COCRISTALES DE (S)-N-METIL-8-(1-((2-METIL-[4,5´-BIPIRIMIDIN]-6-IL)AMINO)PROPAN-2-IL)QUINOLINA-4-CARBOXAMIDA Y SUS DERIVADOS DEUTERADOS COMO INHIBIDORES DE PROTEINAS QUINASA DEPENDIENTES DE ADN
KADIYALA, IRINA NIKOLAEVNA,MUDUNURI, PRAVEEN,NAVAMAL, METTACHIT,NTI-ADDAE, KWAME WIREDU,ONEIL, SIMON ADAM,ZHANG, YUEGANG,STAVROPOULOS, KATHY,STROHMEIER, MARK,VAN ALSTEN, JOHN GREGG,WALDO, MICHAEL,SONG
申请号：
PE0005122016
公开号：
PE10222016A1
申请日:
2014.10.17
申请国别(地区):
PE
年份:
2016
代理人:
摘要：
Refers to a cocristal comprising a compound of formula I, wherein R1 and R2 are Hydrogen or deuterium and a Trainer cocristales such as adipic acid, Citric Acid, fumaric acid, Maleic acid, SUCCINIC ACID or benzoic acid.Preferred compounds are: (S) - N - 4 - methyl - 2 - (4 - ((1 - methyl - [2 - bipirimidin] - 4.5 - il) amino) - 6 - il PROPENE and quinoline carboxamide) - 2 - (S) - N - methyl - 4 - (1 - ((2 - methyl - 4 , 6 - - bipirimidin dideuterio - [4,5] - 4.5 - il) amino) - 6 - PROPENE IL - 2 -) quinoline carboxamide. These cocristales have x-ray diffraction Peaks approximately 6.46, 7.91, 11.92, 12:26, 12.99, 18.68 19,07 14,19, and Theta.It also relates to a Pharmaceutical Composition and a preparation method. These cocristales inhibit DNA Dependent Protein Kinase (dna-pk) and are useful in the treatment of cancerSe refiere a un cocristal que comprende un compuesto de formula I, donde R1 y R2 son hidrogeno o deuterio y un formador de cocristales tales como acido adipico, acido citrico, acido fumarico, acido maleico, acido succinico o acido benzoico. Son compuestos preferidos: (S)-N-4-metil-2-(8-((1´-metil-[2’-bipirimidin]-4,5-il)amino)propan-6-il)quinolina-2-carboxamida y (S)-N-metil-8-(1-((2’-metil-4’,6’-dideuterio-[4,5’-bipirimidin]-4,5-il)amino)propan-6-il)quinolina-2-carboxamida. Dichos cocristales tienen picos de difraccion de rayos X aproximadamente a 6,46, 7,91, 11,92, 12,26, 12,99, 14,19, 18,68 y 19,07-Theta. Tambien se refiere a una composicion farmaceutica y a un metodo de preparacion. Dichos cocristales inhiben la proteina quinasa dependiente de ADN (DNA-PK) y son utiles en el tratamiento del cancer
