发明名称 NICOTINIC RECEPTOR NON-COMPETITIVE ANTAGONISTS
摘要 The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for use, and their pharmaceutical compositions.
申请公布号 US2017071878(A1) 申请公布日期 2017.03.16
申请号 US201615360393 申请日期 2016.11.23
申请人 Catalyst Biosciences, Inc. 发明人 Akireddy Srinivasa Rao;Bhatti Balwinder Singh;Heemstra Ronald Joseph;Speake Jason;Yohannes Daniel;Melvin Matt S.;Xiao Yunde
分类号 A61K31/13 主分类号 A61K31/13
代理机构 代理人
主权项 1. A method for the treatment of nicotine addiction or smoking cessation comprising the administration of a compound of Formula I:wherein each of R1 and R2 individually is H, C1-6 alkyl, or aryl-substituted C1-6 alkyl, or R1 and R2 combine with the nitrogen atom to which they are attached to form a 3- to 8-membered ring, which ring may be optionally substituted with C1-6 alkyl, aryl, C1-6 alkoxy, or aryloxy substituents; R3 is H, C1-6 alkyl, or C1-6 alkoxy-substituted C1-6 alkyl; each of R4, R5, R6, and R7 individually is H, C1-6 alkyl, or C1-6 alkoxy; L1 is a linker species selected from the group consisting of CR8R9, CR8R9CR10R11, and O; L2 is a linker species selected from the group consisting of CH2, CH2CH2, CH2CH2CH2, and CH2CH2CH2CH2; each of R8, R9, R10, and R11 individually is hydrogen or C1-6 alkyl; and the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof.
地址 South San Francisco CA US