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US 2017/0304278 A1Published application
Heteroaryl-substituted imidazo[1,2-a]pyridines and their use
AssigneeBayer Pharma Aktiengesellschaft
InventorsAlexandros VAKALOPOULOS, Damian BROCKSCHNIEDER, Frank WUNDER, Johannes-Peter STASCH, Tobias MARQUARDT, Lisa DIETZ, Volkhart Min-Jian LI
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Abstract
The present application relates to novel heteroaryl-substituted imidazo[1,2-a]pyridines, to processes for preparation thereof, to the use thereof, alone or in combinations, for the treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.
Claims13
A compound of the formula (I)
- in which
- A represents CH2, CD2 or CH(CH3),
- R1 represents (C3-C7)-cycloalkyl, phenyl or pyridyl,
- where (C3-C7)-cycloalkyl may be substituted by 1 to 4 substituents independently of one another selected from the group consisting of fluorine, trifluoromethyl and (C1-C4)-alkyl,
- where phenyl is substituted by 1 to 4 substituents independently of one another selected from the group consisting of halogen, cyano, monofluoromethyl, difluoromethyl, trifluoromethyl, (C1-C4)-alkyl, (C1-C4)-alkoxy and difluoromethoxy
- and
- where pyridyl is substituted by 1 or 2 substituents independently of one another selected from the group consisting of halogen, cyano and (C1-C4)-alkyl,
- R2 represents (C1-C4)-alkyl, cyclopropyl, cyclobutyl, monofluoromethyl, difluoromethyl or trifluoromethyl,
- R3 represents phenyl or 6-membered heteroaryl,
- where phenyl is substituted by —NR7R8,
- in which
- R7 represents hydrogen or (C1-C4)-alkyl,
- R8 represents (C1-C6)-alkyl or (C1-C4)-alkylcarbonyl,
- in which (C1-C6)-alkyl may be substituted by amino and up to three times by fluorine,
- or
- R7 and R8 together with the nitrogen atom to which they are attached form a 4- to 6-membered heterocycle,
- where phenyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of fluorine, chlorine, bromine, methyl and ethyl,
- where 6-membered heteroaryl is up to disubstituted by —NR9R10,
- in which
- R9 represents hydrogen or (C1-C4)-alkyl,
- R10 represents hydrogen, (C1-C6)-alkyl, phenyl or (C1-C4)-alkylcarbonyl,
- in which (C1-C6)-alkyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of (C1-C4)-alkoxy, amino and phenyl, and up to pentasubstituted by fluorine,
- or
- R9 and R10 together with the nitrogen atom to which they are attached form a 4- to 6-membered heterocycle,
- in which the 4- to 6-membered heterocycle may be substituted by 1 or 2 (C1-C4)-alkyl substituents,
- where 6-membered heteroaryl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of fluorine, chlorine, bromine, cyclopropyl, methyl and ethyl,
- R4 represents hydrogen,
- R5 represents hydrogen, fluorine, chlorine, cyano, (C1-C4)-alkyl, cyclopropyl, difluoromethyl or trifluoromethyl,
- R6 represents hydrogen or fluorine,
- and the N-oxides, salts, solvates, salts of the N-oxides and solvates of the N-oxides and salts thereof except for
- N-(3-{8-[(2,6-difluorobenzyl)oxy]-2-methylimidazo[1,2-a]pyridin-3-yl}phenyl)acetamide, and
- 8-[(2,6-difluorobenzyl)oxy]-2-methyl-3-[3-(piperidin-1-yl)phenyl]imidazo[1,2-a]pyridine.
29 more elements
(canceled)
(canceled)
Dependencies are inferred from the claim text.