AT1 antagonists: a patent review (2008-2012)

被引:18
作者
Mavromoustakos, Thomas [1 ]
Agelis, George [2 ,3 ]
Durdagi, Serdar [4 ]
机构
[1] Univ Athens, Dept Chem, Athens 15771, Greece
[2] Univ Patras, Dept Chem, Patras 26500, Greece
[3] Eldrug SA, Platani 26504, Rio Patras, Greece
[4] Bahcesehir Univ, Fac Med, Dept Biophys, Istanbul, Turkey
关键词
angiotensin II; AT1; receptor; RAS system; sartans; ANGIOTENSIN-ALDOSTERONE SYSTEM; IN-SILICO DOCKING; BIOLOGICAL EVALUATION; MOLECULAR-DYNAMICS; RECEPTOR BLOCKERS; RENIN INHIBITORS; VALSARTAN; BLOCKADE;
D O I
10.1517/13543776.2013.830104
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Introduction: For two decades a class of pharmaceutical molecules with proved beneficial therapeutic properties, especially in hypertension, has been introduced in the market aiming to specifically prevent the detrimental effects of the peptide hormone Angiotensin II at the AT1 receptor. The prototype of this class was losartan and based on its structure, several drugs were launched and also called 'Sartans'. New structural features on these molecules can provide multi-target properties in the RAS or other systems. New methodologies were developed for the treatment of hypertension utilizing either AT1 antagonists alone or as cocktails. Areas covered: In this review article, authors aim to cover information provided by patents of the years 2008 - 2012. The rationale of writing this review article is to cover the most important patents which can forward the field with new important discoveries. Expert opinion: From the patent investigation it is clear that new areas on the subject are still offered for new discoveries. New structural features can be still considered in the synthetic compounds that can advance the knowledge and beneficial effects on diseases related to Angiotensin II and AT1 receptor. There is era also for new formulations (i.e., cyclodextrins, polymers and liposomes). The multitarget approach can be further strengthened and more combinations can be sought in the rational drug design for seeking cocktails. Furthermore, the revealing of the complexity of the RAS offers new avenues for novel targets and this must not be overlooked.
引用
收藏
页码:1483 / 1494
页数:12
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