发明名称 HETEROCYCLIC COMPOUNDS, MEDICAMENTS CONTAINING THEM, USE AND PROCESSES FOR THE PREPARATION THEREOF
摘要 The present invention relates to compounds of general formula (I);;and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, and the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
申请公布号 US2015011535(A1) 申请公布日期 2015.01.08
申请号 US201414322940 申请日期 2014.07.03
申请人 HECKEL Armin;KLEY Joerg 发明人 HECKEL Armin;KLEY Joerg
分类号 C07D403/12;A61K31/4965;A61K31/497;A61K45/06;A61K31/541;A61K31/5377;A61K31/551;C07D401/14;C07D241/20;C07D401/12 主分类号 C07D403/12
代理机构 代理人
主权项 1. A compound of formula (I), wherein A and A′ are independently from each other —CH2— or —CH2—CH2—; R is selected from —NR1R2, —NR3R4R5(+)Z1(−) and —OR13; X is halogen; Z1(−) is a halogen anion or an organic acid anion; Z2(−) is a halogen anion or an organic acid anion; Z3(−) is a halogen anion or an organic acid anion; Z4(−) is a halogen anion or an organic acid anion; R1 and R2 are selected independently from each other from H, —C(NH2)NH, —CN(CH3)2N(CH3)2+Z2−, —C1-3-alkyl, —C2-4-alkyl-N(CH3)2, —C1-3-alkyl-phenyl-R12, —C1-3-alkyl-COOH, —C1-4-alkyl-CO—Y2—R11, —CO-phenyl-CO—O—R13, —CO—C1-4-alkyl, —CO—C1-3-alkyl-NR6R7, —CO—C1-3-alkyl-N(CH3)3+Z3−, —CO—C1-4-alkyl-Y1—R9, —CO—O—C1-4-alkyl-R8, —CO—NH—C3-7-cycloalkyl, —CO—NH—C1-4-alkyl, —CH2—CO—O—C1-3-alkyl, —CH2—CO—O—C1-3-alkyl-phenyl and —SO2—R10;R6 is selected from —C1-3-alkyl, H, —C1-4-alkyl-OH, —CH2—CO—O—C1-3-alkyl and —CH2COOH;R7 is selected from —C1-3-alkyl, —CO—O—C1-3-alkyl, —C1-4-alkyl-OH, H, —CH2—CO—O—C1-3-alkyl and —CH2COOH;R8 is H or phenyl;R9 is selected from H, —C1-3-alkyl, OH, —NR6R7 and ═O;R10 is C1-3-alkyl or an optionally substituted N-containing nonaromatic heterocycle;R11 is selected from H, C1-3-alkyl, ═O, —N(CH3)2 and —N(CH3)3+Z4−;R12 is selected from H, halogen, —COOH, —PO(OC1-4-alkyl)OH optionally substituted at the 2, 3 or 4 position of the C1-4-alkyl group by —N(C1-3-alkyl)2 or —N(C1-3-alkyl)3+Z4−, and —PO(OC1-4-alkyl)2, —PO(OH)2;R13 is H or C1-4-alkyl;Y1 is selected from an optionally substituted 5- to 8-membered N-containing nonaromatic heterocycle, —N(C1-3-alkyl)-C2-4-alkyl-N(C1-3-alkyl)2 and —N(C1-3-alkyl)-C2-4-alkyl-N+(C1-3alkyl)3 Z1(−);Y2 is an optionally substituted 5- to 8-membered N-containing nonaromatic heterocycle; or R1 and R2 are together with the nitrogen atom they are attached to an optionally substituted 4-7-membered heterocycle, containing at least one N and optionally one or more heteroatoms selected from the group consisting of piperazino, morpholino, piperidino; thiomorpholino, thiomorpholino-1-oxide, thiomorpholinon-1,1-dioxide, diazepane and pyrrolidino, wherein the nitrogen atoms may be substituted by a group selected from among phenyl, C1-3-alkylsulfonyl, C1-3-alkyl and —CO—C1-3-alkyl; R3, R4 and R5 denote independently from each other —C1-3-alkyl; or tautomers or pharmacologically acceptable acid addition salts thereof.
地址 Biberach an der Riss DE