79491-46-6Relevant articles and documents
COMPOUNDS FOR THE TREATMENT OF KINASE-DEPENDENT DISORDERS
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Paragraph 000571; 000573, (2019/08/12)
Disclosed herein are compounds of Formula I'. Compounds of Formula I' inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase- dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
Phosphoinositide-3-kinase inhibitors: Evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511
Lanman, Brian A.,Reed, Anthony B.,Cee, Victor J.,Hong, Fang-Tsao,Pettus, Liping H.,Wurz, Ryan P.,Andrews, Kristin L.,Jiang, Jian,McCarter, John D.,Mullady, Erin L.,San Miguel, Tisha,Subramanian, Raju,Wang, Ling,Whittington, Douglas A.,Wu, Tian,Zalameda, Leeanne,Zhang, Nancy,Tasker, Andrew S.,Hughes, Paul E.,Norman, Mark H.
supporting information, p. 5630 - 5634 (2015/01/08)
Replacement of the piperazine sulfonamide portion of the PI3Kα inhibitor AMG 511 (1) with a range of aliphatic alcohols led to the identification of a truncated gem-dimethylbenzylic alcohol analog, 2-(5-(4-amino-6-methyl-1,3,5-triazin-2-yl)-6-((5-fluoro-6-methoxypyridin-3-yl)amino)pyridin-3-yl)propan-2-ol (7). This compound possessed good in vitro efficacy and pharmacokinetic parameters and demonstrated an EC50 of 239 ng/mL in a mouse liver pharmacodynamic model measuring the inhibition of hepatocyte growth factor (HGF)-induced Akt Ser473 phosphorylation in CD1 nude mice 6 h post-oral dosing.
Lead identification of benzimidazolone and azabenzimidazolone arylsulfonamides as CC-chemokine receptor 4 (CCR4) antagonists
Miah, Afjal H.,Abas, Hossay,Begg, Malcolm,Marsh, Benjamin J.,O'Flynn, Daniel E.,Ford, Alison J.,Percy, Jonathan M.,Procopiou, Panayiotis A.,Richards, Steve A.,Rumley, Sally-Anne
, p. 4298 - 4311 (2014/08/18)
A knowledge-based library of 2,3-dichlorophenylsulfonyl derivatives of commercially available aryl amines was synthesised and screened as human CCR4 antagonists, in order to identify a suitable hit for the start of a lead-optimisation programme. Hits were required to be more potent than an existing indazole series, have better physicochemical properties (c log P 7.4 116 μg/mL), and be stable to acid and light. The benzimidazol-2-one core was identified as a hit suitable for further investigation. Substitution at N1 with small alkyl groups was tolerated; however, these analogues were inactive in the whole blood assay (pA2 7.4 (2.4), high LE (0.43), and solubility (152 μg/mL). In addition, 38 had human serum albumin binding of around 93% and met all the criteria for progression to lead optimisation.
Thiophene-imidazopyridines
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Page/Page column 30, (2009/02/10)
The invention relates to thiophene-imidazopyridine compounds according to formula (I), wherein the substituents and symbols are as defined in the description. The compounds are inhibitors of PIk1
Synthetic Uses of the Sequential Ring Positional Reactivity in Pyridin-3-ol and Derivatives
Clark, Gary J.,Deady, Leslie W.
, p. 927 - 932 (2007/10/02)
A series of ring-substituted pyridin-3-ols has been prepared.The key to the scheme is the introduction of a bromo group to a specific ring position as a temporary blocking agent.As well as hydrogenolysis of the bromo function, nucleophilic displacement has also been investigated.