Thienyl substituted acylguanidines as inhibitors of bone resorption and vitronectin receptor antagonists
申请人:Hoechst Marion Roussel Deutschland GmbH
公开号:EP0960882A1
公开(公告)日:1999-12-01
The present invention relates to thienyl substituted acylguanidine derivatives, such as compounds of the formula I,
in which R1, R2, R4, R6, A, B und D have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of the present invention are valuable pharmaceutical active compounds. They are vitronectin receptor antagonists and inhibitors of bone resorption by osteoclasts and are suitable, for example, for the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. The invention furthermore relates to processes for the preparation of thienyl substituted acylguanidines, their use, in particular as pharmaceutical active ingredients, and pharmaceutical preparations comprising them.
本发明涉及噻吩基取代的酰基胍衍生物,如式 I 的化合物、
其中 R1、R2、R4、R6、A、B 和 D 具有权利要求中所述的含义,它们的生理可耐受盐及其原药。本发明的化合物是有价值的药物活性化合物。它们是维龙素受体拮抗剂和破骨细胞骨吸收抑制剂,适用于治疗和预防至少部分由不希望的骨吸收程度引起的疾病,例如骨质疏松症。本发明还涉及噻吩基取代的酰基胍的制备工艺、其用途(尤其是作为药物活性成分)以及包含它们的药物制剂。