Palladium-Catalyzed Hydride Addition/C–H Bond Activation Cascade: Cycloisomerization of 1,6-Diynes
作者:José F. Rodríguez、Katherine I. Burton、Ivan Franzoni、David A. Petrone、Ina Scheipers、Mark Lautens
DOI:10.1021/acs.orglett.8b03057
日期:2018.11.2
The use of ammonium halide salts as metal hydride precursors in a new Pd-catalyzed cycloisomerization of 1,6-diynes, which affords unexplored silylated 2-azafluorenes, is reported. This cascade process includes the addition of a Pd–hydride species to a π-system, intramolecular carbopalladation, and C(sp2)–H bond activation. A variety of functional groups are tolerated, and the synthetic utility of
Materials and processes for controlled release of thioamide moiety-containing therapeutic agents by linking to thiol-containing polymers
申请人:——
公开号:US20020122785A1
公开(公告)日:2002-09-05
This invention pertains to disulfide-linked conjugates of therapeutic agents containing at least one thioamide group with polymer comprising at least one thiol group, so as to provide a controlled release pharmaceutical composition for administration to animals for the prophylaxis or treatment of various conditions or diseases. The therapeutic agent conjugate may comprise an inactive or weakly active prodrug form which may be converted into the original therapeutic compound by the natural action of reducing agents in vivo. The composition may comprise a mixture of polymers each with a different thioamide-containing agent attached, or a polymer conjugated with a mixture of thioamide-containing agents. Modified properties of the therapeutic compound potentially provided by the polymer itself, as well as by other compounds also appended to the polymer, include but are not limited to greater water solubility, longer in-vivo half-life (due to larger size of the conjugate), slower release from a sustained-release depot (due to larger size of the conjugate), better oral bioavailability and tissue-specific targeting.
The present invention describes a class of dyes for use in staining cell samples and methods of making such dyes. A preferred class of dyes known as detergent dyes which possess the ability to stain cells in whole blood and are only slowly leached or lost from the stained cells over time are described. The present invention has application, for example, to blood typing for the determination of the presence of blood group antigens A, B, AB, O, and D (Rho) and antibodies to such antigens.
Methods, compositions, and systems for delivering therapeutic and diagnostic agents into cells
申请人:GENEVANT SCIENCES GMBH
公开号:US11219634B2
公开(公告)日:2022-01-11
Disclosed are methods for delivering a therapeutic or diagnostic agent to the cytosol of a cell in a subject. The disclosed methods generally include administering to the subject an effective amount of a lipid nanoparticle comprising the therapeutic or diagnostic agent and an effective amount of a membrane-destabilizing polymer. Also disclosed are related compositions and delivery systems.