发明名称 |
Conformationally constrained, fully synthetic macrocyclic compounds |
摘要 |
<p>The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1 ) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.</p> |
申请公布号 |
AU2013234499(A1) |
申请公布日期 |
2014.10.09 |
申请号 |
AU20130234499 |
申请日期 |
2013.03.15 |
申请人 |
POLYPHOR AG |
发明人 |
OBRECHT, DANIEL;ERMERT, PHILIPP;OUMOUCH, SAID;PIETTRE, ARNAUD;GOSALBES, JEAN-FRANCOIS;THOMMEN, MARC |
分类号 |
C07D273/02;A61K31/395;A61P31/04;C07D291/08;C07D498/04;C07D498/18;C07D515/06;C07D515/18;C07D515/22 |
主分类号 |
C07D273/02 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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