Antimicrobial N-[1-(alkyl or
arylmethyl)-4(1H)-pyridinylidine]-alkanamines and acid addition salts
thereof and methods of use and compositions thereof
    2.
    发明授权
    Antimicrobial N-[1-(alkyl or arylmethyl)-4(1H)-pyridinylidine]-alkanamines and acid addition salts thereof and methods of use and compositions thereof 失效
    抗菌N- [1-(烷基或芳基甲基)-4(1H) - 吡啶基]] - 烷胺及其酸加成盐及其使用方法及其组合物

    公开(公告)号:US4839372A

    公开(公告)日:1989-06-13

    申请号:US809371

    申请日:1985-12-16

    申请人: Denis M. Bailey

    发明人: Denis M. Bailey

    IPC分类号: A01N43/40 C07D213/74

    CPC分类号: C07D213/74 A01N43/40

    摘要: N-[1-alkyl or arylmethyl)-4(1H)-pyridinylidine]-alkanamine and pharmaceutically acceptable acid addition salts thereof, for example, N-(1-octyl-4(1H)-pyridinylidine)-octanamine monohydrochloride salt, which are useful as antimicrobial agents, especially on living tissues and nonliving surfaces and most especially against pathogenic dental microbes, and a process for perparation, methods of use and compositions thereof are disclosed.

    摘要翻译: N- [1-烷基或芳基甲基)-4(1H) - 吡啶基]] - 胺胺及其药学上可接受的酸加成盐,例如N-(1-辛基-4(1H) - 吡啶基) - 辛胺胺一盐酸盐 可用作抗微生物剂,特别是在活组织和非活性表面上,特别是抗病原性牙科微生物,以及用于发生的方法,使用方法及其组合物。

    Gastric cytoprotection with 3,3'-thiobis[propanoic acid] in oral
administration of aspirin
    3.
    发明授权
    Gastric cytoprotection with 3,3'-thiobis[propanoic acid] in oral administration of aspirin 失效
    在口服阿司匹林时用3,3'-硫代双[丙酸]进行胃细胞保护

    公开(公告)号:US4585764A

    公开(公告)日:1986-04-29

    申请号:US725448

    申请日:1985-04-22

    申请人: Denis M. Bailey

    发明人: Denis M. Bailey

    IPC分类号: A61K31/19 A61K31/61

    CPC分类号: A61K31/60 A61K31/19

    摘要: The method of providing cytoprotection of the gastric mucosa in a mammal receiving aspirin (ASA) perorally which comprises orally administering either prior to or in combination with ASA a cytoprotectively effective amount of 3,3'-thiobis[propanoic acid] (TBPA) or in combination with a pharmaceutically acceptable carrier. Also shown is a composition for providing cytoprotection of the gastric mucosa in a mammal receiving ASA perorally which comprises ASA in combination with a cytoprotectively effective amount of TBPA.

    摘要翻译: 在接受阿斯匹林(ASA)口服哺乳动物的哺乳动物中提供胃粘膜的细胞保护的方法,其包括在ASA或与ASA组合之前口服给予细胞保护有效量的3,3'-硫代双[丙酸](TBPA)或在 与药学上可接受的载体组合。 还显示了用于在接受ASA口服的哺乳动物中提供胃粘膜的细胞保护的组合物,其包含ASA与细胞保护有效量的TBPA的组合。

    Benzyloxy or alkoxy substituted phenylaminobenzamides
    4.
    发明授权
    Benzyloxy or alkoxy substituted phenylaminobenzamides 失效
    苄氧基或烷氧基取代的苯基氨基苯甲酰胺

    公开(公告)号:US4549016A

    公开(公告)日:1985-10-22

    申请号:US690013

    申请日:1985-01-09

    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。

    1,3-Dioxolo(4,5-G)quinoline compounds
    5.
    发明授权
    1,3-Dioxolo(4,5-G)quinoline compounds 失效
    1,3-二氧杂环戊烯(4,5-G)喹啉化合物

    公开(公告)号:US4439436A

    公开(公告)日:1984-03-27

    申请号:US405263

    申请日:1982-08-04

    CPC分类号: C07D491/04

    摘要: Novel 5,8-dihydro-8-oxo-1,3-dioxolo[4,5-g]quinoline-7-carboxylic acids substituted in the 5-position by lower-alkylamino or di-lower-alkylamino, useful as antibacterial agents, are prepared from 8-hydroxy-1,3-dioxolo[4,5-g]quinoline-7-carboxylic acid or a lower-alkyl ester thereof via a series of novel intermediates.

    摘要翻译: 在5位被低级烷基氨基或二低级烷基氨基取代的新颖的5,8-二氢-8-氧代-1,3-二氧杂环戊烯并[4,5-g]喹啉-7-羧酸,可用作抗菌剂 由8-羟基-1,3-二氧杂环戊烯并[4,5-g]喹啉-7-羧酸或其低级烷基酯通过一系列新型中间体制备。

    Substituted aminophenylalkyl ketones, their preparation and use
    8.
    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
    9.
    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
    10.
    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。