HERT, Jerôme,HUNZIKER, Daniel,KURATLI, Christoph,MARTIN, Rainer E.,MATTEI, Patrizio,SATZ, Alexander Lee
申请号：
PE0015402017
公开号：
PE17372017A1
申请日:
2016.04.07
申请国别(地区):
PE
年份:
2017
代理人:
摘要：
Refers to quinazolinona bicyclic compounds of formula (i) wherein R1, R2, R3, R4, R5, R6, R7, R9, R10, R12, R13, R14, A1, A2, A3, N and M are as defined in the description.Preferred compounds are (3R) - 3 - [[2 - [6 - (4 - acetilpiperazin - 1 - il) - 4 - oxoquinazolin - 3 - il] acetyl] amino] - 3 - (4-chlorophenyl) - N - metilpropanamida (3R) - 3 - [2 - [[6 - (4 - acetilpiperazin - 1 - il) - 4 - oxoquinazolin - 3 - il] acetyl] amino] - 3 - (4-chlorophenyl) - n, N - dimetilpropanamida (3R) - 3 - [[2 - [6 - (4 - acetilpiperazin - 1 - il) - 4 - oxoqu Inazolin - 3 - il] acetyl] amino] - 3 - (4-chlorophenyl) - N - fenilpropanamida among others.It also refers to a process of Preparation and to a Pharmaceutical composition. These compounds are inhibitors of i.e., Autotaxin (ATX) by inhibiting the production of lysophosphatidic acid (LPA) being useful in the treatment of Eye DiseasesSE REFIERE A COMPUESTOS DERIVADOS DE QUINAZOLINONA BICICLICOS DE FORMULA (I) DONDE R1, R2, R3, R4, R5, R6, R7, R9, R10, R12, R13, R14, A1, A2, A3, n Y m SON TAL COMO SE DEFINEN EN LA DESCRIPCION. SON COMPUESTOS PREFERIDOS: (3R)-3-[[2-[6-(4-ACETILPIPERAZIN-1-IL)-4-OXOQUINAZOLIN-3-IL]ACETIL]AMINO]-3-(4-CLOROFENIL)-N-METILPROPANAMIDA (3R)-3-[[2-[6-(4-ACETILPIPERAZIN-1-IL)-4-OXOQUINAZOLIN-3-IL]ACETIL]AMINO]-3-(4-CLOROFENIL)-N,N-DIMETILPROPANAMIDA (3R)-3-[[2-[6-(4-ACETILPIPERAZIN-1-IL)-4-OXOQUINAZOLIN-3-IL]ACETIL]AMINO]-3-(4-CLOROFENIL)-N-FENILPROPANAMIDA ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCESO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA AUTOTAXINA (ATX) INHIBIENDO LA PRODUCCION DEL ACIDO LISOFOSFATIDICO (LPA) SIENDO UTILES EN EL TRATAMIENTO DE AFECCIONES OCULARES
