286946-77-8Relevant articles and documents
METHODS FOR PREPARING SUBSTITUTED PYRIDINONE-CONTAINING TRICYCLIC COMPOUNDS
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Page/Page column 28-29, (2019/11/04)
The invention relates to novel, scalable methods of making substituted tricyclic compounds that are useful to treat and/or prevent HBV and/or HBV-HDV infection and related conditions in a subject.
Spiro compounds, preparation method thereof, intermediate, pharmaceutical composition and application
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Paragraph 0518-0520, (2018/04/02)
The invention discloses a spiro compound as shown in a formula I, a pharmaceutically acceptable salt, a hydrate, a solvate, an optical isomer or a prodrug of the spiro compound, as well as a preparation method, an intermediate, a pharmaceutical composition and an application of the spiro compound. The spiro compound disclosed by the invention has the activity of serving as protein kinase inhibitors and tyrosine kinase inhibitors such as c-Met, and the spiro compound can be used for treating diseases caused by the abnormal activity of kinases, such as cancer, or used for preparing medicaments for treating the diseases.
POLYCYCLIC PYRIDONE COMPOUNDS AS ANTIVIRALS
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Paragraph 00183, (2018/03/28)
The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by hepatitis B virus, and reducing the occurrence of serious conditions associated with HBV.
AROMATIC RING COMPOUND
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Paragraph 0338, (2015/03/28)
The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.
An efficient large-scale synthesis of alkyl 5-hydroxy-pyridin- and pyrimidin-2-yl acetate
Morgentin, Rémy,Jung, Frédéric,Lamorlette, Maryannick,Maudet, Micka?l,Ménard, Morgan,Plé, Patrick,Pasquet, Georges,Renaud, Fabrice
experimental part, p. 757 - 764 (2009/04/07)
The synthesis of methyl 2-(5-hydroxy-3-methoxypyridin-2-yl)acetate and alkyl 2-(5-hydroxypyrimidin-2-yl)acetate is described. Methodology for an efficient access to 5-hydroxy-pyridin- and pyrimidin-2-yl acetate cores has been developed. Based on the difference in halogen reactivity, 5-bromo-2-chloropyridine and its pyrimidine analogue were functionalized judiciously by SNAr and palladium-catalyzed reactions. The outlined strategy provides a high-yielding route suitable for large-scale synthesis of these compounds as well as paves the way for a potential rapid access to other heterocyclic analogues.
Structure-activity studies and analgesic efficacy of N-(3-pyridinyl)- bridged bicyclic diamines, exceptionally potent agonists at nicotinic acetylcholine receptors
Bunnelle, William H.,Daanen, Jerome F.,Ryther, Keith B.,Schrimpf, Michael R.,Dart, Michael J.,Gelain, Arianna,Meyer, Michael D.,Frost, Jennifer M.,Anderson, David J.,Buckley, Michael,Curzon, Peter,Cao, Ying-Jun,Puttfarcken, Pamela,Searle, Xenia,Ji, Anguo,Putman, C. Brent,Surowy, Carol,Toma, Lucio,Barlocco, Daniela
, p. 3627 - 3644 (2008/02/11)
A series of exceptionally potent agonists at neuronal nicotinic acetylcholine receptors (nAChRs) has been investigated. Several N-(3-pyridinyl) derivatives of bridged bicyclic diamines exhibit double-digit-picomolar binding affinities for the α4β2 subtype, placing them with epibatidine among the most potent nAChR ligands described to date. Structure-activity studies have revealed that substitutions, particularly hydrophilic groups in the pyridine 5-position, differentially modulate the agonist activity at ganglionic vs central nAChR subtypes, so that improved subtype selectivity can be demonstrated in vitro. Analgesic efficacy has been achieved across a broad range of pain states, including rodent models of acute thermal nociception, persistent pain, and neuropathic allodynia. Unfortunately, the hydrophilic pyridine substituents that were shown to enhance agonist selectivity for central nAChRs in vitro tend to limit CNS penetration in vivo, so that analgesic efficacy with an improved therapeutic window was not realized with those compounds.
Heterocyclic substituted aminoazacycles useful as central nervous system agents
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Page 37, (2010/02/07)
Heterocyclic substituted aminoazacyclic compounds of the formula (I):Z-R3, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.
DIAZABICYCLIC DERIVATIVES AS NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
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Page/Page column 30, (2010/02/04)
Compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein: V is selected from the group consisting of a covalent bond and CH2; W is selected from the group consisting of a covalent bond, CH2and CH2CH2; X is selected from the group consisting of a covalent bond and CH2; Y is selected from the group consisting of a covalent bond, CH2, and CH2CH2; Z is selected from the group consisting of CH2, CH2CH2, and CH2 CH2 CH2; L1is selected from the group consisting of a covalent bond and (CH2)n; n is 1-5; R1 is selected from the group consisting of (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), and (l); R2is selected from the group consisting of hydrogen, alkoxycarbonyl, alkyl, aminoalkyl, aminocarbonylalkyl, benzyloxycarbonyl, cyanoalkyl, dihydro-3-pyridinylcarbonyl, hydroxy, hydroxyalkyl, phenoxycarbonyl, and-NH2; are useful for controlling synaptic transmission in mammal.
Diazabicyclic CNS active agents
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Page 28, (2010/02/05)
Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.
Diazabicyclic central nervous system active agents
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, (2008/06/13)
Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.