18617-50-0Relevant articles and documents
Original synthesis of radiolabeling precursors for batch and on resin one-step/late-stage radiofluorination of peptides
Richard, Mylène,Specklin, Simon,Roche, Mélanie,Hinnen, Fran?oise,Kuhnast, Bertrand
supporting information, p. 2507 - 2510 (2020/03/06)
Radiolabeling of peptides with fluorine-18 is hurdled by their chemical sensitivity and complicated processes. Original triflyl-pyridine intermediates afforded ammonium precursors that were radiolabeled at low temperature. From that study, a generic tag h
SUBSTITUTED 6-(1H-PYRAZOL-1-YL)PYRIMIDIN-4-AMINE DERIVATIVES AND USES THEREOF
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Page/Page column 309-310, (2018/04/27)
The present invention covers substituted 6-(1H-pyrazol-1-yl)pyrimidin-4-amine compounds of general formula (I) as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular and renal diseases, as a sole agent or in combination with other active ingredients.
Tri- and difluoromethoxylated N-based heterocycles ? Synthesis and insecticidal activity of novel F3CO- and F2HCO-analogues of Imidacloprid and Thiacloprid
Landelle, Gregory,Schmitt, Etienne,Panossian, Armen,Vors, Jean-Pierre,Pazenok, Sergiy,Jeschke, Peter,Gutbrod, Oliver,Leroux, Frédéric R.
, p. 155 - 165 (2017/09/07)
The preparation of F3CO- and F2HCO-analogues of Imidacloprid and Thiacloprid and the evaluation of their biological activity have been performed. For this purpose, a first synthetic approach allowed the preparation of a desired F3CO-containing key intermediate. To allow a facile access to the second F2HCO-containing key intermediate, the difluoromethylation of hydroxylated N-based heterocycles has been developed using difluoromethyl triflate (a liquid non-ODS reagent) under air in aqueous conditions and with very short reaction time. The broad diversity of compatible heterocycles includes a large series of substituted hydroxy-pyridines, but also ?pyrazoles, ?pyrazine, ?pyridazine, and ?quinolines. The couplings of both key intermediates with the required 4,5-dihydro-N-nitro-1H-imidazol-2-amine and [N(Z)]-N-2-thiazolidinylidene-cyanamide were successfully achieved using literature conditions. This work enables the preparation of valuable building blocks, which could lead to the discovery of new bioactive entities.
SPIRO-OXADIAZOLINE COMPOUNDS AS AGONISTS OF α-7-NICOTINIC ACETYLCHOLINE RECEPTORS
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Paragraph 00496-00497, (2015/05/19)
The present invention relates to novel spiro-oxadiazoline compounds that are suitable as agonists or partial agonists of a7-nAChR, and pharmaceutical compositions of the same, methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering a spiro-oxadiazoline cx7-nAChR agonist or partial agonist, to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.
CARBINOL DERIVATIVES HAVING CYCLIC LINKER
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Page/Page column 83, (2010/03/31)
[Object] To provide a novel LXRβ agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate.
PYRIDAZINYL AMINE DERIVATIVES, THE USE THEREOF IN THE PREPARATION OF PICORNA VIRUS INHIBITORS
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Page/Page column 14-15, (2008/06/13)
The present invention relates to substituted pyridazinylamine derivatives of the formula I or pharmaceutically acceptable salts or hydrates thereof, wherein the substituents are defined as in the description, their preparation process, pharmaceutical compositions comprising them, and uses of the said compounds as picorna virus inhibitors for prevention and/or treatment of diseases caused by picorna viruses.
SUBSTITUTED PYRAZOLE COMPOUNDS USEFUL AS SOLUBLE EPOXIDE HYDROLASE INHIBITORS
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Page/Page column 90, (2008/06/13)
Disclosed are compounds active against soluble epoxide hydrolase (sEH), compositions thereof and methods of using and making same.
NOVEL ANTIMALARIA AGENT CONTAINING HETEROCYCLIC COMPOUND
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Page/Page column 61, (2008/06/13)
Disclosed is an antimalarial agent containing a compound represented by the formula: [wherein A1 represents a 3-pyridyl group that may have a substituent, a 6-quinolyl group that may have a substituent, or the like; X1 represents a group represented by the formula -C(=O)-NH- or the like; E represents a furyl group, a thienyl group or a phenyl group; with the proviso that A1 may have one to three substituents, and E has one of two substituents] or a salt thereof or hydrates thereof.
NOVEL ANTIFUNGAL AGENT COMPRISING HETEROCYCLIC COMPOUND
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Page/Page column 69, (2010/11/08)
The present invention provides an antifungal agent represented by the formula: [wherein A1 represents a 3-pyridyl group which may have a substituent, a quinolyl group which may have a substituent, or the like; X1 represents a group represented by the formula -NH-C(=O)-, a group represented by the formula -C(=O)-NH-, or the like; E represents a furyl group, a thienyl group, a pyrrolyl group, a phenyl group, a pyridyl group, a tetrazolyl group, a thiazolyl group or a pyrazolyl group; with the proviso that A1 may have 1 to 3 substituents, and E has one or two substituents].
Synthesis of 2,3-disubstituted 4-pyridone from a β-aminocarboxylate derivative and acetoacetate
Sobczak, Adam,Antkowiak, Wieslaw Z.
, p. 2993 - 3001 (2007/10/03)
The reaction of diethyl aminomethylenemalonate with ethyl acetoacetate proceeded, when catalyzed by anhydrous hydrogen chloride, toward a respectively substituted α- instead of γ-pyridone derivative formation, contrary to the literature report. Additionally, it was found that the amine used as a starting component in this reaction showed a great tendency to autocondensation under the influence of anhydrous hydrogen chloride to yield 5-ethoxycarbonyl-2- pyridone. The most convenient method to prepare 4-pyridone 2,3-disubstituted derivative appeared to be a three-step synthesis, starting from a chain enamine formation, which was subjected to cyclization, followed by oxidation of the last intermediate. The usefulness of the stepwise synthesis was demonstrated on the 3-ethoxycarbonyl-2-methyl-4-pyridone preparation as an example. Copyright Taylor & Francis, Inc.