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PHARMACEUTICAL COMPOSITION containing thienotriazolodiazepine compounds
专利权人:
ОНКОЭТИКС ГМБХ (CH)
发明人:
ГАУЧИ Джефф (US),МИНИКИС Райан (US)
申请号:
RU2015115634
公开号:
RU2015115634A
申请日:
2013.09.27
申请国别(地区):
RU
年份:
2016
代理人:
摘要:
1. A solid dispersion containing an amorphous thienotriazolodiazepine compound of the formula (1) where X is halogen, R is C-Calkyl, R is C-Calkyl, a is an integer 1-4, R is C-Calkyl, C-C hydroxyalkyl, C-alkoxy, phenyl optionally containing substituent (s), or heteroaryl optionally containing substituent (s), a pharmaceutically acceptable salt or hydrate thereof, and a pharmaceutically acceptable polymer. 2. The solid dispersion according to claim 1, wherein formula (1) is selected from the group consisting of: (i) (S) -2- [4- (4-chlorophenyl) -2,3,9-trimethyl-6H-thieno [3 , 2-f] [1,2,4] triazolo- [4,3-a] [1,4] diazepin-6-yl] -N- (4-hydroxyphenyl) acetamide or its dihydrate, (ii) methyl- (S) - {4- (3'-cyanobiphenyl-4-yl) -2,3,9-trimethyl-6H-thieno [3,2-f] [1,2,4] triazolo [4,3-a ] [1,4] diazepin-6-yl} acetate, (iii) methyl- (S) - {2,3,9-trimethyl-4- (4-phenylaminophenyl) -6H-thieno [3,2-f] [1,2,4] triazolo [4,3-a] [1,4] diazepin-6-yl} acetate and (iv) methyl- (S) - {2,3,9-trimethyl-4- [4 - (3-phenylpropionylamino) phenyl] -6H-thieno [3,2-f] [1,2,4] triazolo [4,3-a] [1,4] diazepin-6-yl} acetate. 3. Solid dispersion according to paragraphs. 1 and 2, where the formula (1) is (S) -2- [4- (4-chlorophenyl) -2,3,9-trimethyl-6H-thieno [3,2-f] [1,2,4 ] triazolo [4,3-a] [1,4] diazepin-6-yl] -N- (4-hydroxyphenyl) acetamide dihydrate. 4. The solid dispersion according to any one of paragraphs. 1 and 2, wherein the pharmaceutically acceptable polymer is hydroxypropyl methylcellulose acetosuccinate. 5. The solid dispersion according to claim 4, wherein the weight ratio of the compound of thienotriazolodiazepine to hydroxypropyl methylcellulose acetosuccinate (HPMCAS) in the solid dispersion is from 1: 3 to 1: 1.6. The solid dispersion according to any one of paragraphs. 1 and 2, where the pharmaceutically acceptable polymer is PVP. 7. The solid dispersion according to claim 6, wherein the weight ratio of the thienotriazolodiazepine compound to PVP in the solid dispersion is from
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