XIE, Zhifeng,WANG, Ce,RUEBSAM, Frank,RENZETTI, Louis,MULVIHILL, Mark J.,KEEFE, Anthony D.,CLARK, Matthew,BABISS, Lee,ZHANG, Ying,NI, Haihong
申请号：
PE0018852016
公开号：
PE02062017A1
申请日:
2015.04.03
申请国别(地区):
PE
年份:
2017
代理人:
摘要：
Refers to espirociclicos inhibitors of formula (i) where x1 and x2 are c1-c2, c = o, among others X3 is c1-c2, or, among others M and N are 0, 1 or 2 R1, R2 and 2a are C0 - C12 alkyl, cycloalkyl C3 C12 alkyl C0 - C12 - between each other, optionally substituted alkyl R4 is C0 - C12, heterocicloalquilo C3 - C12 alkyl C0 - C12 - among others, optionally substituted.Preferred compounds are: (R) - 3 - (N - fluoro - 3 - methyl - 1 - (3 - methyl - 2 - [- 1 - phenyl - 1,3,8 - triazaespiro [4.5] decan - 8 - yl) - 1 - oxobutan - 2 - il) benzamide (R) - 2 - fluoro - 3 - methyl - N - (3 - (1 - methyl - 3 - methyl - 2 - [- 1 - phenyl - 1,3,8 - triazaespiro [4.5] decan - 8 - yl) - 1 - oxobutan - 2 - il) benzamide among others. It also relates to a composition.These compounds inhibit the activity of i.e., Autotaxin (ATX) by modulating the level of lysophosphatidic acid (LPA) and associated signalling being useful as agents for Treatment or prophylaxis of diseases such as cancer, Chronic inflammation, neuropathic pain, among othersSe refiere a inhibidores espirociclicos de formula (I) en donde X1 y X2 son alquilo C1-C2, C=O, entre otros X3 es alquilo C1-C2, O, entre otros m y n son 0, 1 o 2 R1, R2 y R2a son alquilo C0-C12, cicloalquilo C3-C12-alquilo C0-C12-, entre otros cada uno opcionalmente sustituido R4 es alquilo C0-C12, heterocicloalquilo C3-C12- alquilo C0-C12-, entre otros, opcionalmente sustituido. Son compuestos preferidos: (R)-3-Fluoro-N-(3-metil-1-(3-metil-2,4-dioxo-1-fenil-1,3,8-triazaespiro[4.5]decan-8-il)-1-oxobutan-2-il)benzamida (R)-2-Fluoro-3-metil-N-(3-metil-1-(3-metil-2,4-dioxo-1-fenil-1,3,8-triazaespiro[4.5]decan-8-il)-1-oxobutan-2-il)benzamida entre otros. Tambien se refiere a una composicion. Dichos compuestos inhiben la actividad de la autotaxina (ATX) modulando el nivel del acido lisofosfatidico (LPA) y la senalizacion asociada siendo utiles como agentes de tratamiento o profilaxis de enfermedades como cancer, inflamacion cronica, dolor neuropatico, entre
