发明名称 Amino-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 their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
申请公布号 US9126998(B2) 申请公布日期 2015.09.08
申请号 US201313789655 申请日期 2013.03.07
申请人 BAYER PHARMA AG 发明人 Vakalopoulos Alexandros;Follmann Markus;Hartung Ingo;Buchgraber Philipp;Jautelat Rolf;Haβfeld Jorma;Lindner Niels;Wunder Frank;Stasch Johannes-Peter;Redlich Gorden;Li Volkhart Min-Jian;Becker Eva-Maria;Knorr Andreas
分类号 A61K31/439;A61K45/06;C07D471/04;A61K31/437;A61K31/496;A61K31/5377;A61K31/541;A61K31/4545;A61K31/46;A61K31/4709;A61K31/4725 主分类号 A61K31/439
代理机构 Buchanan Ingersoll & Rooney 代理人 Buchanan Ingersoll & Rooney
主权项 1. A compound of formula (I)in which A represents CH2, CD2 or CH(CH3), R1 represents (C4-C6)-alkyl, (C3-C7)-cycloalkyl or phenyl, where (C4-C6)-alkyl may be substituted up to six times 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, (C1-C4)-alkoxy, difluoromethoxy and trifluoromethoxy, 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 carbonyl group,L1A represents a bond or (C1-C4)-alkanediyl, where (C1-C4)-alkanediyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of fluorine, trifluoromethyl, (C1-C4)-alkyl, (C3-C7)-cycloalkyl, hydroxy and (C1-C4)-alkoxy,L1B represents a bond or (C1-C4)-alkanediyl,L1C represents a bond or (C1-C4)-alkanediyl, where (C1-C4)-alkanediyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of fluorine, trifluoromethyl, (C3-C7)-cycloalkyl, hydroxy and (C1-C4)-alkoxy,R7 represents hydrogen, (C1-C6)-alkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl, (C3-C7)-cycloalkyl, 5- or 6-membered heteroaryl or phenyl, where (C1-C6)-alkyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of fluorine, trifluoromethyl, difluoromethoxy, trifluoromethoxy, hydroxy, (C1-C4)-alkoxy, (C1-C4)-alkoxycarbonyl, (C1-C4)-alkyl sulphonyl, phenyl, phenoxy and benzyloxy, where phenyl, phenoxy and benzyloxy for their part may be substituted by 1 to 3 halogen substituents,where (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 and (C1-C4)-alkoxy,andwhere phenyl and 5- or 6-membered heteroaryl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of halogen, cyano, trifluoromethyl, (C1-C4)-alkyl, (C1-C4)-alkylsulphonyl and (C1-C4)-alkoxy,R8 represents hydrogen or (C1-C4)-alkyl,orR7 and R8 together with the carbon atom to which they are attached form a 3- to 7-membered carbocycle or a 4- to 7-membered heterocycle, where the 3- to 7-membered carbocycle and the 4- to 7-membered heterocycle for their part may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of fluorine and (C1-C4)-alkyl,R9 represents hydrogen, (C1-C6)-alkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl, (C3-C7)-cycloalkyl, 5- or 6-membered heteroaryl or phenyl, where (C1-C6)-alkyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of fluorine, difluoromethyl, trifluoromethyl, difluoromethoxy, trifluoromethoxy, hydroxy, (C1-C4)-alkoxy, (C1-C4)-alkoxycarbonyl, (C1-C4)-alkylsulphonyl, phenyl, phenoxy and benzyloxy, where phenyl, phenoxy and benzyloxy for their part may be substituted by 1 to 3 halogen substituents,where (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 and (C1-C4)-alkoxy,andwhere phenyl and 5- or 6-membered heteroaryl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of halogen, cyano, trifluoromethyl, (C1-C4)-alkyl, (C1-C4)-alkoxy and (C1-C4)-alkylsulphonyl,R10 represents hydrogen or (C1-C4)-alkyl,orR9 and R10 together with the carbon atom to which they are attached form a 3- to 7-membered carbocycle or a 4- to 7-membered heterocycle, where the 3- to 7-membered carbocycle and the 4- to 7-membered heterocycle for their part may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of fluorine and (C1-C4)-alkyl,with the proviso that the radicals R7 and R9 do not both represent phenyl,orR7 and R9 together with the carbon atoms to which they are attached and with the group L1B form a 5- to 7-membered carbocycle or a 4- to 7-membered heterocycle,with the proviso that not more than one of the radical pairs R7 and R8, R9 and R10 and R7 and R9, respectively, forms a carbo- or heterocycle,R11 represents hydrogen or (C1-C4)-alkyl, where (C1-C4)-alkyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of fluorine, trifluoromethyl, hydroxy and (C1-C4)-alkoxy,R12 represents hydrogen, (C1-C6)-alkyl, (C3-C7)-cycloalkyl, phenyl or benzyl, where (C1-C6)-alkyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of fluorine, trifluoromethyl, hydroxy, (C1-C4)-alkoxy and phenoxy, andwhere phenyl and benzyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of halogen and trifluoromethyl,orR11 and R12 together with the nitrogen atom to which they are attached form a 4- to 7-membered azaheterocycle, where the 4- to 7-membered azaheterocycle may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of fluorine, trifluoromethyl, (C1-C4)-alkyl, (C3-C7)-cycloalkyl, hydroxy, (C1-C4)-alkoxy and 4- to 7-membered heterocyclyl,andL2 represents a bond or (C1-C4)-alkanediyl,R13 represents 5- to 9-membered azaheterocyclyl which is attached via a ring carbon atom, where 5- to 9-membered azaheterocyclyl may be substituted by 1 to 5 substituents independently of one another selected from the group consisting of fluorine, trifluoromethyl, (C1-C4)-alkyl, (C3-C7)-cycloalkyl and benzyl,andwhere 5- to 9-membered azaheterocyclyl may be fused to a phenyl ring which for its part may be substituted by 1 or 2 substituents selected from the group consisting of halogen, (C1-C4)-alkyl and trifluoromethyl, R4 represents hydrogen, R5 represents hydrogen, halogen, cyano, difluoromethyl, trifluoromethyl, (C1-C4)-alkyl, (C3-C7)-cycloalkyl, (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 its N-oxides, salts, solvates, salts of the N-oxides and solvates of the N-oxides and salts.
地址 Berlin DE