ANAPHYLATOXIN RECEPTOR LIGANDS CONTAINING LIPOPHILIC RESIDUES
    211.
    发明申请
    ANAPHYLATOXIN RECEPTOR LIGANDS CONTAINING LIPOPHILIC RESIDUES 审中-公开
    含有脂肪酸残基的氨基磷酸酯受体配体

    公开(公告)号:WO1994007518A1

    公开(公告)日:1994-04-14

    申请号:PCT/US1993008246

    申请日:1993-09-01

    CPC classification number: C07K7/06 A61K38/00 C07K14/472

    Abstract: Oligopeptide compounds or oligopeptide analogue compounds of the formula A-B-D-E-G-J-L-M-Arg-OH are ligands for the anaphylatoxin receptor and are useful in the treatment of inflammatory disease states; also disclosed are anaphylatoxin receptor ligand compositions and a method for modulating anaphylatoxin activity.

    Abstract translation: 式A-B-D-E-G-J-L-M-Arg-OH的寡肽化合物或寡肽类似物化合物是过敏毒素受体的配体,可用于治疗炎性疾病状态; 还公开了过敏毒素受体配体组合物和调节过敏毒素活性的方法。

    ETHER-CONTAINING INHIBITORS OF 5-LIPOXYGENASE
    213.
    发明申请
    ETHER-CONTAINING INHIBITORS OF 5-LIPOXYGENASE 审中-公开
    含有5-LIPOXYGENASE的含有抑制剂

    公开(公告)号:WO1994004528A1

    公开(公告)日:1994-03-03

    申请号:PCT/US1993006914

    申请日:1993-07-23

    CPC classification number: C07D405/12 C07D309/10

    Abstract: Compounds of structure (I) where Ar is optionally substituted carboxyclic aryl, 5- or 6-membered heterocyclic aryl, 10-membered bicyclic heterocyclic aryl containing one or two nitrogen atoms, 9- or 10-membered heterocyclic containing one or two nitrogen atoms and optionally containing a further nitrogen or oxygen atom and one oxo or thioxo substituent, benzo(b)furyl, or benzo(b)thienyl, A1 is propynyl, methylene, or a direct link to X, X is oxy, thio, sulfonyl, or NR4, A2 is selected from (II) and (III) where Y is hydrogen, halogen, or nitrile; Z is hydrogen, R1 is alkyl, and R2 is hydrogen or alkyl are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.

    Abstract translation: 其中Ar为任选取代的羧基芳基,5-或6-元杂环芳基,含有一个或两个氮原子的10元双环杂环芳基,含有一个或两个氮原子的9元或10元杂环的结构(I) 任选地含有另外的氮或氧原子和一个氧代或硫代取代基,苯并(b)呋喃基或苯并(b)噻吩基,A1是丙炔基,亚甲基或与X的直接连接,X是氧基,硫代,磺酰基或 NR4,A2选自(II)和(III)其中Y是氢,卤素或腈; Z是氢,R1是烷基,R2是氢或烷基是脂氧合酶的有效抑制剂,从而抑制白细胞三烯的生物合成。 这些化合物可用于治疗或改善过敏性和炎性疾病状态。

    PYRIDINIUM INTERMEDIATES AND THE PROCESS FOR PREPARING THE SAME
    214.
    发明申请
    PYRIDINIUM INTERMEDIATES AND THE PROCESS FOR PREPARING THE SAME 审中-公开
    PYRIDIIUM中间体及其制备方法

    公开(公告)号:WO1994004502A1

    公开(公告)日:1994-03-03

    申请号:PCT/US1993007521

    申请日:1993-08-11

    Abstract: A process for the preparation of halobenzoic acids, comprising the step of reacting a halonitrobenzene with a pyridinium salt to form an intermediate of formula (I), wherein R is selected from the group consisting of hydrogen, alkyl, aryl, alkenyl, alkynyl, -CN, -COOR' and -COR' where R' is alkyl or aryl; X is chloro or fluoro; Y is hydrogen, chloro or fluoro; and Z is chloro, bromo or iodo.

    Abstract translation: 一种制备卤代苯甲酸的方法,包括使卤代硝基苯与吡啶鎓盐反应形成式(I)的中间体的步骤,其中R选自氢,烷基,芳基,烯基,炔基, CN,-COOR'和-COR',其中R'是烷基或芳基; X是氯或氟; Y是氢,氯或氟; Z是氯,溴或碘。

    ANTIFUNGAL COMPOUNDS
    218.
    发明申请
    ANTIFUNGAL COMPOUNDS 审中-公开
    抗真菌化合物

    公开(公告)号:WO1993021770A1

    公开(公告)日:1993-11-11

    申请号:PCT/US1993003617

    申请日:1993-04-16

    CPC classification number: C12R1/80 C07C69/732 C07D311/92 C12P7/62 C12P17/06

    Abstract: Novel compounds having structural formula (I) and pharmaceutically acceptable salts and prodrugs thereof, wherein one of R and R is hydrogen and the other is -CH=CHCOOH, X is >CH-, and Y is -O-; or, alternatively, the bond between X and Y is not present, X is -CH2-, and Y is -OH, as well as methods for their use, pharmaceutical compositions containing the same, and a process for their preparation via fermentation.

    Abstract translation: 具有结构式(I)的新型化合物及其药学上可接受的盐和前药,其中R 1和R 2之一是氢,另一个是-CH = CHCOOH,X是> CH-,Y是-O - ; 或者,X和Y之间的键不存在,X是-CH 2 - ,Y是-OH,以及它们的使用方法,含有它们的药物组合物,以及通过发酵制备的方法。

    HAPTENS, TRACERS, IMMUNOGENS AND ANTIBODIES FOR QUINOLINE
    220.
    发明申请
    HAPTENS, TRACERS, IMMUNOGENS AND ANTIBODIES FOR QUINOLINE 审中-公开
    HAPTENS,TRACERS,IMMUNOGENS AND ANTIBODIES FOR QUINOLINE

    公开(公告)号:WO1993020094A1

    公开(公告)日:1993-10-14

    申请号:PCT/US1993002899

    申请日:1993-03-26

    Abstract: Novel haptens and related conjugates based on quinoline, as well as methods for making and using such conjugates. Haptens based on the above core structure may be substituted at positions 5 and 8. Using intermediates with a tether in the 8 position, immunogens, tracers, solid supports and labeled oligonucleotides are all described; as are methods for using the intermediates to prepare the conjugates, methods of using the conjugates to make and purify antibodies, as assay tracers, and in nucleic acid hybridization assays. Kits containing haptenated oligonucleotides and anti-hapten conjugates are also described.

    Abstract translation: 基于喹啉的新型半抗原和相关缀合物,以及制备和使用这些缀合物的方法。 基于上述核心结构的半抗原可以在5和8位被取代。使用具有8位的系链的中间体,免疫原,示踪剂,固体支持物和标记的寡核苷酸都被描述; 以及使用中间体制备缀合物的方法,使用缀合物制备和纯化抗体的方法,作为测定示踪剂以及核酸杂交测定法。 还描述了含有半抗体的寡核苷酸和抗半抗原缀合物的试剂盒。

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