57684-32-9Relevant articles and documents
NOVEL COMPOUNDS FOR THE TREATMENT OF PARASITIC INFECTIONS
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Page/Page column 37, (2019/08/14)
The present invention relates to novel compounds or pharmaceutically acceptable salts thereof, corresponding compositions, and methods and/or uses in therapy, for example in the treatment of parasitic infections such as malaria, in particular infection by
Synthesis of Gly-ψ[(Z)CFCH]-Phe, a Fluoroalkene Dipeptide Isostere, and Its Incorporation into a Leu-enkephalin Peptidomimetic
Nadon, Jean-Fran?ois,Rochon, Kristina,Grastilleur, Sébastien,Langlois, Guillaume,Dao, Thi Thanh Hà,Blais, Véronique,Guérin, Brigitte,Gendron, Louis,Dory, Yves L.
, p. 40 - 49 (2017/03/08)
A new Leu-enkephalin peptidomimetic designed to explore the hydrogen bond acceptor ability of the third peptide bond has been prepared and studied. This new analog is produced by replacing the third amide of Leu-enkephalin with a fluoroalkene. An efficient and innovative synthesis of the corresponding dipeptide surrogate Fmoc-Gly-ψ[(Z)CFCH]-Phe-OH is described. The key step involves the alkylation of a tin dienolate from the less hindered face of its chiral sulfonamide auxiliary derived from camphor. Once its synthesis was complete, its incorporation into the peptidomimetic sequence was achieved on a solid support with chlorotrityl resin following the Fmoc strategy. The peptidomimetic was characterized using competition binding with [125I]-deltorphin I on membrane extracts of HEK293 cells expressing the mouse delta opioid receptor (DOPr) and based on its abilities to inhibit the electrically induced contractions of the mouse vas deferens and to activate the ERK1/2 signaling pathway in DRGF11/DOPr-GFP cells. Together with our previous observations, our findings strongly suggest that the third amide bond of Leu-enkephalin primarily acts as a hydrogen bond acceptor in DOPr. Consequently, this amide bond can be successfully replaced by an ester, a thioamide, or a fluoroalkene without greatly impacting the binding or biological activity of the corresponding analogs. The lipophilicity (LogD7.4) of the active analog was also measured. It appears that fluoroalkenes are almost as efficient at increasing the lipophilicity as normal alkenes.
HETEROCYCLIC COMPOUND
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Paragraph 0564; 0971; 0972, (2017/04/11)
The present invention provides a heterocyclic compound having a CDK8 and/or CDK19 inhibitory effect. The present invention provides a compound represented by formula (I) (in the formula, the symbols are as defined in the description) or a salt thereof.
Heterocyclic compound
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Paragraph 0334, (2017/09/28)
本發明提供一種具有CDK8/19抑制活性之雜環化合物。本發明提供一種如下式代表之化合物(其中各代號均如本文之定義)或其鹽。 The present invention provides a heterocyclic compound possessing CDK8/19 inhibitory activity. The present invention provides a compound represented by the formula wherein each symbol is as defined herein, or a salt thereof.
HETEROARYL SUBSTITUTED NICOTINAMIDE COMPOUNDS
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Paragraph 0520, (2015/07/15)
Disclosed are compounds of Formula (I) or salts thereof, wherein: HET is a heteroaryl selected from pyrazolyl, indolyl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-d]pyrimidinyl, pyrazolo[3,4-b]pyridinyl, pyrazolo[3,4-d]pyrimidinyl, 2,3-dihydro-1H-pyrrolo[2,3-b]pyridinyl, imidazo[4,5-b]pyridinyl, and purinyl, wherein said heteroaryl is substituted with Ra and Rb; and R1 and R2 are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases.
DIHYDROIMIDAZO [ 1, 5-F] PTERIDINES AS POLO-LIKE KINASE INHIBITORS
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Page/Page column 17-20, (2010/04/06)
The present invention provides PLK inhibitors of the formula (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using the compounds.
POLO-LIKE KINASE INHIBITORS
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Page/Page column 235-236, (2009/05/29)
Compounds of the following formula are provided for use with kinases: (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates use
Methods and fluorinated compositions for treating amyloid-related diseases
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Page/Page column 66-67, (2008/06/13)
Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease. Also described are methods, compounds, pharmaceutical compositions and kits for detecting, diagnosing, monitoring and treating or preventing amyloid-related disease.
Synthesis of vinylogous β-amino esters from N-(N,N-dialkylaminoalkyl)benzotriazoles
Aurrecoechea, Jose M.,Fernandez, Alvaro,Gorgojo, Jose M.,Suero, Ruben
, p. 693 - 702 (2007/10/03)
Treatment of N-(N,N-dialkylaminoalkyl)benzotriazoles with 4- bromocrotonates in the presence of zinc provides a new route to 5-(N,N-dialkylamino)-2-alkenoate esters. This is formally the result of the γ-addition of zinc dienolate reagents to iminium catio
Synthesis of N-[1-(trialkylstannyl)alkyl]amides and -amines by the displacement of benzotriazoles with trialkylstannyllithiums
Pearson,Stevens
, p. 904 - 906 (2007/10/02)
Condensation of benzotriazole, an aldehyde, and either an amine or amide using the method of Katritzky gave N-[1-benzotriazol-1-yl)alkyl]amides and -amines, which were treated with tributylstannyllithium or trimethylstannyllithium to afford N-[1-(trialkylstannyl)alkyl]amides and -amines, respectively. These compounds are important precursors of nitrogen-substituted organolithium reagents.