INTRACELLULAR SUBSTANCE TRANSPORT SYSTEM AND USE THEREOF
申请人:National University Corporation Hokkaido University
公开号:US20200138973A1
公开(公告)日:2020-05-07
The present invention pertains to a complex including nanoparticles and, carried on the surface of the nanoparticles, a lysosomal enzyme inhibitor or kinase inhibitor shown by general formula (A) and a phospholipid mimetic substance shown by general formula (B).
In general formula (A), n1 is an integer of 2-30, n2 is an integer of 2-30, the -S- terminal is a nanoparticle-carrying site, and R10 is a suicide substrate site or a kinase inhibition site. In general formula (B), n3 is an integer in the range of 2-30, and the -S- terminal is a nanoparticle-carrying site. The present invention provides a versatile system capable of efficiently delivering a drug to endolysosomes and allowing the drug to function at a low concentration on lysosomal enzymes, and an anticancer agent in which this system is used.
USES OF SESQUITERPENE LACTONE COMPOUNDS AND THEIR DERIVATIVES IN DRUGS PREPARATION
申请人:ACCENDATECH
公开号:US20160367525A1
公开(公告)日:2016-12-22
The present invention relates to the uses of sesquiterpene lactone compounds and their derivatives in preparing drugs. It belongs to the field of drug technology, specifically relates to the uses of the compounds of Formula (I) in preparing the drugs, especially the uses in preparing the drugs to treat rheumatoid arthritis and treat cancers through inhibiting cancer stem cells.
Synthesis of Pyrrolidines by a Csp
<sup>3</sup>
‐Csp
<sup>3</sup>
/Csp
<sup>3</sup>
‐
<i>N</i>
Transition‐Metal‐Free Domino Reaction of Boronic Acids with γ‐Azido‐
<i>N</i>
‐Tosylhydrazones
The reactionbetween γ‐azido‐N‐tosylhydrazones and boronic acids leads to the obtention of 2,2‐disubstituted pyrrolidines in a domino process that includes 1) diazoalkane formation, 2) intermolecular carboborylation of the diazocompound, and 3) intramolecular carborylation of the azide, and comprises the formation of a Csp3−Csp3 and a Csp3−N bonds on the same carbon atom. The reaction proceeds without
[EN] INSULIN RECEPTOR PARTIAL AGONISTS AND GLP-1 ANALOGUES<br/>[FR] AGONISTES PARTIELS DU RÉCEPTEUR DE L'INSULINE ET ANALOGUES DU GLP-1
申请人:MERCK SHARP & DOHME
公开号:WO2017205191A1
公开(公告)日:2017-11-30
The present invention provides compositions comprising insulin receptor partial agonists in association with GLP-1 analogues (e.g., liraglutide) as well as methods for using the compositions for example, to treat or prevent diabetes or to decrease body weight.
In Situ Generation and Intramolecular Schmidt Reaction of Keto Azides in a Microwave-Assisted Flow Format
作者:Thomas O. Painter、Paul D. Thornton、Mario Orestano、Conrad Santini、Michael G. Organ、Jeffrey Aubé
DOI:10.1002/chem.201100768
日期:2011.8.22
Go with the flow! A method for conversion of keto halides to lactams by means of sequential azidation and intramolecularSchmidtreaction in a combined flowformat is described (see scheme; MWI=microwave irradiation, TFA=trifluoroacetic acid).