- 6-OXO-1,6-DIHYDROPYRIDAZINE DERIVATIVE, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF
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A 6-oxo-1,6-dihydropyridazine derivative, a preparation method therefor and medical use thereof, in particular, a 6-oxo-1,6-dihydropyridazine derivative represented by general formula (I), a preparation method therefor, and a pharmaceutical composition containing the derivative, and use thereof as a NaV inhibitor and use thereof in the preparation of a drug for the treatment and/or prevention of pain and pain-related diseases. Each substituent in general formula (I) is the same as defined in the description.
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Paragraph 0145-0146; 0201-0202
(2021/11/14)
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- Discovery of 1-(β-amino substituted-β-alanyl)-N,N- dimethylindoline-2-carboxamides as novel nonpeptide antagonists of nociceptin/orphanin FQ receptor: Efficient design, synthesis, and structure-activity relationship studies
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Since the discovery of endogenous nociceptin/orphanin FQ (N/OFQ) peptide and N/OFQ peptide (NOP) receptor [or opioid-receptor-like-1 (ORL1) receptor], the structures, distribution, and pharmacology have been reported in detail. N/OFQ and NOP receptor are
- Hayashi, Shigeo,Ohashi, Katsuyo,Nakata, Eriko,Emoto, Chie
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p. 228 - 242
(2012/11/07)
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- Synthesis of the NK1 receptor antagonist GW597599. Part 1: development of a scalable route to a key chirally pure arylpiperazine
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GW5975991 is a novel NK-1 antagonist currently under investigation for the treatment of CNS disorders and emesis. The initial synthetic route devised from the medicinal chemistry one, used several hazardous reagents, gave low yields, and produced high lev
- Guercio, Giuseppe,Bacchi, Sergio,Goodyear, Michael,Carangio, Antonella,Tinazzi, Francesco,Curti, Stefano
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p. 1188 - 1194
(2013/01/03)
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