BISETHERS OF 1-OXA, AZA AND THIANAPHTHALEN-2-ONES AS PHOSPHOLAMBAN INHIBITORS
    1.
    发明公开
    BISETHERS OF 1-OXA, AZA AND THIANAPHTHALEN-2-ONES AS PHOSPHOLAMBAN INHIBITORS 审中-公开
    二醚1-氧杂,氮杂和噻萘-2-酮AS PHOSPHOLAMBANHEMMER

    公开(公告)号:EP1017691A1

    公开(公告)日:2000-07-12

    申请号:EP98946482.1

    申请日:1998-09-24

    摘要: Therapeutically active compounds of formula (I) or (II), in which R1 is hydrogen, alkyl, alkenyl, aryl, arylalkyl, hydroxyalkyl, halogenalkyl, alkoxy, COR10, CONR10R11, OR10, S(O)mR10, NR10COR11 or NR10R11, where R10 is hydrogen, alkyl, alkenyl, aryl, arylalkyl, hydroxyalkyl, halogenalkyl, alkoxy or hydroxy and R11 is hydrogen, alkyl, aryl, arylalkyl, alkoxy, aryloxy, hydroxy or acyl, or in case where X is NR11, R1 can also be carboxylalkyl; R6 is hydrogen, alkyl, alkenyl, aryl, arylalkyl; R2 and R7 mean hydrogen, alkyl, aryl, arylalkyl, alkenyl, COR10, CONR10R11, halogen, trifluoromethyl, nitro or cyano, where R10 and R11 are defined as above; R3 is hydrogen, alkyl, aryl or arylalkyl; A means alkyl or substituted alkyl, m is 0-2 and n is 1-3; Y means O, NR11 or S, where R11 is the same as above; X means O, NR11 or S, where R11 is the same as above, R4, R5, R8 and R9 mean independently one of the following groups (a), (b), (c), (d), (e), (f), (g), or in case where X is NR11, R4, R5, R8 and R9 can also independently mean HOOC-, R12OOC-, H2NCO- or HOHNCO-, wherein R12 means alkyl, arylalkyl or aryl, and wherein each aryl residue defined above by itself or as part of another group may be substituted, and pharmaceutically acceptable salts and esters thereof. The compounds have phospholamban inhibiting activity and are useful for treating heart failure.