1196473-37-6Relevant articles and documents
Synthesis method of benzoxaborole
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Paragraph 0092-0095, (2021/04/10)
The invention belongs to the technical field of organic synthesis, and particularly relates to a synthesis method of benzoxaborole. The synthesis method comprises the step of in an organic solvent, under the condition of a strong acid catalyst, carrying out dehydration condensation reaction on a compound shown in a formula (A) and a compound shown in a formula (B) to obtain a compound shown in a formula (C). The compounds shown in the formulas (A) and (B) and the reaction solvent in the raw materials for preparing the benzoxaborole by adopting the method are simple and easy to obtain; the reaction steps are simple, and the product can be obtained by only one step; the reaction atom economy is high, and the reaction conditions are mild; and the reaction is suitable for mass production.
Preparation method of phenylboronic acid half ester
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Paragraph 0010; 0017, (2020/06/09)
The invention discloses a preparation method of phenylboronic acid half ester. The structural formula of the phenylboronic acid half ester prepared by the method is shown in the specification. The method is mild in reaction condition, the raw materials ar
BTK (Bruton's tyrosine kinase) inhibitors
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Paragraph 0210; 0212; 0215, (2018/08/28)
The invention belongs to the field of medicinal chemistry and particularly relates to compounds shown as formula (I) in the description, medically acceptable salts of the compounds, a preparation method of the compounds and pharmaceutical composition containing the compounds. The invention further relates to an application of the compounds, the medically acceptable salts of the compounds and the pharmaceutical composition containing the compounds to treatment of BTK (Bruton's tyrosine kinase) related diseases.
1 -HYDROXY-BENZOOXABOROLES AS ANTIPARASITIC AGENTS
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, (2014/10/03)
Provided are compounds useful for controlling endoparasites both in animals and agriculture. Further provided are methods for controlling endoparasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling endoparasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. The claimed compounds are described by the following Markush formula:A typical example for a compound according to above formula is: A typical example for a compound according to above formula is:
BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS
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, (2011/05/06)
This invention provides novel compounds of the following formula useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
Synthesis and SAR of novel benzoxaboroles as a new class of β-lactamase inhibitors
Xia, Yi,Cao, Kathy,Zhou, Yasheen,Alley,Rock, Fernando,Mohan, Manisha,Meewan, Maliwan,Baker, Stephen J.,Lux, Sarah,Ding, Charles Z.,Jia, Guofeng,Kully, Maureen,Plattner, Jacob J.
experimental part, p. 2533 - 2536 (2011/05/15)
A new class of benzoxaborole β-lactamase inhibitors were designed and synthesized. 6-Aryloxy benzoxaborole 22 inhibited AmpC P99 and CMY-2 with K i values in the low nanomolar range. Compound 22 restored antibacterial activity of ceftazidime against Enterobacter cloacae P99 expressing AmpC, a class C β-lactamase enzyme. The SAR around the arylbenzoxaboroles, which included the influence of linker and substitutions was also established.
Design, synthesis, and structure-activity relationship of trypanosoma brucei leucyl-tRNA synthetase inhibitors as antitrypanosomal agents
Ding, Dazhong,Meng, Qingqing,Gao, Guangwei,Zhao, Yaxue,Wang, Qing,Nare, Bakela,Jacobs, Robert,Rock, Fernando,Alley, Michael R. K.,Plattner, Jacob J.,Chen, Guoqiang,Li, Dawei,Zhou, Huchen
experimental part, p. 1276 - 1287 (2011/05/07)
African trypanosomiasis, caused by the proto zoal pathogen Trypanosoma brucei (T. brucei), is one of the most neglected tropical diseases that are in great need of new drugs. We report the design and synthesis of T. brucei leucyl-tRNA synthetase (TbLeuRS) inhibitors and their structure-activity relationship. Benzoxaborole was used as the core structure and C(6) was modified to achieve improved affinity based on docking results that showed further binding space at this position. Indeed, compounds with C(7) substitutions showed diminished activity due to clash with the eukaryote specific I4ae helix while substitutions at C(6) gave enhanced affinity. TbLeuRS inhibitors with IC 50 as low as 1.6 μM were discovered, and the structure-activity relationship was discussed. The most potent enzyme inhibitors also showed excellent T. brucei parasite growth inhibition activity. This is the first time that TbLeuRS inhibitors are reported, and this study suggests that leucyl-tRNA synthetase (LeuRS) could be a potential target for antiparasitic drug development.
BORON-CONTAINING SMALL MOLECULES AS ANTI-PROTOZOAL AGENTS
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, (2010/04/30)
This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
BORON-CONTAINING SMALL MOLECULES
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Page/Page column 73, (2012/06/05)
This invention relates to, among other items, 6-substituted benzoxaborole compounds and their use for treating bacterial infections.
Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease
Ding, Charles Z.,Zhang, Yong-Kang,Li, Xianfeng,Liu, Yang,Zhang, Suoming,Zhou, Yasheen,Plattner, Jacob J.,Baker, Stephen J.,Liu, Liang,Duan, Maosheng,Jarvest, Richard L.,Ji, Jingjing,Kazmierski, Wieslaw M.,Tallant, Matthew D.,Wright, Lois L.,Smith, Gary K.,Crosby, Renae M.,Wang, Amy A.,Ni, Zhi-Jie,Zou, Wuxin,Wright, Jon
scheme or table, p. 7317 - 7322 (2011/01/12)
We disclose here a series of P4-benzoxaborole-substituted macrocyclic HCV protease inhibitors. These inhibitors are potent against HCV NS3 protease, their anti-HCV replicon potencies are largely impacted by substitutions on benzoxaborole ring system and P2 groups. P2 2-thiazole-isoquinoline provides best replicon potency. The in vitro SAR studies and in vivo PK evaluations of selected compounds are described herein.
