- Synthesis, SAR, and Pharmacological Characterization of Brain Penetrant P2X7 Receptor Antagonists
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We describe the synthesis and SAR of 1,2,3-triazolopiperidines as a novel series of potent, brain penetrant P2X7 antagonists. Initial efforts yielded a series of potent human P2X7R antagonists with moderate to weak rodent potency, some CYP inhibition, poo
- Savall, Brad M.,Wu, Duncan,De Angelis, Meri,Carruthers, Nicholas I.,Ao, Hong,Wang, Qi,Lord, Brian,Bhattacharya, Anindya,Letavic, Michael A.
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p. 671 - 676
(2015/06/23)
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- P2X7 MODULATORS
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The present invention is directed to compounds of Formulas (I, IIa and IIb): The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, IIa and IIb). Methods of making and using the compounds of Formulas (I, IIa and IIb) are also within the scope of the invention.
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- Use of the graebe-ullmann reaction in the synthesis of 8-methyl-γ- carboline and isomeric aromatic aza-γ-carbolines
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Two variants of the Graebe-Ullmann reaction were used to obtain 8-methyl-5H-pyrido[4,3-b]indole (8-methyl-γ-carboline) and the conditions for this reaction were optimized. The feasibility of using this method was studied for the synthesis of a series of isomeric aromatic aza-γ- carbolines from the corresponding 1-(pyridyl)-1H-1,2,3-triazolo[4,5-c]pyridines under thermal and microwave irradiation conditions.
- Alekseev,Kurkin,Yurovskaya
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p. 1235 - 1250
(2013/03/13)
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- SYNTHESIS AND THERMAL DECOMPOSITION OF 3-(2-PYRIDYL)-3H-1,2,3-TRIAZOLO AND PYRIDINES AND THEIR N-OXIDES
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3-(2-Pyridyl)-3H-1,2,3-triazolopyridine (8) upon heating in paraffin oil or polyphosphoric acid, does not give 1,8-diazacarbazole (14), but yields instead bis(2-pyridyl)amine (15) and 2-(2-pyridylamino)-3-hydroxypyridine phosphate (16), respectively; the latter compound is also obtained by treating 3-(1-oxide-2-pyridyl)-3H-1,2,3-triazolopyridine (10) with polyphosphoric acid.However, 3-(4-pyridyl)-3H-1,2,3-triazolopyridine (20) is converted by polyphosphoric acid into 3,6-diazacarbazole (23) and 4-(4-pyridylamino)-3-hydroxypyridine (24).
- Kalinowski, Jerzy,Rykowski, Andrzej,Nantka-Namirski, Pawel
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p. 125 - 134
(2007/10/02)
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