发明名称 |
Process for the preparation of macrocyclic metalloprotease inhibitors |
摘要 |
The present invention is directed to a process for the preparation of a compound of formula (X-a)or a pharmaceutically acceptable salt form thereof,wherein:R1 is selected from the group consisting of:C1-5 alkyl substituted with 0-5 R1a,-(CH2)r-C3-10 cycloalkyl substituted with 0-5 R1a, and-(CH2)r-aryl substituted with 0-5 R1a.Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.
|
申请公布号 |
US6562963(B2) |
申请公布日期 |
2003.05.13 |
申请号 |
US20010919564 |
申请日期 |
2001.07.31 |
申请人 |
DOROW ROBERTA L.;CAMPAGNA SILVIO;CONFALONE PASQUALE N.;JIN FUQIANG;WANG ZHE |
发明人 |
DOROW ROBERTA L.;CAMPAGNA SILVIO;CONFALONE PASQUALE N.;JIN FUQIANG;WANG ZHE |
分类号 |
A61K31/395;A61K31/55;A61P19/02;A61P29/00;A61P43/00;C07C43/315;C07C53/126;C07C59/58;C07C67/14;C07C69/007;C07C69/24;C07C235/28;C07D267/00;C07D273/01;C07D273/02;C07F7/18;(IPC1-7):C07C231/01;C07C231/71 |
主分类号 |
A61K31/395 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|