BACHOVCHIN, WILLIAM W.,威廉W 巴寇屈,威廉W 巴寇屈,LAI, HUNG-SEN,赖宏森,賴宏森,WU, WENGEN,吴文根,吳文根
申请号：
TW094105369
公开号：
TWI382836B
申请日:
2005.02.23
申请国别(地区):
TW
年份:
2013
代理人:
摘要：
The present invention relates to inhibitors of post-proline cleaving enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention are improved over those in the prior art by selection of particular classes of sidechains in the P1 and/or P2 position of the inhibitor that contain a carboxylic acid moiety. The compounds of the present invention can have a better therapeutic index, owins in part to reduced toxicity and/or improved specificity for the targeted protease.本發明係關於後-脯氨酸切割酵素的抑制劑,諸如二肽基肽酶IV的抑制劑,以及其醫藥組成物,及使用這些抑制劑的方法。特定而言,本發明的抑制劑比那些先前技藝中的抑制劑有進步性,其在含有羧酸部分之抑制劑的P1及/或P2位置選擇特定種類側鏈。本發明的化合物可具有較佳的治療指數,其部分歸因於較低的毒性及/或對標的蛋白酶有改善的專一性。
