Benzylglycosylamides as inhibitors of smooth muscle cell proliferation
    8.
    发明授权
    Benzylglycosylamides as inhibitors of smooth muscle cell proliferation 失效
    苄基糖基酰胺作为平滑肌细胞增殖的抑制剂

    公开(公告)号:US06362170B1

    公开(公告)日:2002-03-26

    申请号:US09444078

    申请日:1999-11-22

    IPC分类号: A61K3170

    摘要: This invention provides smooth muscle cell proliferation inhibitors of formula I having the structure wherein Y is C or N; where n is 0-3; X is R1, and R2 are each independently, hydrogen, alkyl of 1 to 6 carbon atoms, halo, acetyl, phenyl, CF3, CN, OH, NO2, NH2, alkoxy of 1 to 6 carbon atoms, or alkoxynitrile of 1 to 6 carbon atoms; R3 is hydrogen, acylamide of 2 to 6 carbon atoms or alkoxy of 1 to 6 carbon atoms; R4, R5, R6, R7, and R8 are each, independently, acyl of 1 to 6 carbon atoms, benzyl substituted with R1, and R2; or benzoyl substituted with R1 and R2; R9 and R10 are each, independently, acyl of 1 to 6 carbon atoms, or the R9 and R10 groups on the 4′ and 6′ positions of the maltose may be taken together to form a cyclic acetal which may be substituted with alkyl of 1 to 6 carbon atoms, two alkyl groups each having 1 to 6 carbon atoms, pyridine substituted with R1, phenyl substituted with R1, benzyl substituted with R1, 2-phenylethyl substituted with R1, or 3-phenylpropyl substituted with R1; or a pharmaceutically acceptable salt thereof.

    摘要翻译: 本发明提供了具有其中Y为C或N的结构的式I的平滑肌细胞增殖抑制剂,其中n为0-3; X为R 1,R 2各自独立地为氢,1至6个碳原子的烷基,卤素,乙酰基,苯基 ,CF 3,CN,OH,NO 2,NH 2,碳原子数为1〜6的烷氧基,或碳原子数为1〜6的烷氧基腈; R3为氢,2〜6个碳原子的酰基酰胺或1〜6个碳原子的烷氧基; R5,R6,R7和R8各自独立地为1至6个碳原子的酰基,被R1和R2取代的苄基; 或被R 1和R 2取代的苯甲酰基; R 9和R 10各自独立地为1至6个碳原子的酰基,或者麦芽糖的4'和6'位上的R 9和R 10基团可一起形成环状缩醛 其可以被1至6个碳原子的烷基,两个具有1至6个碳原子的烷基,被R1取代的吡啶,被R1取代的苯基,被R1取代的苄基,被R1取代的2-苯乙基或3-苯基丙基 被R1取代;或其药学上可接受的盐。

    Furans, benzofurans, and thiophenes useful in the treatment of insulin resistance and hyperglycemia

    公开(公告)号:US06683107B2

    公开(公告)日:2004-01-27

    申请号:US10215311

    申请日:2002-08-08

    IPC分类号: A61K31381

    摘要: This invention provides compounds of Formula I having the structure wherein R1 and R2 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, perfluoroalkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, phenyl or phenyl substituted with trifluoromethyl, chloro, methoxy, or trifluoromethoxy; R3 and R4 are each, independently, hydrogen, carboxyl, hydroxyl, hydoxyalkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, perfluoroalkoxy of 1-6 carbon atoms, alkanoyloxy of 2-7 carbon atoms, perfluoroalkanoyloxy of 2-7 carbon atoms, arylalkoxy of 7-15 carbon atoms, aryloxy of 6-12 carbon atoms, aroyloxy of 6-12 carbon atoms, aryloxycarbonyl of 7-13 carbon atoms, alkoxycarbonyl of 2-7 carbon atoms, perfluoroalkoxycarbonyl of 2-7 carbon atoms, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, alkylamino of 1-6 carbon atoms, dialkylamnino of 1-6 carbon atoms per alkyl group, tetrazolyl, mercapto, nitrile, nitro, amino, —NHSO2CF3, carbamoyl, carboxyaldehyde, halogen, acylamino, 3-hydroxy-cyclobut-3-ene-4-yl-1,2-dione, pyridyl, isoxazolyl, pyrimidyl or pyrimidyl substituted with mercapto, or tetronic acid; R5 is hydrogen, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, naphthalenylmethyl, benzyl or benzyl substituted with halogen, R6 and R7 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, or perfluoroalkyl of 1-6 carbon atoms, or R6 and R7 may be taken together as a diene unit having the structure —CH═CH—CH═CH—; W is S or O, X is —NR8CH2—, —NR8—, or O; R8 is hydrogen or alkyl; Y is carbonyl, methylene, ethyl, or —NHCH2—; Z is phenyl, pyridyl, naphthyl, thienyl, furyl, pyrrolyl, pyrazolyl, isoxazolyl, or isothiazolyl; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.