6908-38-9Relevant articles and documents
THIAZOLOPIPERAZINE DERIVATIVES AND COMPOSITION FOR PREVENTING OR TREATING AUTOIMMUNE DISEASES COMPRISING THE SAME
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Paragraph 0118-0124; 0133; 0134, (2020/04/01)
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
Method for synthesizing biphenylcarboxylic acid compound by using Suzuki coupling reaction
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Paragraph 0027, (2018/09/21)
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.
SAR Studies on tetrahydroisoquinoline derivatives: The role of flexibility and bioisosterism to raise potency and selectivity toward P-glycoprotein
Capparelli, Elena,Zinzi, Laura,Cantore, Mariangela,Contino, Marialessandra,Perrone, Maria Grazia,Luurtsema, Gert,Berardi, Francesco,Perrone, Roberto,Colabufo, Nicola A.
, p. 9983 - 9994 (2015/02/05)
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.