首页> 外国专利> (S) -N- (3- (6-Isopropoxypyridin-3-yl) -1H-indazol-5-yl) -1- (2- (4- (4- (1-methyl) for pharmaceutical preparations -1H-1,2,4-triazol-3-yl) phenyl) -3,6-dihydropyridin-1 (2H) -yl) -2-oxoethyl) -3- (methylthio) pyrrolidine-3-carboxamide composition

(S) -N- (3- (6-Isopropoxypyridin-3-yl) -1H-indazol-5-yl) -1- (2- (4- (4- (1-methyl) for pharmaceutical preparations -1H-1,2,4-triazol-3-yl) phenyl) -3,6-dihydropyridin-1 (2H) -yl) -2-oxoethyl) -3- (methylthio) pyrrolidine-3-carboxamide composition

机译:(S)-N-(3-(6-异丙氧基吡啶-3-基)-1H-吲唑-5-基)-1-(2-(4-(4-(1-甲基))药物制剂-1H- 1,2,4-三唑-3-基)苯基)-3,6-二氢吡啶-1-1(2H)-基)-2-氧代乙基)-3-(甲硫基)吡咯烷-3-羧酰胺组合物

摘要

The present invention relates to an 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 The total amount of active ingredients, including the granular composition, is about 60-90% by weight 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) pyrrolidine-3-carbox Mid-form 1HCl, about 10-30 wt% 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) pyrrolidine- 3-carboxamide amorphous HCl, and about 0-5 wt% (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-carboxami Containing amorphous free base. [Selection] Figure 1
机译:本发明涉及活性成分(S)-N-(3-(6-异丙氧基吡啶-3-基)-1H-吲唑-5-基)-1-(2-(4-(4-(1-甲基-1H-1,2,4-三唑-3-基)苯基)-3,6-二氢吡啶-1((2H)-基)-2-氧代乙基)-3-(甲硫基)吡咯烷-3-甲酰胺活性成分的量,包括颗粒状组合物,为(S)-N-(3-(6-异丙氧基吡啶-3-基)-1H-吲唑-5-基)-1(-)的约60-90重量%。 2-(4-(4-(1-甲基-1H-1,1,2,4-三唑-3-基)苯基)-3,6-二氢吡啶-1-1(2H)-基)-2-氧乙基)-3 -(甲硫基)吡咯烷-3-羧基中型1HCl,(S)的约10-30 wt%-N-(3-(6-异丙氧基吡啶-3-基)-1H-吲唑-5-基)-1 -(2-(4-(4-(4-(1-甲基-1H-1,2,4-三唑-3-基)苯基)-3,6-二氢吡啶-1(2H)-基)-2-氧乙基) -3-(甲硫基)吡咯烷-3-羧酰胺无定形HCl,和约0-5 wt%(S)-N-(3-(6-异丙氧基吡啶-3-基)-1H-吲唑-5-基)-1 -(2-(4-(4-(1-甲基-1H-1,2,4-三唑-3-基)苯基)-3,6-二氢吡啶-1-1(2H)-基)-2-氧乙基) -3-(甲基硫代)吡咯烷-3-羧酰胺含无定形游离碱。 [选择]图1

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