19819-95-5Relevant articles and documents
Dihydroxy pyrimidine compound and use thereof
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Paragraph 0026-0028, (2019/07/04)
The invention provides a dihydroxy pyrimidine compound, its structural general formula is: Wherein R1 In order to contain the substituent of the aryl, heterocyclic or containing substituent is C1 - C6 alkyl; R2 Is C1 - C6 alkyl, C1 - C6 alkyl aryl, C1 - C6 alkyl heterocyclic group or a hydrogen atom; x, y each is between 0 - 6 is any natural number. The invention also provides a two-hydroxy pyrimidine compounds in the preparation of anti-influenza virus in the application. The present invention provides a dihydroxy pyrimidine compounds to the influenza virus activity has better inhibition, can remarkably reduce the toxicity of the influenza virus, and cytotoxicity is relatively low, thus can such compounds for the preparation of anti-influenza virus drugs.
Discovery, synthesis, and structure-activity relations of 3,4-dihydro-1H-spiro(naphthalene-2,2′-piperidin)-1-ones as potassium-competitive acid blockers
Imaeda, Toshihiro,Ono, Koji,Nakai, Kazuo,Hori, Yasunobu,Matsukawa, Jun,Takagi, Terufumi,Fujioka, Yasushi,Tarui, Naoki,Kondo, Mitsuyo,Imanishi, Akio,Inatomi, Nobuhiro,Kajino, Masahiro,Itoh, Fumio,Nishida, Haruyuki
, p. 3719 - 3735 (2017/06/13)
With the aim to discover a gastric antisecretory agent more potent than the existing proton pump inhibitors, novel 3,4-dihydro-1H-spiro(naphthalene-2,2′-piperidin)-1-one derivatives, which could occupy two important lipophilic pockets (described as LP-1 and LP-2) of H+,K+-ATPase and can strongly bind to the K+-binding site, were designed based on a docking model. Among the compounds synthesized, compound 4d showed a strong H+,K+-ATPase-inhibitory activity and a high stomach concentration in rats, resulting in potent inhibitory action on histamine-stimulated gastric acid secretion in rats. Furthermore, 4d exerted significant inhibitory action on histamine-stimulated gastric-acid secretion in rats with a rapid onset and moderate duration of action after the administration. These findings may lead to a new insight into the drug design of potassium-competitive acid blockers.
Preparation method for hemihydrate lorcaserin hydrochloride
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Paragraph 0106; 0107, (2017/08/28)
The invention discloses a preparation method for hemihydrate lorcaserin hydrochloride. The preparation method comprises the following steps: (1) making a compound shown as a formula III react with ammonia to obtain a compound shown as a formula II; (2) under the protection of nitrogen gas, dissolving the compound shown as the formula II in an organic solvent, adding a hydrogen chloride solution of which the solvent is the organic solvent to salify, and adding water and cyclohexane to form a hemihydrate in order to obtain the compound shown as a formula I, wherein the organic solvent is isopropanol or 1,4-dioxane. In the preparation method disclosed by the invention, ammonium hydroxide substitutes for potassium carbonate in the prior art, so that unqualified ignition residues of a finial product caused by potassium chloride generated after salt removal can be avoided; an isopropoxide hydrochloride solution substitutes for the conventional hydrogen chloride gas, so that other impurities can be prevented from being introduced in a preparation process under the improper control of dosage and rate of the gas.
