29026-75-3Relevant academic research and scientific papers
Exploration of the structure-activity relationship of the diaryl anilide class of ligands for translocator protein - Potential novel positron emitting tomography imaging agents
Wadsworth, Harry,Jones, Paul A.,Chau, Wai-Fung,Durrant, Clare,Morisson-Iveson, Veronique,Passmore, Joanna,O'Shea, Dennis,Wynn, Duncan,Khan, Imtiaz,Black, Andrew,Avory, Michelle,Trigg, William
, p. 5795 - 5800,6 (2020/07/30)
A series of novel ligands based on the diaryl anilide (DAA) class of translocator protein (TSPO) ligands was synthesised and evaluated as potential positron emitting tomography (PET) ligands for imaging TPSO in vivo. Fluorine-18 labelling of the molecules was achieved using direct radiolabelling or synthon based labelling approaches. Several of the ligands prepared have promising profiles as potential TSPO PET imaging ligands and will be evaluated further as potential clinical imaging agents.
NOVEL USE OF THIENOPYRIMIDINES
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Page/Page column 34, (2010/11/27)
The present invention relates to the use of thienopyrimidine compounds for the production of pharmaceutical compositions for the treatment of inflammatory diseases.
THIENOPYRIMIDINES FOR PHARMACEUTICAL COMPOSITIONS
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Page/Page column 51, (2010/11/25)
The present invention relates to novel pharmaceutical compositions of general formula (I) comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
Aryl piperidine amides
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Page/Page column 15, (2010/02/11)
The invention provides novel GlyT2 inhibiting compounds useful in modulating, treating, or preventing: anxiolytic disorders; a condition requiring treatment of injured mammalian nerve tissue; a condition amenable to treatment through administration of a neurotrophic factor; a neurological disorder; or obesity; an obesity-related disorder.
Inhibitors of the glycine transporter type-2 (GlyT-2): synthesis and biological activity of benzoylpiperidine derivatives.
Wolin, Ronald L,Santillan Jr., Alejandro,Tang, Liu,Huang, Charles,Jiang, Xiaoxia,Lovenberg, Timothy W
, p. 4511 - 4532 (2007/10/03)
A series of benzoylpiperidine analogs related to 4a was prepared, and their ability to inhibit the uptake of [(14)C]-glycine in COS7 cells transfected with human glycine transporter type-2 (GlyT-2) was evaluated. Small structural changes to the benzoylpiperidine region of the molecule led to a significant decrease in GlyT-2 inhibitory activity. In contrast, the distal aryl ring was more tolerant to functional group modifications and could accommodate a variety of substitutes at the C-2 or C-3 positions. Comparable activities to 4a were obtained by replacing the anilino nitrogen with an ether linkage 27 or by exchanging the isopropoxy ether moiety with an isopropyl amino group 15. A distinct preference for a 2-carbon tether (n=1) was observed relative to the corresponding 3-carbon homolog (n=2).
N-(N'-Methylenepyrrolidonyl)-2-substituted anilines
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, (2008/06/13)
This invention relates to novel N-(N'-methylenepyrrolidonyl)-2-substituted anilines which are useful intermediates in the synthesis of herbicides. The intermediate compounds of the invention have the formula: STR1 Where R is alkyl, C1 -C6, alkenyl, C3 -C5, alkyleneoxyalkyl, --(CH2)n OR", where n=1-3, and R" is alkyl, C1 -C3, and cycloalkyl, STR2 where n'=0-3, R' is hydrogen or alkyl, C1 -C3, and, Y is oxygen or sulfur.
Process for making N-(N'-methylenepyrrolidonyl)-2-substituted anilines
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, (2008/06/13)
This invention relates to a process for making N-(N'-methylenepyrrolidonyl)-2-substituted anilines in high yield. The products are useful intermediates in the synthesis of herbicides. The process comprises reacting substantially equivalent molar concentrations of a 2-substituted aniline, as defined herein, with N-methylolpyrrolidone in an aromatic hydrocarbon solvent in the absence of an acid or base catalyst at a reflux temperature of 80°-140° C. while simultaneously and continuously distilling out from the reaction mixture an azeotrope consisting essentially of water and solvent until substantially all the water produced during the reaction has been removed thereby, and, thereafter, crystallizing the product from the remaining solution.
Process for making N-(N'-methylenepyrrolidonyl)-2-substituted anilines
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, (2008/06/13)
This invention relates to an improved process for making N-(N'-methylenepyrrolidonyl)-2-substituted anilines which are useful intermediates in the synthesis of agricultural herbicides. This process of the invention comprises reacting a 2-substituted aniline with N-chloromethylpyrrolidone at about room temperature in the presence of an acid acceptor. Such room temperature alkylation of the aniline prevents excessive side reactions, particularly with a substituent in the 2-position of the aniline, such as an alkenyl group, which is sensitive to alkylating agents which require excessive heating to effective the condensation reaction.
Herbicidal N-(haloacetyl)-N'-methylenepyrrolidonyl)-2-cycloalkoxyanilines
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, (2008/06/13)
Herbicidal compounds having the formula: STR1 where N=0-3, R is hydrogen or alkyl of 1-3 carbon atoms, and X is chloro or bromo, Are provided herein. The compounds of the invention are effective herbicides, particularly against wild grasses.
