发明名称 Morpholine-spirocyclic piperidine amides as modulators of ion channels
摘要 The invention relates to morpholine spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
申请公布号 US9181273(B2) 申请公布日期 2015.11.10
申请号 US201414454227 申请日期 2014.08.07
申请人 VERTEX PHARMACEUTICALS INCORPORATED 发明人 Hadida-Ruah Sara Sabina;Binch Hayley Marie;DeNinno Michael Paul;Fanning Lev Tyler Dewey;Frieman Bryan A.;Grootenhuis Peter Diederik Jan;Hilgraf Nicole;Joshi Pramod;Kallel Edward Adam;Miller Mark Thomas;Pontillo Joseph;Silina Alina;Sheth Urvi Jagdishbhai;Hurley Dennis James;Arumugam Vijayalaksmi
分类号 C07D498/10 主分类号 C07D498/10
代理机构 Brinks Gilson & Lione 代理人 Brinks Gilson & Lione
主权项 1. A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein, independently for each occurrence: at least two R1 taken together form an oxo group; wherein additional R1 groups are selected from the group consisting of C1-C6 alkyl, C1-C6 fluoroalkyl, C3-C8 cycloalkyl, halo, NR8SO2R8, SO2R8, SR8, SOR8, NR8COR8, NR8CO2R8, CN, CON(R8)2, SO2N(R8)2, CF3, optionally substituted heterocycloalkyl, phenyl, heteroaryl, and a straight chain, branched, or cyclic (C3-C8)-R9-wherein up to two CH2 units may be replaced with O, CO, S, SO, SO2, N, CF2, or NR8; R2 is H, C1-C6 alkyl, C1-C6 fluoroalkyl, an optionally substituted cycloalkyl, aryl, heteroaryl, or heterocycloalkyl, COR8, CO2R8, CON(R8)2, CF3, CHF2, or a straight chain, branched, or cyclic (C3-C8)-R9-wherein up to two CH2 units may be replaced with O, CO, S, SO, SO2, N, CF2, or NR8; R3 is C1-C6 alkyl or halo; R8 is H, C1-C6 alkyl, or C3-C8 cycloalkyl, a straight chain, branched, or cyclic (C3-C8)-R9-wherein up to two CH2 units may be replaced with O, CO, S, SO, SO2, N, CF2, or NR, or 2 R8 taken together with the atoms to which they are attached form a ring; R9 is H, CF3, CHF2, CH2F, CO2R, OH, optionally substituted aryl, heteroaryl, C3-C8 cycloalkyl, heterocycloalkyl, N(R)2, NRCOR, CON(R)2, CN, or SO2R; R is H, C1-C6 alkyl, optionally substituted aryl, heteroaryl, C3-C8 cycloalkyl, or heterocycloalkyl; A is aryl, heteroaryl or heterocyclic in which each is optionally substituted with C1-C6 alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkoxy, C1-C6 alkoxy, halo, CN, OH, OR8, N(R8)2, NR8SO2R8, SO2R8, SOR8, SR8, CO2R8, NR8COR8, NR8CO2R8, CON(R8)2, SO2N(R8)2, CHF2, CF3, OCF3, OCHF2, R9, heterocycloalkyl, heterocycloalkoxy, aryl, heteroaryl, or a straight chain, branched, or cyclic (C3-C8)-R9 wherein up to three CH2 units may be replaced with O, CO, S, SO, SO2, N, CF2, or NR8; n is an integer from 3 or 4; and o is an integer from 0, 1, 2, 3, or 4.
地址 Boston MA US