- Novel, potent, selective, and metabolically stable stearoyl-CoA desaturase (SCD) inhibitors
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We identified a series of structurally novel SCD (Δ9 desaturase) inhibitors via high-throughput screening and follow-up SAR studies. Modification of the central bicyclic scaffold has proven key to our potency optimization effort. The most potent analog (8
- Koltun, Dmitry O.,Parkhill, Eric Q.,Vasilevich, Natalya I.,Glushkov, Andrei I.,Zilbershtein, Timur M.,Ivanov, Alexei V.,Cole, Andrew G.,Henderson, Ian,Zautke, Nathan A.,Brunn, Sandra A.,Mollova, Nevena,Leung, Kwan,Chisholm, Jeffrey W.,Zablocki, Jeff
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scheme or table
p. 2048 - 2052
(2009/11/30)
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- PTERIDINONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS
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The present invention discloses pteridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like.
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Page/Page column 11
(2008/12/08)
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- Pyrimidine derivatives
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The present invention relates to trisubstituted pyrimidines of formula (I) 1wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterised by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.
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