Substituted pyridines as inhibitors of dipeptidyl peptidase IV and their application for the treatment of diabetes and related diseases
申请人:EMC microcollections GmbH
公开号:EP2308847A1
公开(公告)日:2011-04-13
The present invention relates to novel 2-aryl and 4-aryl substituted pyridines, which are highly selective and potent inhibitors of the dipeptidyl peptidase IV enzyme, and which are useful in the treatment and prevention of multiple diseases and disorders mediated by dipeptidyl peptidase IV, such as diabetes, particularly type II diabetes. The invention also relates to procedures for synthesis of such compounds and pharmaceutical compositions thereof.
In view of the rapid increase of diabetes there is a considerable demand for the development of new agents in this field. There is particularly a need for agents with superior efficacy, high selectivity, long duration of action, better bioavailability, and physiological compatibility, which supplement the conventional therapies.
The provided compounds are usable as really effective agents, exhibiting precious pharmacological properties as well as an excellent safety profile, for treatment and prophylaxis of diseases mediated by dipeptidyl peptidase IV, such as diabetes, particularly type II diabetes and related diseases.
本发明涉及新型 2-芳基和 4-芳基取代的吡啶,它们是二肽基肽酶 IV 酶的高选择性强效抑制剂,可用于治疗和预防二肽基肽酶 IV 介导的多种疾病和紊乱,如糖尿病,特别是 II 型糖尿病。本发明还涉及合成此类化合物及其药物组合物的程序。
鉴于糖尿病发病率的快速增长,该领域对新制剂的开发有相当大的需求。尤其需要疗效好、选择性高、作用时间长、生物利用度高、生理相容性好的药物,以补充传统疗法的不足。
所提供的化合物是真正有效的药物,具有珍贵的药理特性和出色的安全性,可用于治疗和预防由二肽基肽酶 IV 介导的疾病,如糖尿病,特别是 II 型糖尿病和相关疾病。
Ag/CdS Nanocomposite: An Efficient Recyclable Catalyst for the Synthesis of Novel 8-Aryl-8H-[1,3]dioxolo[4,5-g]chromene-6-carboxylic Acids under Mild Reaction Conditions
作者:Shahrzad Abdolmohammadi、Seyed Reza Rasouli Nasrabadi、Ahmad Seif、Narges Elmi Fard
DOI:10.2174/1386207321666180604104456
日期:2018.7.20
properties. The effectiveness of catalytic activity of CdS NPs can be improved due to the combined effect of Ag particles. RESULTS Ag/CdS nanocomposite is a readily available, recyclable, and non-toxic catalystused for the highly efficientsynthesis of novel 8-aryl-8H-[1,3]dioxolo[4,5-g]chromrne-6-carboxylic acids. This reaction is conveniently performed under mild reaction conditions. All synthesized compounds