- USE OF T-TYPE CALCIUM CHANNEL BLOCKER FOR TREATING PRURITUS
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A medicament for treating or preventing pruritus is provided. For the medicament for treating or preventing pruritus, a compound having a blocking action on Cav3.2T-type calcium channels represented by General Formulas (I) to (VI), a tautomer of the compo
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- T-TYPE CALCIUM CHANNEL BLOCKER
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To provide a novel T-type calcium channel blocker. A compound represented by the following General Formula (I), a tautomer or a stereoisomer of the compound, a pharmaceutically acceptable salt of the compound, or a solvate of the compound, the tautomer, the stereoisomer, or the salt is used as a T-type calcium channel blocker. wherein A represents a phenyl which may have a substituent, a 4-membered to 6-membered heteroaryl ring composed of one to three identical or different heteroatoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom and carbon atoms as ring-constituting atoms, or a heterocondensed ring composed of the heteroaryl ring and either a benzene ring or a 6-membered heteroaryl ring composed of one to two nitrogen atoms and carbon atoms, wherein the heteroaryl ring or the heterocondensed ring may have a substituent and is bonded to a nitrogen atom of the adjacent cyclic amino by means of a carbon atom constituting these rings; B represents a phenyl which may have a substituent, a 5-membered or 6-membered heteroaryl ring composed of one to three identical or different heteroatoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom and carbon atoms as ring-constituting atoms, or a heterocondensed ring composed of the heteroaryl ring and either a benzene ring or a 6-membered heteroaryl ring composed of one to two nitrogen atoms and carbon atoms, wherein the heteroaryl ring or the heterocondensed ring may have a substituent and is bonded to the adjacent cyclopropyl ring by means of a carbon atom constituting these rings; R1 and R2, which may be identical or different, each represent a hydrogen atom, a halogen atom, or the like; R3 represents a hydrogen atom, a halogen atom, or the like; n and m, which may be identical or different, each represent 0 or 1; and p represents 1 or 2.
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- Preparation method of (5-trifluoromethyl-pyridin-2-yl)-acetate
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The invention relates to a preparation method of (5-trifluoromethyl-pyridin-2-yl)-acetate. The preparation method comprises the following steps: 1), dissolving 2-bromo-5-trifluoromethylpyridine, diethyl malonate, a catalyst A and a catalyst B in a first organic solvent, adding alkali, and reacting to obtain 2-(5-trifluoromethyl-pyridin-2-yl) diethyl malonate; 2), dissolving the alkali in a secondsolvent, adding the 2-(5-trifluoromethyl-pyridin-2-yl) diethyl malonate, and reacting to obtain (5-trifluoromethyl-pyridin-2-yl)-acetic acid; 3), dissolving the alkali in the second solvent, adding the (5-trifluoromethyl-pyridin-2-yl)-acetic acid, and reacting to obtain a final product. By the preparation method, the product is easy to separate and purify, the product value is high, the stabilityis strong and the reaction controllability is strong.
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Paragraph 0022; 0025; 0027; 0030
(2019/01/08)
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- Optimization of a series of quinazolinone-derived antagonists of CXCR3
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The evaluation of the CXCR3 antagonist AMG 487 in clinic trials was complicated due to the formation of an active metabolite. In this Letter, we will discuss the further optimization of the quinazolinone series that led to the discovery of compounds devoi
- Liu, Jiwen,Fu, Zice,Li, An-Rong,Johnson, Michael,Zhu, Liusheng,Marcus, Andrew,Danao, Jay,Sullivan, Tim,Tonn, George,Collins, Tassie,Medina, Julio
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scheme or table
p. 5114 - 5118
(2010/03/31)
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