Title:
【発明の名称】大員環メタロプロテアーゼ阻害剤の製造法
Document Type and Number:
Japanese Patent JP2002517488
Kind Code:
A
Abstract:
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.
Inventors:
Roberta El. Drow
Silvio Campaguna
Pascal N. Conference loan
Fukyan gin
Tsewan
Silvio Campaguna
Pascal N. Conference loan
Fukyan gin
Tsewan
Application Number:
JP2000553415A
Publication Date:
June 18, 2002
Filing Date:
June 10, 1999
Export Citation:
Assignee:
DuPont Pharmaceuticals Company
International Classes:
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): C07D267/00; C07C43/315; C07C53/126; C07C59/58; C07C67/14; C07C69/007; C07C69/24; C07C235/28; C07D273/02
Attorney, Agent or Firm:
Yoshikazu Tani (2 outside)