ALCARAZ, LILIAN,HEALD, ROBERT ANDREW,SUTTON, JONATHAN MARK,ARMANI, ELISABETTA,CAPALDI, CARMELIDA
申请号：
PE0009312015
公开号：
PE10842015A1
申请日:
2013.12.16
申请国别(地区):
PE
年份:
2015
代理人:
摘要：
Refers to Derivatives of 3 - oxo - 7 - methyl - 4 - (3-trifluoromethyl-phenyl) - [1, 2, 4] triazolo [4, 3] - pyrimidine of formula (i), where a, B and D are independently CH o n r1 is H, (C1 - C6) alkyl, phenyl alkyl (C1 - C6), - CH2 - (CH2) Oh, ch2conh2, - ch2so2nh2, among others R2 is CONH2, C2 - C6 alquenilo opcionalm Body replaced with Oh or NH2, among others and R3 is cn or - C (o) - XR4, where X is - or -- CH2 - or - NH - and R IS h, alkyl (C1 - C6), among others. The compounds of the invention are inhibitors of Human Neutrophil Elastase (HNE), which are useful in the treatment of diseases mediated by the action of hne, such as chronic obstructive pulmonary disease (COPD), cystic fibrosis, bronchiectasis, among othersSe refiere a derivados de 3-oxo-7-metil-8-(3-trifluorometil-fenil)-[1, 2, 4]triazolo[4, 3-a]pirimidina de formula (I), donde A, B y D son independientemente CH o N R1 es H, (C1-C6)alquilo, fenil(C1-C6)alquilo, -CH2(CH2)OH, -CH2CONH2, -CH2SO2NH2, entre otros R2 es -CONH2, C2-C6-alquenilo opcionalmente sustituido con OH o NH2, entre otros y R3 es CN o -C(O)-XR4, donde X es -O-, -CH2- o -NH- y R4 es H, (C1-C6)alquilo, entre otros. Los compuestos de la invencion son inhibidores de la elastasa de neutrofilos humanos (HNE), por lo cual son utiles en el tratamiento de enfermedades mediadas por la accion de la HNE, tales como enfermedad pulmonar obstructiva cronica (EPOC), fibrosis quistica, bronquiectasias, entre otros
