申请人:Sasaki Satoshi
公开号:US20090156646A1
公开(公告)日:2009-06-18
The present invention provides a compound which has metastin receptor antagonist activity and is useful for preventing and treating hormone-dependent cancer, benign prostatomegaly, endometriosis, precocious puberty, uterine myoma or the like. More specifically, the present invention provides a compound, represented by the formula:
or a salt thereof, a prodrug thereof, and a pharmaceutical agent containing the same; wherein Ring A represents a 5- to 8-membered homocyclic or heterocyclic group optionally having a substituent other than formula —X-R
1
wherein X represents a bond or a spacer, and R
1
represents optionally substituted amino or an optionally substituted nitrogen-containing heterocyclic group; Ring B represents an optionally substituted benzene ring; R
2
represents an optionally substituted homocyclic or heterocyclic group; and R
3
and R
4
independently represent a hydrogen atom, cyano, acyl or an optionally substituted hydrocarbon group.
本发明提供了一种具有转移素受体拮抗活性的化合物,可用于预防和治疗激素依赖性癌症、良性前列腺增生、子宫内膜异位症、早熟、子宫肌瘤等。更具体地,本发明提供了一种化合物,其表示为以下公式:或其盐、前药及含有该化合物的药物制剂;其中环A表示一个5-至8-成员的同环或异环族群,可选地具有除公式—X-R1以外的取代基,其中X表示键或空间组分,而R1表示可选地取代的氨基或可选地取代的含氮杂环族群;环B表示可选地取代的苯环;R2表示可选地取代的同环或异环族群;而R3和R4独立地表示氢原子、氰基、酰基或可选地取代的碳氢基团。