- Efficient salt-induced kinase inhibitor and preparation method thereof
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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.
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- Functionally selective dopamine D2, D3 receptor partial agonists
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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
- M?ller, Dorothee,Kling, Ralf C.,Skultety, Marika,Leuner, Kristina,Hübner, Harald,Gmeiner, Peter
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p. 4861 - 4875
(2014/07/07)
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- AMIDO-BENZYL SULFONE AND SULFOXIDE DERIVATIVES
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The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
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- PYRIDINYL AND PYRIMIDINYL SULFOXIDE AND SULFONE DERIVATIVES
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Disclosed are certain pyridinyl and pyrimidinyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds and methods of treatment using such compounds.
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- AMIDO-BENZYL SULFOXIDE DERIVATIVES
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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
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- ALKYL-AND DI-SUBSTITUTED AMIDO-BENZYL SULFONAMIDE DERIVATIVES
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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,
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- Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors
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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.
- 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.
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experimental part
p. 69 - 85
(2012/03/08)
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- PYRAZOLO[1,5-A]PYRIDINES AND THEIR USE IN CANCER THERAPY
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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.
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Page/Page column 44; 64
(2009/03/07)
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- Indolizines and aza-analog derivatives thereof as CNS active compounds
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Presently disclosed are indolicine-based compounds of the general formula which have medical utility, for example as antipsychotics.
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Page/Page column 29
(2008/12/08)
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- Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists
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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
- Elsner, Jan,Boeckler, Frank,Heinemann, Frank W.,Hübner, Harald,Gmeiner, Peter
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p. 5771 - 5779
(2007/10/03)
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- The Pyrolytic Rearrangement of 1-Alkynoyl-3-methylpyrazoles: Synthesis of Pyrazolopyridin-5-ols and Related Compounds
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Flash vacuum pyrolysis of 1-(alkyn-2'-oyl)-3-methylpyrazoles at 650 deg/0.03 mm forms pyrazolopyridin-5-ols, often in high yield, which may bear substituents at C2, C3 or C7.In the absence of a 3-methyl group in the precursor, N-ethynylpyrazoles are formed in low yield.The formation of both types of product is interpreted as involving 3-(N-pyrazolyl)propadienones formed by N1 --> N2 migration of the N-alkynoyl group with inversion of the three-carbon chain.The fused-ring structure of 2-methylpyrazolopyridin-5-ol (25) was established by X-ray crystallography of the O-benzoyl derivative (27).
- Brown, Roger F. C.,Eastwood, Frank W.,Fallon, Gary D.,Lee, Swee Choo,McGeary, Ross P.
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p. 991 - 1008
(2007/10/02)
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