- 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 0118-0124; 0133; 0134
(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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- Method for synthesizing biphenylcarboxylic acid compound by using Suzuki coupling reaction
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The invention provides a method for synthesizing a biphenylcarboxylic acid compound by using the Suzuki coupling reaction. According to the method, brominated aromatic hydrocarbon and arylboronic acidare used as raw materials, and water-soluble fullerene nanopalladium is used as a catalyst; and the equation of the Suzuki coupling reaction is as described in the specification. In the equation, R1and R2 represent substituents at different positions, may be acceptor or donor substituents, and may be monosubstitutents or polysubstitutent; and R1 and R2 may be identical or different groups. The water-soluble fullerene nanopalladium catalyst is cheap, easily available and environmentally friendly, and has high catalytic activity and stable properties. When the catalyst is used for catalysis ofthe Suzuki coupling reaction, conditions are mild, anhydrous anaerobic treatment and high-temperature treatment are not needed, and cost is low. The method can be applied to the industrial synthesisof non-steroidal anti-inflammatory drugs such as diphenylacetic acid and diflunisal.
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Paragraph 0027
(2018/09/21)
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- [...] compound and mesogenic medium
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wherein R11, R12, MG11, MG12 and CG1 have the meaning given in claim 1, to the use of bimesogenic compounds of formula I in liquid crystal media and particular to flexoelectric liquid crystal devices comprising a liquid crystal medium according to the pre
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Paragraph 0209; 0211
(2018/04/11)
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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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- 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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- Compositions and methods of treating cell proliferation disorders
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The invention relates to compounds and methods for treating cell proliferation disorders.
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Page/Page column 75
(2008/06/13)
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