发明名称 Cyclic thienouracil-carboxamides and use thereof
摘要 The present application relates to novel 2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidine-6-carboxamide derivatives (“thienouracil”-carboxamides), to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases and to their use for the preparation of medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of pulmonary and cardiovascular disorders.
申请公布号 US9604996(B2) 申请公布日期 2017.03.28
申请号 US201415027519 申请日期 2014.10.02
申请人 Bayer Pharma Aktiengesellschaft 发明人 Härter Michael;Delbeck Martina;Kalthof Bernd;Lustig Klemens;Lindner Niels;Kast Raimund;Wasnaire Pierre;Süβmeier Frank
分类号 C07D495/04;A61K31/519;A61K45/06;C07D519/00 主分类号 C07D495/04
代理机构 代理人 Mehta Aseem
主权项 1. A compound of the formula (I) in whichR1 represents methyl, where methyl may be substituted up to three times by fluorine,R2 represents methyl or represents a group of the formula in which * denotes the point of attachment to the CH2 group, Ar represents phenyl or 5- or 6-membered heteroaryl having up to two ring nitrogen atoms, where phenyl and heteroaryl may be mono- or disubstituted by identical or different radicals selected from the group consisting of fluorine, chlorine, methyl, trifluoromethyl, methoxy and trifluoromethoxy, R4A represents hydrogen, fluorine or methyl, R4B represents hydrogen, fluorine, methyl, trifluoromethyl, hydroxy or methoxy, or R4A and R4B are attached to one another and together with the carbon atom to which they are attached form a cyclopropyl or cyclobutyl ring,R3 represents (C1-C6)-alkyl, where alkyl may be substituted up to three times by fluorine and where in alkyl up to two CH2 groups may be replaced by —O— or —S—, with the proviso that there are at least two carbon atoms between such heteroatoms including the uracil N1-atom, andthe ring A represents an aza heterocycle of the formula in which ** denotes the point of attachment to the carbonyl group, R5 represents hydrogen, methyl, trifluoromethyl, hydroxymethyl or ethyl, R6A and R6B each independently of one another represent hydrogen, methyl or ethyl, and their salts, solvates and solvates of the salts.
地址 Berlin DE