2-Phenylindole derivatives, their use as complement inhibitors
    11.
    发明授权
    2-Phenylindole derivatives, their use as complement inhibitors 失效
    2-苯基吲哚衍生物,它们用作补体抑制剂

    公开(公告)号:US4510158A

    公开(公告)日:1985-04-09

    申请号:US586377

    申请日:1984-03-05

    申请人: Denis M. Bailey

    发明人: Denis M. Bailey

    IPC分类号: C07D209/18 A61K31/40

    CPC分类号: C07D209/18

    摘要: 4-(1-R'-2-phenyl-1H-indol-3-yl)-3-cyclohexene-1-carboxylic acids, 4-(1'R'-2-phenyl-1H-indol-3-yl)cyclohexane-1-carboxylic acids, 4-(1-R'-2-phenyl-1H-indol-3-yl)benzoic acids, the corresponding cyclohexene- and cyclohexane-1,1-dicarboxylic acids, and lower-alkyl esters thereof, wherein R' is hydrogen or lower-alkyl, are prepared by reacting a 1-R'-2-phenyl-1H-indole with a cyclohexanone-4-carboxylic acid or -4,4-dicarboxylic acid, followed as desired by a hydrogenation or aromatization process. The compounds which are free carboxylic acids or salts thereof are useful as complement inhibitors. The corresponding esters are useful as intermediates.

    摘要翻译: 4-(1-R'-2-苯基-1H-吲哚-3-基)-3-环己烯-1-羧酸,4-(1'R'-2-苯基-1H-吲哚-3-基) 环己烷-1-羧酸,4-(1-R'-2-苯基-1H-吲哚-3-基)苯甲酸,相应的环己烯和环己烷-1,1-二羧酸及其低级烷基酯 其中R'是氢或低级烷基,是通过使1-R'-2-苯基-1H-吲哚与环己酮-4-羧酸或-4,4-二羧酸反应来制备的,随后根据需要由 氢化或芳构化过程。 作为游离羧酸或其盐的化合物可用作补体抑制剂。 相应的酯可用作中间体。

    Pyrrolyl oxyphenyl ketones
    12.
    发明授权
    Pyrrolyl oxyphenyl ketones 失效
    吡咯烷基酮

    公开(公告)号:US4000160A

    公开(公告)日:1976-12-28

    申请号:US567592

    申请日:1975-04-14

    申请人: Denis M. Bailey

    发明人: Denis M. Bailey

    CPC分类号: C07D207/333 C07D207/34

    摘要: 4,5-Dihalopyrrol-2-yl oxyphenyl ketones, prepared either by Friedel-Crafts condensation of a 4,5-dihalopyrrole-2-carboxylic acid halide with an appropriate hydroxy or lower-alkoxy-substituted benzene or by condensation of a hydroxy or lower-alkoxy-substituted benzaldehyde with pyrrole in the presence of sodium hydride followed by halogenation, with elemental chlorine or bromine, of the resulting pyrrol-2-yl oxyphenyl ketone, useful as antibacterial and antifungal agents.

    Antimicrobial and plant-active 4,5-dihalopyrrole-2-carbonitriles
    13.
    发明授权
    Antimicrobial and plant-active 4,5-dihalopyrrole-2-carbonitriles 失效
    抗菌和植物活性的4,5-二卤代吡咯-2-碳腈

    公开(公告)号:US3932458A

    公开(公告)日:1976-01-13

    申请号:US443740

    申请日:1974-02-19

    申请人: Denis M. Bailey

    发明人: Denis M. Bailey

    IPC分类号: C07D207/34 C07D207/46

    CPC分类号: C07D207/34

    摘要: Phytoresponsive and antimicrobial compositions containing, as the active ingredient, a 4,5-dihalopyrrole-2-carbonitrile and methods of combatting microorganisms and plant growth comprising applying an effective antimicrobial or phytotoxic quantity of the active ingredient to a surface to be disinfected or to undesirable plant growth.

    摘要翻译: 含有作为活性成分的4,5-二卤代吡咯-2-腈的植物保护和抗微生物组合物以及与微生物和植物生长相抵消的方法,包括将有效的抗微生物剂或植物毒性量的活性成分施用于待消毒的表面或不期望的 植物生长。

    Substituted aminophenylalkyl ketones, their preparation and use
    15.
    发明授权
    Substituted aminophenylalkyl ketones, their preparation and use 失效
    取代的氨基苯基烷基酮,其制备和用途

    公开(公告)号:US4539429A

    公开(公告)日:1985-09-03

    申请号:US512791

    申请日:1983-07-11

    申请人: Denis M. Bailey

    发明人: Denis M. Bailey

    IPC分类号: C07C87/50

    CPC分类号: C07C225/22

    摘要: Novel lower-alkyl 2-(hydroxyphenylamino)phenyl ketones, useful as inhibitors of lipoxygenase activity, are of the formula ##STR1## wherein R is hydrogen, lower-alkyl, lower-alkoxy or halo; R' is hydrogen or lower-alkyl; R" is hydrogen, lower-alkyl or halo; and Alk is lower-alkyl. The compounds are prepared by de-etherification of the corresponding alkyl or benzyl ethers which are in turn prepared by reacting a 2-(alkoxy- or benzyloxyphenylamino)benzoic acid with an alkyllithium.

    摘要翻译: 可用作脂氧合酶活性抑制剂的新型低级烷基2-(羟基苯基氨基)苯基酮具有下式:其中R是氢,低级烷基,低级烷氧基或卤素; R'是氢或低级烷基; R“是氢,低级烷基或卤素; 而Alk为低级烷基。 这些化合物是通过相应的烷基或苄基醚的脱醚制备的,其又通过使2-(烷氧基 - 或苄氧基苯基氨基)苯甲酸与烷基锂反应制得。

    Substituted aminobenzamides and their use as agents which inhibit
lipoxygenase activity
    16.
    发明授权
    Substituted aminobenzamides and their use as agents which inhibit lipoxygenase activity 失效
    取代的氨基苯甲酰胺及其用作抑制脂氧合酶活性的试剂

    公开(公告)号:US4510139A

    公开(公告)日:1985-04-09

    申请号:US568870

    申请日:1984-01-06

    申请人: Denis M. Bailey

    发明人: Denis M. Bailey

    摘要: Novel 2-(hydroxyphenylamino)benzamides and oxidation products thereof, useful as inhibitors of lipoxygenase, are of the formulas ##STR1## wherein R is hydrogen, lower-alkyl, halo or lower-alkoxy; R' is hydrogen or lower-alkyl; R" is hydrogen, lower-alkyl or halo; and N.dbd.Z is amino or substituted amino. The compounds of Formula I are prepared by de-etherification of the corresponding alkyl or benzyl ethers; and the compounds of Formula II are prepared by oxidation of the compounds of Formula I where R' is hydrogen and OH is in the 4-position.

    摘要翻译: 可用作脂氧合酶抑制剂的新型2-(羟基苯基氨基)苯甲酰胺及其氧化产物具有下式:其中R是氢,低级烷基,卤素或低级烷氧基; R'是氢或低级烷基; R“是氢,低级烷基或卤素; 并且N = Z是氨基或取代的氨基。 式I的化合物通过相应的烷基或苄基醚的脱醚化来制备; 并且式II化合物通过式Ⅰ化合物的氧化制备,其中R'为氢且OH为4-位。

    1-Amino (or substituted
amino)-1,4-dihydro-4-oxo-6-fluoro-7-heterylquinoline-3-carboxylic acids
and their use as antibacterial agents
    17.
    发明授权
    1-Amino (or substituted amino)-1,4-dihydro-4-oxo-6-fluoro-7-heterylquinoline-3-carboxylic acids and their use as antibacterial agents 失效
    1-氨基(或取代的氨基)-1,4-二氢-4-氧代-6-氟-7-杂环喹啉-3-羧酸及其作为抗菌剂的用途

    公开(公告)号:US4499091A

    公开(公告)日:1985-02-12

    申请号:US466095

    申请日:1983-02-14

    CPC分类号: C07D401/04 C07D215/58

    摘要: Novel 1-R-1,4-dihydro-4-oxo-6-fluoro-7-(Z.dbd.N--)-quinolinecarboxylic acids and esters thereof, where R is amino, lower-alkylamino, 2-propenylamino or di-lower-alkylamino, R" is hydrogen or lower-alkyl, and Z.dbd.N is a heterocyclic group, useful as antibacterial agents, are prepared by reacting the corresponding 7-chloroquinoline derivatives with the appropriate heterocyclic compound, Z.dbd.NH. A preferred group of compounds are those where Z.dbd.N is 1-piperazinyl or 4-lower-alkyl-1-piperazinyl.

    摘要翻译: 新的1-R-1,4-二氢-4-氧代-6-氟-7-(Z = N - ) - 喹啉羧酸及其酯,其中R是氨基,低级烷基氨基,2-丙烯基氨基或二低级 - 烷基氨基,R“是氢或低级烷基,Z = N是可用作抗菌剂的杂环基团,通过使相应的7-氯喹啉衍生物与适当的杂环化合物Z = NH反应来制备。 一组优选的化合物是其中Z = N是1-哌嗪基或4-低级 - 烷基-1-哌嗪基的化合物。