16024-66-1Relevant articles and documents
BENZODICYCLOALKANE DERIVATIVE, PREPARATION METHOD AND USE THEREOF
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, (2019/06/19)
It is provided herein a benzobicycloalkane derivative, and a preparation method and use thereof. In particular, it is provided herein a compound of Formula (I), or a pharmaceutically acceptable salt, stereoisomer or solvate thereof, a preparation method, and a use thereof in preparation of drugs for treating pain.
Monodisperse oligoethylene glycols modified Propofol prodrugs
Deng, Tao,Mao, Xianglan,Li, Yu,Bo, Shaowei,Yang, Zhigang,Jiang, Zhong-Xing
, p. 3502 - 3505 (2018/10/15)
The low water solubility of Propofol resulted in complicated formulation and adverse effects during its clinical application. To improve its water solubility and maintain its anesthetic effects, Propofol prodrugs with monodisperse oligoethylene glycols as solubility enhancer were designed and synthesized. Monodisperse oligoethylene glycols enable the concise manipulation of water solubility, biocompatibility and anesthetic effects. Through the physicochemical and biological assay, a few water soluble prodrugs of Propofol were identified as promising anesthetic to overcome the drawbacks associated with Propofol.
Preparation and application of monodisperse polyethylene glycol monomethyl ether modified propofol prodrug
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Paragraph 0042; 0043; 0048; 0049, (2018/07/06)
Belonging to the field of organic chemistry and pharmaceutical chemicals, the invention discloses preparation and application of a monodisperse polyethylene glycol monomethyl ether modified propofol prodrug with a novel structure. Monodisperse polyethylene glycol monomethyl ether and propofol can be connected by an in-vivo degradable chemical bond to prepare a series of carbonic ester type and acetic ester type prodrugs respectively. By adjusting the length of the monodisperse polyethylene glycol monomethyl ether chain, the method can synthesize corresponding water-soluble propofol prodrugs, the longer the monodisperse polyethylene glycol monomethyl ether chain is, the better the water solubility is, along with the improvement of the water solubility, the prodrug can be made into aqueous solution preparations so as to avoid the defects of fat emulsion in propofol fat emulsions. The method provided by the invention has the advantages of simple reaction, mild conditions and low cost, andis convenient for industrial production.
ALKYNYL INDAZOLE DERIVATIVE AND USE THEREOF
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Paragraph 0202; 0203; 0204; 0205, (2017/02/24)
The main object of the present invention is to provide a novel compound which has a VEGF receptor tyrosine kinase inhibitory activity and is useful as an active ingredient for the treatment of diseases accompanying angiogenesis or edema, for example, age-related macular degeneration or the like. The present invention includes, for example, an alkynyl indazole derivative represented by the following general formula (I), a pharmaceutical acceptable salt thereof, and a medicine containing thereof.
Gold nanoparticles generated by thermolysis of "all-in-one" gold(i) carboxylate complexes
Tuchscherer,Schaarschmidt,Schulze,Hietschold,Lang
scheme or table, p. 2738 - 2746 (2012/04/10)
Consecutive synthesis methodologies for the preparation of the gold(i) carboxylates [(Ph3P)AuO2CCH2(OCH 2CH2)nOCH3] (n = 0-6) (6a-g) are reported, whereby selective mono-alkylation of diols HO(CH2CH 2O)nH (n = 0-6), Williamson ether synthesis and metal carboxylate (Ag, Au) formation are the key steps. Single crystal X-ray diffraction studies of 6a (n = 0) and 6b (n = 1) were carried out showing that the P-Au-O unit is essentially linear. These compounds were applied in the formation of gold nanoparticles (NP) by a thermally induced decomposition process and hence the addition of any further stabilizing and reducing reagents, respectively, is not required. The ethylene glycol functionalities, providing multiple donating capabilities, are able to stabilise the encapsulated gold colloids. The dependency of concentration, generation time and ethylene glycol chain lengths on the NP size and size distribution is discussed. Characterisation of the gold colloids was performed by TEM, UV/Vis spectroscopy and electron diffraction studies revealing that Au NP are formed with a size of 3.3 (±0.6) to 6.5 (±0.9) nm in p-xylene with a sharp size distribution. Additionally, a decomposition mechanism determined by TG-MS coupling experiments of the gold(i) precursors is reported showing that 1 st decarboxylation occurs followed by the cleavage of the Au-PPh 3 bond and finally release of ethylene glycol fragments to give Au-NP and the appropriate organics. The Royal Society of Chemistry 2012.
Structural requirements for a lipoamino acid in modulating the anticonvulsant activities of systemically active galanin analogues
Zhang, Liuyin,Robertson, Charles R.,Green, Brad R.,Pruess, Timothy H.,White, H. Steve,Bulaj, Grzegorz
experimental part, p. 1310 - 1316 (2009/12/26)
Introduction of lipoamino acid (LAA), Lys-palmitoyl, and cationization into a series of galanin analogues yielded systemically active anticonvulsant compounds. To study the relationship between the LAA structure and anticonvulsant activity, orthogonally p
Poly(ethylene glycol)-based stable isotope labeling reagents for the quantitative analysis of low molecular weight metabolites by LC-MS
Abello, Nicolas,Geurink, Paul P.,Van Der Toorn, Marco,Van Oosterhout, Antoon J. M.,Lugtenburg, Johan,Van Der Marel, Gijs A.,Kerstjens, Huib A. M.,Postma, Dirkje S.,Overkleeft, Hermen S.,Bischoff, Rainer
experimental part, p. 9171 - 9180 (2009/06/20)
Stable isotope labeling (SIL) in combination with liquid chromatography-mass spectrometry is one of the most widely used quantitative analytical methods due to its sensitivity and ability to deal with extremely complex biological samples. However, SIL methods for metabolite analysis are still often limited in terms of multiplexing, the chromatographic properties of the derivatized analytes, or their ionization efficiency. Here we describe a new family of reagents for the SIL of primary amine-containing compounds based on pentafluorophenyl-activated esters of 13C-containing poly(ethylene glycol) chains (PEG) that addresses these shortcomings. A sequential buildup of the PEG chain allowed the introduction of various numbers of 13C atoms opening extended multiplexing possibilities. The PEG derivatives of rather hydrophilic molecules such as amino acids and glutathione were successfully retained on a standard C18 reversed-phase column, and their identification was facilitated based on m/z values and retention times using extracted ion chromatograms. The mass increase due to PEG derivatization moved low molecular weight metabolite signals out of the often noisy, low m/z region of the mass spectra, which resulted in enhanced overall sensitivity and selectivity. Furthermore, elution at increased retention times resulted in efficient electrospray ionization due to the higher acetonitrile content in the mobile phase. The method was successfully applied to the quantification of intracellular amino acids and glutathione in a cellular model of human lung epithelium exposed to cigarette smoke-induced oxidative stress. It was shown that the concentration of most amino acids increased upon exposure of A549 cells to gas-phase cigarette smoke with respect to air control and cigarette smoke extract and that free thiol-containing species (e.g., glutathione) decreased although disulfide bond formation was not increased. These labeling reagents should also prove useful for the labeling of peptides and other compounds containing primary amine functionalities.
Hydrophilic Lipids
Heimann, Ulrich,Voegtle, Fritz
, p. 858 - 862 (2007/10/02)
The new triesters of glycerol 1-8 with different oligoethylene glycol carboxylic acids ("hydrophilic lipids") have been synthesized and their complexation with alkali and alkaline earth metal cations has been investigated.