申请人:Nishida Haruyuki
公开号:US20100210696A1
公开(公告)日:2010-08-19
Provided is a compound having a superior acid secretion suppressive action, which shows an antiulcer activity and the like.
A compound represented by the formula (I) or a salt thereof:
wherein ring A is a saturated or unsaturated 5-membered heterocycle containing, as a ring-constituting atom besides carbon atoms, at least one heteroatom selected from a nitrogen atom, an oxygen atom and a sulfur atom, the ring-constituting atoms X
1
and X
2
are the same or different and each is C or N, the ring-constituting atoms X
3
and X
4
are the same or different and each is C, N, 0 or S (provided that a pyrrole ring wherein X
1
is N is excluded from ring A), and when the ring-constituting atom X
3
or X
4
is C or N, each ring-constituting atom optionally has substituent(s) selected from an optionally substituted alkyl, an acyl, an optionally substituted hydroxy, an optionally substituted mercapto, an optionally substituted amino, a halogen, a cyano and a nitro;
R
1
and R
2
are each a cyclic group optionally having substituent(s); R
3
and R
4
are each H or alkyl, or R
3
and R
4
form, together with the adjacent N, an nitrogen-containing heterocycle; and Y is a spacer.
所提供的化合物具有卓越的抑制酸分泌作用,表现出抗溃疡活性等。化合物由式(I)或其盐表示,其中环A是饱和或不饱和的5元杂环,除碳原子外,至少包含一个从氮原子、氧原子和硫原子中选择的杂原子,环构成原子X1和X2相同或不同,均为C或N,环构成原子X3和X4相同或不同,均为C、N、O或S(前提是不包括X1为N的吡咯环),当环构成原子X3或X4为C或N时,每个环构成原子可选地具有取代基,所述取代基选择自可选取代的烷基、酰基、可选取代的羟基、可选取代的巯基、可选取代的氨基、卤素、氰基和硝基;R1和R2分别为环状基团,可选地具有取代基;R3和R4分别为H或烷基,或R3和R4与相邻的N形成含氮杂环;Y为间隔基。