申请人:Mitsubishi Tanabe Pharma Corporation
公开号:US08258131B2
公开(公告)日:2012-09-04
The present invention provides a novel fused bicyclic compound having an affinity to a receptor of mineral corticoid (MR), shown by the formula [I]:
wherein the ring A is a benzene ring having a substituent R1, fused to an adjacent 6-membered heterocyclic ring and further optionally having a substituent(s) other than R1, R1 is an alkylsulfonylamino group etc.,
R2 and R3 are (a) the same of different and a hydrogen atom, an alkyl group or a substituted or unsubstituted aryl group, (b) combined each other to form an oxo group or (c) combined each other at its terminal together with the adjacent carbon atom to form a cycloalkyl group,
X is a group of ═N—, ═C(R4)— or —CH(R4)—,
R4 is (a) a hydrogen atom, (b) a cyano group, (c) a halogen atom, (d) an alkyl group, (e) an alkenyl group, (f) a cycloalkyl group (g) an alkanoyl group, (h) a carbamoyl group or (i) a cycloalkenyl group,
Ar is an optionally substituted aromatic cyclic group and
a dotted line means presence or absence of a double bond,
or a pharmaceutically acceptable salt thereof,
which is useful as an antihypertensive agent etc.
本发明提供了一种新型的融合双环化合物,具有对矿物质醛固酮受体(MR)的亲和力,其化学式为[I]:其中,环A是具有取代基R1的苯环,与相邻的6元杂环环融合,并且还可以具有除R1以外的取代基;R1是烷基磺酰氨基等;R2和R3是(a)相同或不同的氢原子、烷基或取代或未取代的芳基;(b)组合在一起形成氧代基;或(c)与相邻的碳原子在其末端组合在一起形成环烷基;X是═N—、═C(R4)—或—CH(R4)—的基团;R4是(a)氢原子;(b)氰基;(c)卤素原子;(d)烷基;(e)烯基;(f)环烷基;(g)烷酰基;(h)氨基甲酰基;或(i)环烯基;Ar是可选取代的芳香环基;虚线表示双键的存在或不存在;或其药学上可接受的盐,可作为降压剂等用途。