申请人:Haga Yuji
公开号:US20120035155A1
公开(公告)日:2012-02-09
To provide an indole compound having a human QRFP receptor antagonistic activity and useful as a preventive or a remedy for various disorders. A compound of a formula (I) or a pharmaceutically-acceptable salt thereof is provided: [wherein, R
1
represents a hydrogen atom, a halogen, a C
1-6
alkyl, etc,; R
2
represents a C
1-6
alkyl, or a halo-C
1-6
alkyl; R
3
represents a hydrogen atom, a C
1-6
alkyl, etc.; R
4
represents a hydrogen atom, a C
1-6
alkyl, a halo-C
1-6
alkyl, etc.; or R
3
and R
4
, taken together with the nitrogen atom to which they bond, form a 3- to 6-membered aliphatic nitrogen-containing hetero ring; or R
3
and Y
3
, taken together, form —CH
2
—CH
2
—; Y
1
and Y
2
are both hydrogen atoms; or Y
1
and Y
2
, taken together, form —CH
2
—CH
2
—; and Y
3
represents a hydrogen atom; or Y
3
and R
3
, taken together, form —CH
2
—CH
2
—].
提供一种具有人类QRFP受体拮抗活性并可用于预防或治疗各种疾病的吲哚类化合物。提供一种公式(I)的化合物或其药学上可接受的盐:[其中,R1代表氢原子、卤素、C1-6烷基等;R2代表C1-6烷基或卤代C1-6烷基;R3代表氢原子、C1-6烷基等;R4代表氢原子、C1-6烷基、卤代C1-6烷基等;或R3和R4共同与它们键合的氮原子形成一个3至6成员的脂肪族含氮杂环;或R3和Y3共同形成—CH2—CH2—;Y1和Y2都是氢原子;或Y1和Y2共同形成—CH2—CH2—;且Y3代表氢原子;或Y3和R3共同形成—CH2—CH2—]。