ALFRED LEE,DAN ZHANG,DEEPAK BAHL,TAO FENG,WILLIAM ANTHONY MARINARO JR.,YUNG-CHI LEE
申请号：
BR112017012558
公开号：
BR112017012558A2
申请日:
2015.12.14
申请国别(地区):
BR
年份:
2018
代理人:
摘要：
The invention includes a granular composition comprising the active ingredient (s) -n- (3- (6-isopropoxypyridin-3-yl) -1h-indazol-5-yl) -1- (2- (4- (4- (1-methyl-1h-1,2,4-triazol-3-yl) phenyl) -3,6-dihydropyridin-1 (2h) -yl) -2-oxoethyl) -3- (methylthio) pyrrolidin-3 carboxamide, wherein the total amount of active ingredient comprises by weight about 60 to 90% of form 1 of (s) -n- (3- (6-isopropoxypyridin-3-yl) -1h-indazol-5- yl) -1- (2- (4- (4- (1-methyl-1h-1,2,4-triazol-3-yl) phenyl) -3,6-dihydropyridin-1 (2h) -yl) - 2-oxoethyl) -3- (methylthio) pyrrolidin-3-carboxamide hcl, about 10 to 30% of (s) -n- (3- (6-isopropoxypyridin-3-yl) -1h-indazol-5-yl ) -1- (2- (4- (4- (1-methyl-1h-1,2,4-triazol-3-yl) phenyl) -3,6-dihydropyridin-1 (2h) -yl) -2 amorphous -oxoethyl) -3- (methylthio) pyrrolidin-3-carboxamide and about 0 to 5% free base of (s) -n- (3- (6-isopropoxypyridin-3-yl) -1h-indazol-2-yl) 5-yl) -1- (2- (4- (4- (1-methyl-1h-1,2,4-triazol-3-yl) phenyl) -3,6-dihydropyridin-1 (2h) -yl ) -2-oxoethyl) -3- (methylthio) pyrrolidine-3-amorphous carboxamide.a invenção inclui uma composição granular que compreende o ingrediente ativo (s)-n-(3-(6-isopropoxipiridin-3-il)-1h-indazol-5-il)-1-(2-(4-(4-(1-metil-1h-1,2,4-triazol-3-il)fenil)-3,6-diidropiridin-1(2h)-il)-2-oxoetil)-3-(metiltio)pirrolidina-3-carboxamida, em que a quantidade total de ingrediente ativo compreende em % em peso cerca de 60 a 90% de forma 1 de (s)-n-(3-(6-isopropoxipiridin-3-il)-1h-indazol-5-il)-1-(2-(4-(4-(1-metil-1h-1,2,4-triazol-3-il) fenil)-3,6-diidropiridin-1(2h)-il)-2-oxoetil)-3-(metiltio)pirrolidina-3-carboxamida hcl, cerca de 10 a 30% de (s)-n-(3-(6-isopropoxipiridin-3-il)-1h-indazol-5-il)-1-(2-(4-(4-(1-metil-1h-1,2,4-triazol-3-il)fenil)-3,6-diidropiridin-1(2h)-il)-2-oxoetil)-3-(metiltio)pirrolidina-3-carboxamida hcl amorfa e cerca de 0 a 5% de base livre de (s)-n-(3-(6-isopropoxipiridin-3-il)-1h-indazol-5-il)-1-(2-(4-(4-(1-metil-1h-1,2,4-triazol-3-il)fenil)-3,6-diidropiridin-1(2h)-il)-2-oxoetil)-3-
