6602-33-1Relevant academic research and scientific papers
Inducing Axial Chirality in a Supramolecular Catalyst
Wenz, Katharina Marie,Leonhardt-Lutterbeck, Günter,Breit, Bernhard
, p. 5100 - 5104 (2018/03/27)
A new type of ligand, which is able to form axially chiral, supramolecular complexes was designed using DFT calculations. Two chiral monomers, each featuring a covalently bound chiral auxiliary, form a bidentate phosphine ligand with a twisted, hydrogen-bonded backbone upon coordination to a transition metal center which results in two diastereomeric, tropos complexes. The ratio of the diastereomers in solution is very temperature- and solvent-dependent. Rhodium and platinum complexes were analyzed through a combination of NMR studies, ESI-MS measurements, as well as UV-VIS and circular dichroism spectroscopy. The chiral self-organized ligands were evaluated in the rhodium-catalyzed asymmetric hydrogenation of α-dehydrogenated amino acids and resulted in good conversion and high enantioselectivity. This research opens the way for new ligand designs based on stereocontrol of supramolecular assemblies through stereodirecting chiral centers.
HETEROCYCLIC COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Paragraph 0088; 0089, (2018/01/11)
The invention relates to a novel heterocyclic compound inhibiting a cyclin-dependent kinase (CDK) and a pharmaceutical composition comprising the same as an effective ingredient. The heterocyclic compound according to the present invention or pharmaceutically acceptable salt thereof can be effectively used in treating or preventing cancers, degenerative brain diseases, etc.
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.
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.
PESTICIDALLY ACTIVE PYRIDYL- AND PYRIMIDYL- SUBSTITUTED PYRAZOLE DERIVATIVES
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Page/Page column 45; 46, (2014/03/25)
Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as insecticides and can be prepared in a manner known per se.
5-HT RECEPTOR MODULATORS
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Paragraph 0594; 0595; 0596, (2013/03/26)
The invention relates to compounds of formula (I), useful for treating disorders mediated by the 5-hydroxytryptamine (serotonin) receptor IB (5-HT1B), e.g. vascular disorders, cancer and CNS disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.
PESTICIDALLY ACTIVE PYRIDYL- AND PYRIMIDYL- SUBSTITUTED THIAZOLE DERIVATIVES
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Page/Page column 40, (2014/01/08)
Disclosed are pesticidally active pyridyl- and pyrimidyl- substituted thiazole derivatives, processes for their preparation, compositions lcomprising those compounds, and their use for controlling insects.
5-HT RECEPTOR MODULATORS
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Page/Page column 61, (2011/09/15)
The invention relates to compounds of formula (I), useful for treating disorders mediated by the 5-hydroxytryptamine (serotonin) receptor 1B (5-HT1B), e.g. vascular disorders, cancer and CNS disorders. The invention also provides methods of treating such disorders, and componnds and compositions etc. for their treatment
Synthesis of the phenylpyridal scaffold as a helical peptide mimetic
Bourne, Gregory T.,Kuster, Daniel J.,Marshall, Garland R.
supporting information; experimental part, p. 8439 - 8445 (2010/09/08)
Phenylpyridal- and phenyldipyridal-based scaffolds have been designed and synthesized as novel helical peptide mimetics. The synthesis required optimisation and selective alkylation in producing 2,6-functionalized 3-hydroxypyridine derivatives for a convergent scheme. The pyridine analogues were coupled by a series of Suzuki/Stille types cross-coupling reactions. A series of biaryl and ter-aryl substituted heterocycles were produced. The synthetic approach was concise and high yielding allowing large variability at the wanted sidechain attachment points. A number of compounds were synthesised to show the versatility of the strategy.
PYRIDINE, BICYCLIC PYRIDINE AND RELATED ANALOGS AS SIRTUIN MODULATORS
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Page/Page column 97, (2010/06/15)
The present invention provides novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders relating to aging or stress, diabetes, obesity, neurodegenerative disease, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorder that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. The compounds are of general formula (III) wherein R1, R2, R", X, Y, W, Z1 and Z2 are as defined in the specification.
