3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL COA DESATURASE INHIBITORS
The present invention discloses 3-hydroquinazolm-4-one derivatives for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especial
We discovered a structurally novel SCD (Δ9 desaturase) inhibitor 4a (CVT-11,563) that has 119 nM potency in a human cell-based (HEPG2) SCD assay and selectivity against Δ5 and Δ6 desaturases. This compound has 90% oral bioavailability (rat) and excellent
Koltun, Dmitry O.,Vasilevich, Natalya I.,Parkhill, Eric Q.,Glushkov, Andrei I.,Zilbershtein, Timur M.,Mayboroda, Elena I.,Boze, Melanie A.,Cole, Andrew G.,Henderson, Ian,Zautke, Nathan A.,Brunn, Sandra A.,Chu, Nancy,Hao, Jia,Mollova, Nevena,Leung, Kwan,Chisholm, Jeffrey W.,Zablocki, Jeff
scheme or table
p. 3050 - 3053
(2010/01/16)
3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS
The present invention discloses 3-hydroquinazolin-4-one derivatives for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especia
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(2008/12/04)
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