16024-60-5Relevant academic research and scientific papers
Effect of Oligoethylene Chains on the Formation of Photoresponsive Nanotubes by Azobenzene Dyad
Saito, Takuho,Yagai, Shiki
, p. 2475 - 2478 (2020)
Azobenzene dyad 1 possessing hydrophobic side chains has previously been reported to assemble into toroidal nanostructures, which can further stack to afford nanotubes in nonpolar media. In this study, amphiphilic dyad 2 was synthesized to obtain nanotubes with the hydrophilic interior. Dyad 2 directly assembled into nanotubes without forming isolatable toroidal nanostructures. UV light irradiation to the nanotubes resulted in monomerization by trans→cis photoisomerization, but following reconstruction by visible light irradiation afforded amorphous films, suggesting a kinetic trap of trans-2 by residual cis-2 through co-aggregation.
Poly(oligo(ethylene glycol) vinyl acetate)s: A Versatile Class of Thermoresponsive and Biocompatible Polymers
Hedir, Guillaume G.,Arno, Maria C.,Langlais, Marvin,Husband, Jonathan T.,O'Reilly, Rachel K.,Dove, Andrew P.
, p. 9178 - 9182 (2017)
Polymers with a thermally triggered phase transition are important in the design of materials for biological applications, where their behavior can be used to trigger release or (dis)assembly events. Despite their advantages, a system with tunable thermal response, end-group reactive sites, low toxicity, and controlled main-chain degradability has not been realized, yet this would be a significant advance. The versatile new poly(oligo(ethylene glycol) vinyl acetate)s are presented with excellent control over their molecular properties obtained through RAFT/MADIX polymerization. Furthermore, we demonstrate structure-controlled thermal transitions, conjugation to human lysozyme through the retained end-group, and moreover show that this class of polymers can uniquely be copolymerized with 2-methylene-1,3-dioxepane (MDO) to generate polymers in which the degradability and cloud point can be independently tuned to create materials that display the same cloud point but degrade differently.
NOVEL TRITERPENE DERIVATIVES AS HIV INHIBITORS
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Page/Page column 54-55, (2020/08/28)
The present invention relates to novel triterpene derivatives of formula (I); and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and ring are as defined herein. The invention also relates to novel triterpene derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases.
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.
A CONJUGATE OF A TUBULYSIN ANALOG WITH BRANCHED LINKERS
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, (2019/07/17)
The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.
ARYL HYDROCARBON RECEPTOR MODULATOR
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Paragraph 0053-0054, (2019/10/20)
Disclosed is an aryl hydrocarbon receptor modulator of formula (I), and a pharmaceutically acceptable salt thereof, wherein R′ is H, CN, CH2(OH)R0, CmH2m+1, CnH2n-1, CnH2n-3, two Ra are independently H or two Ra together form ═O or ═N—W3—R1; A is a C6 to C10 aromatic ring unsubstituted or substituted with 1 to 3 R, or a C2-C10 heteroaromatic ring interrupted by 1 to 5 heteroatoms selected from N, O, and S or a 4 to 7 membered nonaromatic heterocyclic ring containing C═N and interrupted by 1 to 3 heteroatoms selected from N, O, and S, with either one unsubstituted or substituted with 1 to 3 R; Q is R, or is a C6 to C10 aromatic ring or a C2 to C10 heteroaromatic ring unsubstituted or substituted with 1 to 3 R and interrupted by 1 to 5 heteroatoms selected from N, O, and S; and R is Rc which is C-attached or RN which is N-attached. The compounds of formula (I) of the present invention can regulate AhR activity, and can be used to inhibit the growth of cancer cells and inhibit the metastasis and invasion of tumor cells.
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; 0046; 0047, (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.
Phenothiazine derivatives and methods of use thereof
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Page/Page column 45, (2017/08/01)
The present disclosure relates to phenothiazine derivatives such as conjugates of phenothiazine compounds, as well as pharmaceutical compositions thereof. The present disclosure also relates to a method of making and the use of such compounds for treating cancer, e.g., a lung cancer, a colon cancer, breast cancer or pancreatic cancer.
ALKYNYL INDAZOLE DERIVATIVE AND USE THEREOF
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Paragraph 0202; 0203, (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.
