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Compounds and compositions for inhibiting the activity of the ABL1, ABL2 and BCR - ABL1
专利权人:
NOVARTIS AG
发明人:
STEPHANIE KAY, DODD,PASCAL, FURET,ROBERT MARTIN, GROTZFELD,DARRYL BRYNLEY, JONES,PAUL, MANLEY,ANDREAS, MARZINZIK,XAVIER FRANCOIS ANDRE, PELLE,BAHAA, SALEM,JOSEPH, SCHOEPFER,WOLFGANG, JAHNKE
申请号:
TR201807023
公开号:
TR201807023T4
申请日:
2013.05.09
申请国别(地区):
TR
年份:
2018
代理人:
摘要:
Compounds capable of inhibiting the activity of BCR - ABL1 and Mutants thereof. Also provided is a process for the preparation of the compounds, Pharmaceutical preparations comprising such compounds and Methods of using such compounds in the treatment of cancers. Abl protein tyrosine kinase Abelson.Claim 1: The Compound of claim 1 of the formula (1) in which r u00b9 is pirazolilo; wherein Said pirazolilo is replaced or not replaced with 1 to 2 groups r u2076; R u00b2 is pirrolidinilo; wherein Said pirrolidinilo is replaced by a Group r u2077; r u00b3 is selected from H Idr u00f3geno and Halo; r u2074 is selected from - - - - sf u2085 and y u00b2 cf u2082 or r u2076 is independently at each occurrence; SEleccionado from Hydrogen, hydroxyl, Methyl, methoxyl, cyano, trifluoromethyl Methyl, Hydroxy, amino, Halo, fluoro -, Ethyl Ethyl and ciclopropilo; r u2077 is selected from hydroxyl, Methyl, methoxyl, Halo - methyl, hydroxyl, amino, methyl - amino amino -, methyl -, trifluoromethyl, 2 Hydrox Ipropan thiocyanatoacetate, metilocarbonil - Dimethyl amino, amino, 2-amino-3 - oxilo, carboxyl, metilbutanoil)Carbonyl methoxyl, fosfonooxilo, cyano and amino carbonyl; and selected from Ch and N; y u00b9 is selected from Ch and N; y u00b2 is selected from cf u2082 or s, and (OR) and u2080 u208b u2082; or is selected from Hydrogen, Methyl, Chlorine, Fluorine, difluorometilo and trifluoromethyl or s; Ales pharmaceutically acceptable to them.Mevcut buluş, Abelson proteini (ABL1), Abelson- ilişkili protein (ABL2) ve ilgili kimerik proteinlerin, özellikle BCR- ABL1'in tirosin kinaz enzimatik aktivitesini inhibe edebilen bileşikler ile ilgilidir. Buluş ayrıca buluşun bileşiklerinin hazırlanması için bir işlem, bu tür bileşikleri içeren farmasötik preparatlar ve bu tür bileşiklerin kanserlerin tedavisinde kullanılma yöntemleri ile ilgilidir.
来源网站:
中国工程科技知识中心
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