130628-75-0Relevant articles and documents
TRPV4 ANTAGONISTS
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Page/Page column 57-58, (2013/02/28)
The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
Substituted imidazo [1,5-a] pyrimido [5,4-d] [1] benzazepine derivatives
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, (2008/06/13)
The present invention is a compound of formula wherein R1 is halogen or lower alkyl; R2 is hydrogen, lower alkyl, cycloalkyl, —(CH2)m-phenyl, wherein the phenyl ring may be substituted by lower alkoxy, or is —(CH2)m-indolyl; R3 is —C(O)O-lower alkyl, —C(O)OH, or a five membered heteroaromatic group, which rings may be substituted by lower alkyl or cycloalkyl; n is 0, 1 or 2; m is 0, 1 or 2; or a pharmaceutically acceptable acid addition salt thereof. Compound I shows high affinity and selectivity for GALA A α5 receptor binding sites.
Synthese d'isoxazoles substitues en α de l'azote par une chaine alkyle ou alcenyle
Cherton, Jean-Claude,Lanson, Marc,Ladjama, Daif,Guichon, Yvette,Basselier, Jean-Jacques
, p. 1271 - 1276 (2007/10/02)
Several syntheses of special isoxazoles bearing a long alkyl or alkenyl side chain in the α position of the nitrogen are presented.A very convenient route in the case of an alkyl side chain is the classical 1,3-dipolar cycloaddition of a nitrile-oxide to a vinyl acetate.Although it is a rather long approach, the reaction of hydroxylamine with enone-epoxides represents a new and unequivocal method compatible with alkenyl side chains.The isomerisation of the easily synthesized isoxazoles bearing such substituents α to the oxygen, by the reaction of their isoxazolium salts with hydroxylamine, is a fast and general method.Another very convenient access to "α-N substituted" isoxazoles is the coupling of magnesium compounds with 3-bromomethyl 5-methyl isoxazole.
