发明名称 BICYCLICALLY SUBSTITUTED URACILS AND THE USE THEREOF
摘要 The present application relates to novel bicyclically substituted uracil derivatives, 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.
申请公布号 US2015148340(A1) 申请公布日期 2015.05.28
申请号 US201314399945 申请日期 2013.05.03
申请人 BAYER PHARMA AKTIENGESELLSCHAFT 发明人 Fürstner Chantal;Ackerstaff Jens;Straub Alexander;Meier Heinrich;Tinel Hanna;Zimmermann Katja;Tersteegen Adrian;Zubov Dmitry;Kast Raimund;Schamberger Jens;Schäfer Martina;Börngen Kirsten
分类号 C07D417/14;A61K31/513;C07D405/14;A61K45/06;C07D417/04;C07D401/04;C07D409/14;C07D403/04;C07D413/04 主分类号 C07D417/14
代理机构 代理人
主权项 1. A compound of the formula (I) in which R1 is hydrogen or (C1-C4)-alkyl, R2 is a group of the formula where* is the attachment site to the uracil nitrogen atom,A is —CH2—, —CH2—CH2—, —O—CH2-## or oxygen, in which## is the attachment site to the phenyl ring,m is a number 0, 1 or 2,R4 is halogen, difluoromethyl, trifluoromethyl, (C1-C4)-alkyl, difluoromethoxy, trifluoromethoxy or (C1-C4)-alkoxy,R5A is hydrogen or deuterium,R5B is hydrogen, deuterium or (C1-C4)-alkyl,R6 is hydrogen or fluorine,R7 is hydrogen or fluorine,R8 is halogen, difluoromethyl, trifluoromethyl, (C1-C4)-alkyl or nitro,R9 is hydrogen, halogen, difluoromethyl, trifluoromethyl, (C1-C4)-alkyl, nitro or (C1-C4)-alkylthio, R3 is a group of the formula where# is the attachment site to the uracil nitrogen atom,the ring Q is 5- to 7-membered heterocyclyl or 5- or 6-membered heteroaryl, in which 5- to 7-membered heterocyclyl and 5- or 6-membered heteroaryl 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)-alkylsulphonyl, in which (C1-C6)-alkyl and (C3-C7)-cycloalkyl may in turn be substituted by 1 to 3 substituents independently selected from the group of halogen, cyano, trifluoromethyl, (C3-C7)-cycloalkyl, hydroxyl, (C1-C4)-alkoxy and 4- to 7-membered heterocyclyl, andin which two (C1-C6)-alkyl radicals bonded to a carbon atom of 5- to 7-membered heterocyclyl and 5- or 6-membered heteroaryl, together with the carbon atom to which they are bonded, may form a 3- to 6-membered carbocycle,R24 is halogen, (C1-C4)-alkyl or (C1-C4)-alkoxy,n is a number 0, 1, 2 or 3, and the salts, solvates and solvates of the salts thereof.
地址 Berlin DE