发明名称 PYRIDINE DERIVATIVES AS CFTR MODULATORS
摘要 A compound having the structure of Formula II, or a stereoisomer, tautomer, or a pharmaceutically acceptable salt thereof:;;The compound is useful as CFTR modulator. Further, a method of using the compound and pharmaceutical composition comprising the compound are provided for treating diseases in lungs, pancreas, gastrointestinal system, sinuses, reproductive system, and the sweat glands.
申请公布号 US2017101394(A1) 申请公布日期 2017.04.13
申请号 US201615287473 申请日期 2016.10.06
申请人 NuBridge BioSciences 发明人 ZHANG Lin
分类号 C07D401/14;A61K31/444;A61K45/06;C07D213/81;C07D405/14;A61K31/4545;A61K31/55 主分类号 C07D401/14
代理机构 代理人
主权项 1. A compound having a structure of Formula II, or a stereoisomer, tautomer, or a pharmaceutically acceptable salt thereof: wherein R1 is a hydrogen (H), —NHR5, a halogen, a hydroxyl, an alkyl, a cyano, or a nitro group; R2 is a hydrogen, —NHR6, a halogen, a hydroxyl, a substituted or unsubstituted alkyl, an alkenyl, an alkynyl, an alkoxyl, a cycloalkyl, an amino, a cyano, or a nitro group; R3 is a hydrogen, —NHR6, a halogen, a hydroxyl, a halogenated alkyl, a substituted or unsubstituted alkyl, alkenyl, alkynyl, alkoxyl, or cycloalkyl, an amino, a cyano, and a nitro group; R4 is a substituted or unsubstituted alkyl, alkenyl, alkynyl, alkoxyl, aryl, heteroaryl, cycloalkyl, or heterocyclyl, an alkyl amino, substituents on the substituted R4 group are selected from a halogen, a cyano, an amino, a C1-4 alkylamine, a C1-4 alkyl, a C3-6 cycloalkyl, an alkoxyl, a nitro, a carboxy, a carbonyl, a carboalkoxy, or an aminocarboxy; R5 is a hydrogen, —C(═O)—R6, a substituted or unsubstituted alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; R6 is a substituted or unsubstituted alkyl, alkenyl, alkynyl, alkoxyl, or cycloalkyl, an amino, or a substituted amino group; Z is an OR7, a SR7, or a SO2R7; R7 is an optionally substituted C1-8 hydrocarbon group, or a group described in the following formula: or a group described in the following formula: Wherein each of R8, R9, R10, R11 is independently selected from a hydrogen, a halogenated C1-8 alkyl, a hydroxyl substituted C1-8 alkyl, a substituted or unsubstituted C1-8 hydrocarbon group, and each of R12, R13, R14 is independently selected from a hydrogen, a halogen, an OR15, a NR16R17, a C(═O)N R18R19, or an optionally substituted C1-C8 hydrocarbon group; or R12, R13 and R14, together with the atoms to which they are attached, may be joined together to form a chain so that the ring to which they are attached is a substituted C6-C14 membered spiral ring, a bicyclic ring, or a fused ring group, and m1=2, 3, 4, 5, and m2=0, 1, 2, and Ring A is a 4-8 membered substituted or unsubstituted aryl, heteroaryl, cycloalkyl, cycloalkenyl, and heterocyclyl containing 1 or 2 hetero atoms that are independently selected from an oxygen, a nitrogen or a sulfur, and Each of R15, R16, R17, R18, R19, is independently selected from a hydrogen (H) or an optionally substituted C1-C8 hydrocarbon group, and R20 is H, an optionally substituted hydrocarbon group, an optionally substituted cyclic hydrocarbon group, an optionally substituted heterocyclyl group, a C(═O)R22, a C(═O)OR22, or a C(═O)NHR22, and R21 is an OH, an NHR22, a C(═O)OR22, or a C(═O)NHR22, and R22 is a H or an optionally substituted C1-8 hydrocarbon group.
地址 San Diego CA US
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