AURELL, Carl-Johan,CONNOLLY, Stephen,DOYLE, Kevin James,JONES, Graham Peter,LONN, Hans Roland,WATSON, David Wyn,PALMER, Nicholas John,PO KARLSSON, Staffan,PONTEN, John Fritiof,SWALLOW, Steven,VAN DE P
申请号：
PE0012362016
公开号：
PE12182016A1
申请日:
2015.01.23
申请国别(地区):
PE
年份:
2016
代理人:
摘要：
Refers to a compound derived from (2S) - N - [(1S) - 1 - 2 - cyano - 1.4 - oxazepan 2-phenylethyl] - 2 - carboxamidas Formula 1 or pharmaceutically acceptable salts thereof, where: (a) R1 R2 is Hydrogen, F, CL, BR, among others R3 Hydrogen, F, CL, CN, R1 is among others or (b), (c), among others, where X is o, S Or or or CF2 is s and R6 is C1 - C3 alkyl, optionally substituted by 1, 2 or 3 (F, ohAmong others R7 IS F, cl or CH3. Preferred compounds are (2S) - N - [(1S) - 1 - (2 - cyano - 4 - cianobifenil - 4-yl) ethyl] - 1.4 - oxazepan - 2 - carboxamide (2S) - N - [(1S) - 1 - cyano - 2 - [4 - (3 - methyl - 2 - oxo 2,3 dihydro - 1.3 - benzoxazole - 5 - il) phenyl] ethyl} - 1.4 - oxazepan - 2 - carboxamide among others. It also relates to a Treatment method and a Pharmaceutical composition.These compounds inhibit the activity of the dipeptidilpeptidasa (dpp1), being useful in the treatment of respiratory diseases such as Asthma, chronic obstructive pulmonary disease (COPD), among othersSe refiere a un compuesto derivado de (2S)-N-[(1S)-1-ciano-2-feniletil]-1,4-oxazepan-2-carboxamidas de formula I o sales farmaceuticamente aceptables, donde: R1 es (a) R2 es hidrogeno, F, Cl, Br, entre otros R3 es hidrogeno, F, Cl, CN, entre otros o R1 es (b), (c), entre otros, donde: X es O, S o CF2 Y es O o S R6 es alquilo C1-C3 opcionalmente sustituido por 1, 2 o 3 F, OH, entre otros R7 es F, Cl o CH3. Son compuestos preferidos: (2S)-N-[(1S)-1-Ciano-2-(4-cianobifenil-4-il)etil]-1,4-oxazepan-2-carboxamida (2S)-N-{(1S)-1-Ciano-2-[4-(3-metil-2-oxo-2,3-dihidro-1,3-benzoxazol-5-il)fenil]etil}-1,4-oxazepan-2-carboxamida entre otros. Tambien se refiere a un metodo de tratamiento y a una composicion farmaceutica. Dichos compuestos inhiben la actividad de la dipeptidilpeptidasa (DPP1), siendo utiles en el tratamiento de enfermedades respiratorias tales como asma, enfermedad pulmonar obstructiva cronica (COPD), entre otros
