- Benzyl substituted aniline compound and use thereof
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The invention provides a benzyl-substituted aniline compound represented by a formula I shown in a drawing or pharmaceutically acceptable salts thereof, wherein R1 is independently selected from -COOH, -CONH2, H, -COOR5 (R5 is methyl or ethyl), -CN, -OH and -NH2COCH3, R2 and R3 are independently selected from C6-C10 aryl, C3-C6 cyclane and C1-C3 saturated alkyl or unsaturated alkyl respectively, and R4 is independently selected from -H, ethyl and acetyl. The compound and the pharmaceutically acceptable salts thereof, provided by the invention, can be used as farnesyltransferase inhibitors or can be used for preparing drugs for preventing or treating diseases related to farnesyltransferase, thereby having good medicine preparation prospects.
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Paragraph 0033-0035
(2017/02/02)
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- Heterocyclic substituted styrene compound and use thereof
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The invention relates to a heterocyclic substituted styrene compound and its use. The invention discloses a heterocyclic radical, alkoxy and halogen modified styrene compound. Results of inhibition activity of the compound against Syk (spleen tyrosine kinase) show that the compound has inhibition activity against the Syk (spleen tyrosine kinase), and part of the compound has stronger inhibition activity against the Syk, and a structure foundation for further design and development of new Syk inhibitor-class rheumatoid arthritis (RA) therapy drugs is laid.
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Paragraph 0066; 0067; 0068; 0069
(2016/10/07)
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- Practical Ligand-Free Copper-Catalysed Short-Chain Alkoxylation of Unactivated Aryl Bromides
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An efficient and practical short-chain alkoxylation of unactivated aryl bromides has been developed with special attention focussed on the applicability of the reaction. Sodium alkoxide is used as the nucleophile, and the corresponding alcohol as the solvent. The reaction requires neither precious metals nor organic ligands. It uses a catalytic system consisting of copper(I) bromide as a catalyst, the corresponding alkyl formate as a noncontaminating cocatalyst, and lithium chloride as an additive. A wide range of substrates and test cases highlight the synthetic utility of the approach. Considering the commercial accessibility and affordability of the feedstocks, this protocol shows promise as a new alternative for the sustainable preparation of aryl alkyl ethers.
- Guo, Ying,Fan, Xue-Min,Nie, Min,Liu, Hong-Wei,Liao, Dao-Hua,Pan, Xian-Dao,Ji, Ya-Fei
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p. 4744 - 4755
(2015/08/03)
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- Discovery of Benzylidene Derivatives as Potent Syk Inhibitors: Synthesis, SAR Analysis, and Biological Evaluation
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Four scaffolds of varied benzylidene derivatives were synthesized and evaluated as Syk inhibitors for the treatment of rheumatoid arthritis (RA). Among these 31 compounds, 3-benzylidene pyrrolidine-2,5-dione derivatives (including 12k) universally showed good Syk inhibitory activities in the low micromolar to submicromolar range. In the cellular profiling, compound 12k, the most efficient compound, showed excellent antiproliferative activity against fibroblast-like synoviocytes (FLS)-RA, and demonstrated potencies for suppression of IL-6 and MMP-3 secretion almost equal to R406 (positive control). The oral efficacy of 12k in the murine collagen-induced arthritis model was significant, despite being weaker than R406. Taken together, all preliminary pharmacological results supported 12k as a potential small-molecule inhibitor targeting Syk for the treatment of RA.
- Zhang, Lingling,Liu, Wei,Mao, Fei,Zhu, Jin,Dong, Guoqiang,Jiang, Hualiang,Sheng, Chunquan,Miao, Liyan,Huang, Lixin,Li, Jian
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p. 463 - 474
(2015/07/07)
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- Efficient Co(OAc)2-catalyzed aerobic oxidation of EWG-substituted 4-cresols to access 4-hydroxybenzaldehydes
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We reported an efficient ligand-free Co(OAc)2·4H 2O/NaOH/O2/ethylene glycol reaction system that enables selective aerobic oxidation of a wide range of substrates covering 2,6-di-EWG-, 2,3,6-tri-EWG-, 2-EWG-, and 2-EWG-6-EDG-substituted 4-cresols into the corresponding 4-hydroxybenzaldehydes. Based on the experimental investigations and well-defined p-benzoquinone methides, a plausible reaction mechanism was proposed. Considering the simplicity of the procedure and importance of the products, the methodology was expected to become a favorable and practical tool in related benzylic C(sp3)-H functionalization chemistry.
- Jiang, Jian-An,Du, Jia-Lei,Liao, Dao-Hua,Wang, Zhan-Guo,Ji, Ya-Fei
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supporting information
p. 1406 - 1411
(2014/03/21)
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- Ester derivatives and medicinal use thereof
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The present invention relates to an ester represented by the formula [1]: or its pharmaceutically acceptable salt, or use of the same. The compound represented by the formula [1] or its pharmaceutically acceptable salt is useful as an agent for the treatment or prophylaxis of hyperlipidemia or the like, since it disappears very rapidly in the living body and has an excellent MTP inhibitory activity.
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Page/Page column 43
(2010/11/08)
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