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    Substituted indole-, indene-, pyranoindole- and tetrahydrocarbazole-alkanoic acid derivatives as inhibitors of PLA2 and lipoxygenase
    1.
    发明授权
    Substituted indole-, indene-, pyranoindole- and tetrahydrocarbazole-alkanoic acid derivatives as inhibitors of PLA2 and lipoxygenase 失效
    取代的吲哚，茚，吡喃吲哚和四氢咔唑 - 链烷酸衍生物作为PLA2和脂氧合酶的抑制剂

    公开(公告)号：US5229516A

    公开(公告)日：1993-07-20

    申请号：US911434

    申请日：1992-07-10

    申请人： John H. Musser ,  Anthony F. Kreft, III ,  Amedeo A. Failli ,  Christopher A. Demerson ,  Uresh S. Shah ,  James A. Nelson

    发明人： John H. Musser ,  Anthony F. Kreft, III ,  Amedeo A. Failli ,  Christopher A. Demerson ,  Uresh S. Shah ,  James A. Nelson

    IPC分类号： C07C323/62 ,  C07D209/22 ,  C07D215/14 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12 ,  C07D491/04

    CPC分类号： C07D401/12 ,  C07C323/62 ,  C07D209/22 ,  C07D215/14 ,  C07D401/14 ,  C07D417/12 ,  C07D491/04

    摘要： There are disclosed compounds of the formulaA(CH.sub.2).sub.n O-BwhereinA is C.sub.4 -C.sub.8 alkyl, phenoxyethyl, phenoxyphenyl or a group having the formula ##STR1## wherein ##STR2## R.sup.1 is hydrogen, lower alkyl, phenyl or phenyl substituted with trifluoromethyl;R.sup.2 is hydrogen or lower alkyl; orR.sup.1 and R.sup.2 taken together form a benzene ring;R.sup.3 is hydrogen or lower alkyl;n is 1-2;B is ##STR3## wherein ##STR4## m is 0-3; R.sup.5 is ##STR5## or phenyl or phenyl substituted by halo, lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl;R.sup.6 is A(CH.sub.2).sub.n O-- or halo; with the proviso that when R.sup.6 is halo, R.sup.5 is ##STR6## R.sup.7 is lower alkyl; Y is --CH.sub.2 -- or --O--;R.sup.8 is lower alkyl or --(CH.sub.2).sub.m CO.sub.2 R.sup.3 ;R.sup.9 is ##STR7## or --CH.sub.2 R.sup.10 ; R.sup.10 is lower alkyl, phenyl, phenyl substituted with carboxy, halo, loweralkylthio or loweralkylsulfinyl, pyridyl, furanyl or quinolinyl;R.sup.11 is lower alkyl or phenyl;Z is hydrogen, lower alkyl or --N(CH.sub.3)OH;and the pharmacologically acceptable salts thereof, and their use in the treatment of inflammatory conditions, such as rheumatoid arthritis, ulcerative colitis, psoriasis and other immediate hypersensitivity reactions; in the treatment of leukotriene-mediated naso-bronchial obstructive air-passageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like; and as gastric cytoprotective agents.

    摘要翻译： 公开了式A（CH 2）n O-B的化合物，其中A是C 4 -C 8烷基，苯氧基乙基，苯氧基苯基或具有下式的基团：其中R 1是氢，低级烷基 ，苯基或被三氟甲基取代的苯基; R2是氢或低级烷基; 或R 1和R 2一起形成苯环; R3是氢或低级烷基; n为1-2; B是 其中 m是0-3; R 5为苯基或被卤素，低级烷硫基，低级烷基亚磺酰基或低级烷基磺酰基取代的苯基; R6是A（CH2）nO-或卤素; 条件是当R 6为卤素时，R 5为低级烷基; Y是-CH 2 - 或-O-; R8是低级烷基或 - （CH2）mCO2R3; R9是或-CH2R10; R 10为低级烷基，苯基，被羧基，卤素，低级烷硫基或低级烷基亚磺酰基取代的苯基，吡啶基，呋喃基或喹啉基; R11为低级烷基或苯基; Z是氢，低级烷基或-N（CH 3）OH; 及其药理学上可接受的盐及其在治疗炎性病症如类风湿性关节炎，溃疡性结肠炎，牛皮癣和其他立即超敏反应中的用途; 治疗白三烯介导的鼻支气管阻塞性通气条件，如过敏性鼻炎，过敏性支气管哮喘等; 和作为胃细胞保护剂。

    2-Anilino phenylacetic acid derivatives
    6.
    发明授权
    2-Anilino phenylacetic acid derivatives 失效
    2-苯胺基苯乙酸衍生物

    公开(公告)号：US5021576A

    公开(公告)日：1991-06-04

    申请号：US428092

    申请日：1989-10-27

    申请人： Amedeo A. Failli ,  Anthony F. Kreft, III ,  John H. Musser

    发明人： Amedeo A. Failli ,  Anthony F. Kreft, III ,  John H. Musser

    IPC分类号： A61K31/165 ,  A61K31/19 ,  A61K31/215 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/47 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07C229/40 ,  C07C229/42 ,  C07D209/34 ,  C07D215/14 ,  C07D215/18 ,  C07D235/12 ,  C07D235/16 ,  C07D401/04 ,  C07D401/12 ,  C07D521/00

    CPC分类号： C07D401/04 ,  C07C229/42 ,  C07D215/14 ,  C07D215/18 ,  C07D235/12

    摘要： There are disclosed compounds of the formula ##STR1## wherein R is hydroxy, lower alkoxy or lower alkoxyamino;R.sup.1 is hydrogen or A(CH.sub.2).sub.n O--;R.sup.2 is hydrogen or A(CH.sub.2).sub.n O--, with the proviso that one of R.sup.1 and R.sup.2 is A(CH.sub.2).sub.n O-- and the other is hydrogen;n is 1-2;A is phenoxyethyl, phenoxyphenyl or a group having the formula ##STR2## X is --N-- or ##STR3## Z is ##STR4## R.sup.3 is hydrogen, lower alkyl or phenyl; R.sup.4 is hydrogen or lower alkyl; orR.sup.3 and R.sup.4 taken together form a benzene ring;R.sup.5 is hydrogen or lower alkyl;R.sup.6 is hydrogen, halo or lower alkyl;and the pharmacologically acceptable salts thereof, and their use in the treatment of inflammatory conditions, such as rheumatoid arthritis, ulcerative colitis, psoriasis and other immediate hypersensitivity reactions; in the treatment of leukotriene-mediated naso-bronchial obstructive air-passageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like; and as gastric cytoprotective agents.

    摘要翻译： 公开了下式的化合物：其中R是羟基，低级烷氧基或低级烷氧基氨基; R1是氢或A（CH2）nO-; R2是氢或A（CH2）nO-，条件是R1和R2之一是A（CH2）nO-，另一个是氢; n为1-2; A是苯氧基乙基，苯氧基苯基或具有下式的基团X是-N-或Z是R 3是氢，低级烷基或苯基; R4是氢或低级烷基; 或R3和R4一起形成苯环; R5是氢或低级烷基; R6是氢，卤素或低级烷基; 及其药理学上可接受的盐及其在治疗炎性病症如类风湿性关节炎，溃疡性结肠炎，牛皮癣和其他立即超敏反应中的用途; 治疗白三烯介导的鼻支气管阻塞性通气条件，如过敏性鼻炎，过敏性支气管哮喘等; 和作为胃细胞保护剂。

    2-anilino phenylacetic acid derivatives as inhibitors of PLA.sub.2 and lipoxygenase
    7.
    发明授权
    2-anilino phenylacetic acid derivatives as inhibitors of PLA.sub.2 and lipoxygenase 失效
    2-苯胺基苯乙酸衍生物作为PLA2和脂氧合酶的抑制剂

    公开(公告)号：US5159085A

    公开(公告)日：1992-10-27

    申请号：US667732

    申请日：1991-04-04

    申请人： Amedeo A. Failli ,  Anthony F. Kreft, III ,  John H. Musser

    发明人： Amedeo A. Failli ,  Anthony F. Kreft, III ,  John H. Musser

    IPC分类号： C07C229/42 ,  C07D215/14 ,  C07D215/18 ,  C07D235/12 ,  C07D401/04

    CPC分类号： C07D401/04 ,  C07C229/42 ,  C07D215/14 ,  C07D215/18 ,  C07D235/12

    摘要： There are disclosed compounds of the formula ##STR1## wherein R is hydroxy, lower alkoxy or lower alkoxyamino;R.sup.1 is hydrogen or A(CH.sub.2).sub.n O--;R.sup.2 is hydrogen or A(CH.sub.2).sub.n O--, with the proviso that one of R.sup.1 and R.sup.2 is hydrogen;n is 1-2;A is phenoxyethyl, phenoxyphenyl or a group having the formula ##STR2## R.sup.3 is hydrogen, lower alkyl or phenyl; R.sup.4 is hydrogen or lower alkyl; orR.sup.3 and R.sup.4 taken together form a benzene ring;R.sup.5 is hydrogen or lower alkyl;R.sup.6 is hydrogen, halo or lower alkyl;and the pharmacologically acceptable salts thereof, and their use in the treatment of inflammatory conditions, such as rheumatoid arthritis, ulcerative colitis, psoriasis and other immediate hypersensitivity reactions; in the treatment of leukotriene-mediated naso-bronchial obstructive air-passageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like; and as gastic cytoprotective agents.

    摘要翻译： 公开了下式的化合物：其中R是羟基，低级烷氧基或低级烷氧基氨基; R1是氢或A（CH2）nO-; R2是氢或A（CH2）nO-，条件是R1和R2之一是氢; n为1-2; A是苯氧基乙基，苯氧基苯基或具有下式的基团：R 3是氢，低级烷基或苯基; R4是氢或低级烷基; 或R3和R4一起形成苯环; R5是氢或低级烷基; R6是氢，卤素或低级烷基; 及其药理学上可接受的盐及其在治疗炎性病症如类风湿性关节炎，溃疡性结肠炎，牛皮癣和其他立即超敏反应中的用途; 治疗白三烯介导的鼻支气管阻塞性通气条件，如过敏性鼻炎，过敏性支气管哮喘等; 和作为胶质细胞保护剂。

    Substituted 1-aryl-3-heteroaryl-thioureas and substituted 1-aryl-3-heteroaryl-isothioureas as antiatherosclerotic agents
    9.
    发明授权
    Substituted 1-aryl-3-heteroaryl-thioureas and substituted 1-aryl-3-heteroaryl-isothioureas as antiatherosclerotic agents 失效
    新型取代的1-芳基-3-杂芳基硫脲和取代的1-芳基-3-杂芳基 - 异硫脲作为抗动脉粥样硬化剂

    公开(公告)号：US06686476B2

    公开(公告)日：2004-02-03

    申请号：US10212888

    申请日：2002-08-06

    申请人： Robert J. Steffan ,  Amedeo A. Failli

    发明人： Robert J. Steffan ,  Amedeo A. Failli

    IPC分类号： C07D27728

    CPC分类号： C07D275/03 ,  A61K31/415 ,  C07D231/40 ,  C07D263/48 ,  C07D277/48 ,  C07D277/82 ,  C07D277/84 ,  C07D285/135

    摘要： Antiatherosclerotic agents are provided which are represented by Formulas I or II: wherein R is wherein R9, R10, R11, R12, R13, and R14 are each, independently, hydrogen or a lower alkyl of 1-6 carbon atoms; R6, and R7 are each, independently, hydrogen, lower alkyl of 1-6 carbon atoms, or CH2COOR8, where R8 is a lower alkyl of 1-6 carbon atoms; and X is O or S; R1 is hydrogen or a lower alkyl of 1-6 carbon atoms; R2, R3, and R4 are each, independently, hydrogen or halogen; and R5 is a lower alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 提供由式I或II表示的抗动脉粥样硬化剂：其中R在其中R 9，R 10，R 11，R 12，R 13和R 14各自独立地为氢或1-6个碳原子的低级烷基; R 6和R 7各自为 独立地是氢，1-6个碳原子的低级烷基或CH2COOR8，其中R8是1-6个碳原子的低级烷基; 且X为O或S; R 1为氢或1-6个碳原子的低级烷基; R 2，R 3和R 4各自独立地为氢或卤素; 和R 5是1-6个碳原子的低级烷基;或其药学上可接受的盐。