- A high-yielding method for the preparation of isoxazolopyridin-3-amine derivatives
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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.
- Yu, Wensheng,Bulger, Paul G.,Maloney, Kevin M.
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p. 4941 - 4946
(2016/10/12)
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- Heteroaryl urea inhibitors of fatty acid amide hydrolase: Structure-mutagenicity relationships for arylamine metabolites
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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.
- 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
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p. 7357 - 7362
(2013/02/21)
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- SUBSTITUTED 3-AMINOISOXAZOLOPYRIDINES AS KCNQ2/3 MODULATORS
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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.
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Page/Page column 16
(2010/09/18)
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- HETEROARYL-SUBSTITUTED UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE
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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).
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Page/Page column 30
(2010/07/02)
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- HETEROARYL-SUBSTITUTED UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE
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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).
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Page/Page column 26
(2010/07/02)
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