55559-75-6Relevant academic research and scientific papers
Lipids, lipid compositions, and methods of using them
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Page/Page column 105-106, (2016/05/02)
Disclosed are formulation and optimization protocols for delivery of therapeutically effective amounts of biologically active agents to liver, tumors, and/or other cells or tissues. Also provided are compositions and uses for cationic lipid compounds of formula (I). The invention also relates to compositions and uses for stealth lipids of formula (XI). Also provided are processes for making such compounds, compositions, and formulations, plus methods and uses of such compounds, compositions, and formulations to deliver biologically active agents to cells and/or tissues.
High-selectivity ratio fluorescence probe for detecting periodate radicals
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Paragraph 0085; 0093; 0094; 0095; 0096, (2016/10/27)
The invention provides a high-selectivity ratio fluorescence probe for detecting periodate radicals. The probe has a structure represented by formula I. In the formula I, R1 is selected from H or C1-C4 alkyl groups; R2 is selected from C2-C8 alkyl groups with two adjacent carbon atoms respectively being substituted by one hydroxyl group; R3 is selected from H and C1-C4 alkyl groups; and R4 is selected from H and C1-C4 alkyl groups. The invention also provides an intermediate compound represented by formula II and used for preparing the compound of the formula I, a preparation method of the compound of the formula I, a detection composition containing the compound of the formula I, a detection kit containing the compound of the formula I, and an application of the compound of the formula I in detection of the periodate radicals in a chemical system, fluorescence imaging test of the periodate radicals in biological living cells, construction of high-flux hydrolase test platforms, and exploitation of detection test strips as a fluorescence probe.
Development of Fluorine-18 Labeled Metabolically Activated Tracers for Imaging of Drug Efflux Transporters with Positron Emission Tomography
Sander, Kerstin,Galante, Eva,Gendron, Thibault,Yiannaki, Elena,Patel, Niral,Kalber, Tammy L.,Badar, Adam,Robson, Mathew,Johnson, Sean P.,Bauer, Florian,Mairinger, Severin,Stanek, Johann,Wanek, Thomas,Kuntner, Claudia,Kottke, Tim,Weizel, Lilia,Dickens, David,Erlandsson, Kjell,Hutton, Brian F.,Lythgoe, Mark F.,Stark, Holger,Langer, Oliver,Koepp, Matthias,?rstad, Erik
, p. 6058 - 6080 (2015/08/24)
Increased activity of efflux transporters, e.g., P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), at the blood-brain barrier is a pathological hallmark of many neurological diseases, and the resulting multiple drug resistance represents a major clinical challenge. Noninvasive imaging of transporter activity can help to clarify the underlying mechanisms of drug resistance and facilitate diagnosis, patient stratification, and treatment monitoring. We have developed a metabolically activated radiotracer for functional imaging of P-gp/BCRP activity with positron emission tomography (PET). In preclinical studies, the tracer showed excellent initial brain uptake and clean conversion to the desired metabolite, although at a sluggish rate. Blocking with P-gp/BCRP modulators led to increased levels of brain radioactivity; however, dynamic PET did not show differential clearance rates between treatment and control groups. Our results provide proof-of-concept for development of prodrug tracers for imaging of P-gp/BCRP function in vivo but also highlight some challenges associated with this strategy.
LIPIDS AND LIPID COMPOSITIONS FOR THE DELIVERY OF ACTIVE AGENTS
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Page/Page column 139; 140, (2014/09/29)
This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1–R4, L and X are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
CATIONIC LIPIDS AND USES THEREOF
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Page/Page column 91, (2009/12/02)
Cationic lipids, cationic lipid based drug delivery systems, ways to make them and methods of treating diseases using them are disclosed.
CATIONIC LIPIDS AND USES THEREOF
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Page/Page column 88-89, (2009/12/02)
Cationic lipids, cationic lipid based drug delivery systems, ways to make them and methods of treating diseases using them are disclosed.
CHIRAL CIS-IMIDAZOLINES
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Page/Page column 115, (2009/05/30)
There are provided compounds of Formula (I), or the pharmaceutically acceptable salts thereof, wherein X, Y, Z, V1, V2, R1, R2, R3, R4 and R5 are as herein described, processes for obtaining said compounds and pharmaceutical preparations containing them. These compounds are useful as anticancer agents, in particular as agents in the treatment of solid tumors.
Isolation and synthesis of a novel β-carboline guanidine derivative tiruchanduramine from the Indian ascidian Synoicum macroglossum
Ravinder,Vijender Reddy,Krishnaiah,Ramesh,Ramakrishna,Laatsch,Venkateswarlu
, p. 5475 - 5478 (2007/10/03)
The isolation and synthesis of the racemic form of a novel β-carboline guanidine alkaloid, tiruchanduramine, a potent α-glucosidase inhibitor from the Indian ascidian, Synoicum macroglossum has been achieved.
Open-chain carbocyclic analogs of adenosine with dihalovinyl unit as potential inhibitors of S-adenosyl-L-homocysteine hydrolase
Lewandowska, Elzbieta,Lalama, Jennifer,Yuan, Chong-Sheng,Wnuk, Stanislaw F.
, p. 1747 - 1755 (2007/10/03)
Vinylogously extended deoxyeritadenine derivatives were synthesized as acyclic/carbocyclic analogues of the 6′-halo(homovinyl)adenosines, which are known to be potent inhibitors of S-adenosyl-L-homocysteine hydrolase. Swern oxidation of 9-[3-(t-butyldimet
Synthesis of the eight enantiomerically pure diastereomers of the 12-F2-isoprostanes
Taber, Douglass F.,Xu, Ming,Hartnett, John C.
, p. 13121 - 13126 (2007/10/03)
Syntheses of the eight enantiomerically pure diastereomers of the 12-F2-isoprostanes (4-11) are described. The key steps included rhodium-mediated intramolecular cyclopropanation and enzymatic resolution of the racemic diol 12.
