MEERPOEL, Lieven,PANDE, Vineet,PARADE, Marcus Cornelis Bernardus Catharina,SCHEPENS, Wim Bert Griet,SUN, Weimei,THURING, Johannes Wilhelmus John F.,VIELLEVOYE, Marcel,WU, Tongfei,BREHMER, Dirk,BEKE, L
申请号：
PE2019000723
公开号：
PE20190706A1
申请日:
2017.10.02
申请国别(地区):
PE
年份:
2019
代理人:
摘要：
1. A formula compound (I) or a salt with acceptable efficacy, wherein R1 and R2 are H-C (= O) (-) (C1-4 tar)；This is - ch2-o-cf2Z is -CH2.-C? Page: 1Among other things, AR is a monocyclic aromatic ring, such as pyridine, pyridinediol or bicycle ring system； het is a heterocyclic aromatic bicycle ring system selected from (A-1),(A-2) and (A-3)；R3a, R3d and R3e are H, halo, among others； R4a, R4d, R4e, R4f and R4g are H, C1-4 alkyl, among others； Q1 is N or CR6a； Q2 is N or CR6b； Q8 is N or CR6g； Q9 is N or CR6h； Q10 is N or CR6i； Q11 is N or CR6j； R6a, R6b, R6h, R6i and R6j are H, halo, among others； Q5 is N or CR3d, Q6 is N or CR4e； Q7 is N or CR4f. It also refers to pharmaceutical compositions comprising the compound of the invention and methods of preparation. These compounds are inhibitors of the protein arginine methyltransferase 5 (PRMT5) and are useful in the treatment of diseases such as cancer.Se refiere a un compuesto de formula (I) o su sal farmaceuticamente aceptable, donde: R1 y R2 son H o -C(=O)-(alquilo C1-4)； Y es -CH2- o -CF2-； Z es -CH2-, -C?C-, entre otros； Ar es un anillo aromatico monociclico tal como piridinilo, pirimidinilo, entre otros o un sistema anular biciclico； Het es un sistema anular heterociclico aromatico biciclico seleccionado entre (a-1), (a-2) y (a-3)； R3a, R3d y R3e son H, halo, entre otros； R4a, R4d, R4e, R4f y R4g son H, alquilo C1-4, entre otros； Q1 es N o CR6a； Q2 es N o CR6b； Q8 es N o CR6g； Q9 es N o CR6h； Q10 es N o CR6i； Q11 es N o CR6j； R6a, R6b, R6h, R6i y R6j son H, halo, entre otros； Q5 es N o CR3d, Q6 es N o CR4e； Q7 es N o CR4f. Tambien se refiere a composiciones farmaceuticas que comprenden al compuesto de la invencion y a metodos de preparacion. Dichos compuestos son inhibidores de la proteina arginina metiltransferasa 5 (PRMT5) y son utiles en el tratamiento de enfermedades tales como el cancer
