- Novel anticancer compound and usage thereof
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The invention provides a novel anticancer compound. The novel anticancer compound is a compound shown in chemical formula 1 in the description or pharmaceutically acceptable salt of the compound, andthe compound and the salt are active ingredients of a pharmaceutical composition for inhibiting the activity of hepatocyte growth factor receptor (c-Met) tyrosine kinase and pharmaceutical compositionfor preventing or curing excessive or abnormal proliferative diseases. The compound effectively inhibits the activity of the hepatocyte growth factor receptor tyrosine kinase, thereby being suitablefor treating the diseases with the characteristics of excessive or abnormal cell proliferation.
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- PYRIDYL DERIVATIVES AS BROMODOMAIN INHIBITORS
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The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.
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- BENZO[B]FURANS AS BROMODOMAIN INHIBITORS
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The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.
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- Discovery of novel selective norepinephrine inhibitors: 1-(2-morpholin-2-ylethyl)-3-aryl-1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxides (WYE-114152)
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Sequential modification of the previously identified 4-[3-aryl-2,2-dioxido- 2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols led to the identification of a new series of 1-(2-morpholin-2-ylethyl)-3-aryl-1,3-dihydro- 2,1,3-benzothiadiazole 2,2-dioxides that are potent and selective inhibitors of the norepinephrine transporter over both the serotonin and dopamine transporters. One representative compound 10b (WYE-114152) had low nanomolar hNET potency (IC50 = 15 nM) and good selectivity for hNET over hSERT (>430-fold) and hDAT (>548-fold). 10b was additionally bioavailable following oral dosing and demonstrated efficacy in rat models of acute, inflammatory, and neuropathic pain.
- O'Neill, David J.,Adedoyin, Adedayo,Bray, Jenifer A.,Deecher, Darlene C.,Fensome, Andrew,Goldberg, Joel A.,Harrison, Jim,Leventhal, Liza,Mann, Charles,Mark, Lilly,Nogle, Lisa,Sullivan, Nicole R.,Spangler, Taylor B.,Terefenko, Eugene A.,Trybulski, Eugene J.,Uveges, Albert J.,Vu, An,Whiteside, Garth T.,Zhang, Puwen
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supporting information; experimental part
p. 6824 - 6831
(2011/12/04)
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- Substituted morpholine-2S-acetic acid derivatives: SCH 50911 and related compounds as novel GABA(B) antagonists
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The synthesis and GABA(B) antagonist activity of a series of substituted morpholine-2-acetic acid derivatives is described. Resolution of the lead compound from the series produces one active and one inactive enantiomer. X- ray analysis of a halogenated derivative (25) of the active enantiomer Sch 50911 (23) shows that it possesses the 2S configuration.
- Blythin, David J.,Kuo, Shen-Chun,Shue, Ho-Jane,McPhail, Andrew T.,Chapman, Richard W.,Kreutner, William,Rizzo, Charles,She, Hoyan S.,West, Robert
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p. 1529 - 1534
(2007/10/03)
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