[EN] SOLUBLE GUANYLATE CYCLASE ACTIVATORS<br/>[FR] ACTIVATEURS SOLUBLES DE GUANYLATE CYCLASE
申请人:MERCK SHARP & DOHME
公开号:WO2015088886A1
公开(公告)日:2015-06-18
A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (" cGMP") and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceuticall acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula I or a pharmaceutically acceptable salt thereof.
Novel angiotensin-II receptor antagonists are disclosed having the general formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, W and X are as defined herein.
pH-Driven Mechanistic Switching from Electron Transfer to Energy Transfer between [Ru(bpy)<sub>3</sub>]<sup>2+</sup> and Ferrocene Derivatives
作者:Claire Drolen、Eric Conklin、Stephen J. Hetterich、Aditi Krishnamurthy、Gabriel A. Andrade、John L. Dimeglio、Maxwell I. Martin、Linh K. Tran、Glenn P. A. Yap、Joel Rosenthal、Elizabeth R. Young
DOI:10.1021/jacs.8b03933
日期:2018.8.15
[Ru(bpy)3]2+ (bpy = 2,2'-bipyridine) may be deactivated via energy transfer or electron transfer with ferrocene derivatives in aqueous conditions. Stern-Volmer quenching analysis revealed that the rate constant for [Ru(bpy)3]2+ excited-state quenching depends on solution pH when a ferrocenyl-amidinium derivative (Fc-am) containing a proton-responsive functionality tethered to the ferrocene center was
소포체에서 리소좀으로 소포 수송의 영상화를 위한 아미딘 유래 이광자 형광 프로브 및 이의 영상화 방법
申请人:AJOU UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION 아주대학교산학협력단(220040257423) BRN ▼124-82-14602
公开号:KR101906956B1
公开(公告)日:2018-10-11
본 발명은 살아있는 세포 내 소포체(endoplasmic reticulum; ER)에서 리소좀(lysosome)으로의 소포 수송을 관찰하기 위한 아미딘(amidine) 유래 소분자인 이광자 형광 프로브(ELP1)에 관한 것으로, 상기 이광자 형광 프로브는 초기에 소포체에 국한되어 있다가 소포 수송을 통해 리소좀 구획으로 전달되며, 강한 이광자 능력, 우수한 수용성, pH 독립성, 낮은 세포 독성 및 높은 세포 로딩 능력을 가짐으로써, 소포 수송 관련 생물학 및 세포 병리학을 실시간으로 연구할 수 있는 효과적인 도구로 유용하게 활용될 수 있다.
This invention relates to an amidine-derived small molecule fluorescent probe (ELP1) for observing the transport of vesicles from the endoplasmic reticulum (ER) to lysosomes within living cells. The fluorescent probe initially localizes to the vesicles within the ER and is then transported to the lysosomal compartment through vesicle transport. With strong fluorescence capability, excellent solubility, pH-independence, low cell toxicity, and high cell loading capacity, this fluorescent probe can be effectively utilized as a useful tool for real-time research in vesicle transport-related biology and cell pathology.
Digitoxigenin and dihydrodigitoxigenin 3.beta.-derivatives and
Digitoxigenin and dihydrodigitoxigenin 3.beta.-derivatives, a process for their preparation and pharmaceutical compositions containing same for the treatment of cardiovascular disorders such as heart failure and hypertension are disclosed.