发明名称 SUBSTITUTED URACILS AS CHYMASE INHIBITORS
摘要 Substituted uracil derivatives of formula (I), processes for their preparation, their use alone or in combinations for the treatment and/or prophylaxis of diseases, and their use for preparing medicaments for the treatment and/or prophylaxis of diseases.
申请公布号 US2016244415(A1) 申请公布日期 2016.08.25
申请号 US201415034995 申请日期 2014.11.05
申请人 Bayer Pharma Aktiengesellschaft 发明人 Furstner Chantal;Ackerstaff Jens;Straub Alexander;Meier Heinrich;Tinel Hanna;Zimmermann Katja;Zubov Dmitry;Schamberger Jens
分类号 C07D239/557;A61K31/513;C07D413/10;C07D413/04;C07D417/04;A61K9/08;C07D403/14;C07D417/14;C07D413/14;A61K45/06;A61K9/00;A61K9/20;C07D403/10;C07D403/04 主分类号 C07D239/557
代理机构 代理人
主权项 1. A compound of the formula (I) in which R1 represents cyano, 5- to 7-membered heterocyclyl or 5- or 6-membered heteroaryl, where 5- to 7-membered heterocyclyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of oxo, (C1-C4)-alkyl and halogen, and where 5- or 6-membered heteroaryl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of (C1-C4)-alkyl, hydroxy and halogen, or R1 represents a group of the formula where* represents the point of attachment to the uracil group,m represents 0 or 1,L1A represents a bond or (C1-C4)-alkanediyl, in which (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, R5 represents hydrogen or (C1-C4)-alkyl,R6 represents hydrogen or (C1-C4)-alkyl, in which (C1-C4)-alkyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of fluorine, trifluoromethyl, (C1-C4)-alkyl, hydroxy and (C1-C4)-alkoxy,orR5 and R6 together with the carbon atoms to which they are attached form a 3- to 7-membered carbocycle,R7 represents hydrogen, cyano, (C3-C7)-cycloalkyl, hydroxycarbonyl or (C1-C4)-alkoxycarbonyl,or R1 represents a group of the formula where*** represents the point of attachment to the uracil group, R2 represents a group of the formula where** represents the point of attachment to the uracil nitrogen atom,A represents —CH2—, —CH2—CH2—, —O—CH2-## or oxygen, in which ## represents the point of attachment to the phenyl ring,n represents a number 0, 1 or 2,R10 represents hydrogen, halogen, difluoromethyl, trifluoromethyl, (C1-C4)-alkyl, difluoromethoxy, trifluoromethoxy or (C1-C4)-alkoxy,R11A represents hydrogen or deuterium,R11B represents hydrogen, deuterium or (C1-C4)-alkyl, R12 represents hydrogen, halogen, (C1-C4)-alkyl, difluoromethyl or trifluoromethyl,R13 represents halogen, (C1-C4)-alkyl, difluoromethyl or trifluoromethyl,R14 represents hydrogen or halogen, R15 represents hydrogen or halogen,R3 represents where# represents the point of attachment to the uracil nitrogen atom,R16 represents hydrogen,R17 represents hydrogen, halogen, (C1-C4)-alkyl or (C1-C4)-alkoxy,R18 represents (C1-C4)-alkyl, (C1-C4)-alkoxy, (C1-C4)-alkylthio, (C1-C4)-alkylsulfinyl, (C1-C4)-alkylsulfonyl or —N(R21R22), in which (C1-C4)-alkoxy may be substituted by a substituent independently of one another selected from the group consisting of hydroxy, (C1-C4)-alkoxycarbonyl, amino, mono-(C1-C4)-alkylamino, di-(C1-C4)-alkylamino, aminocarbonyl, mono-(C1-C4)-alkylaminocarbonyl and di-(C1-C4)-alkylaminocarbonyl,where R21 represents (C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl or (C1-C4)-alkylaminocarbonyl, in which (C1-C4)-alkylaminocarbonyl may be substituted by hydroxy or (C1-C4)-alkoxy,R22 represents hydrogen or (C1-C4)-alkyl,orR18 represents 4- to 7-membered heterocyclyl or 5- to 6-membered heteroaryl, in which 4- to 7-membered heterocyclyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of halogen, trifluoromethyl, (C1-C4)-alkyl, hydroxy, oxo, amino and (C1-C4)-alkoxycarbonyl, in which (C1-C4)-alkyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of halogen, hydroxy and —N(R23R24),in which R23 represents hydrogen, (C1-C4)-alkyl or (C1-C4)-alkylcarbonyl, in which R24 represents hydrogen or (C1-C4)-alkyl,in which 5- to 6-membered heteroaryl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of halogen, trifluoromethyl, (C1-C4)-alkyl, hydroxy, amino and (C1-C4)-alkoxycarbonyl, in which (C1-C4)-alkyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of halogen, hydroxy and —N(R23R24),in which R23 represents hydrogen, (C1-C4)-alkyl or (C1-C4)-alkylcarbonyl, in which R24 represents hydrogen or (C1-C4)-alkyl,R19 represents hydrogen, halogen, cyano, (C1-C4)-alkyl or (C1-C4)-alkoxy,R20 represents hydrogen, halogen, (C1-C4)-alkyl or (C1-C4)-alkoxy,orR3 represents in which# represents the point of attachment to the uracil nitrogen atom,the ring Q represents 5- to 7-membered heterocyclyl or 5- or 6-membered heteroaryl, in which 5- to 7-membered heterocyclyl may be substituted by 1 to 4 substituents independently selected from the group of halogen, difluoromethyl, trifluoromethyl, trideuteromethyl, (C1-C6)-alkyl, (C3-C7)-cycloalkyl, oxo, hydroxyl, (C1-C4)-alkylcarbonyl, (C1-C4)-alkoxycarbonyl, aminocarbonyl and (C1-C4)-alkylsulfonyl,in which 5- or 6-membered heteroaryl may be substituted by 1 to 2 substituents independently of one another selected from the group consisting of (C1-C6)-alkyl, (C3-C7)-cycloalkyl, hydroxy, (C1-C4)-alkylcarbonyl, (C1-C4)-alkoxycarbonyl, aminocarbonyl and (C1-C4)-alkylsulfonyl,andin which two (C1-C6)-alkyl radicals attached to a carbon atom of 5- to 7-membered heterocyclyl together with the carbon atom to which they are attached may form a 3- to 6-membered carbocycle,R25 represents halogen, (C1-C4)-alkyl or (C1-C4)-alkoxy,p represents a number 0, 1, 2 or 3,R4 represents hydrogen or (C1-C4)-alkyl, and the salts, solvates and solvates of the salts thereof.
地址 Berlin DE