- THIAZOLOPIPERAZINE DERIVATIVES AND COMPOSITION FOR PREVENTING OR TREATING AUTOIMMUNE DISEASES COMPRISING THE SAME
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The present invention provides a thiazolopiperazine derivative, and a pharmaceutical composition and a health functional food composition for preventing or treating autoimmune diseases containing the same as an active component. A compound represented by chemical formula 1 or a pharmaceutically acceptable salt thereof according to the present invention can have an effect of inhibiting lysophosphatidic acid 1 (LPA1) receptor activation, thereby being able to be usefully used as the pharmaceutical composition or the health functional food composition for preventing or treating LPA1-related diseases. In addition, it is possible to effectively prevent or treat not only autoimmune diseases, but also other immune-related diseases with similar mechanisms of occurrence by using the pharmaceutical composition and the health functional food composition.COPYRIGHT KIPO 2020
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Paragraph 0118-0126
(2020/04/01)
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- Green synthesis of biphenyl carboxylic acids via Suzuki–Miyaura cross-coupling catalyzed by a water-soluble fullerene-supported PdCl2 nanocatalyst
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A green synthesis of variously substituted biphenyl carboxylic acids was achieved through Suzuki–Miyaura cross-coupling of a bromobenzoic acid with an aryl boronic acid using a water-soluble fullerene-supported PdCl2 nanocatalyst (C60-TEGs/ PdCl2). Yields of more than 90% were obtained at room temperature in 4 h using 0.05 mol% catalyst and 2 equiv. K2CO3.
- Liu, Wanyun,Zhou, Xiuming,Huo, Ping,Li, Jingbo,Mei, Guangquan
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- Visible-Light-Driven External-Reductant-Free Cross-Electrophile Couplings of Tetraalkyl Ammonium Salts
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Cross-electrophile couplings between two electrophiles are powerful and economic methods to generate C-C bonds in the presence of stoichiometric external reductants. Herein, we report a novel strategy to realize the first external-reductant-free cross-electrophile coupling via visible-light photoredox catalysis. A variety of tetraalkyl ammonium salts, bearing primary, secondary, and tertiary C-N bonds, undergo selective couplings with aldehydes/ketone and CO2. Notably, the in situ generated byproduct, trimethylamine, is efficiently utilized as the electron donor. Moreover, this protocol exhibits mild reaction conditions, low catalyst loading, broad substrate scope, good functional group tolerance, and facile scalability. Mechanistic studies indicate that benzyl radicals and anions might be generated as the key intermediates via photocatalysis, providing a new direction for cross-electrophile couplings.
- Liao, Li-Li,Cao, Guang-Mei,Ye, Jian-Heng,Sun, Guo-Quan,Zhou, Wen-Jun,Gui, Yong-Yuan,Yan, Si-Shun,Shen, Guo,Yu, Da-Gang
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p. 17338 - 17342
(2019/01/04)
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- A highly efficient catalyst of a nitrogen-based ligand for the Suzuki coupling reaction at room temperature under air in neat water
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Glycine, as a kind of commercially available and inexpensive ligand, is used to prepare an air-stable and water-soluble catalyst for the Suzuki-Miyaura reaction in our study. In the presence of 0.1% [PdCl2(NH 2CH2COOH)2] as the catalyst, extremely excellent catalytic activity towards the Suzuki-Miyaura coupling of aryl halides containing the carboxyl group with various aryl boronic acids is observed at room temperature under air in neat water. the Partner Organisations 2014.
- Liu, Shiwen,Lv, Meiyun,Xiao, Daoan,Li, Xiaogang,Zhou, Xiuling,Guo, Mengping
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supporting information
p. 4511 - 4516
(2014/06/23)
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- SAR Studies on tetrahydroisoquinoline derivatives: The role of flexibility and bioisosterism to raise potency and selectivity toward P-glycoprotein
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The development of P-glycoprotein (P-gp) ligands remains of considerable interest, mostly for investigating the proteins structure and transport mechanism. In recent years, many different generations of ligands have been tested for their ability to modulate P-gp activity. The aim of the present work is to perform SAR studies on tetrahydroisoquinoline derivatives in order to design potent and selective P-gp ligands. For this purpose, the effect of bioisosteric replacement and the role of flexibility have been investigated, and four series of tetrahydroisoquinoline ligands have been developed: (a) 2-aryloxazole bioisosteres, (b) elongated analogues, (c) 2H-chromene, and (d) 2-biphenyl derivatives. The results showed that both 2-biphenyl derivative 20b and elongated derivative 6g behaved as strong P-gp substrates. In conclusion, important aspects for developing potent and selective P-gp ligands have been highlighted, providing a solid starting point for further optimization.
- Capparelli, Elena,Zinzi, Laura,Cantore, Mariangela,Contino, Marialessandra,Perrone, Maria Grazia,Luurtsema, Gert,Berardi, Francesco,Perrone, Roberto,Colabufo, Nicola A.
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p. 9983 - 9994
(2015/02/05)
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- Fluorous-silica-supported perfluoro-tagged palladium complexes catalyze Suzuki couplings in water
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Different Pd-complexes (see 2a-d and 3) with and without perfluoroalkyl tags were deposited on fluorous reversed-phase silica 1 and unmodified silica gel. These supported complexes were successfully used as precatalysts for the Suzuki reaction in H2O. H2O-Soluble aryl bromides were easily converted to the corresponding biphenyls. Although none of the complexes is H2O-soluble, the active catalyst is most likely homogeneously dissolved. Nevertheless, the Pd-leaching into the product was low.
- Tzschucke, Carl Christoph,Bannwarth, Willi
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p. 2882 - 2889
(2007/10/03)
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- Photostimulated reactions of phenylacetic acid dianions with aryl halides. Influence of the metallic cation on the regiochemistry of arylation.
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[reaction: see text]Phenylacetic acid dianions react via what appears to be an S(RN)1 process with aryl halides under photostimulation to afford aryl substitution products 5 and 6. When the counterion is K+, only 4-biphenylacetic acids 5 are obtained. Both alpha- and para-coupling occurs with Na+ to give a mixture of 5 and 6, while exclusive formation of diphenylacetic acids 6 is observed with the dilithio salt of 1.
- Nwokogu,Wong,Greenwood,Wolfe
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p. 2643 - 2646
(2007/10/03)
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- Control of porphyrin orientation in thermotropic liquid crystals by molecular design. A time-resolved EPR study
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Molecular compatibility of a guest porphyrin in a thermotropic nematic liquid crystalline host phase was shown to control the orientation of the porphyrin chromophore. In this manner, the normal alignment of a porphyrin plane parallel to the director in a nematic phase was inverted to a perpendicular orientation by attachment of mesogenic type appendages orthogonal to a porphyrin ring on one side of the ring plane. This molecular design also leads to a head-to-tail ordering of the porphyrin even in isotropic phases. The conclusions reached are based on detection and analysis of time-resolved EPR spectra of photoexcited triplet states.
- Michaeli, Shalom,Hugerat, Muhamad,Levanon, Haim,Bernitz, Mazal,Natt, Aliza,Neumann, Ronny
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p. 3612 - 3618
(2007/10/02)
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- SYNTHESIS OF NEW OPTICALLY ACTIVE CYANOCYCLOPROPANES AS CHIRAL DOPANTS FOR FERROELECTRIC LIQUID CRYSTALS
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Optically active 2-alkyl-1-aryl-cyanocyclopropanes were synthesized from 2-aryl-4-hydroxyalkanenitriles which in turn were obtained by the reaction of chiral 1,2-epoxyalkanes with the carbanions derived from arylacetonitriles.
- Kusumoto, Tetsuo,Nakayama, Akiko,Sato, Ken-ichi,Hiyama, Tamejiro,Takehara, Sadao,et al.
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p. 939 - 942
(2007/10/02)
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- Optically active compound, intermediate therefor, process for producing the intermediate, and liquid-crystal composition
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The present invention discloses an optically active compound represented by the following general formula (I): STR1 wherein R1 represents an alkyl, alkoxyl, or alkoxyalkanoyloxy group which has 1 to 18 carbon atoms and may be substituted with f
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- Biphenyloxy derivatives and antihyperlipidemic use
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Compounds of the formula STR1 wherein R1 is straight or branched alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, phenylalkyl, phenylalkenyl, pyridyl or STR2 where X, Y and Z are each hydrogen, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms, R2 is hydrogen or alkyl of 1 to 4 carbon atoms, R3 is hydroxymethyl, carboxyl, alkoxycarbonyl of 2 to 7 carbon atoms or cycloalkoxycarbonyl or 4 to 8 carbon atoms, A is --CO--NH-- or --NH--CO--, and n is 1, 2 or 3, And, when R3 is carboxyl, non-toxic salts thereof formed with an inorganic or organic base; the compounds as well as the salts are useful as antihyperlipidemics.
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