发明名称 Substituted 2-oxy-quinoline-3-carboxamides as KCNQ2/3 modulators
摘要 The invention relates to substituted 2-oxy-quinoline-3-carboxamides, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
申请公布号 US9073862(B2) 申请公布日期 2015.07.07
申请号 US201314089842 申请日期 2013.11.26
申请人 GRUENENTHAL GMBH 发明人 Kühnert Sven;Bahrenberg Gregor;Kless Achim;Schröder Wolfgang
分类号 C07D215/56;A61K31/47;C07D215/54;C07D409/12;A61K45/06 主分类号 C07D215/56
代理机构 Norris McLaughlin & Marcus, P.A. 代理人 Norris McLaughlin & Marcus, P.A.
主权项 1. A substituted compound of general formula (I) wherein R1 represents a C1-10-aliphatic residue, unsubstituted or mono- or polysubstituted; a C3-10-cycloaliphatic residue or a 3 to 10 membered heterocycloaliphatic residue, in each case unsubstituted or mono- or polysubstituted and in each case optionally bridged via a C1-8 aliphatic group, which in turn may be unsubstituted or mono- or polysubstituted; aryl or heteroaryl, in each case unsubstituted or mono- or polysubstituted and in each case optionally bridged via a C1-8 aliphatic group, which in turn may be unsubstituted or mono- or polysubstituted; R2 represents H; F; Cl; Br; I; CN; CF3; C(═O)H; NO2; OCF3; SCF3; a C1-4-aliphatic residue, a C(═O)—C1-4 aliphatic residue, a C(═O)—O—C1-4 aliphatic residue, a C(═O)—NH—C1-4 aliphatic residue, a C(═O)—N(C1-4 aliphatic residue)2, wherein the C1-4 aliphatic residue may be in each case be unsubstituted or mono- or polysubstituted; a O—C1-4-aliphatic residue, a O—C(═O)—C1-4-aliphatic residue, a S—C1-4-aliphatic residue, a S(═O)2—C1-4-aliphatic residue, a S(═O)2—O—C1-4-aliphatic residue, wherein the C1-4 aliphatic residue may be in each case be unsubstituted or mono- or polysubstituted; a C3-6-cycloaliphatic residue or a 3 to 6 membered heterocycloaliphatic residue, in each case unsubstituted or mono- or polysubstituted and in each case optionally bridged via a C1-4 aliphatic group, which in turn may be unsubstituted or mono- or polysubstituted; R3, R4, R5 and R6 each independently of one another represent H; F; Cl; Br; I; CN; CF3; C(═O)H; C(═O)—OH; C(═O)—NH2; SCF3; S(═O)2—OH; NO2; OCF3; a C1-4-aliphatic residue, a C(═O)—C1-4 aliphatic residue, a C(═O)—O—C1-4 aliphatic residue, a C(═O)—NH—C1-4 aliphatic residue, a C(═O)—N(C1-4 aliphatic residue)2, wherein the C1-4 aliphatic residue may be in each case be unsubstituted or mono- or polysubstituted; a O—C1-4-aliphatic residue, a O—C(═O)—C1-4-aliphatic residue, a S—C1-4-aliphatic residue, a S(═O)2—C1-4-aliphatic residue, a S(═O)2—O—C1-4-aliphatic residue, wherein the C1-4 aliphatic residue may be in each case be unsubstituted or mono- or polysubstituted; a NH(C1-4 aliphatic residue), a N(C1-4 aliphatic residue)2, a NH—C(═O)—C1-4 aliphatic residue, a NH—S(═O)2—C1-4-aliphatic residue, a N(C1-4 aliphatic residue)-C(═O)—C1-4 aliphatic residue, or a N(C1-4 aliphatic residue)-S(═O)2—C1-4 aliphatic residue, wherein the C1-4 aliphatic residue may in each case be unsubstituted or mono- or polysubstituted; a C3-6-cycloaliphatic residue or a 3 to 6 membered heterocycloaliphatic residue, in each case unsubstituted or mono- or polysubstituted and in each case optionally bridged via a C1-4 aliphatic group, which in turn may be unsubstituted or mono- or polysubstituted; R7 represents a C1-10-aliphatic residue, unsubstituted or mono- or polysubstituted; a C3-10-cycloaliphatic residue or a 3 to 10 membered heterocycloaliphatic residue, in each case unsubstituted or mono- or polysubstituted and in each case optionally bridged via a C1-8 aliphatic group, which in turn may be unsubstituted or mono- or polysubstituted; on the condition that if R7 represents an unsubstituted aliphatic residue, then R7 does not represent methyl or ethyl, andon the condition that if R7 denotes a 3 to 10 membered heterocycloaliphatic residue, the 3 to 10 membered heterocycloaliphatic residue is linked via a carbon atom, in which an “aliphatic group” and “aliphatic residue” can in each case be branched or unbranched, saturated or unsaturated, in which a “cycloaliphatic residue” and a “heterocycloaliphatic residue” can in each case be saturated or unsaturated, in which “mono- or polysubstituted” with respect to an “aliphatic group” and an “aliphatic residue” relates, with respect to the corresponding residues or groups, to the substitution of one or more hydrogen atoms each independently of one another by at least one substituent selected from the group consisting of F, Cl, Br, I, NO2, NH2, an NH(C1-4 aliphatic residue), an N(C1-4 aliphatic residue)2, a NH—C(═O)—C1-4 aliphatic residue, a NH—S(═O)2—C1-4 aliphatic residue, ═O, OH, OCF3, a O—C1-4-aliphatic residue, a O—C(═O)—C1-4-aliphatic residue, SH, SCF3, a S—C1-4-aliphatic residue, S(═O)2OH, a S(═O)2—C1-4-aliphatic residue, a S(═O)2—O—C1-4-aliphatic residue, a S(═O)2—NH—C1-4-aliphatic residue, CN, CF3, CHO, COOH, a C1-4-aliphatic residue, a C(═O)—C1-4-aliphatic residue, a C(═O)—O—C1-4-aliphatic residue, a C3-6-cycloaliphatic residue, a 3 to 6 membered heterocycloaliphatic residue, C(═O)—NH2, a C(═O)—NH(C1-4 aliphatic residue), and a C(═O)—N(C1-4 aliphatic residue)2; in which “mono- or polysubstituted” with respect to a “cycloaliphatic residue” and a “heterocycloaliphatic residue” relates, with respect to the corresponding residues, to the substitution of one or more hydrogen atoms each independently of one another by at least one substituent selected from the group consisting of F, Cl, Br, I, NO2, NH2, an NH(C1-4 aliphatic residue), an N(C1-4 aliphatic residue)2, a NH—C(═O)—C1-4 aliphatic residue, a NH—S(═O)2—C1-4 aliphatic residue, ═O, OH, OCF3, a O—C1-4-aliphatic residue, a O—C(═O)—C1-4-aliphatic residue, SH, SCF3, a S—C1-4-aliphatic residue, S(═O)2OH, a S(═O)2—C1-4-aliphatic residue, a S(═O)2—O—C1-4-aliphatic residue, a S(═O)2—NH—C1-4-aliphatic residue, CN, CF3, CHO, COOH, a C1-4-aliphatic residue, a C(═O)—C1-4-aliphatic residue, a C(═O)—O—C1-4-aliphatic residue, a C3-6-cycloaliphatic residue, a 3 to 6 membered heterocycloaliphatic residue, C(═O)—NH2, a C(═O)—NH(C1-4 aliphatic residue), and a C(═O)—N(C1-4 aliphatic residue)2; in which “mono- or polysubstituted” with respect to “aryl” and a “heteroaryl” relates, with respect to the corresponding residues, to the substitution of one or more hydrogen atoms each independently of one another by at least one substituent selected from the group consisting of F, Cl, Br, I, NO2, NH2,an NH(C1-4 aliphatic residue), an N(C1-4 aliphatic residue)2, an NH—C(═O)—C1-4 aliphatic residue, an NH—S(═O)2—C1-4 aliphatic residue, OH, OCF3, a O—C1-4-aliphatic residue, a O—C(═O)—C1-4-aliphatic residue, SH, SCF3, a S—C1-4-aliphatic residue, S(═O)2OH, a S(═O)2—C1-4-aliphatic residue, a S(═O)2—O—C1-4-aliphatic residue, a S(═O)2—NH—C1-4-aliphatic residue, CN, CF3, C(═O)H, C(═O)OH, a C1-4-aliphatic residue, a C(═O)—C1-4-aliphatic residue, a C(═O)—O—C1-4-aliphatic residue, a C3-6-cycloaliphatic residue, a 3 to 6 membered heterocycloaliphatic residue, benzyl, aryl, heteroaryl, C(═O)—NH2, a C(═O)—NH(C1-4 aliphatic residue), and a C(═O)—N(C1-4 aliphatic residue)2; in the form of the free compounds, the racemate, the enantiomers, diastereomers, mixtures of the enantiomers or diastereomers in any mixing ratio, or of an individual enantiomer or diastereomer, or in the form of the salts of physiologically acceptable acids or bases.
地址 Aachen DE