392-04-1Relevant academic research and scientific papers
Discovery of highly potent SARS-CoV-2 Mpro inhibitors based on benzoisothiazolone scaffold
Chen, Weixiong,Feng, Bo,Han, Sheng,Wang, Peipei,Chen, Wuhong,Zang, Yi,Li, Jia,Hu, Youhong
supporting information, (2022/01/14)
The COVID-19 pandemic has drastically impacted global economies and public health. Although vaccine development has been successful, it was not sufficient against more infectious mutant strains including the Delta variant indicating a need for alternative treatment strategies such as small molecular compound development. In this work, a series of SARS-CoV-2 main protease (Mpro) inhibitors were designed and tested based on the active compound from high-throughput diverse compound library screens. The most efficacious compound (16b-3) displayed potent SARS-CoV-2 Mpro inhibition with an IC50 value of 116 nM and selectivity against SARS-CoV-2 Mpro when compared to PLpro and RdRp. This new class of compounds could be used as potential leads for further optimization in anti COVID-19 drug discovery.
BENZOTHIOPHENE, THIENOPYRIDINE AND THIENOPYRIMIDINE DERIVATIVES FOR THE MODULATION OF STING
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Page/Page column 86, (2021/02/12)
A compound of formula (I): wherein: Y is (CH2)n, where n is from 2 to 4; W1 and W11 are independently selected from OH and ORP, where RP is Me or Et.
BENZOTHIOPHENE, THIENOPYRIDINE AND THIENOPYRIMIDINE DERIVATIVES FOR THE MODULATION OF STING
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Page/Page column 96-97, (2021/02/12)
A compound of formula (I); wherein: W is O or NH; A1 1 is CRAA or N; A22 is CRBB or N; A3A3 is CRCC or N; A44 is CRDD or N; where no more than two of A11, A
ASK1 INHIBITING AGENTS
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Page/Page column 176, (2018/09/08)
Provided are compounds of Formulas (I'), (I), (II') and (II), or pharmaceutically acceptable salts thereof, and methods for their use and production.
SUBSTITUTED DIHYDROINDENE-4-CARBOXAMIDES AND ANALOGS THEREOF, AND METHODS USING SAME
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Page/Page column 214; 222-223, (2018/10/19)
The present invention includes novel substituted bicyclic compounds, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infections in a patient. In certain embodiments, the compounds and compositions of the invention are capsid inhibitors. (Formula I)
MODIFIED COMPOUND OF ANDROGRAPHOLIDE
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Paragraph 0192-0194, (2019/01/04)
The present disclosure discloses a modified compound of andrographolide, and particularly discloses a compound shown in formula (I) and (II) or a pharmaceutically acceptable salt thereof.
A Bcl - 2 inhibitor venetoclax and intermediate preparation method (by machine translation)
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Paragraph 0030; 0031; 0032; 0035; 0036, (2018/01/11)
The invention relates to a process for preparing Bcl - 2 inhibitor venetoclax required intermediate preparation method, a synthetic route thereof are shown below, in particular comprises the following steps: to compound I 2, 4 - difluoro-benzoic acid as the raw material, and after hydroxy methyl esterification reaction to obtain compound II 4 - fluorosalicylic acid methyl ester, compound II with the piperazine coupling to make the compound III, compound III and IV by the reaction of the raw material compound V, the compound V with compound VI 5 - bromo - 7 - aza indole C - O prepared by coupling compound VII, is intermediate. Preparation method of this invention mild reaction conditions, the operation is simple, environmental protection and high-efficiency and low cost, easy to manufacture on a large scale. (by machine translation)
5-SULFAMOYL-2-HYDROXYBENZAMIDE DERIVATIVES
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Page/Page column 91, (2017/09/27)
The invention is directed to substituted salicylamide derivatives. Specifically, the invention is directed to compounds according to Formula (I): wherein R, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof. The compounds of the invention are inhibitors of CD73 and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with CD73 inhibition, such as AIDS, the treatment of HIV, autoimmune diseases, infections, atherosclerosis, and ischemia–reperfusion injury. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CD73 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Design and synthesis of ruthenium bipyridine catalyst: An approach towards low-cost hydroxylation of arenes and heteroarenes
Shome, Sanchari,Singh, Surya Prakash
supporting information, p. 3743 - 3746 (2017/09/01)
Two new ruthenium bipyridine complexes were designed and synthesized for intermolecular Csp2-H hydroxylation. An environmentally begin and inexpensive oxidant was employed as an oxygen source thereby enhancing its applicability and resulting in the remarkable increase of yield. In the catalytic process a ruthenium (IV) cationic complex is formed which enables the regioselective C–O bonds formation and also proves to be tolerant to a broad substrate scope. Activation of C–H bonds adjacent to removable and non-removable directing groups have been explored efficiently.
