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US 8,912,173 B2Granted
Substituted quinolines and their use as medicaments
AssigneeBoehringer Ingelheim International GmbH
InventorsMatthias Hoffmann, Daniel Bischoff, Georg Dahmann, Jasna Klicic, Gerhard Schaenzle, Stefan Ludwig Michael Wollin, Serge Gaston Convers-Reignier, Stephen Peter East, Frederic Jacques Marlin, Clive McCarthy, John Scott
Life of this patent
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Abstract
Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.
Claims35
A compound of the formula 1
- wherein
- R1 is a linear or branched C1-6-alkyl,
- wherein R1 is substituted by R3 which is selected from the group consisting of a three-, four-, five-, six- or seven-membered cycloalkyl;
- a five-, six- or seven-membered, saturated heterocycle comprising one, two or three heteroatoms each independently selected from the group consisting of N, S and O;
- and a five- or six-membered heteroaryl comprising one, two or three heteroatoms each independently selected from the group consisting of N, S and O;
- wherein the R3 may optionally be substituted by one, two, three or four substituents each independently selected from the group consisting of oxo, OH, —CO—NH2, —CO—NH(CH3), —CO—N(CH3)2, —C1-5-alkyl, —C1-3-alkylene-CO—NH2, —C1-3-alkylene-CO—NH(CH3), —C1-3-alkylene-CO—N(CH3)2, —C1-3-alkylene-CN and —CN, and wherein
- R2 is selected from the group consisting of halogen, phenyl, a five- or six-membered monocyclic heteroaryl comprising one, two or three heteroatoms each independently selected from the group consisting of N, S and O;
- a bicyclic nine-, ten- or eleven-membered, either aromatic or non-aromatic, but not fully saturated heterocycle comprising one, two, three or four heteroatoms each independently selected from the group consisting of N, S and O;
- wherein the R2 may optionally be substituted by one, two, three or four substituents R4 which independently from one another are selected from the group consisting of linear or branched —O—C1-5-alkyl, —OH, oxo, halogen, —C1-5-haloalkyl, —SO2CH3, —C1-3-alkylene-SO2—C1-3-alkyl), —SO2—CF3, —CN, —C3-6-cycloalkyl, linear or branched —C1-5-alkyl, a four, five- or six-membered saturated heterocycle comprising one, two or three heteroatoms each independently from one another selected from the group of N, S, —SO2 and O;
- —C1-3-alkylene-N(C1-3-alkyl)-CO—C1-3-alkyl, —NH—CO—C1-3-alkyl, —CO—NH(CH3), —CO—NH2, —CO—N(CH3)2, —O—R5, —CO—R5, —C1-3-alkylene-O—CO—C1-3-alkyl and
- wherein the R4 may optionally be substituted by one or two substituents R5,
- wherein each R5 is independently from one another selected from the group consisting of linear or branched —C1-4-alkyl, oxo, —C1-3-haloalkyl, —OH, halogen, —C1-2-alkylene-C1-3-haloalkyl, a five- or six-membered saturated heterocycle comprising one, two or three heteroatoms each independently selected from the group of N, S and O, a three, four-, five-, six- or seven-membered cycloalkyl, a five- or six-membered heteroaryl comprising one or two heteroatoms each independently selected from the group consisting of N, O and S,
- wherein the R5 may optionally be substituted by a group consisting of oxo, —C1-3-alkyl and —C1-3-haloalkyl,
- or a pharmacologically acceptable salt thereof.
11 more elements
A compound of formula 1 selected from a group consisting of:
Dependencies are inferred from the claim text.