KIM, Myeong-Seop,KIM, Sumin,KIM, Jin Kwan,KIM, Hadong,RYU, Ki Moon,PARK, Seong Jin,PARK, Taesun,SHEEN, Joon-Ho,YOON, Taeyoung,JANG, Mi Yeon
申请号：
PE0003082018
公开号：
PE10172018A1
申请日:
2016.08.31
申请国别(地区):
PE
年份:
2018
代理人:
摘要：
The present Invention relates to a Heterocyclic Compound represented by formula I, where X is chr8 CR7 o n and it is, or nr8 u Z is CH2, CH2O, C (= o), among others r1 is H, halogen, c1-c4 alkyl,Among others R2 is Halogen, c1-c4 alkyl and alkylaryl C1 - C2, among others R3 is Halogen, CN, aryl, among others R4 and R5 are each independently C1 - C6 h, alkyl, alkoxy C1 - C6Among others, R5 H is or may be combined to form a carbonyl with R5, R6 h, c1-c4 alkyl, alkoxy C1 - C6, among others R7 is H, alkyl or Halogen C1 - C3 R8 is H, alkyl of C1 - C6Fluoroalquilo c1-c4, among others.Are preferred compound: 2 - amino - N - ((1S, 2S) - 2 - (Benzyloxy) ciclopentil) - 5 - (1 - methyl - 1h-pyrazol-4-yl) Nicotinamide, 2-amino-n - ((1R, 2S) - 2 - (Benzyloxy) - 5 ciclopentil) - (1 - methyl - 1h-pyrazol-4-yl) Nicotinamide,Among others.It also relates to pharmaceutical compositions that comprise the Heterocyclic Compounds, the stereoisomer thereof,The enantiomer thereof or pharmaceutically Stable Salt of These vehicles along with pharmaceutically Stable.The Invention is useful for the Prevention or treatment of a disease influenced by inhibition of kinase Mer, as in the case of glioma, colorectal cancerLung Cancer, among others.La presente invencion refiere un compuesto heterociclico representado por la formula I, donde: X es CR7 o N Y es CHR8, NR8 u O Z es CH2, CH2O, C(=O), entre otros R1 es H, halogeno, alquilo C1-C4, entre otros R2 es halogeno, alquilo C1-C4, alquilarilo C1-C2, entre otros R3 es halogeno, CN, arilo, entre otros R4 y R5 son cada uno en forma independiente H, alquilo C1-C6, alcoxi C1-C6, entre otros R5 es H o se puede combinar con R5 para formar un carbonilo R6 es H, alquilo C1-C4, alcoxi C1-C6, entre otros R7 es H, halogeno o alquilo C1-C3 R8 es H, alquilo C1-C6, fluoroalquilo C1-C4, entre otros. Son compuesto preferidos: 2-amino-N-((1S, 2S)-2-(benciloxi)ciclopentil)-5-(1-metil-1H-pirazol-4-il)nicotinamida, 2-amino-N-((1R, 2S)-2-(benciloxi)ciclopentil)-5-(1-metil
