- N3-Arylmalonamides: A new series of thieno[3,2-b]pyridine based inhibitors of c-Met and VEGFR2 tyrosine kinases
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A family of thieno[3,2-b]pyridine based small molecule inhibitors of c-Met and VEGFR2 were designed based on lead structure 2. These compounds were shown to have IC50 values in the low nanomolar range in vitro and were efficacious in human tumo
- Saavedra, Oscar,Claridge, Stephen,Zhan, Lijie,Raeppel, Franck,Granger, Marie-Claude,Raeppel, Stéphane,Mannion, Michael,Gaudette, Frédéric,Zhou, Nancy,Isakovic, Ljubomir,Bernstein, Naomy,Déziel, Robert,Nguyen, Hannah,Beaulieu, Normand,Beaulieu, Carole,Dupont, Isabelle,Wang, James,Macleod, A. Robert,Besterman, Jeffrey M.,Vaisburg, Arkadii
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scheme or table
p. 6836 - 6839
(2010/06/19)
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- Inhibitors of VEGF receptor and HGF receptor signaling
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The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions
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Page/Page column 79-80
(2010/11/25)
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- Reactions of Acetoacetic Ester Blocked Cyclohexyl Isocyanate
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Acetoacetic ester has been widely reported to be a blocking agent for isocyanates.However, we find that only a trace of isocyanate is formed by thermolysis of acetoacetic ester blocked cyclohexyl isocyanate, 1, at 150 deg C and atmospheric pressure.The major portion is unchanged even after 8 h, with some conversion to acetylmalonic ester, 2, and acetyl-N,N'-dicyclohexylmalonamide, 3.Alcoholysis does not yield the "normal" urethane as blocked isocyanates do but rather esters of 1 with some diesters of 2 and smaller amounts of 3.Significant amounts of N-cyclohexylacetamide, N-cyclohexylmalonamate ester, and some N,N'-dicyclohexylmalonamide are also obtained.Aminolysis leads to N-substituted acetamides and N-cyclohexylmalonamate but no substituted ureas, the "normal" products for aminolysis of blocked isocyanates.In the presence of acid catalysts, alcoholysis leads to N-cyclohexylmalonamates with acetate esters as the other product.
- Wicks, Zeno W.,Wu, Kuang-Jong
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p. 2446 - 2448
(2007/10/02)
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