- Substituted heteroaryl compounds and compositions and uses thereof
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The present invention relates to a novel heteroaromatic compound, and a pharmaceutical composition containing the compound. The heteroaromatic compound or pharmaceutical composition containing the compound can be used for exciting a melatonin receptor. The present invention also relates to a preparation method of the compound and pharmaceutical composition thereof, and application of the compound and pharmaceutical composition in treating central nervous system dysfunction of mammals especially human.
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Paragraph 0183; 0185-0188
(2019/06/05)
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- Indole derivatives and their application on the medicament
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The invention provides a series of indole derivatives or stereoisomers, tautomers, nitrogen oxides, metabolic products and pharmaceutically acceptable salts or prodrugs thereof. The indole derivatives can be taken as melatonin receptor stimulants. The invention also discloses a pharmaceutical composition containing the compounds, and a use of the compounds or the pharmaceutical composition of the compounds in treating the functional disorder of the central nervous system of mammal and in particular human.
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Paragraph 0187-0190
(2017/01/05)
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- Use of derivatives of indoles for the treatment of cancer
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The present invention relates to the use of derivatives of indoles having a general formula (I) as follow: for the manufacture of a pharmaceutical composition intended for the treatment of cancer.
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Page/Page column 57; 58
(2016/01/09)
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- Use of derivatives of indoles for the treatment of cancer
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The present invention relates to the use of derivatives of indoles having a general formula (I) as follow: for the manufacture of a pharmaceutical composition intended for the treatment of cancer.
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- The discovery of carboline analogs as potent MAPKAP-K2 inhibitors
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The discovery of a series of potent, carboline-based MK2 inhibitors is described. These compounds inhibit MK2 with IC50s as low as 10 nM, as measured in a DELFIA assay. An X-ray crystal structure reveals that they bind in a region near the p-lo
- Wu, Jiang-Ping,Wang, Ji,Abeywardane, Asitha,Andersen, Denise,Emmanuel, Michel,Gautschi, Elda,Goldberg, Daniel R.,Kashem, Mohammed A.,Lukas, Susan,Mao, Wang,Martin, Leslie,Morwick, Tina,Moss, Neil,Pargellis, Christopher,Patel, Usha R.,Patnaude, Lori,Peet, Gregory W.,Skow, Donna,Snow, Roger J.,Ward, Yancey,Werneburg, Brian,White, Andre
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p. 4664 - 4669
(2008/02/13)
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- Mapping the melatonin receptor. 7. Subtype selective ligands based on β-substituted N-acyl-5-methoxytryptamines and β-Substituted N-acyl-5-methoxy-1-methyltryptamines
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A series of β-substituted and β,β-disubstituted N-acyl 5-methoxy-1-methyltryptamines and 5-methoxytryptamines have been prepared as melatonin analogues to investigate the nature of the binding site of the melatonin receptor. The affinity of analogues was determined in a radioligand binding assay using cloned human MT1 and MT2 receptor subtypes expressed in NIH 3T3 cells. Agonist and antagonist potency of all analogues was measured using the pigment aggregation response of a clonal line of Xenopus laevis melanophores, β-Methylmelatonin (17a) and β,β-dimethylmelatonin (17b), though showing a slight decrease in binding at human receptors, show an increase in potency on Xenopus, N-Butanoyl 5-methoxy-1-methyl-β,β-trimethylenetryptamine (12c) is an antagonist at human MT1 receptors but an agonist at MT2, while N-butanoyl 5-methoxy-1-methyl-β,β-tetramethylenetryptamine (13c) is an antagonist at MT1 but had no action at MT2 and is one of the first examples of an MT1 selective antagonist.
- Tsotinis, Andrew,Vlachou, Margarita,Papahatjis, Demetris P.,Calogeropoulou, Theodora,Nikas, Spyros P.,Garratt, Peter J.,Piccio, Vincent,Vonhoff, Stefan,Davidson, Kathryn,Teh, Muy-Teck,Sugden, David
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p. 3509 - 3519
(2007/10/03)
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