180344-10-9Relevant academic research and scientific papers
3-HYDROXY-IMIDAZOLIDIN-4-ONE COMPOUNDS AS INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE
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, (2019/03/17)
The invention relates to a compound of Formula (I) : Formula (I), or pharmaceutically acceptable enantiomers, or salts thereof. The present invention also relates to the use of compounds of Formula (I) as selective inhibitors of indoleamine 2,3-dioxygenas
INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE
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, (2017/09/28)
The invention relates to a compound of Formula (I), or pharmaceutically acceptable enantiomers, or salts thereof. The present invention also relates to the use of compounds of Formula (I) as selective inhibitors of indoleamine 2,3-dioxygenase. The inventi
Discovery of non-peptidic P2-P3 butanediamide renin inhibitors with high oral efficacy
Simoneau, Bruno,Lavallee, Pierre,Anderson, Paul C.,Bailey, Murray,Bantle, Gary,Berthiaume, Sylvie,Chabot, Catherine,Fazal, Gulrez,Halmos, Ted,Ogilvie, William W.,Poupart, Marc-Andre,Thavonekham, Bounkham,Xin, Zhili,Thibeault, Diane,Boelger, Gordon,Panzenbeck, Maret,Winquist, Raymond,Jung, Grace L.
, p. 489 - 508 (2007/10/03)
A new series of non-peptidic renin inhibitors having a 2-substituted butanediamide moiety at the P2 and P3 positions has been identified. The optimized inhibitors have IC50 values of 0.8 to 1.4nM and 2.5 to 7.6nM in plasma renin assays at pH 6.0 and 7.4, respectively. When evaluated in the normotensive cynomolgus monkey model, two of the most potent inhibitors were orally active at a dose as low as 3mg/kg. These potent renin inhibitors are characterized by oral bioavailabilities of 40 and 89% in the cynomolgus monkey. Inhibitor 3z (BILA 2157 BS) was selected as candidate for pre-development. Copyright (C) 1999 Elsevier Science Ltd.
