
基本信息:
- 专利标题: Acylated benzylmaltosides as inhibitors of smooth muscle cell proliferation
- 申请号:US10699233 申请日:2003-10-31
- 公开(公告)号:US20050176652A1 公开(公告)日:2005-08-11
- 发明人: Scott Mayer , Robert McDevitt , Paul Dollings
- 申请人: Scott Mayer , Robert McDevitt , Paul Dollings
- 申请人地址: US NJ Madison
- 专利权人: Wyeth
- 当前专利权人: Wyeth
- 当前专利权人地址: US NJ Madison
- 主分类号: A61K31/704
- IPC分类号: A61K31/704 ; C07H5/06
摘要:
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.
公开/授权文献:
IPC结构图谱:
A | 人类生活必需 |
--A61 | 医学或兽医学;卫生学 |
----A61K | 医用、牙科用或梳妆用的配制品 |
------A61K31/00 | 含有机有效成分的医药配制品 |
--------A61K31/70 | .碳水化合物;糖;其衍生物 |
----------A61K31/7028 | ..含有通过配糖键与非糖化合物连接的糖基的化合物 |
------------A61K31/7034 | ...与碳环化合物相连的,例如根皮苷 |
--------------A61K31/704 | ....与稠合的碳环相连的,例如番泻叶苷、硫代秋水仙碱苷、七叶树皂角素、柔红霉素、洋地黄毒苷 |