156969-42-5Relevant articles and documents
Efficient salt-induced kinase inhibitor and preparation method thereof
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, (2021/09/04)
The invention discloses an efficient salt-induced kinase inhibitor and a preparation method thereof, and the efficient salt-induced kinase inhibitor is characterized by comprising substances of a chemical formula in the invention. The salt-induced kinase inhibitor with excellent performance has high inhibitory activity for in-vitro experiments and also has high cell inhibitory activity.
Functionally selective dopamine D2, D3 receptor partial agonists
M?ller, Dorothee,Kling, Ralf C.,Skultety, Marika,Leuner, Kristina,Hübner, Harald,Gmeiner, Peter
, p. 4861 - 4875 (2014/07/07)
Dopamine D2 receptor-promoted activation of Gαo over Gαi may increase synaptic plasticity and thereby might improve negative symptoms of schizophrenia. Heterocyclic dopamine surrogates comprising a pyrazolo[1,5-a]pyridine
AMIDO-BENZYL SULFONE AND SULFOXIDE DERIVATIVES
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, (2013/09/12)
The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
PYRIDINYL AND PYRIMIDINYL SULFOXIDE AND SULFONE DERIVATIVES
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, (2013/09/12)
Disclosed are certain pyridinyl and pyrimidinyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds and methods of treatment using such compounds.
AMIDO-BENZYL SULFOXIDE DERIVATIVES
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, (2013/09/12)
The present invention relates to certain amido-benzyl sulfoxide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment of an NAMPT-mediated disease or condition in a subject, selected from solid or liquid tumor, rheumat
ALKYL-AND DI-SUBSTITUTED AMIDO-BENZYL SULFONAMIDE DERIVATIVES
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, (2013/09/12)
The present invention relates to certain alkyl- and di-substituted amido-benzyl sulfonamide compounds, pharmaceutical compositions comprising such compounds, and to methods of treatment of NAMPT-mediated disorders, such as diabetes, rheumatoid arthritis,
Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors
Kendall, Jackie D.,O'Connor, Patrick D.,Marshall, Andrew J.,Frédérick, Rapha?l,Marshall, Elaine S.,Lill, Claire L.,Lee, Woo-Jeong,Kolekar, Sharada,Chao, Mindy,Malik, Alisha,Yu, Shuqiao,Chaussade, Claire,Buchanan, Christina,Rewcastle, Gordon W.,Baguley, Bruce C.,Flanagan, Jack U.,Jamieson, Stephen M.F.,Denny, William A.,Shepherd, Peter R.
experimental part, p. 69 - 85 (2012/03/08)
We have made a novel series of pyrazolo[1,5-a]pyridines as PI3 kinase inhibitors, and demonstrated their selectivity for the p110α isoform over the other Class Ia PI3 kinases. We investigated the SAR around the pyrazolo[1,5-a]pyridine ring system, and found compound 5x to be a particularly potent example (p110α IC50 0.9 nM). This compound inhibits cell proliferation and phosphorylation of Akt/PKB, a downstream marker of PI3 kinase activity, and showed in vivo activity in an HCT-116 human xenograft model.
PYRAZOLO[1,5-A]PYRIDINES AND THEIR USE IN CANCER THERAPY
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Page/Page column 44; 64, (2009/03/07)
Pyrazolo[1,5-a]pyridines are described, including methods for their preparation, and their use as agents or drugs for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.
Indolizines and aza-analog derivatives thereof as CNS active compounds
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Page/Page column 29, (2008/12/08)
Presently disclosed are indolicine-based compounds of the general formula which have medical utility, for example as antipsychotics.
Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists
Elsner, Jan,Boeckler, Frank,Heinemann, Frank W.,Hübner, Harald,Gmeiner, Peter
, p. 5771 - 5779 (2007/10/03)
Taking advantage of a 3D-QSAR based pharmacophore hypothesis, synthesis and biological evaluation of dopaminergic 5-aminotetrahydropyrazolo[1,5-a]pyridines are described. The data displayed substantial and selective D3 receptor affinity for the heterocycl