107582-20-7Relevant academic research and scientific papers
Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: Discovery and preliminary SAR of benzimidazole derivatives
Beaulieu, Pierre L.,Boes, Michael,Bousquet, Yves,Fazal, Gulrez,Gauthier, Jean,Gillard, James,Goulet, Sylvie,LaPlante, Steven,Poupart, Marc-Andre,Lefebvre, Sylvain,McKercher, Ginette,Pellerin, Charles,Austel, Volkhard,Kukolj, George
, p. 119 - 124 (2004)
Benzimidazole 5-carboxamide derivatives from a combinatorial screening library were discovered as specific inhibitors of the NS5B polymerase of the hepatitis C virus (HCV). Initial hit-to-lead activities taking advantage of high-throughput parallel synthetic techniques, identified a 1,2-disubstituted benzimidazole 5-carboxylic acid scaffold as the minimum core for biological activity. Potent analogues in this series inhibit the polymerase at low micromolar concentrations and provide an attractive 'drug-like' lead structure for further optimization and the development of potential HCV therapeutics.
MODIFIED PROTEINS AND PROTEIN DEGRADERS
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Paragraph 00805-00807, (2021/12/08)
Provided herein are compounds, pharmaceutical compositions, and methods for binding or degrading target proteins. Further provided herein are compounds having a DNA damage-binding protein 1 (DDB1) binding moiety. Some such embodiments include a linker. Some such embodiments include a target protein binding moiety. Further provided herein are ligand-DDB1 complexes. Further provided herein are in vivo modified DDB1 proteins.
Method for Producing Alpha-Azidoaniline Derivative or Alpha,AlphaPrime-Diazide Derivative
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Paragraph 0202-0204, (2021/08/13)
Provided is a method for producing an α-azidoaniline derivative or an α,α′-diazide derivative using an aniline derivative as a starting material that includes a method for producing an α-azidoaniline derivative or an α,α′-diazide derivative represented by Formula (2), including the step of: contacting an aniline derivative represented by Formula (1) with an azidating agent in presence of water, a persulfate, and a copper compound.
Regioselective C-H Azidation of Anilines and Application to Synthesis of Key Intermediate for Pharmaceutical
Seki, Masahiko,Takahashi, Yusuke
, p. 7842 - 7848 (2021/06/28)
A catalytic system for regioselective C-H azidation of inactive anilines was developed. In the presence of CuSO4·5H2O, simultaneous addition of NaN3 and Na2S2O8 to aq. CH3CN solution of free anilines under weakly acidic conditions (pH 4.5) smoothly underwent C-H azidation to provide corresponding α-azidated products in high yields. Methyl α-azidoanthranilate obtained by this method was readily transformed via simple reduction followed by cyclization to methyl 2-ethoxybenzimidazol-7-carboxylate, a key intermediate for antihypertensive Candesartan Cilexetil.
BIS(2-HALOACETAMIDO)-COMPOUNDS FOR USE AS LINKING AGENTS AND RESULTANT PRODUCTS WHICH COMPRISE ANTIBODIES, HALF-ANTIBODIES AND ANTIBODY FRAGMENTS
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Page/Page column 27; 30, (2021/01/23)
Bis(2-haloacetamido)- compounds for use as linkers to chemically cross-linking multiple thiol groups, and particularly, although not exclusively, the thiol groups of cysteine amino acids in peptide chains are described, along with their use as linking age
IMMUNOMODULATORY COMPOUNDS
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Paragraph 0303-0305, (2020/01/24)
Disclosed are immunomodulatory compounds, pharmaceutical compositions containing them, and methods of making and using the compounds to treat diseases and disorders characterized by aberrant protein activity that can be targeted by cereblon.
TRANSGLUTAMINASE 2 (TG2) INHIBITORS
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Paragraph 00471, (2020/03/02)
Described herein are compounds and pharmaceutical compositions containing such compounds which inhibit transglutaminase 2 (TG2). Also described herein are methods for using such TG2 inhibitors, alone or in combination with other compounds, for treating diseases or conditions that would benefit from TG2 inhibition.
Multi-substituted amine compound and its preparation and use (by machine translation)
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Paragraph 0463; 0464; 0469-0471, (2018/04/27)
The invention belongs to the field of medical technology, in particular, the present invention provides the following formula I shown multi-substituted amine compound or its isomer or its pharmaceutically acceptable salt, ester, prodrug or hydrate, its pharmaceutical composition, preparation method thereof and its use in the preparation of medicine for treating aids in use. The compound or pharmaceutical composition containing the compound can be used as an inhibitor for inhibiting HIV integrase with LEDGF/p75 between protein - protein interaction and HIV integrase dimerization, then can be used for the treatment of aids. . (by machine translation)
A 2 - ethoxy benzimidazole - 7 - carboxylic acid methyl ester
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Paragraph 0033; 0059-0068, (2018/05/24)
The invention discloses a synthesis method of 2-ethoxy benzimidazole-7-carboxylic acid methyl ester. The problem that an existing process is not high in content and is very low in yield is solved. According to the synthesis method, 3-nitryl phthalic acid is used as a raw material, rearrangement is performed in a water solution after methyl esterification, acylation and re-nitridation, then tin powder is adopted to perform reduction and loop closing so as to obtain the 2-ethoxy benzimidazole-7-carboxylic acid methyl ester. By the adoption of the synthesis method, produced impurities are very little, the content is high, and the yield is also high.
The discovery of new scaffold of plant activators: From salicylic acid to benzotriazole
Chang, Kang,Chen, Jian-Qin,Shi, Yan-Xia,Sun, Mei-Jian,Li, Peng-Fei,Zhao, Zhen-Jiang,Zhu, Wei-Ping,Li, Hong-Lin,Xu, Yu-Fang,Li, Bao-Ju,Qian, Xu-Hong
, p. 919 - 926 (2017/05/16)
Started from salicylic acid (SA) and related commercialized plant activators, based on molecular three-dimensional shape and pharmacophore similarity comparison (SHAFTS), a new lead compound benzotriazole was predicted and a series of benzotriazole derivatives were designed and synthesized. The bioassay showed that benzotriazole had high activity against a broad spectrum of diseases including fungi and oomycetes in vivo, but no activity in vitro. And the introduction of proper groups at the 1’-position and 5’-position was beneficial to the activity. So, they had the potential to be exploited as novel plant activators.
