NAIMISHA TRIVEDI,CHARLES BAKER-GLENN,HERV VAN DE POL,IAN LINNEY,WESLEY BLACKABY,CARMELIDA CAPALDI,GABRIELE AMARI,ELISABETTA ARMANI
申请号：
ARP150101772
公开号：
AR100732A1
申请日:
2015.06.04
申请国别(地区):
AR
年份:
2016
代理人:
摘要：
The present invention relates to compounds which are both inhibitors of the enzyme phosphodiesterase 4 (PDE4) and antagonists of the muscarinic M3 receptor, methods of preparing said compounds, compositions containing them. Claim 1: A compound characterized in that it is of general formula (1) where each R¹ is hydrogen or is independently selected from the group consisting of: halogen, C₁₋₄ alkyl, C₁₋₄ alkoxy, C₁₋₄ haloalkyl, hydroxy , -SO₂NRIRII, -CN, -NRISO₂RIII, -NRIRII, - (CO) NRIRII and -NRI (CO) RIII, and wherein said C₁₋₄ alkyl is optionally substituted with one or more groups selected from C₃₋₇ cycloalkyl,hydroxy and -NRIRII and where said C₁₋₄ alkoxy is optionally substituted with one or more halogens or C₃₋₇ cycloalkyl groups where, RI is hydrogen or C₁₋₆ alkyl； RII is hydrogen or C₁₋₆ alkyl； RIII is hydrogen or C₁₋₆ alkyl； n is an integer in the range of 1 to 3； each R² is hydrogen or is independently selected from the group consisting of: halogen, C₁₋₄ alkyl, C₁₋₄ alkoxy, C₁₋₄ haloalkyl, hydroxy, -SO₂NRIRII, -CN, -NRISO₂RIII, -NRIRII, - ( CO) NRIRII and -NRI (CO) RIII and wherein said C₁₋₄ alkyl is optionally substituted with one or more groups selected from C₃₋₇ cycloalkyl,hydroxy and -NRIRII and where said C₁₋₄ alkoxy is optionally substituted with one or more halogens or C₃₋₇ cycloalkyl groups where, RI is hydrogen or C₁₋₆ alkyl； RII is hydrogen or C₁₋₆ alkyl； RIII is hydrogen or C₁₋₆ alkyl； m is an integer in the range of 1 to 3； R³ and R⁴ are different or the same and are independently selected from the group consisting of: H, C₃₋₇ cycloalkylcarbonyl, C₁₋₆ alkyl optionally substituted with one or more substituents selected from C₃₋₇ cycloalkyl and C₅₋₇ cycloalkenyl, C₁₋₆ haloalkyl, C₃₋₇ cycloalkyl, C₅₋₇ cycloalkenyl, C₂₋₅ alkenyl,e. C832283331 and c832626 asphalt； or R3 and r83088；Together with the atoms connecting them, they form a formula (2) ring of 2,2-fluoro-1,3-nitrogen dioxide, which is combined with the phenyl units of the binding group - or
