发明名称 SUBSTITUTED IMIDAZO[1,2-A]PYRIDINECARBOXAMIDES AND THEIR USE
摘要 The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.
申请公布号 US2017057954(A1) 申请公布日期 2017.03.02
申请号 US201515120343 申请日期 2015.03.19
申请人 Bayer Pharma Aktiengesellschaft 发明人 VAKALOPOULOS Alexandros;VALOT Gaelle;LINDNER Niels;FOLLMANN Markus;WUNDER Frank;STASCH Johannes-Peter;MARQUARDT Tobias;REDLICH Gorden;DIETZ Lisa;Ll Volkhart Min-Jian
分类号 C07D471/04;A61K31/437;A61K31/5377;A61K31/55;A61K31/444;A61K31/506;A61K31/498;A61K31/4709;A61K45/06;A61K31/496 主分类号 C07D471/04
代理机构 代理人
主权项 1. Compound of the formula (I) in which A represents CH2, CD2 or CH(CH3), R1 represents (C4-C6)-alkyl, (C3-C7)-cycloalkyl, pyridyl or phenyl, where (C4-C6)-alkyl may be up to hexasubstituted by fluorine,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,andwhere phenyl may be substituted by 1 to 4 substituents independently of one another selected from the group consisting of halogen, cyano, monofluoromethyl, difluoromethyl, trifluoromethyl, (C1-C4)-alkyl, cyclopropyl, (C1-C4)-alkoxy, difluoromethoxy and trifluoromethoxy,where pyridyl may be substituted by 1 to 4 substituents independently of one another selected from the group consisting of fluorine, monofluoromethyl, difluoromethyl, trifluoromethyl and (C1-C4)-alkyl, R2 represents hydrogen, (C1-C4)-alkyl, cyclopropyl, monofluoromethyl, difluoromethyl or trifluoromethyl, R3 represents a group of the formula where* represents the point of attachment to the nitrogen atom,R7 represents hydrogen, (C1-C10)-alkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl, (C3-C7)-cycloalkyl, 4- to 7-membered heterocyclyl, (C1-C6)-alkylcarbonyl, (C3-C7)-cycloalkylcarbonyl, 5- to 6-membered heteroarylcarbonyl, 5- to 10-membered heteroaryl, phenyl or naphthyl, in which (C1-C10)-alkyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of fluorine, cyano, trifluoromethyl, difluoromethoxy, trifluoromethoxy, hydroxy, monoalkylamino, dialkylamino, (C3-C7)-cycloalkyl, 4- to 7-membered azaheterocyclyl, (C1-C4)-alkoxy, (C1-C4)-alkoxycarbonyl, (C1-C4)-alkylsulphanyl, (C1-C4)-alkylsulphonyl, (C1-C4)-alkylaminosulphonyl, (C1-C4)-alkylsulphonylamino, hydroxycarbonyl, (C1-C4)-alkoxycarbonyl, amino, phenyl and 5- to 6-membered heteroaryl, in which phenyl and 5- to 6-membered heteroaryl for their part may be substituted by 1 to 4 substituents independently of one another selected from the group consisting of (C1-C4)-alkyl, trifluoromethyl, halogen and cyano,in which (C3-C7)-cycloalkyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of fluorine, trifluoromethyl, (C1-C4)-alkyl, hydroxy, amino and (C1-C4)-alkoxy, in which 4- to 7-membered heterocyclyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of fluorine, trifluoromethyl, (C1-C4)-alkyl, hydroxy, amino, oxo and (C1-C4)-alkoxy,in which phenyl and naphthyl may be substituted by 1 to 4 substituents independently of one another selected from the group consisting of halogen, cyano, trifluoromethyl, (C1-C4)-alkyl, (C1-C4)-alkoxy, trifluoromethoxy, phenoxy and (C1-C4)-alkylsulphonyl,in which 5- to 10-membered heteroaryl may be substituted by 1 to 4 substituents independently of one another selected from the group consisting of halogen, cyano, trifluoromethyl, (C1-C4)-alkyl and (C1-C4)-alkoxy,andin which (C1-C6)-alkylcarbonyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of halogen, trifluoromethyl, hydroxy, amino, monoalkylamino, dialkylamino, 4- to 7-membered azaheterocyclyl and (C1-C4)-alkoxy, in which 4- to 7-membered azaheterocyclyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of (C1-C4)-alkyl and oxo,R8 represents hydrogen or (C1-C4)-alkyl,orR7 and R8 together with the nitrogen atom to which they are bonded form a 4- to 7-membered azaheterocycle, in which the 4- to 7-membered azaheterocycle for its part may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of fluorine, trifluoromethyl, oxo and (C1-C4)-alkyl, in which (C1-C4)-alkyl may be substituted by hydroxy or trifluoromethyl,R9 represents hydrogen, (C1-C10)-alkyl, (C3-C7)-cycloalkyl or 4- or 7-membered heterocyclyl, in which (C1-C10)-alkyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of fluorine, cyano, trifluoromethyl, (C2-C4)-alkenyl, hydroxy, amino, monoalkylamino, dialkylamino, (C3-C7)-cycloalkyl, 4- to 7-membered heterocyclyl, (C1-C4)-alkoxy, (C1-C4)-alkoxycarbonyl, —(C═O)NR10R11, phenyl, naphthyl and 5- to 6-membered heteroaryl, in which phenyl and naphthyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of halogen, cyano, trifluoromethyl and (C1-C4)-alkyl,in whichR10 represents hydrogen or (C1-C4)-alkyl,R11 represents hydrogen or (C1-C4)-alkyl, in which (C1-C4)-alkyl may be substituted by phenyl, in which phenyl may be substituted by halogen or cyano,orR10 and R11 together with the nitrogen atom to which they are bonded form a 4- to 7-membered azaheterocycle, in which the 4- to 7-membered azaheterocycle may be substituted by phenyl,andin which 4- to 7-membered heterocyclyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of halogen, hydroxy, cyano and (C1-C4)-alkyl, R4 represents hydrogen, R5 represents hydrogen, halogen, cyano, monofluoromethyl, difluoromethyl, trifluoromethyl, (C1-C4)-alkyl, (C3-C7)-cycloalkyl, (C2-C4)-alkenyl, (C2-C4)-alkynyl, difluoromethoxy, trifluoromethoxy, (C1-C4)-alkoxy, amino, 4- to 7-membered heterocyclyl or 5- or 6-membered heteroaryl, R6 represents hydrogen, cyano or halogen, and the N-oxides, salts, solvates, salts of the N-oxides and solvates of the N-oxides and salts thereof.
地址 Berlin DE