申请人:FORD John
公开号:US20100041695A1
公开(公告)日:2010-02-18
The invention provides compounds of the formula:
wherein
R1 is aryl, heteroaryl, cycloalkyl or alkyl;
R2 is H, alkyl, nitro, CO
2
R7, CONR5R6 or halo;
R3 and R4 are H, NR5R6, NC(O)R7, halo, trifluoromethyl, alkyl, CONR5R6, CO
2
R7, nitrile or alkoxy;
R5 and R6 may be the same or different and may be H, alkyl, aryl, heteroaryl or cycloalkyl; or R5 and R6 may together form a saturated, unsaturated or partially saturated 4 to 7 member ring, wherein said ring may optionally comprise one or more further heteroatoms selected from N, O or S;
R7 is H or alkyl;
A is H, halo, or a group of formula X-L-Y;
X is O, S or NR8;
R8 is H or alkyl;
L is (CH
2
)
n
, where n is 0, 1, 2, 3 or 4; and
Y is aryl, a heterocyclic group, alkyl, alkenyl or cycloalkyl; the products of mono- and di-oxidation of sulphur and/or mono-oxidation of nitrogen moieties in compounds of formula I;
or a pharmaceutically acceptable salt thereof.
These compounds find use as inhibitors of potassium ion channels and thus are useful in the treatment of various conditions including arrhythmia and type-2 diabetes mellitus.
该发明提供了以下式子的化合物:其中,R1是芳基,杂环芳基,环烷基或烷基;R2是H,烷基,硝基,CO2R7,CONR5R6或卤素;R3和R4是H,NR5R6,NC(O)R7,卤素,三氟甲基,烷基,CONR5R6,CO2R7,腈或烷氧基;R5和R6可能相同或不同,可以是H,烷基,芳基,杂环芳基或环烷基;或者R5和R6可以共同形成饱和的、不饱和的或部分饱和的4到7成员环,其中该环可以选择地包含一个或多个来自N、O或S的进一步杂原子;R7是H或烷基;A是H、卤素或公式X-L-Y的基团;X是O、S或NR8;R8是H或烷基;L是(CH2)n,其中n为0、1、2、3或4;而Y是芳基、杂环基、烷基、烯基或环烷基;该式I中硫单氧化物和/或氮单氧化物基团的单氧化和二氧化产物;或其药学上可接受的盐。这些化合物可用作钾离子通道的抑制剂,因此对于治疗包括心律不齐和2型糖尿病在内的各种疾病是有用的。