- Disulfide bond bridged docetaxel-fatty acid prodrugs and self-assembled nanoparticles thereof
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According to the invention, a series of reduction-sensitive disulfide bond bridged docetaxel fatty acid prodrugs are designed and synthesized. The series of prodrugs can be self-assembled into a nano drug delivery system through a one-step nano precipitation method. The nano drug delivery system has the following advantages that: docetaxel is prepared into a disulfide bond connected prodrug, so that the system toxicity of a docetaxel parent drug is reduced, the parent drug can be specifically released in a high reduction environment in tumor cells, and the effects of synergy and toxicity reduction are achieved; the drug loading capacity is high, the use of a solubilizer with higher toxicity is avoided, and the tolerance and the compliance of a patient are expected to be improved; through the one-step nano precipitation method, the preparation process is simple, and large-scale production is easy; the nanoparticles are small and uniform in particle size and are easily enriched at a tumor part through an EPR effect; and surface modification is easy, and removal of a reticuloendothelial system can be slowed down through modification of PEG modification.
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Paragraph 0031-0032
(2021/04/07)
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- DRUG DELIVERY SYSTEM INCLUDING DRUG-LOADED PHOSPHATE MICELLE
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The present invention relates to a drug carrier comprising a drug and a carrier loaded with the drug, wherein the carrier is a micelle composed of a phosphate surfactant. The micelle, consisting of the phosphate surfactant contained in a drug carrier, can selectively release the drug loaded into the micelle by being cleaved by an overexpressed enzyme around a target, thereby significantly reducing drug side effects in vivo compared to the prior art, while maximizing a therapeutic effect.COPYRIGHT KIPO 2020
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Paragraph 0037-0041
(2019/12/25)
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- PARTICLE INCLUDING UCNPs-LOADED PHOSPHATE MICELLE AND BEING USED FOR BIOIMAGING
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The present invention relates to particles for bioimaging, comprising up-conversion fluorescent nanoparticles and a carrier loaded with the up-conversion fluorescent nanoparticles, wherein the carrier is a micelle formed by a phosphate surfactant. According to the present invention, the particles for bioimaging are capable of releasing up-conversion nanoparticles (UCNP) in a specific location in vivo, thereby being capable of delivering the UCNP in a low concentration, and thus can significantly reduce adverse side effects in vivo; can improve dispersibility in vivo; and can have high selectivity to specific cells such as prostate cancer cells. Thus, the particles for bioimaging may be beneficially used as a marker substance for bioimaging.(AA) Phospholipase A_2(BB) UCNP-loaded micelle(CC) PEGylated ethylene glycol phosphate(DD) Stearic acid(EE) Upconversion nanoparticles (UCNPs)(FF) Extracellular space(GG) Cell membrane(HH) Intracellular spaceCOPYRIGHT KIPO 2018
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Paragraph 0044-0045
(2018/09/12)
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- Esterification of free fatty acids (Biodiesel) using nano sulfated-titania as catalyst in solvent-free conditions
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Nano sulfated titania was tested as catalyst for esterification of free fatty acids, specially methanolic and ethanolic esterification of stearic acid (biodiesels). Factorial design evidenced a positive effect of reaction temperature, amount of catalyst, and solvents on ester conversion. This nano-sized sulfated titania has been prepared by a sol-gel hydrothermal process. This prepared sulfated titania showed high catalytic activity in direct esterification of fatty acids as well as benzoic acids with various alcohols and phenols under solvent-free conditions. This method is of great value because of its environmentally benign character, easy handling, high yields, convenient operation, and green. FT-IR studies are shown that the catalyst can be reused for acylation without loss of catalytic activity.
- Hosseini-Sarvari, Mona,Sodagar, Esmat
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p. 229 - 238
(2013/05/09)
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- Rapid transesterification of aliphatic and aromatic esters using sodium bis(ethylenedioxy)borate-a mild catalyst
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A simple, selective transesterification of aliphatic and aromatic esters using a mild base sodium bis(ethylenedioxy)borate is described. The transesterification reactions were performed both in microwave and ultrasonication. Aromatic compounds forms diesters of ethylene glycol while aliphatic compounds forms only monoesters. The IR, MS and NMR characterization are given. In this work, an environmentally benign process for the production of biodiesel from oils using heterogeneous catalyst was developed. Mild borate catalyst was adopted for the production of biodiesel. A study for optimizing the reaction conditions such as the reaction time, the reaction condition, the use of co-solvent and the amount of catalyst, was performed.
- Ramasubramanian,Gopi, Sreeraj,Matharasi, D. Priya,Narasimhan
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experimental part
p. 3660 - 3662
(2012/01/30)
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- Synthesis and evaluation of lysophosphatidylserine analogues as inducers of mast cell degranulation. Potent activities of lysophosphatidylthreonine and its 2-deoxy derivative
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In response to various exogenous stimuli, mast cells (MCs) release a wide variety of inflammatory mediators stored in their cytoplasmic granules and this release initiates subsequent allergic reactions. Lysophosphatidylserine (lysoPS) has been known as an exogenous inducer to potentiate histamine release from MCs, though even at submicromolar concentrations. In this study, through SAR studies on lysoPS against MC degranulation, we identified lysoPT, a threonine-containing lysophospholipid and its 2-deoxy derivative as novel strong agonists. LysoPT and its 2-deoxy derivative induced histamine release from MCs both in vitro and in vivo at a concentration less than one-tenth that of lysoPS. Notably, lysoPT did not activate a recently proposed lysoPS receptor on MCs, GPR34, demonstrating the presence of another undefined receptor reactive to both lysoPS and lysoPT that is involved in MC degranulation. Thus, the present strong agonists, lysoPT and its 2-deoxy derivative, will be useful tools to understand the mechanisms of lysoPS-induced activation of degranulation of MCs. 2009 American Chemical Society.
- Iwashita, Masazumi,Makide, Kumiko,Nonomura, Taro,Misumi, Yoshimasa,Otani, Yuko,Ishida, Mayuko,Taguchi, Ryo,Tsujimoto, Masafumi,Aoki, Junken,Arai, Hiroyuki,Ohwada, Tomohiko
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experimental part
p. 5837 - 5863
(2010/03/24)
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- Combinatorial synthesis of PEG oligomer libraries
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A simple chain-extending approach was established for the scale-up of the monoprotected monodisperse PEG diol materials. Reactions of THP-(OCH2CH2)n—OMs (n=4, 8, 12) with a large excess of commercially available H—(OCH2CH2)n—OH (n=1-4) under basic conditions led to THP-(OCH2CH2)n—OH (n=5-15). Similarly, Me-(OCH2CH2)n—OH (n=4-11, 13) were prepared from Me-(OCH2CH2)n—OMs (n=3, 7, 11). For the chain elongation steps, 40-80% yields were achieved through extraction purification. PEG oligomer libraries I and II were generated in 50-95% overall yields by alkylation or acylation of THP-(OCH2CH2)n—OH (n=1-15) followed by deprotection. Alkylation of Me-(OCH2CH2)n—OH (n=1-11, 13) with X—(CH2)m—CO2R (X=Br or OMs) and subsequent hydrolysis led to PEG oligomer library III in 30-60% overall yields. Combinatorial purification techniques were adapted to the larger-scale library synthesis. A total of 498 compounds, each with a weight of 2-5 g and a minimum purity of 90%, were synthesized.
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Page/Page column 11
(2010/02/15)
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- SYNTHETIC MOLECULES HAVING IMMUNE ACTIVITY
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The present invention is directed to synthetic molecules having biological activity similar to PIM (acyl glycerol phosphatidylinositol manno-oligosaccharide) activity, for use in the treatment and prevention of inflammatory or immune cell mediated diseases or disorders.
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Page/Page column 61
(2010/02/12)
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- Al2O3/MeSO3H (AMA) as a new reagent with high selective ability for monoesterification of diols
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A new facile method for monoesterification of diols has been developed. A variety of diols, in particular oligoethylene glycols, were selectively monoesterified in excellent yields by reaction with aromatic and aliphatic acids in the presence of Al2O3/MeSO3H as a new reagent without use of any solvents.
- Sharghi, Hashem,Sarvari, Mona Hosseini
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p. 3627 - 3633
(2007/10/03)
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- Compositions of iodophenoxy alkanes and iodophenyl ethers in combination with cellulose derivatives for visualization of the gastrointestinal tract
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Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising an iodophenoxy alkane, iodophenyl alkenylalkyl ether or an iodophenyl alkynylalkyl ether x-ray producing agent in combination with a cellulose derivative in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
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- Compositions of iodobenzoic acid derivatives and pharmaceutically acceptable clays for visualization of the gastrointestinal tract
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Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising iodobenzoic acid derivatives as the x-ray producing agents in combination with a pharmaceutically acceptable clay in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
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- Compositions of iodophenoxy alkanes and iodophenyl ethers and pharmaceutically acceptable clays for visualization of the gastrointestinal tract
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Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising iodophenoxy alkanes and iodophenyl ethers as the x-ray producing agents in combination with a pharmaceutically acceptable clay in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
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- Compositions of iodoaniline derivatives and cellulose derivatives for visualization of the gastrointestinal tract
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Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising an x-ray producing agent of the formula or a pharmaceutically acceptable salt thereof STR1 and methods for their use in diagnostic radiology of the gastrointestinal tract, wherein Z is H, halo, C1 -C20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups; R1 and R2 are independently H, C1 -C25 alkyl, cycloalkyl, acetyl or halo-lower-alkyl, wherein said C1 -C25 alkyl, cycloalkyl and halo lower-alkyl are optionally substituted with fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy and said acetyl is optionally substituted with fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy; n is 1-4; y is 1-4; and x is 1 or 2 in a pharmaceutically acceptable carrier comprising a cellulose derivative.
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- X-ray contrast compositions containing iodophenoxyalkanes and cellulose derivatives
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Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a nonionic x-ray producing agent in combination with a cellulose derivative in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
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- X-ray contrast compositions containing film-forming materials
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Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material capable of forming a coating on the gastrointestinal tract and a nonionic x-ray producing agent in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
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- Compositions of alkylbenzenes and cellulose derivatives for visualization of the gastrointestinal tract
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Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising an x-ray producing agent of the formula or a pharmaceutically acceptable salt thereof STR1 wherein R is methyl, ethyl, n-propyl, C4 -C25 alkyl, cycloalkyl, unsaturated allyl or halo-lower-alkyl, each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl; (CR1 R2)p --(CR3 =CR4)m Q, or (CR1 R2)p --C C--Q; R1, R2, R3 and R4 are independently H, lower-alkyl, optionally substituted with halo; n is 2-5; m is 2-5; p is 1-10; and Q is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl; in a pharmaceutically acceptable carrier comprising a cellulose derivative.
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- Compositions of iodophenyl esters and iodophenyl sulfonates and cellulose derivatives for visualization of the gastrointestinal tract
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Disclosed are contrast agents of the formula STR1 wherein STR2 Z is H, halo, C5 -C20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups; R is C1 -C25 alkyl, cycloalkyl, aryl or halo-lower-alkyl, each of which may be optionally substituted with lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl, lower-alkenyl, lower-alkynyl, lower-alkylene or lower-alkoxy-carbonyloxy; n is 1-5; y is 0-4; and w is 1-4; in a pharmaceutically acceptable carrier comprising a cellulose derivative.
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- Compositions of iodophenoxy alkylene ethers and cellulose derivatives for visualization of the gastrointestinal tract
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Disclosed are contrast agents of the formula STR1 wherein Z is H, halo, C1 -C20 alkyl, cycloalkyl, lower alkoxy, alkoxycarbonyl, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups; R is C1 -C25 alkyl, cycloalkyl, STR2 or halo-lower-alkyl; each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy; R1, R2, R3 and R4 are independently H or lower-alkyl, optionally substituted with halo; x is 1-4; n is 1-4; m is 1-15; p is 1-20; and Q is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl; in an aqueous, pharmaceutically acceptable carrier comprising a cellulose derivative.
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- X-ray contrast compositions containing iodophenoxyalkanes and pharmaceutically acceptable clays
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Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a nonionic x-ray producing agent in combination with a pharmaceutically acceptable clay in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
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- Compositions of alkylbenzenes for visualization of the gastrointestinal tract using X-ray contrast
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Disclosed are contrast agents of the formula STR1 contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract wherein R=C1 -C25 alkyl, cycloalkyl, unsaturated allyl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CR1 R2)p --(CR3 =CR4)m Q, or (CR1 R2)p --C C--Q; R1, R2, R3 and R4 are independently H, lower-alkyl, optionally substituted with halo; n is 1-5; m is 1-5; p is 1-10; and Q is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl.
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- Polymeric x-ray contrast compositions containing an organic crystalline x-ray contrast agent
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Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material in combination with a divalent cation capable of forming a coating on the gastrointestinal tract and a crystalline contrast agent in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
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- Polymeric X-ray compositions containing iodinated polymeric beads
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Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material in combination with a divalent cation capable of forming a coating on the gastrointestinal tract and iodinated polymeric, water-insoluble beads having a particle size of from about 0.01 to about 1000μ wherein said iodinated polymeric beads comprise a polymer containing repeating units of the formula (I) STR1 wherein A is a repeating organic unit in the backbone chain of the polymer; and X is an organic moiety containing or iodinated eromatic group and a hydrophilic group, said moiety having an iodine content within the range of from about 40 to about 80 weight percent based or the molecular weight of X, in a pharmaceutically acceptable carrier.
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- X-ray contrast compositions containing an organic crystalline X-ray contrast agent in combination with pharmaceutically acceptable clays
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Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a crystalline organic constrast agent in combination with a pharmaceutically acceptable clay in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
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- Compositions of alkylbenzenes in film-forming materials for visualization of the gastrointestinal tract
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Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material capable of forming a coating on the gastrointestinal tract and an x-ray producing agent of the formula STR1 and methods for their use in diagnostic radiology of the gastrointestinal tract wherein R=C1 -C25 alkyl, cycloalkyl, unsaturated allyl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CR1 R2)p --(CR3 =CR4)m Q, or (CR1 R2)p --C C--Q; R1, R2, R3 and R4 are independently H, lower-alkyl, optionally substituted with halo; n is 1-5; m is 1-5; p is 1-10; and Q is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl.
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- X-ray contrast compositions comprising alkoxyphenols
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Disclosed are aqueous compositions containing a contrast agent of the formula STR1 and methods for their use in diagnostic radiology of the gastrointestinal tract, wherein R is a substituted or unsubstituted alkyl group containing from 2 to 8 carbon atoms, wherein said substituents are selected from the group consisting of C1 -C6 alkyl, hydroxy and alkoxy; and n is 1 to 5.
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