Siosomal formulation for intracellular delivery and targeting of therapeutic agents
申请人:Salama, Zoser B.
公开号:EP2384743A1
公开(公告)日:2011-11-09
The invention relates to a carrier and targeting system for the intracellular delivery and triggered release of a siosome- and/or siosome-liposome-entrapped or encapsulated active substance or therapeutic agent. The invention further relates to the targeted release and delivery of doxorubicin, cis-platin, carbo-platin and/or oxali-platin, characterized in that one or more anionic lipids, such as cholesteryl hemisuccinate residues, cardiolipin and/or their derivatives and/or other anionic groups, are covalently linked to the silicone central atom of the silanes, sugar silanes and/or amino-sugar silanes. The invention further relates to the use of cationic lipids that are covalently attached to the silicone central atom of the silanes. The invention also relates to a method for preparing such carrier and targeting systems and methods for their administration.
Radical Decarboxylation/Annulation of Acrylamides with Aliphatic Acyl Peroxides
作者:Changduo Pan、Yu Fu、Qingting Ni、Jin-Tao Yu
DOI:10.1021/acs.joc.7b00663
日期:2017.5.5
A radical decarboxylation/annulation of acrylamides with aliphatic acyl peroxides was developed, giving a series of linear alkylated oxindoles in moderate to good yields. The reaction used aliphatic acyl peroxides as the linear alkyl radical source and tolerated a broad scope of substrates under metal-free conditions, offering a simple and efficient approach toward alkylated oxindoles.
Synthetic analogs having the activity of naturally occurring forms of
申请人:——
公开号:US03974187A1
公开(公告)日:1976-08-10
Synthetic 2,3-dimethoxy-5-methyl-1,4-benzoquinone is converted into a series of new 6-alkyl derivatives. These 6-alkyl derivatives have straight carbon chains which are both saturated and unsaturated. The unsaturated derivatives contain one, two, three and four double bonds. These new synthetic quinones are analogs of the naturally occurring forms of coenzyme Q and have the same fundamental electron-transfer capacity of the natural forms of coenzyme Q. Although the degree of the activity of these new synthetic analogs differ, some of these new synthetic analogs are effective substitutes for the natural forms of coenzyme Q.
Ultrasonic visualisation of a subject, particularly of perfusion in the myocardium and other tissues, is performed using novel gas-containing contrast agent preparations which promote controllable and temporary growth of the gas phase in vivo following administration and can therefore act as deposited perfusion tracers. The preparations comprise an injectable aqueous medium comprising dispersed gas and an injectable oil-in-water emulsion in which the oil phase comprises a diffusible component capable of diffusion in vivo into the dispersed gas to promote temporary growth thereof, such that material present at the surfaces of the dispersed gas phase and material present at the surfaces of the dispersed oil phase have affinity for each other, e.g. as a result of having opposite charges. In cardiac perfusion imaging the preparations may advantageously be coadministered with vasodilator drugs such as adenosine in order to enhance the differences between return signal intensity from normal and hypoperfused myocardial tissue respectively.