ZHANG, Dan,Yung- Chi LEE,Alfred LEE,William Anthony., Jr. MARINARO,Tao FENG,Deepak BAHL
申请号：
MX2017008078
公开号：
MX2017008078A
申请日:
2015.12.14
申请国别(地区):
MX
年份:
2017
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)pyrrolidine-3-carboxamide, wherein a total amount of active ingredient comprises by weight % about 60-90% (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-y1)-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-carboxamide Form 1 HCl, about 10-30% (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)pyrrolidine-3-carboxamide amorphous HCl, and about 0-5% (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)pyrrolidine-3-carboxamide amorphous free base.La invención incluye una composición granular que comprende el ingrediente activo (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-dihidr opiridin-1(2H)-il)-2-oxoetil)-3-(metiltio)pirrolidin-3-carboxamid a, en donde la cantidad total del ingrediente activo comprende, en % en peso, aproximadamente 60-90 % de la Forma 1 de HCI 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-dihidropiridin-1(2H)-il) -2-oxoetil)-3-(metiltio)pirrolidin-3-carboxamida, aproximadamente 10-30 % de HCI de (S)-N-(3-(6-isopropoxipiridin-3-il)-1H-indazol-5 -il)-1-(2-(4-(4-(1-metil-1H-1,2,4-triazol-3-iI)fenil)-3,6-dihidro piridin-1(2H)-il)-2-oxoetil)-3-(metiltio)pirrolidin-3-carboxamida amorfo, y aproximadamente 0-5 % de la base libre amorfa 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-dihidropiridin-1(2H)-il) -2-oxoetil)-3-(metiltio)pirrolidin-3-carbo
