公开(公告)号：US06265445B1

公开(公告)日：2001-07-24

申请号：US09555602

申请日：2000-07-28

申请人： Gyula Papp ,  András Varró ,  Péter Mátyus ,  Ildikó Varga ,  Tivadar Rettegi ,  Alice Druga ,  Antal Simay ,  Imre Moravcsik ,  Pál Berzsenyi ,  Daniella Barlocco ,  Giorgio Cignarella ,  Márta Pátfalusi

发明人： Gyula Papp ,  András Varró ,  Péter Mátyus ,  Ildikó Varga ,  Tivadar Rettegi ,  Alice Druga ,  Antal Simay ,  Imre Moravcsik ,  Pál Berzsenyi ,  Daniella Barlocco ,  Giorgio Cignarella ,  Márta Pátfalusi

IPC分类号： A61K3117

CPC分类号： C07C233/36 ,  C07C217/18 ,  C07C233/78 ,  C07C275/40 ,  C07C311/08 ,  C07C335/20 ,  Y10S514/821

摘要： The present invention relates to novel, antiarrhythmically active phenoxyalkylamine derivatives possessing a double point of attack. More particularly, the present invention relates to new phenoxyalkylamine derivatives of the formula (1) wherein R1 and R2, independently from each other, mean hydrogen, halogen or C1-4 alkyl group; R3, R4 and R5, independently from each other, stand for hydrogen or C1-4 alkyl group; R6 represents hydrogen, C1-4 alkyl or benzyl group; R7 means nitro group or amino group optionally monosubstituted by C1-4 alkyl, benzoyl, C1-4 alkylcarbonyl, C1-4 alkylsulfonyl, C1-4 alkylcarbamoyl or C1-4 alkylthiocarbamoyl group; both n and m are 0 or 1, with the proviso that R2 is different from hydrogen, when R1 is hydrogen, as well as stereoisomers or mixtures of stereoisomers thereof, acid addition salts thereof and hydrates, prodrugs and metabolites of all these compounds.

摘要翻译： 本发明涉及具有双重攻击点的新型抗心律失活的苯氧基烷基胺衍生物。 更具体地说，本发明涉及式（1）的新的苯氧基烷基胺衍生物，其中R 1和R 2彼此独立地表示氢，卤素或C 1-4烷基; R 3，R 4和R 5彼此独立地代表 氢或C 1-4烷基; R 6表示氢，C 1-4烷基或苄基; R 7表示硝基或任选被C 1-4烷基，苯甲酰基，C 1-4烷基羰基，C 1-4烷基磺酰基，C 1-4的单取代的氨基 烷基氨基甲酰基或C 1-4烷基硫代氨基甲酰基; n和m均为0或1，条件是当R 1为氢时，R 2不同于氢，以及立体异构体或其立体异构体的混合物，其酸加成盐和水合物，前药 和所有这些化合物的代谢物。