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    • 4. 发明申请
      US20060276429A1 Acylated benzylmaltosides as inhibitors of smooth muscle cell proliferation 失效
    • Acylated benzylmaltosides as inhibitors of smooth muscle cell proliferation
    • US20060276429A1
    • 2006-12-07
    • US11505543
    • 2006-08-17
    • Scott Mayer , Robert McDevitt , Paul Dollings
    • Scott Mayer , Robert McDevitt , Paul Dollings
    • A61K31/7052 , A61K31/7024 , C07H17/02
    • C07H17/02 , A61K31/704 , C07H5/06
    • This invention provides smooth muscle cell proliferation inhibitors of formula I having the structure wherein R1, R2, R3, R4, and R5 are each, independently, hydrogen, acyl of 2-7 carbon atoms, haloacyl of 2-7 carbon atoms, nitroacyl of 2-7 carbon atoms, cyanoacyl of 2-7 carbon atoms, trifluoromethylacyl of 3-8 carbon atoms, or benzoyl in which the phenyl moiety is substituted with R8; R6 and R7 are each, independently, —OH, —OR9, O-tert-butyldimethylsilyl, O-trialkylsilyl of 1-6 carbon atoms per alkyl moiety, O-triphenylsilyl, R8, R10, R11, and R12 are each, independently, hydrogen, —CN, —NO2, halogen, CF3, alkyl of 1-6 carbon atoms, acetyl, benzoyl, or alkoxy of 1-6 carbon atoms; R9 is acyl of 2-7 carbon atoms, haloacyl of 2-7 carbon atoms, nitroacyl of 2-7 carbon atoms, cyanoacyl of 2-7 carbon atoms, trifluoromethylacyl of 3-8 carbon atoms, or benzoyl in which the phenyl moiety is substituted with R8; Y is O, S, NH, NMe, or CH2; W is halogen, —CN, CF3, alkyl of 1-6 carbon atoms, haloalkyl of 1-6 carbon atoms, nitroalkyl of 1-6 carbon atoms, cyanoalkyl of 1-6 carbon atoms, alkoxyalkyl of 2-12 carbon atoms, alkoxy of 1-6 carbon atoms, or phenyl mono-, di-, or tri-substituted with R8; Z is —NO2, —NH2, —NHR13, or —NHCO-Het; R13 is acyl of 2-7 carbon atoms, haloacyl of 2-7 carbon atoms, nitroacyl of 2-7 carbon atoms, cyanoacyl of 2-7 carbon atoms, trifluoromethylacyl of 3-8 carbon atoms, benzoyl in which the phenyl moiety is substituted with R8, or R13 is an α-amino acid in which the α carboxyl group forms an amide with the nitrogen of Z, wherein if said amino acid is glutamic acid or aspartic acid, the non-α carboxylic acid is an alkyl ester in which the alkyl moiety contains from 1-6 carbon atoms; Het is pyridyl substituted with R8, thienyl substituted with R8, furyl substituted with R8, oxazolyl substituted with R8, pyrazinyl substituted with R8, pyrimidinyl substituted with R8, or thiazolyl substituted with R8; R14 is R8, —NH2, —CO2H, or —NH-acyl of 2-7 carbon atoms; n=0-3; with the proviso that when Z is —NHR13 and Y is O, at least one of R1, R2, R3, R4, and R5 is hydrogen, or at least one of R6 and R7 is OH, or a pharmaceutically acceptable salt thereof.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 7. 发明申请
      US20050176652A1 Acylated benzylmaltosides as inhibitors of smooth muscle cell proliferation 有权
    • Acylated benzylmaltosides as inhibitors of smooth muscle cell proliferation
    • US20050176652A1
    • 2005-08-11
    • US10699233
    • 2003-10-31
    • Scott Mayer , Robert McDevitt , Paul Dollings
    • Scott Mayer , Robert McDevitt , Paul Dollings
    • A61K31/704 , C07H5/06
    • C07H17/02 , A61K31/704 , C07H5/06
    • This invention provides smooth muscle cell proliferation inhibitors of formula I having the structure wherein R1, R2, R3, R4, and R5 are each, independently, hydrogen, acyl of 2-7 carbon atoms, haloacyl of 2-7 carbon atoms, nitroacyl of 2-7 carbon atoms, cyanoacyl of 2-7 carbon atoms, trifluoromethylacyl of 3-8 carbon atoms, or benzoyl in which the phenyl moiety is substituted with R8; R6 and R7 are each, independently, —OH, —OR9, O-tert-butyldimethylsilyl, O-trialkylsilyl of 1-6 carbon atoms per alkyl moiety, O-triphenylsilyl, R8, R10, R11, and R12 are each, independently, hydrogen, —CN, —NO2, halogen, CF3, alkyl of 1-6 carbon atoms, acetyl, benzoyl, or alkoxy of 1-6 carbon atoms; R9 is acyl of 2-7 carbon atoms, haloacyl of 2-7 carbon atoms, nitroacyl of 2-7 carbon atoms, cyanoacyl of 2-7 carbon atoms, trifluoromethylacyl of 3-8 carbon atoms, or benzoyl in which the phenyl moiety is substituted with R8; Y is O, S, NH, NMe, or CH2; W is halogen, —CN, CF3, alkyl of 1-6 carbon atoms, haloalkyl of 1-6 carbon atoms, nitroalkyl of 1-6 carbon atoms, cyanoalkyl of 1-6 carbon atoms, alkoxyalkyl of 2-12 carbon atoms, alkoxy of 1-6 carbon atoms, or phenyl mono-, di-, or tri-substituted with R8; Z is —NO2, —NH2, —NHR13, or —NHCO-Het; R13 is acyl of 2-7 carbon atoms, haloacyl of 2-7 carbon atoms, nitroacyl of 2-7 carbon atoms, cyanoacyl of 2-7 carbon atoms, trifluoromethylacyl of 3-8 carbon atoms, benzoyl in which the phenyl moiety is substituted with R8, or R13 is an α-amino acid in which the a carboxyl group forms an amide with the nitrogen of Z, wherein if said amino acid is glutamic acid or aspartic acid, the non-α carboxylic acid is an alkyl ester in which the alkyl moiety contains from 1-6 carbon atoms; Het is pyridyl substituted with R8, thienyl substituted with R8, furyl substituted with R8, oxazolyl substituted with R8, pyrazinyl substituted with R8, pyrimidinyl substituted with R8, or thiazolyl substituted with R8; R14 is R8, —NH2, —CO2H, or —NH-acyl of 2-7 carbon atoms; n=0-3; with the proviso that when Z is —NHR13 and Y is O, at least one of R1, R2, R3, R4, and R5 is hydrogen, or at least one of R6 and R7 is OH, or a pharmaceutically acceptable salt thereof.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明申请
      US20060014725A1 Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1) 失效
    • Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
    • 取代的萘基吲哚衍生物作为纤溶酶原激活物抑制剂1型（PAI-1）的抑制剂
    • US20060014725A1
    • 2006-01-19
    • US11158881
    • 2005-06-22
    • Scott Mayer , Eric Gundersen , Hassan Elokdah , David Crandall
    • Scott Mayer , Eric Gundersen , Hassan Elokdah , David Crandall
    • A61K31/415 , A61K31/404 , C07D403/02 , C07D209/12
    • C07D403/12 , C07D209/12
    • This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.
    • 本发明提供了PAI-1抑制式I化合物：其中：R 1，R 2，R 3和R 4 每个H，烷基，烷酰基，卤素，OH，任选被R 8 8，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基取代的芳基; R 5是H，烷基，全氟烷基，任选被R 8取代的芳基，烷酰基，任选被R 8取代的芳酰基; R 6是H，烷基，烷基芳基，任选被R 8取代的苄基，烷酰基，任选被R 8取代的芳酰基; R 7是H，烷基，烷芳基，任选被R 8取代的芳基; n为0-6; A是COOH或酸模拟物，例如四唑，SO 3 H，PO 3 H 2 H 2，次ronic酸等; R 8是H，烷基，环烷基，烷酰基，卤素，OH，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基; 或其药学上可接受的盐; 以及使用这些化合物的药物组合物和治疗方法。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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