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Aminobenzene derivatives as inhibitors of triphosphate 4 (PDE4) and antagonists of M3 receptor
专利权人:
CHIESI FARMACEUTICI S.P.A.
发明人:
NAIMISHA TRIVEDI,CHARLES BAKER-GLENN,HERV VAN DE POL,WESLEY BLACKABY,ELISABETTA ARMANI,GABRIELE AMARI
申请号:
ARP160101282
公开号:
AR104532A1
申请日:
2016.05.05
申请国别(地区):
AR
年份:
2017
代理人:
摘要:
Compounds that are both phosphodiesterase 4 enzyme (PDE4) inhibitors and muscarinic M3 receptor antagonists, methods of preparing such compounds, compositions containing them, and therapeutic use. 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 , -SO₂NR⁶R⁷,-Cn, - No. 831222; - No. 183228313;-8310; 8311;-CONR⁶R⁷ and -NR⁸COR⁹ and wherein said C₁₋₄ alkyl is optionally substituted with one or more groups selected from C₃₋₇ cycloalkyl, hydroxy and -NR⁶R⁷ and where said C₁₋₄ alkoxy is optionally substituted with one or more halogens or C₃₋ groups ₇ cycloalkyl where, R⁶ is hydrogen or C₁₋₆ alkyl; R⁷ is hydrogen or C₁₋₆ alkyl; R⁸ is hydrogen or C₁₋₆ alkyl; R⁹ is hydrogen or C₁₋₆ alkyl; n is an integer in the range of 1 to 3; each R² is hydrogen or is selected from the group consisting of: halogen, C₁₋₄ alkyl, C₁₋₄ alkoxy, C₁₋₄ haloalkyl, hydroxy, -SO₂NR¹⁰R¹¹,-CN and -NR¹²SO₂R¹³ and where said C₁₋₄ alkyl and said C₁₋₄ alkoxy are optionally substituted with one or more C₃₋₇ cycloalkyl groups where R¹⁰ is hydrogen or C₁₋₆ alkyl; R¹¹ is hydrogen or C₁₋₆ alkyl; R¹² is hydrogen or C₁₋₆ alkyl; R¹³ 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 C₁₋₄ alkoxy, C₃₋₇ cycloalkyl or C₅₋₇ cycloalkenyl,C₁₋₆ haloalkyl, C₃₋₇ cycloalkyl, C₅₋₇ cycloalkenyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl; each R⁵,When attending the meeting, they shall be selected independently from the following groups:Cf.8323 and halogen atoms; K is an integer of level 0 or 1 to 3; L1 is a link; W1 is selected from a divergent arileno and a pagan group; W2 is selected from an arilo and a pagan group; L2 is an integer of level 1 to 4 selected f
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