BENZENE-SULFONATE DE 2-[[[2-[(HYDROXYACETYL)AMINO]-4-PYRIDINYL]METHYL]THIO]-N-[4-(TRIFLUOROMETHOXY)PHENYL]-3-PYRIDINECARBOXAMIDE, CRISTAUX DE CELUI-CI, SES POLYMORPHES ET SES PROCEDES DE FABRICATION
In the course of developing 2-[[[2-[(hydroxyacetyl) amino]- 4 -pyridinyl]methyl] thiol- N -[4 -(trifluoromethoxy) phenyl]- 3 -pyridinecarboxamide(compoundA), there are the multiple problems: 1) compound A or its salt is difficult toberecrystallized, the storage stability largely differs depending on the kind ofthe salt, andit is very difficult to obtain a salt of compound A having excellent storagestability； 2)in a crystallization process of compound A, it is very difficult to control acrystalpolymorph, and 3) compound A (free body) causes mineral deposition in thestomachwhen it is orally administered repeatedly. For solving these problems, we madeexamination focusing on the kind of the salt and, as a result, found that 1)benzenesulfonate of compound A does not decompose by light, humidity and otherfactors in a 1-week preliminary stability test (severe test), and has noproblem in itsstorage stability, 2) a method of selectively producing two kinds of crystalforms ofbenzenesulfonate of compound A, and that 3) no mineral deposition in thestomach isobserved even after a 4-week repeated oral administration.
