| 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. |
| 主权项 |
1. A compound of the formula (I) in which R1 represents hydrogen, methyl or ethyl, where methyl and ethyl may be substituted up to three times by fluorine, R2 represents methyl, ethyl, n-propyl, isopropyl, cyclopropyl, cyclopropylmethyl, 2,2-difluorovinyl, 3,3-difluoroallyl or propargyl 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,orR4A and R4B are attached to one another and together with the carbon atom to which they are attached form a cyclopropyl or cyclobutyl ring,R8 represents methyl or trifluoromethyl, andR9A and R9B independently of one another represent hydrogen, methyl or trifluoromethyl, R3 represents (C1-C6)-alkyl, (C2-C6)-alkenyl, (C3-C7)-cycloalkyl or [(C3-C7)-cycloalkyl]methyl,
where alkyl and alkenyl may be substituted up to three times and cycloalkyl may be substituted up to two times by fluorine andwhere in alkyl and cycloalkyl 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, and the ring A represents a mono- or bicyclic 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,R10A represents methyl, ethyl, hydroxy or methoxy, andR10B represents hydrogen, methyl or ethyl, andtheir salts, solvates and solvates of the salts. |
