- Method for preparing 6-chlorine-5-trifluoromethyl-2-aminopyridine
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The invention provides a method for preparing 6-chlorine-5-trifluoromethyl-2-aminopyridine. According to the method, a product is obtained by taking 6-chlorine-5-iodine-2-aminopyridine as a raw material and adopting reaction steps such as amino protection, trifiuoroniethylation and deprotection.
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Paragraph 0007-0008
(2019/06/07)
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- FUSED BICYLIC PYRIDINE COMPOUNDS AND THEIR USE AS AMPA RECEPTOR MODULATORS
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Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, N-oxides, or solvates thereof, Also provided herein are pharmaceutical compositions comprising compounds of Formula (I) and methods of using compounds of Formula (I).
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Paragraph 0243
(2018/05/03)
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- Ligand structure includes a new metal complexes
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Compounds comprising a metal complex having novel ligands are provided. In particular, the compound is an iridium complex comprising novel aza DBX ligands. The compounds may be used in organic light emitting devices, particularly as emitting dopants, providing improved efficiency, low operating voltage, and long lifetime.
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Paragraph 0332; 0333; 0334
(2016/11/24)
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- FACTOR XIa INHIBITORS
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The present invention provides a compound of Formula (I); and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
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Page/Page column 50
(2016/11/02)
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- Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABAA receptor agonists
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A series of 6-aminonicotinic acid analogues have been synthesized and pharmacologically characterized at native and selected recombinant GABA A receptors. 6-Aminonicotinic acid (3) as well as 2- and 4-alkylated analogues (9-11, 14-16) display low to mid-micromolar GABAAR binding affinities to native GABAA receptors (Ki 1.1-24 μM). The tetrahydropyridine analogue of 3 (22) shows low-nanomolar affinity (K i 0.044 μM) and equipotency as an agonist to GABA itself as well as the standard GABAA agonist isoguvacine. Cavities surrounding the core of the GABA binding pocket were predicted by molecular interaction field calculations and docking studies in a α1β 2γ2 GABAA receptor homology model, and were confirmed by affinities of substituted analogues of 3. The tight steric requirements observed for the remarkably few GABAAR agonists reported to date is challenged by our findings. New openings for agonist design are proposed which potentially could facilitate the exploration of different pharmacological profiles within the GABAAR area.
- Petersen, Jette G.,S?rensen, Troels,Damgaard, Maria,Nielsen, Birgitte,Jensen, Anders A.,Balle, Thomas,Bergmann, Rikke,Fr?lund, Bente
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p. 404 - 416
(2014/08/05)
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- PYRIDINONE AND PYRIMIDINONE DERIVATIVES AS FACTOR XIA INHIBITORS
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The present invention provides compounds of the general formula (I), their salts and N- oxides, and solvates and prodrugs thereof (wherein the characters are as defined in the description). The compounds of the general formula (I) are inhibitors of Factor XIa, so that they are useful in the prevention of and/or therapy for thromboembolic diseases.
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Page/Page column 243
(2013/07/05)
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- Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A2B adenosine receptor antagonists
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The synthesis and SAR of a series of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent A2B adenosine receptor antagonists is described. Several compounds showed good selectivity versus other adenosine receptors. The potent and selective analogue 9 was shown to have good oral bioavailability in the rat.
- Eastwood, Paul,Gonzalez, Jacob,Paredes, Sergio,Nueda, Arsenio,Domenech, Teresa,Alberti, Joan,Vidal, Bernat
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scheme or table
p. 1697 - 1700
(2010/08/06)
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