[EN] PHARMACEUTICAL FORMULATION OF CROTONYLAMINOPYRIDINE SALT<br/>[FR] FORMULATION PHARMACEUTIQUE DE SEL DE CROTONYLAMINOPYRIDINE
申请人:INTERVET INT BV
公开号:WO2018178345A1
公开(公告)日:2018-10-04
The present invention is directed to a salt of a compound of formula (I), R1 is halogen or methyl; X is methyl, OR2, or SR2; Y1, Y2 is CR3 or N, and one of Y1, Y2 is N and one of Y1, Y2 is CR3; R2 is methyl or ethyl; R3 is hydrogen or methyl, wherein the salt is chosen from the group 10 consisting of malate salt, citrate salt, tartrate salt, oxalate salt, fumarate salt, lactate salt, glucoronate salt, oxoglucoronate salt, ethanesulfonate salt, and succinate salt. The present invention is further related to a pharmaceutical formulation comprising the salt of the invention wherein the base compound is present in an amount of 2-30% (w/v) and having a pH value of at least 3.7 and to methods of treatment using the salt of the invention.
本发明涉及公式(I)化合物的盐,其中R1为卤素或甲基;X为甲基,OR2或SR2;Y1,Y2为CR3或N,其中Y1,Y2中的一个为N,另一个为CR3;R2为甲基或乙基;R3为氢或甲基,所述盐选自以下组中的一种:苹果酸盐,柠檬酸盐,酒石酸盐,草酸盐,富马酸盐,乳酸盐,葡萄糖醛酸盐,草醛酸盐,乙烷磺酸盐和琥珀酸盐。本发明还涉及一种制药配方,包括本发明的盐,其中基础化合物的含量为2-30%(w/v),pH值至少为3.7,并涉及使用本发明的盐进行治疗的方法。