发明名称 Quaternary ammonium salt compounds
摘要 [Problem];The object of the present invention is to provide a novel compound having β2 adrenergic receptor agonist activity and muscarinic receptor antagonist activity.;[Means for Solving the Problem];The present invention is a quaternary ammonium salt compounds represented by formula (I), or a pharmaceutically acceptable salt thereof, with superior β2 adrenergic receptor agonist activity and muscarinic receptor antagonist activity.;
申请公布号 US9072734(B2) 申请公布日期 2015.07.07
申请号 US201013266651 申请日期 2010.04.27
申请人 Teijin Pharma Limited 发明人 Mitsuyama Etsuko;Hara Takayuki;Igarashi Junji;Sugiyama Hiroyuki;Yamamura Satoshi;Nomura Johji;Segawa Kei
分类号 A61K31/445;C07D215/16;A61K31/4709;C07D401/12;C07D413/12;C07D417/12;C07D491/18 主分类号 A61K31/445
代理机构 Sughrue Mion, PLLC 代理人 Sughrue Mion, PLLC
主权项 1. A quaternary ammonium salt compound represented by general formula (I):wherein R1 represents a hydrogen atom or an unsubstituted C1-8 alkyl group; R2 represents a single bond, unsubstituted C1-8 alkylene or C1-8 alkylene substituted on carbon atoms by 1 to 2 oxygen atoms, unsubstituted C2-4 alkenylene, or unsubstituted —O—C1-4 alkylene; X represents a single bond, —O—, —CONR3—, —NR3CO—, or —NR3CO—CH2—O—; where R3 represents a hydrogen atom or an unsubstituted C1-8 alkyl group; A1 represents a single bond, unsubstituted C6-10 arylene or C6-10 arylene substituted with 1 to 4 substituents selected from the group consisting of halogen atom, hydroxyl group, cyano group, nitro group, carboxyl group, trifluoromethyl group, unsubstituted C1-6 alkyl group, unsubstituted C3-8 cycloalkyl group, unsubstituted C1-6 alkoxy group, unsubstituted C3-8 cycloalkyloxy group, mercapto group, unsubstituted C1-6 alkylthio group, unsubstituted C3-8 cycloalkylthio group, amino group, unsubstituted mono(C1-6 alkyl)amino group and unsubstituted di(C1-6 alkyl)amino group, unsubstituted 5- to 10-membered heteroarylene or 5- to 10-membered heteroarylene substituted with 1 to 4 substituents selected from the group consisting of halogen atom, hydroxyl group, cyano group, nitro group, carboxyl group, trifluoromethyl group, unsubstituted C1-6 alkyl group, unsubstituted C3-8 cycloalkyl group, unsubstituted C1-6 alkoxy group, unsubstituted C3-8 cycloalkyloxy group, mercapto group, unsubstituted C1-6 alkylthio group, unsubstituted C3-8 cycloalkylthio group, amino group, unsubstituted mono(C1-6 alkyl)amino group and unsubstituted di(C1-6 alkyl)amino group, unsubstituted C1-4 alkylene-substituted or unsubstituted C6-10 arylene where the substituents of C6-10 arylene are 1 to 3 substituents selected from the group consisting of halogen atom, hydroxyl group, cyano group, nitro group, carboxyl group, trifluoromethyl group, unsubstituted C1-6 alkyl group, unsubstituted C3-8 cycloalkyl group, unsubstituted C1-6 alkoxy group, unsubstituted C3-8 cycloalkyloxy group, mercapto group, unsubstituted C1-6 alkylthio group, unsubstituted C3-8 cycloalkylthio group, amino group, unsubstituted mono(C1-6 alkyl)amino group and unsubstituted di(C1-6 alkyl)amino group, unsubstituted C1-4 alkylene-substituted or unsubstituted 5- to 10-membered heteroarylene where the substituents of 5- to 10-membered heteroarylene are 1 to 3 substituents selected from the group consisting of halogen atom, hydroxyl group, cyano group, nitro group, carboxyl group, trifluoromethyl group, unsubstituted C1-6 alkyl group, unsubstituted C3-8 cycloalkyl group, unsubstituted C1-6 alkoxy group, unsubstituted C3-8 cycloalkyloxy group, mercapto group, unsubstituted C1-6 alkylthio group, unsubstituted C3-8 cycloalkylthio group, amino group, unsubstituted mono(C1-6 alkyl)amino group and unsubstituted di(C1-6 alkyl)amino group, or unsubstituted C3-8 cycloalkylene or C3-8 cycloalkylene substituted with 1 to 3 substituents selected from the group consisting of halogen and unsubstituted C1-6 alkyl group; R4 represents unsubstituted C1-10 alkylene; R8 and R9 each independently represent a halogen atom, a cyano group, an unsubstituted C1-6 alkyl group, a nitro group, —NR10R11 where R10 and R11 each independently represent a hydrogen atom or an unsubstituted C1-6 alkyl group, an unsubstituted C1-6 alkoxy group, a carboxyl group, an unsubstituted C1-6 alkoxycarbonyl group, a hydroxyl group, a trifluoromethyl group, a mercapto group, or an unsubstituted C1-6 alkylthio group; a and b each independently represent an integer of 0 to 3; Y represents a group represented by formula (II): Q represents formula (III):wherein R6 and R7 each independently represent an unsubstituted C1-6 alkyl group or a C1-6 alkyl group substituted with 1 to 4 substituents selected from the group consisting of halogen atom, hydroxyl group and unsubstituted C1-6 alkoxy group, or an unsubstituted C8-10 phenoxyalkyl group or a C8-10 phenoxyalkyl group substituted with 1 to 4 substituents selected from the group consisting of halogen atom, hydroxyl group, unsubstituted C1-6 alkyl group and unsubstituted C1-6 alkoxy group; R5 represents an unsubstituted C1-6 alkyl group or a C1-6 alkyl group substituted with 1 to 4 substituents selected from the group consisting of halogen atom, hydroxyl group and unsubstituted C1-6 alkoxy group; n represents an integer of 1; and m represents an integer of 0 to 3; W− represents a negative ion;or a pharmaceutically acceptable salt thereof.
地址 Tokyo JP
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