LU, Tianbao,ALLISON, Brett Douglas,BARBAY, Joseph Kent,CONNOLLY, Peter J.,CUMMINGS, Maxwell David,DIELS, Gaston,EDWARDS, James Patrick,KREUTTER, Kevin D.,PHILIPPAR, Ulrike,SHEN, Fang,THURING, Johannes
申请号：
PE2019001288
公开号：
PE20191755A1
申请日:
2017.12.20
申请国别(地区):
PE
年份:
2019
代理人:
摘要：
A formula compound (I),R1 is selected from the following aspects: (I) naftalen-1-ilo, which can be replaced by fluorine or amino group； (II) a 9-10 member heterocompound, including 1-4 heterocompounds selected from the alternative o, N and S； R2 is selected from C1-4, 1-methoxi-ethyl tar； G1 is n or C (R4)；G2 is n or C (R3)；R3 is selected from trifluoromethyl, cyano, among others； R4 is selected from H, C1-4 alkoxy, cyano, among others； R5 is selected from H, Cl, fluoro, among others； R6 is H, C1-4 alkyl； R7 is H or fluoro. Preferred compounds are: N- (2-cyanopyridin-4-yl) -1- (naphthalen-1-yl) -5- (trifluoromethyl) -1H-pyrazol-4-carboxamide, N- (5-chloro-6- ( 2H-1,2,3-triazol-2-yl) pyridin-3-yl) -1- (naphthalen-1-yl) -5- (trifluoromethyl) -7H-pyrazol-4-carboxamide, among others. These compounds are inhibitors of MALT1 (mucosa-associated lymphoid tissue lymphoma translocation protein 1),As an effective treatment for a disease, sindrome, disease, condition or disease, is associated with MALT1, including cancer and immune diseases. He also mentioned a pharmacology composer who included the compound.Referido a un compuesto de formula (I), en donde R1 se selecciona de i) naftalen-1-ilo, opcionalmente sustituido con fluoro o amino； y ii) un heteroarilo de nueve a diez miembros que contiene de uno a cuatro heteroatomos seleccionados de O, N y S, opcionalmente sustituido； R2 se selecciona de alquilo C1-4, 1-metoxi-etilo, entre otros； G1 es N o C(R4)； G2 es N o C(R3)； R3 se selecciona de trifluorometilo, ciano, entre otros； R4 se selecciona de H, alcoxi C1-4, ciano, entre otros； R5 se selecciona de H, Cl, fluoro, entre otros； R6 es H, alquilo C1-4； R7 es H o fluoro. Son compuestos preferidos: N-(2-cianopiridin-4-il)-1-(naftalen-1-il) -5- (trifluorometil)-1H-pirazol-4-carboxamida, N-(5-cloro-6-(2H-1,2,3-triazol-2-il)piridin-3-il)-1-(naftalen-1-il)-5-(trifluorometil)-7H-pirazol-4-carboxamida, entre otros. Dichos compuestos son inhibidores de MALT1 (proteina de translocacion d
