(4-alkoxypyran-4-yl) substituted arylalkylaryl-, arylalkenylaryl-, and
arylalkynylarylurea inhibitors of 5-lipoxygenase
    51.
    发明授权
    (4-alkoxypyran-4-yl) substituted arylalkylaryl-, arylalkenylaryl-, and arylalkynylarylurea inhibitors of 5-lipoxygenase 失效
    (4-烷氧基吡喃-4-基)取代的芳烷基芳基 - ,芳基烯基芳基 - 和芳基炔基芳基脲抑制剂5-脂氧合酶

    公开(公告)号:US5346914A

    公开(公告)日:1994-09-13

    申请号:US61988

    申请日:1993-05-14

    CPC分类号: C07D405/12 C07D309/12

    摘要: Compounds of the structure ##STR1## wherein W is selected from ##STR2## where Q is oxygen or sulfur, R.sup.6 and R.sup.7 are hydrogen or alkyl, or R.sup.6 and R.sup.7, together with the nitrogen atoms to which they are attached, define a radical of formula ##STR3## R.sup.8 is selected from hydrogen, alkyl, haloalkyl, optionally substituted phenyl, hydroxyalkyl, aminoalkyl, carboxyalkyl, (alkoxycarbonyl)alkyl, and (alkylaminocarbonyl)alkyl; Z is --CH.sub.2 --, oxygen, sulfur, or --NR.sup.9 where R.sup.9 is hydrogen or alkyl, L.sup.1 and L.sup.2 are selected from a valence bond, alkylene, propenylene, and propynylene, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from alkyl, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl, Y is selected from oxygen, --NR.sup.10, where R.sup.10 is hydrogen or alkyl, and ##STR4## where n=0, 1, or 2, and R.sup.5 is alkyl, inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.

    摘要翻译: 其中W选自其中Q是氧或硫的结构的化合物,R6和R7是氢或烷基,或R6和R7与它们所连接的氮原子一起定义为 烷基,卤代烷基,任选取代的苯基,羟基烷基,氨基烷基,羧基烷基,(烷氧基羰基)烷基和(烷基氨基羰基)烷基; Z是-CH 2 - ,氧,硫或-NR 9,其中R 9是氢或烷基,L 1和L 2选自价键,亚烷基,亚丙烯基和亚丙炔基,R 1,R 2,R 3和R 4独立地选自烷基 卤素,卤素,氰基,氨基,烷氧基羰基和二烷基氨基羰基,Y选自氧,-NR10,其中R10是氢或烷基,和其中n = 0,1或2,R5是烷基,抑制 白三烯的生物合成。 这些化合物可用于治疗或改善过敏性和炎性疾病状态。

    Packaged blanket
    55.
    外观设计
    Packaged blanket 有权
    包装毯

    公开(公告)号:USD665612S1

    公开(公告)日:2012-08-21

    申请号:US29408085

    申请日:2011-12-06

    申请人: Wendy Lee

    设计人: Wendy Lee

    5-ANILINOIMIDAZOPYRIDINES AND METHODS OF USE
    57.
    发明申请
    5-ANILINOIMIDAZOPYRIDINES AND METHODS OF USE 有权
    5-ANILINOIMIDAZOPYRIDINES和使用方法

    公开(公告)号:US20100004269A1

    公开(公告)日:2010-01-07

    申请号:US12432529

    申请日:2009-04-29

    摘要: The invention relates to imidazopyridines of formula I with anti-cancer and/or anti-inflammatory activity and more specifically to imidazopyridines which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

    摘要翻译: 本发明涉及式I的咪唑并吡啶与抗癌和/或抗炎活性,更具体地涉及抑制MEK激酶活性的咪唑并吡啶类。 本发明提供了可用于抑制异常细胞生长或治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。 本发明还涉及将化合物用于体外,原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。

    Oxime derivatives of indole and indene compounds as inhibitors of
prostaglandin biosynthesis
    59.
    发明授权
    Oxime derivatives of indole and indene compounds as inhibitors of prostaglandin biosynthesis 失效
    吲哚和茚化合物的肟衍生物作为前列腺素生物合成的抑制剂

    公开(公告)号:US5750558A

    公开(公告)日:1998-05-12

    申请号:US660048

    申请日:1996-06-06

    摘要: Described herein are compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein L is selected from the group consisting of ##STR2## R.sup.2 is selected from (a) ##STR3## R.sup.3 is selected from optionally substituted phenyl, and optionally substituted pyridyl; Y is selected from halogen, alkyl, haloalkyl, alkoxy, pyridylmethoxy, thiazolylmethoxy, benzothiazolylmethoxy, quinolylmethoxy, and optionally substituted quinolylmethoxy; W is selected from hydrogen, alkyl, hydroxyalkyl, and hydroxy; A is absent or is selected from optionally substituted alkylene optionally substituted cycloalkylene, optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, and ##STR4## and X is absent or is alkylene; Z is selected from (a) hydrogen, (b) COM wherein M is selected from (b-1) a pharmaceutically acceptable metabolically cleavable group, (b-2)--OR.sup.10,(b-3)--O(CH.sub.2).sub.w --CH(OR.sup.12)--CH.sub.2 OR.sup.13, and (b-4)--NR.sup.15 R.sup.16 (c)--OR.sup.17, (d) tetrazolyl, (e)--CH(OR.sup.17)--CH.sub.2 OR.sup.18,(f)--CH(OR.sup.17)--CH.sub.2 --CH.sub.2 OR.sup.18, (g)--CH(OR.sup.17)--CH(OR.sup.18)--CH.sub.2 OR.sup.19, and (h).dbd.N--OR.sup.17 ; and R.sup.1 and R.sup.4 selected from (a) hydrogen, (b) alkyl, and (c) optionally substituted phenyl, are prostaglandin biosynthesis inhibitors and are useful in the treatment of inflammatory disease states. Also disclosed are prostaglandin inhibiting compositions, and a method of inhibiting prostaglandin biosynthesis in a mammal.

    摘要翻译: 本文描述的是具有式“IMAGE”的化合物或其药学上可接受的盐,其中L选自由下列组成的组:R 2选自(a)图像(b)图像(c) (d)R 3选自任选取代的苯基和任选取代的吡啶基; Y选自卤素,烷基,卤代烷基,烷氧基,吡啶基甲氧基,噻唑基甲氧基,苯并噻唑基甲氧基,喹啉基甲氧基和任选取代的喹啉基甲氧基; W选自氢,烷基,羟基烷基和羟基; A不存在或选自任选取代的亚烷基任选取代的亚环烷基,任选取代的亚环烷基,其中一个或两个碳原子被一个或两个独立地选自O,S和N的杂原子替代,并且X不存在 或者是亚烷基; Z选自(a)氢,(b)COM,其中M选自(b-1)可药用代谢裂解基团,(b-2)-OR10,(b-3)-O(CH2)w- CH(OR 12)-CH 2 OR 13和(b-4)-NR 15 R 16(c)-OR 17,(d)四唑基,(e)-CH(OR 17)-CH 2 OR 18,(f)-CH(OR 17) (g)-CH(OR 17)-CH(OR 18)-CH 2 OR 19,和(h)= N-OR 17; 并且选自(a)氢,(b)烷基和(c)任选取代的苯基的R 1和R 4是前列腺素生物合成抑制剂,并且可用于治疗炎性疾病状态。 还公开了前列腺素抑制组合物和抑制哺乳动物中前列腺素生物合成的方法。

    (4-alkoxypyran-4-yl) substituted arylalkylaryl-, aryalkenylaryl-, and
aryalkynylarylurea inhibitors of 5-lipoxygenase
    60.
    发明授权
    (4-alkoxypyran-4-yl) substituted arylalkylaryl-, aryalkenylaryl-, and aryalkynylarylurea inhibitors of 5-lipoxygenase 失效
    (4-烷氧基吡喃-4-基)取代的芳基烷基芳基 - 芳烯基芳基和芳氧基炔基芳基脲抑制剂5-脂氧合酶

    公开(公告)号:US5432194A

    公开(公告)日:1995-07-11

    申请号:US236001

    申请日:1994-05-09

    CPC分类号: C07D405/12 C07D309/12

    摘要: Compounds of the structure ##STR1## wherein W is selected from ##STR2## where Q is oxygen or sulfur, R.sup.6 and R.sup.7 are hydrogen or alkyl, or R.sup.6 and R.sup.7, together with the nitrogen atoms to which they are attached, define a radical of formula ##STR3## R.sup.8 is selected from hydrogen, alkyl, haloalkyl, optionally substituted phenyl, hydroxyalkyl, aminoalkyl, carboxyalkyl, (alkoxycarbonyl)alkyl, and (alkylaminocarbonyl)alkyl; Z is --CH.sub.2 --, oxygen, sulfur, or --NR.sup.9 where R.sup.9 is hydrogen or alkyl, L.sup.1 and L.sup.2 are selected from a valence bond, alkylene, propenylene, and propynylene, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from alkyl, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl, Y is selected from oxygen, --NR.sup.10, where R.sup.10 is hydrogen or alkyl, and ##STR4## where n=0, 1, or 2, and R.sup.5 is alkyl, inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.

    摘要翻译: 其中W选自其中Q是氧或硫的结构的化合物,R6和R7是氢或烷基,或R6和R7与它们所连接的氮原子一起定义为 烷基,卤代烷基,任选取代的苯基,羟基烷基,氨基烷基,羧基烷基,(烷氧基羰基)烷基和(烷基氨基羰基)烷基; Z是-CH 2 - ,氧,硫或-NR 9,其中R 9是氢或烷基,L 1和L 2选自价键,亚烷基,亚丙烯基和亚丙炔基,R 1,R 2,R 3和R 4独立地选自烷基 卤素,卤素,氰基,氨基,烷氧基羰基和二烷基氨基羰基,Y选自氧,-NR10,其中R10是氢或烷基,和其中n = 0,1或2,R5是烷基,抑制 白三烯的生物合成。 这些化合物可用于治疗或改善过敏性和炎性疾病状态。