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114 条记录 (耗时 0.032 秒)

    2-Oxo-1,3-oxazolo[4,5-h] quinolines useful as anti-allergy agents
    1.
    发明授权
    2-Oxo-1,3-oxazolo[4,5-h] quinolines useful as anti-allergy agents 失效
    可用作抗过敏剂的2-氧代-1,3-恶唑并[4,5-h]喹啉

    公开(公告)号：US4563463A

    公开(公告)日：1986-01-07

    申请号：US667667

    申请日：1984-11-02

    申请人： John H. Musser ,  Richard E. Brown

    发明人： John H. Musser ,  Richard E. Brown

    IPC分类号： C07D215/28 ,  C07D498/04 ,  A61K31/47

    CPC分类号： C07D215/28

    摘要： New quinoline compound, and the corresponding 1,2-; 1,3-; and 1,4-benzodiazines, the quinoline compounds being of the formulae: ##STR1## and salts thereof, wherein R is hydrogen, acyl, carboethoxy,(3-methoxyphen)acetyl,(2-phenyl)propionyl, dimethylcarbamoyl or methyl,R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, halo, trifluoromethyl, amino, lower alkyl amino, lower acylamino, cyano, aryl, aryl/lower alkylene, nitro, lower alkynyl, lower alkenyl, lower alkyl sulfinyl, lower alkyl sulfonyl, lower alkoxycarbonyl, carboxyl, lower alkoxy, lower alkanoyl, or lower alkenoyl,Y is oxygen, sulfur, nitrogen or R.sub.3 N wherein R.sub.3 is hydrogen, lower alkyl, alkenyl, alkynyl, aryl, aralkyl, acyl, aminoalkyl, or carboxyalkyl,Z is oxygen, sulfur or nitrogen,X is cyano, carbalkoxy, carboxyl, formyloximino, tetrazolyl, carbalkoxyalkyl or carboxyalkyl, andm is 0 or 1, are useful as medicinals, especially for treatment of asthma, and/or as intermediates in the preparation of compounds useful for treating asthma.

    摘要翻译： 新喹啉化合物及相应的1,2-; 1,3- 其中R为氢，酰基，乙酰乙氧基，（3-甲氧基苯基）乙酰基，（2-苯基）丙酰基，二甲基氨基甲酰基或甲基，R 1，R 2， 氰基，芳基，芳基/低级亚烷基，硝基，低级炔基，低级烯基，低级烷基亚磺酰基，低级烷基磺酰基，低级烷氧基羰基，低级烷基氨基，低级烷基氨基， 羧基，低级烷氧基，低级烷酰基或低级烯酰基，Y是氧，硫，氮或R3N，其中R3是氢，低级烷基，烯基，炔基，芳基，芳烷基，酰基，氨基烷基或羧基烷基，Z是氧，硫或 氮，X为氰基，烷氧羰基，羧基，甲酰肟基，四唑基，碳烷氧基烷基或羧基烷基，m为0或1，可用作药物，特别是用于治疗哮喘，和/或作为制备用于治疗哮喘的化合物的中间体 。

    Thiazolo[5,4-h]quinoline compounds useful as anti-allergy agents
    2.
    发明授权
    Thiazolo[5,4-h]quinoline compounds useful as anti-allergy agents 失效
    噻唑并[5,4-h]喹啉化合物可用作抗过敏剂

    公开(公告)号：US4698346A

    公开(公告)日：1987-10-06

    申请号：US889021

    申请日：1986-07-24

    申请人： John H. Musser ,  Richard E. Brown

    发明人： John H. Musser ,  Richard E. Brown

    IPC分类号： C07D215/28 ,  C07D498/04 ,  A61K31/425 ,  C07D513/04

    CPC分类号： C07D215/28

    摘要： New quinoline compound, and the corresponding 1,2-; 1,3-; and 1,4-benzodiazines, the quinoline compounds being of the formula: ##STR1## and salts thereof, wherein R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, halo, trifluoromethyl, amino, lower alkyl amino, lower acylamino, cyano, aryl, aryl/lower alkylene, nitro, lower alkynyl, lower alkenyl, lower alkyl sulfinyl, lower alkyl sulfonyl, lower alkoxycarbonyl, carboxyl, lower alkoxy, lower alkanoyl, or lower alkenoyl,Y is oxygen, sulfur, nitrogen or R.sub.3 N wherein R.sub.3 is hydrogen, lower alkyl, alkenyl, alkynyl, aryl, aralkyl, acyl, aminoalkyl, or carboxyalkyl,Z is oxygen, sulfur or nitrogen,X is cyano, carbalkoxyl, carboxyl, formyloximino, tetrazolyl, carbalkoxyalkyl or carboxyalkyl, andm is 0 or 1, are useful as medicinals, especially for treatment of asthma, and/or as intermediates in the preparation of compounds useful for treating asthma.

    摘要翻译： 新喹啉化合物及相应的1,2-; 1,3- 和1,4-苯并二嗪，喹啉化合物具有下式：其中R1和R2独立地是氢，低级烷基，卤素，三氟甲基，氨基，低级烷基氨基，低级酰氨基，氰基，芳基 ，芳基/低级亚烷基，硝基，低级炔基，低级烯基，低级烷基亚磺酰基，低级烷基磺酰基，低级烷酰基，羧基，低级烷氧基，低级烷酰基或低级烯酰基，Y为氧，硫，氮或R 3 N，其中R 3为氢 低级烷基，烯基，炔基，芳基，芳烷基，酰基，氨基烷基或羧基烷基，Z是氧，硫或氮，X是氰基，烷氧羰基，羧基，甲酰肟基，四唑基，烷氧基烷基或羧基烷基，m是0或1， 可用作药物，特别是用于治疗哮喘，和/或作为制备用于治疗哮喘的化合物的中间体。

    Imidazo quinoline compounds useful as anti-allergy agents
    3.
    发明授权
    Imidazo quinoline compounds useful as anti-allergy agents 失效
    咪唑喹啉化合物可用作抗过敏剂

    公开(公告)号：US4656281A

    公开(公告)日：1987-04-07

    申请号：US731689

    申请日：1985-05-08

    申请人： John H. Musser ,  Richard E. Brown

    发明人： John H. Musser ,  Richard E. Brown

    IPC分类号： C07D215/28 ,  C07D498/04 ,  C07D471/04

    CPC分类号： C07D215/28

    摘要： The quinoline compounds being of the formula: ##STR1## and salts thereof, wherein R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, halo, trifluoromethyl, amino, lower alkyl amino, lower acylamino, cyano, aryl, aryl/lower alkylene, nitro, lower alkynyl, lower alkenyl, lower alkyl sulfinyl, lower alkyl sulfonyl, lower alkoxycarbonyl, carboxyl, lower alkoxy, lower alkanoyl, or lower alkenoyl,Y is nitrogen or R.sub.3 N wherein R.sub.3 is hydrogen, lower alkyl, alkenyl, alkynyl, aryl aralkyl, acyl, aminoalkyl, or carboxyalkyl,Z is nitrogen,X is cyano, carbalkoxyl, carboxyl, formyloximino, tetrazolyl, carbalkoxyalkyl or carboxyalkyl, andm is 0 or 1, are useful as medicinals, especially for treatment of asthma, and/or intermediates in the preparation of compounds useful for treating asthma.

    摘要翻译： 喹啉化合物具有下式：其中R1和R2独立地是氢，低级烷基，卤素，三氟甲基，氨基，低级烷基氨基，低级酰氨基，氰基，芳基，芳基/低级亚烷基，硝基 低级炔基，低级烯基，低级烷基亚磺酰基，低级烷基磺酰基，低级烷氧基羰基，羧基，低级烷氧基，低级烷酰基或低级烯酰基，Y为氮或R3N，其中R3为氢，低级烷基，烯基，炔基，芳基芳烷基， 酰基，氨基烷基或羧基烷基，Z是氮，X是氰基，甲酰氧基，羧基，甲酰肟基，四唑基，烷氧基烷基或羧基烷基，m是0或1，可用作药物，特别是用于治疗哮喘和/ 可用于治疗哮喘的化合物的制备。

    Certain 1,3-oxazolo[4,5H]quinolines useful as anti-allergy agents
    4.
    发明授权
    Certain 1,3-oxazolo[4,5H]quinolines useful as anti-allergy agents 失效
    某些用作抗过敏剂的1,3-恶唑并[4,5H]喹啉

    公开(公告)号：US4522947A

    公开(公告)日：1985-06-11

    申请号：US476673

    申请日：1983-03-18

    申请人： John H. Musser ,  Richard E. Brown

    发明人： John H. Musser ,  Richard E. Brown

    IPC分类号： C07D215/28 ,  C07D498/04 ,  A61K31/47

    CPC分类号： C07D215/28

    摘要： New quinoline compound, and the corresponding 1,2-; 1,3-; and 1,4-benzodiazines, the quinoline compounds being of the formula: ##STR1## and salts thereof, wherein R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, halo, trifluoromethyl, amino, lower alkyl amino, lower acylamino, cyano, aryl, aryl/lower alkylene, nitro, lower alkynyl, lower alkenyl, lower alkyl sulfinyl, lower alkyl sulfonyl, lower alkoxycarbonyl, carboxyl, lower alkoxy, lower alkanoyl, or lower alkenoyl,Y is oxygen, sulfur, nitrogen or R.sub.3 N wherein R.sub.3 is hydrogen, lower alkyl, alkenyl, alkynyl, aryl, aralkyl, acyl, aminoalkyl, or carboxyalkyl,Z is oxygen, sulfur or nitrogen,X is cyano, carbalkoxyl, carboxyl, formyloximino, tetrazolyl, carbalkoxyalkyl or carboxyalkyl, andm is 0 or 1, are useful as medicinals, especially for treatment of asthma, and/or as intermediates in the preparation of compounds useful for treating asthma.

    摘要翻译： 新喹啉化合物及相应的1,2-; 1,3- 和1,4-苯并二嗪，喹啉化合物具有下式：其中R1和R2独立地是氢，低级烷基，卤素，三氟甲基，氨基，低级烷基氨基，低级酰氨基，氰基，芳基 ，芳基/低级亚烷基，硝基，低级炔基，低级烯基，低级烷基亚磺酰基，低级烷基磺酰基，低级烷酰基，羧基，低级烷氧基，低级烷酰基或低级烯酰基，Y为氧，硫，氮或R 3 N，其中R 3为氢 低级烷基，烯基，炔基，芳基，芳烷基，酰基，氨基烷基或羧基烷基，Z是氧，硫或氮，X是氰基，烷氧羰基，羧基，甲酰肟基，四唑基，烷氧基烷基或羧基烷基，m是0或1， 可用作药物，特别是用于治疗哮喘，和/或作为制备用于治疗哮喘的化合物的中间体。

    Uses of diterpenoid triepoxides as an anti-proliferative agent
    8.
    发明授权
    Uses of diterpenoid triepoxides as an anti-proliferative agent 失效
    使用二萜类三环氧化物作为抗增殖剂

    公开(公告)号：US06294546B1

    公开(公告)日：2001-09-25

    申请号：US09385917

    申请日：1999-08-30

    申请人： Glenn D. Rosen ,  Edwin S. Lennox ,  John H. Musser

    发明人： Glenn D. Rosen ,  Edwin S. Lennox ,  John H. Musser

    IPC分类号： A61K3144

    CPC分类号： A61K31/704 ,  A61K31/365 ,  A61K31/47 ,  A61K31/555 ,  A61K31/70 ,  A61K45/06 ,  A61K31/335 ,  A61K2300/00

    摘要： Combinations of diterpenoid triepoxides and anti-proliferative agents are used in a combination therapy to treat hyperproliferative disorders. Anti-proliferative agents of interest include agents active in killing tumor cells, as well as immunosuppressants, and a variety of other agents that reduce cellular proliferation in targeted tissues. Synergistic combinations provide for comparable or improved therapeutic effects, while lowering adverse side effects.

    摘要翻译： 在联合治疗中使用二萜类三环氧化物和抗增殖剂的组合来治疗过度增殖性疾病。 感兴趣的抗增殖剂包括杀死肿瘤细胞的活性剂，以及免疫抑制剂，以及减少靶向组织中的细胞增殖的各种其他试剂。 协同组合提供可比较或改善的治疗效果，同时降低不良副作用。

    Substituted indole-, indene-, pyranoindole- and tetrahydrocarbazole-alkanoic acid derivatives as inhibitors of PLA2 and lipoxygenase
    10.
    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。