl, alkenyloxycarbonyl, aralkyloxycarbonyl, aryloxycarbonyl, heterocyclylalkyl, carbamyl, dithiocarboxyl or X'R (where X' represents oxygen or a group NR ), provided that when R is alkenyl, aralkenyl or alkynyl said group does not have an unsaturated carbon atom bonding directly to the ring nitrogen of formula (I); Ar is optionally substituted phenyl or an optionally substituted 5- or 6-membered heterocyclic ring system containing from 1 to 3 heteroatoms individually selected from nitrogen, oxygen and sulfur atoms, and at least one unsaturation (double bond) between adjacent atoms in the ring, said heterocyclic ring being optionally fused to a benzene ring, wherein the substituents, if present, are selected from halogen atoms, cyano, alkyl, alkenyl, alkynyl, alkoxy, haloalkyl, haloalkenyl, alkylthio and alkyl amino groups, any of which groups contain up to six carbon atoms; W, X, Y and Z are, independently, hydrogen, hydroxy, acyloxy, alkoxy, alkylsilyloxy, cyano or halogen; alkyl moieties of R, R and R comprise from 1 to 15 carbon atoms, and are optionally substituted with one or more substituents selected from halogen, cyano, carboxyl, carboxylic acyl, carbamyl, alkoxycarbonyl, alkoxy, alkylenedioxy, hydroxy, nitro, amino, acylamino, imidate and phosphonato groups; aryl, heteroaryl, aralkyl, heteroarylalkyl, alkenyl, aralkenyl, alkynyl, alkoxycarbonyl, alkanesulfonyl, arenesulfonyl, alkanyloxycarbonyl, aralkyloxycarbonyl, aryloxycarbonyl, heterocyclylalkyl, carbamyl, dithiocarboxyl moieties of R, R and R comprise from 1 to 15 carbon atoms, and are optionally substituted with one or more substituents selected from halogen, cyano, carboxyl, carboxylic acyl, carbamyl, alkoxycarbonyl, alkoxy, alkylenedioxy, hydroxy, nitro, haloalkyl, alkyl, amino, acylamino, imidate and phosphonato groups; or an acid addition salt, quaternary ammonium salt or N -oxide derived therefrom; or an effective amount of a composition comprising a compound of formula (I), as hereinbefore defined, and an insecticidally, acaricidally or nematocidally acceptable carrier or diluent therefor. In other aspects the invention concerns compositions comprising a compound of formula (I), certain compounds of formula (I) and processes for making said compounds.

    Abstract translation: 本发明涉及一种防治昆虫，螨虫或线虫害虫的方法，其包括用有效量的式（I）化合物处理所述害虫或所述害虫的场所，其中A是WXC-CYZ或XC = CY; R是氢，甲酰基或氰基或选自烷基，芳基，杂芳基，芳烷基，杂芳基烷基，烯基，芳烯基，炔基，烷氧基羰基，链烷磺酰基，芳烃磺酰基，烯氧基羰基，芳烷氧基羰基，芳氧基羰基，杂环基烷基，氨基甲酰基，二硫代羧基或X'R （其中X'表示氧或基团NR 4），条件是当R是烯基时，所述基团不具有与式（I）的环氮直接键合的不饱和碳原子。 Ar是任选取代的苯基或任选取代的含有1至3个选自氮，氧和硫原子的杂原子的5或6元杂环系统，以及环中相邻原子之间的至少一个不饱和键（双键） 所述杂环任选地与苯环稠合，其中取代基（如果存在的话）选自卤素原子，氰基，烷基，烯基，炔基，烷氧基，卤代烷基，卤代烯基，烷硫基和烷基氨基， 至6个碳原子; W，X，Y和Z独立地为氢，羟基，酰氧基，烷氧基，烷基甲硅烷氧基，氰基或卤素; R 3，R 3和R 4的烷基部分含有1至15个碳原子，并且任选地被一个或多个选自卤素，氰基，羧基，羧基酰基，氨基甲酰基，烷氧基羰基，烷氧基，亚烷基二氧基， 羟基，硝基，氨基，酰氨基，亚胺基和膦酸基; 芳基，杂芳基，芳烷基，杂芳基烷基，烯基，芳烯基，炔基，烷氧基羰基，烷磺酰基，芳烃磺酰基，烷氧基羰基，芳烷氧基羰基，芳氧基羰基，杂环基烷基，氨基甲酰基，R 3，R 3和R 4的二硫代羧基部分包含1至15个碳 氰基，羧基，羧基酰基，氨基甲酰基，烷氧基羰基，烷氧基，亚烷基二氧基，羟基，硝基，卤代烷基，烷基，氨基，酰氨基，亚氨酸酯和膦酸酯基中的一个或多个取代基任选取代。 或由其衍生的酸加成盐，季铵盐或N，N-氧化物; 或有效量的包含如上文所定义的式（I）化合物的组合物和杀虫，杀螨剂或杀线虫可接受的载体或稀释剂。 在其它方面，本发明涉及包含式（I）化合物，某些式（I）化合物和制备所述化合物的方法的组合物。

    SCREENING ASSAY FOR THE IDENTIFICATION OF INHIBITORS OF MACROPHAGE MIGRATION INHIBITORY FACTOR
    75.
    发明申请
    SCREENING ASSAY FOR THE IDENTIFICATION OF INHIBITORS OF MACROPHAGE MIGRATION INHIBITORY FACTOR 审中-公开
    用于识别大量移动抑制因子抑制剂的筛选测定

    公开(公告)号：WO1997029635A1

    公开(公告)日：1997-08-21

    申请号：PCT/US1997002448

    申请日：1997-02-14

    Applicant: PICOWER INSTITUTE FOR MEDICAL RESEARCH

    Inventor： PICOWER INSTITUTE FOR MEDICAL RESEARCH ,  BUCALA, Richard ,  ULRICH, Peter, C. ,  XHANG, Xini ,  CERAMI, Anthony ,  BENDRAT, Klaus

    IPC: A01N43/34

    CPC classification number: A61K31/404 ,  A61K38/00 ,  C07K14/52

    Abstract: There is disclosed assays to identify compounds that inhibit an enzymatic activity of MIF (macrophage migration inhibitory factor). The enzyme activity catalyzes a tautomerization of MIF-substrates, such as D-dopachrome to DHICA. In general, the assay is conducted in vitro by adding, mixing or combining MIF polypeptide and a suitable substrate in the presence or absence of a test compound, and measuring the tautomerization of the substrate. The test compounds that inhibit tautomerization in the assay are identified as MIF inhibitors.

    Abstract translation: 公开了鉴定抑制MIF的酶活性（巨噬细胞迁移抑制因子）的化合物的测定法。 酶活性催化MIF-底物的互变异构，例如D-多巴色素到DHICA。 通常，通过在存在或不存在测试化合物的情况下通过加入，混合或组合MIF多肽和合适的底物并测量底物的互变异构体进行测定。 在测定中抑制互变异构化的测试化合物被鉴定为MIF抑制剂。

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