COMPOSITIONS DE (S)-N-(3-(6-ISOPROPOXYPYRIDIN-3-YL)-1H-INDAZOL-5-YL)-1-(2-(4-(4-(1-MÉTHYL-1H-1,2,4-TRIAZOL-3-YL)PHÉNYL)-3,6-DIHYDROPYRIDIN-1(2H)-YL)-2-OXOÉTHYL)-3- (MÉTHYLTHIO)PYRROLIDINE-3-CARBOXAMIDE POUR PRÉPARATIONS PHARMACEUTIQUES

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专利权人:

MARINARO, William Anthony, Jr.;BAHL, Deepak;ZHANG, Dan;LEE, Yung-Chi;FENG, Tao;MERCK SHARP & DOHME CORP.;LEE, Alfred

发明人:

BAHL, Deepak,LEE, Yung-Chi,LEE, Alfred,MARINARO, William Anthony, Jr.,ZHANG, Dan,FENG, Tao

申请号：

USUS2015/065434

公开号：

WO2016/100152A1

申请日:

2015.12.14

申请国别(地区):

US

年份:

2016

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.L'invention comprend une composition granulaire comprenant le principe actif (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-méthyl-1H-1,2,4-triazol-3-yl)phényl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoéthyl)-3-(méthylthio)pyrrolidine-3-carboxamide, une quantité totale de principe actif comprenant en % en poids environ 60-90 % de (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-y1)-1-(2-(4-(4-(1-méthyl-1H-1,2,4-triazol-3-yl)phényl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoéthyl)-3-(méthylthio)pyrrolidine-3-carboxamide HCl Forme 1, environ 10-30 % de (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-méthyl-1H-1,2,4-triazol-3-yl)phényl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoéthyl)-3-(méthylthio)pyrrolidine-3-carboxamide HCl amorphe, et environ 0-5 % de (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-méthyl-1H-1,2,4-triazol-3-yl)phényl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoéthyl)-3-(méthylthio)pyrrolidine-3-carboxamide base libre amorphe.

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