203512-53-2Relevant academic research and scientific papers
AMIDINOPHENYL-PYRROLIDINES, -PYRROLINES, AND -ISOXAZOLIDINES AND DERIVATIVES THEREOF
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, (2008/06/13)
The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula (I), or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(=NH)NH2 and the other H and J and J may be O or CH2, which are useful as inhibitors of factor Xa.
Design, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors.
Song, Yonghong,Clizbe, Lane,Bhakta, Chhaya,Teng, Willy,Li, Wenhao,Wu, Yanhong,Jia, Zhaozhong Jon,Zhang, Penglie,Wang, Lingyan,Doughan, Brandon,Su, Ting,Kanter, James,Woolfrey, John,Wong, Paul,Huang, Brian,Tran, Katherine,Sinha, Uma,Park, Gary,Reed, Andrea,Malinowski, John,Hollenbach, Stan,Scarborough, Robert M,Zhu, Bing-Yan
, p. 1511 - 1515 (2007/10/03)
Substituted acrylamides were used as templates that bridge P1 and P4 binding elements, resulting in a series of potent (sub-nanomolar) and selective factor Xa inhibitors. In this template, cis-geometry of P1 and P4 ligands is highly preferred. SAR on the substituting groups, as well as on modification of P1 and P4 moieties is described. Compounds in this series show good in vivo efficacy in animal models.
Amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof
-
, (2008/06/13)
The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(=NH)NH2 and the other H, and J1 and J2 may be O or CH2, which are useful as inhibitors of factor Xa.
