937396-49-1Relevant academic research and scientific papers
IMIDAZOLIDINONE COMPOUNDS USEFUL AS BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 65, (2008/06/13)
The present invention is directed to imidazolidinone compounds which are inhibitors of the beta- secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
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.
