| 摘要 |
A bispidine compound or a prodrug, salt, solvate, alkyl quaternary ammonium salt or N-oxide thereof of formula I wherein: R1 is optionally substituted alkyl, -(CH2)a-aryl, or -(CH2)a-Het1; and a is 0 to 4; Het1 is a 5 to 10 membered heterocyclic ring containing one or more heteroatoms of oxygen, nitrogen and/or sulphur which can optionally includes one or more oxo substituents; X is O or S; R5a, R5b, R5c, R5d, R5e and R5f independently are H or alkyl; R2 and R3 are independently H, optionally substituted alkyl, OR7, N(R7a)R7b or OC(O)R8 or together form-O-(CH2)2-O-, -(CH2)3-,-(CH2)4- or -(CH2)5-; R4 is H or alkyl; D is H, alkyl, -OR9 or -(CH2)cN(R10)(R11); R6 is H, -OH, cyano, halo, amino, nitro, alkyl (optionally terminated by N(H)C(O)OR20a), alkoxy, -C(O)N(H)R21, -NHC(O)N(H)R22, -N(H)S(O)2R23 and/or -OS(O)2R24; A is a single bond, alkylene, -N(R25)(CH2)m-, -O(CH2)m- or -(CH2)mC(H)(OR25)(CH2)n- (in which latter three groups, the -(CH2)m group is attached to the bispidine nitrogen atom and which latter four groups are optionally substituted by one or more-OH groups); B is a single bond, alkylene, -(CH2)pN(R26)-, -(CH2)pS(O)q-, -(CH2)pO- (in which three latter groups, the -(CH2)p- group is attached to the carbon atom bearing D and R4), -C(O)N(R26)- (in which latter group, the -C(O)- group is attached to the carbon atom bearing D and R4), -N(R26)C(O)O(CH2)p- or -N(R26)(CH2)p- (in which latter two groups, the N(R26) group is attached to the carbon atom bearing D and R4); m, n and p independently are 0 to 4; q is 0 to 2 and R7 to R11 and R20a to R26 are as defined in the specification limited by the provisos as listed in the specification. The compounds are useful in treating arrhythmia.
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