申请人:Kubo Keiji
公开号:US20090105253A1
公开(公告)日:2009-04-23
The present invention relates to a thrombin receptor antagonist containing a compound represented by the formula (I)
wherein R
1a
, R
1b
and R
2
are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or an optionally substituted alkoxy, R
3
is a group represented by the formula —NHCOR
4
, —NHSO
2
R
5
, —NHCON(R
6a
)(R
6b
), —NHCOOR
7
or —CONHR
8
wherein R
4
, R
5
, R
6a
, R
6b
, R
7
and R
8
are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group and the like), ring A is monocyclic aromatic ring optionally further having substituent(s), R
1a
and R
1b
are optionally bonded to each other to form an optionally substituted nitrogen-containing non-aromatic heterocycle, or a salt thereof or a prodrug thereof. The thrombin receptor antagonist of the present invention has a thrombin receptor (particularly PAR-1) antagonistic action and is useful for the prophylaxis or treatment of PAR-1 mediated pathological condition or disease.
本发明涉及一种含有式(I)所表示的化合物的凝血酶受体拮抗剂,其中R1a、R1b和R2分别是氢原子、可选取代的碳氢基团、可选取代的杂环基团或可选取代的烷氧基,R3是由式—NHCOR4、—NHSO2R5、—NHCON(R6a)(R6b)、—NHCOOR7或—CONHR8所表示的基团,其中R4、R5、R6a、R6b、R7和R8分别是氢原子、可选取代的碳氢基团、可选取代的杂环基团等,环A是单环芳香环,可选地进一步具有取代基,R1a和R1b可选择性地连接在一起形成可选取代的含氮非芳香杂环,或其盐或前药。本发明的凝血酶受体拮抗剂具有凝血酶受体(特别是PAR-1)拮抗作用,可用于预防或治疗PAR-1介导的病理状态或疾病。