114080-93-2Relevant articles and documents
A high-yielding method for the preparation of isoxazolopyridin-3-amine derivatives
Yu, Wensheng,Bulger, Paul G.,Maloney, Kevin M.
, p. 4941 - 4946 (2016/10/12)
A highly efficient and green method has been developed for the rapid preparation of highly functionalized isoxazolopyridin-3-amine derivatives in excellent yields. This process has a broad substrate scope, is operationally simple, and generally requires no chromatographic purification. In addition, the process is scalable and significantly greener than current alternatives with a PMI of 18 and water as the reaction solvent.
Discovery of novel 2-[2-(3-hydroxy-pyridin-2-yl)-thiazol-4-yl]-acetamide derivatives as HIF prolyl 4-hydroxylase inhibitors; SAR, synthesis and modeling evaluation
Hong, Yong Rae,Kim, Hyun Tae,Ro, Seonggu,Cho, Joong Myung,Lee, Sang Hwi,Kim, In Su,Jung, Young Hoon
, p. 3142 - 3145 (2014/06/24)
The design, synthesis, and capacity to inhibit HIF prolyl 4-hydroxylases (PHDs) are described for 2-[2-(3-hydroxy-pyridin-2-yl)-thiazol-4-yl]-acetamide analogs. These analogs revealed two kinds of novel scaffolds as PHD2 inhibitors. Synthetic routes were
Discovery of novel 2-[2-(3-hydroxy-pyridin-2-yl)-thiazol-4-yl]-acetamide derivatives as HIF prolyl 4-hydroxylase inhibitors; SAR, synthesis and modeling evaluation
Hong, Yong Rae,Kim, Hyun Tae,Ro, Seonggu,Cho, Joong Myung,Lee, Sang Hwi,Kim, In Su,Jung, Young Hoon
, p. 3142 - 3145 (2015/02/19)
The design, synthesis, and capacity to inhibit HIF prolyl 4-hydroxylases (PHDs) are described for 2-[2-(3-hydroxy-pyridin-2-yl)-thiazol-4-yl]-acetamide analogs. These analogs revealed two kinds of novel scaffolds as PHD2 inhibitors. Synthetic routes were
Heteroaryl urea inhibitors of fatty acid amide hydrolase: Structure-mutagenicity relationships for arylamine metabolites
Tichenor, Mark S.,Keith, John M.,Jones, William M.,Pierce, Joan M.,Merit, Jeff,Hawryluk, Natalie,Seierstad, Mark,Palmer, James A.,Webb, Michael,Karbarz, Mark J.,Wilson, Sandy J.,Wennerholm, Michelle L.,Woestenborghs, Filip,Beerens, Dominiek,Luo, Lin,Brown, Sean M.,Boeck, Marlies De,Chaplan, Sandra R.,Breitenbucher, J. Guy
, p. 7357 - 7362 (2013/02/21)
The structure-activity relationships for a series of heteroaryl urea inhibitors of fatty acid amide hydrolase (FAAH) are described. Members of this class of inhibitors have been shown to inactivate FAAH by covalent modification of an active site serine with subsequent release of an aromatic amine from the urea electrophile. Systematic Ames II testing guided the optimization of urea substituents by defining the structure-mutagenicity relationships for the released aromatic amine metabolites. Potent FAAH inhibitors were identified having heteroaryl amine leaving groups that were non-mutagenic in the Ames II assay.
Design, synthesis and evaluation of new α-nucleophiles for the hydrolysis of organophosphorus nerve agents: Application to the reactivation of phosphorylated acetylcholinesterase
Saint-Andre, Geraldine,Kliachyna, Maria,Kodepelly, Sanjeevarao,Louise-Leriche, Ludivine,Gillon, Emilie,Renard, Pierre-Yves,Nachon, Florian,Baati, Rachid,Wagner, Alain
scheme or table, p. 6352 - 6361 (2011/09/19)
A series of new α-nucleophiles including oximes and amidoximes have been synthesized, and their ability to efficiently and selectively cleave the P-S bond of organophosphorus nerve agents has been evaluated. The relationship between the chemical structure
SUBSTITUTED 3-AMINOISOXAZOLOPYRIDINES AS KCNQ2/3 MODULATORS
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Page/Page column 16, (2010/09/18)
The invention relates to substituted 3-aminoisoxazolopyridines, to processes for their preparation, to medicaments containing these compounds and to the use of these compounds in the preparation of medicaments.
HETEROARYL-SUBSTITUTED UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE
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Page/Page column 27, (2010/07/02)
Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).
HETEROARYL-SUBSTITUTED UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE
-
Page/Page column 31, (2010/07/02)
Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).