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    • 5. 发明公开
    • CHROMENYLMETHYLPYRIMIDINEDIAMINES AS ANTIBACTERIAL AGENTS
    • 作为抗菌剂的铬酸甲基亚氨基二亚胺
    • EP1278742A1
    • 2003-01-29
    • EP01925562.9
    • 2001-04-20
    • Basilea Pharmaceutica AG
    • MOHR, PeterPFLIEGER, Philippe
    • C07D405/06C07D405/14C07D409/14C07D491/20C07D493/20A61K31/506A61P31/04
    • C07D405/06C07D409/14C07D491/10C07D493/10C07F7/0814
    • This invention is concerned with substituted chromene derivatives of the general formula (I) in which R1 represents alkyl or cycloalkylalkyl, R?2 and R3¿ each independently represent alkyl or cycloalkyl or taken together with the adjacent carbon atom represent a saturated 3- to 6- membered carbocyclic or heterocyclic ring, the alkyl, cycloalkyl, carbocyclic or heterocyclic ring being unsubstituted or substituted, and R4 represents hydrogen, halogen cyano, alkyl, alkylthio, alkenyl, alkynyl, hydroxyalkyl, hydroxyalkynyl, alkoxyalkyl, alkoxyalkynyl, trialkylsilyl, aryl or heteroaryl, and pharmaceutically acceptable acid addition salts of these compounds, their use as therapeutically active substances; medicaments based on these substances, optionally in combination with sulphonamides, and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula (I) and their pharmaceutically acceptable acid addition salts and intermediates for their manufacture.
    • 本发明涉及通式(Ⅰ)的取代苯并吡喃衍生物,其中R 1代表烷基或环烷基烷基,R 2和R 3各自独立地代表烷基或环烷基或与相邻碳原子一起代表饱和的3-6 烷基,烷基,羟基炔基,烷氧基烷基,烷氧基炔基,三烷基甲硅烷基,芳基或杂芳基, 和这些化合物的药学上可接受的酸加成盐,它们作为治疗活性物质的用途; 基于这些物质的药物,任选地与磺酰胺组合以及它们的生产; 这些物质作为药物的用途以及用于生产抗菌活性药物的用途; 以及制备式(I)化合物及其药学上可接受的酸加成盐和用于其制备的中间体。