42872-74-2Relevant academic research and scientific papers
Discovery of benzhydrol-oxaborole derivatives as Streptococcus pneumoniae leucyl-tRNA synthetase inhibitors
Hao, Guiyun,Li, Hao,Yang, Fei,Dong, Duoling,Li, Zezhong,Ding, Yingying,Pan, Wei,Wang, Enduo,Liu, Rujuan,Zhou, Huchen
, (2020/11/25)
Pneumonia caused by bacterium S. pneumoniae is a severe acute respiratory infectious disease with high morbidity and mortality, especially for children and immunity-compromised patients. The emergence of multidrug-resistant S. pneumoniae also presents a c
Preparation method of 2 -bromine -4-nitrile benzaldehyde
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Paragraph 0061-0063, (2021/10/02)
The invention relates to a preparation method of 2 - bromo -4 nitrile benzaldehyde, and belongs to the field of pharmaceutical chemistry. The preparation method can be used for preparing 2 - bromo -4 nitrile benzaldehyde by taking methylbenzonitrile as a
A NEW TYPE OF BENZOXABOROLE-BASED ANTI-PNEUMOCOCCAL COMPOUNDS TARGETING LEUCYL-TRNA SYNTHETASE
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Page/Page column 5-6, (2021/01/22)
Provided is benzoxaborole-based derivatives and their preparation and use. The structural general formula of the derivatives is (I). The derivatives are used for the preparation of a medicament for the prevention and treatment of Pneumonia. Compared with
GLUCOSE SENSITIVE INSULIN DERIVATIVES
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Page/Page column 160, (2020/10/20)
The present invention relates to novel insulin derivatives and their use in the treatment or prevention of medical conditions relating to diabetes. The insulin derivatives are glucose sensitive and display glucose-sensitive albumin binding. The invention
PROTECTIVE GROUPS AND METHODS FOR PROTECTING BENZOXABOROLES OR OXABOROLES
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Page/Page column 35, (2019/10/01)
The present invention relates in part protective groups that can be used to reversibly protect benzoxaboroles and/or oxaboroles and yield the corresponding protected complexes. The invention further relates to the use of these protective groups to protect benzoxaboroles and/or oxaboroles.
2-ARYL SELENAZOLE COMPOUND AND PHARMACEUTICAL COMPOSITION THEREOF
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Paragraph 0130; 0131, (2015/11/16)
Disclosed are a 2-aryl selenazole compound and a pharmaceutical composition thereof, where the 2-aryl selenazole compound is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof. The 2-aryl selenazole compound has the activi
Synthesis and structure-activity relationships of novel benzoxaboroles as a new class of antimalarial agents
Zhang, Yong-Kang,Plattner, Jacob J.,Freund, Yvonne R.,Easom, Eric E.,Zhou, Yasheen,Gut, Jiri,Rosenthal, Philip J.,Waterson, David,Gamo, Francisco-Javier,Angulo-Barturen, Inigo,Ge, Min,Li, Zhiya,Li, Lingchao,Jian, Yong,Cui, Han,Wang, Hailong,Yang, Jian
experimental part, p. 644 - 651 (2011/03/18)
A series of boron-containing benzoxaborole compounds was designed and synthesized for a structure-activity relationship investigation surrounding 7-(HOOCCH2CH2)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (1) with the goal of discovering
BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS
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Page/Page column 103-104, (2011/04/13)
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.
Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR
Angell, Richard M.,Angell, Tony D.,Bamborough, Paul,Brown, David,Brown, Murray,Buckton, Jacky B.,Cockerill, Stuart G.,Edwards, Chris D.,Jones, Katherine L.,Longstaff, Tim,Smee, Penny A.,Smith, Kathryn J.,Somers, Don O.,Walker, Ann L.,Willson, Malcolm
, p. 324 - 328 (2008/12/22)
The biphenyl amides are a novel series of p38 MAP kinase inhibitors. Structure-activity relationships of the series against p38α are discussed with reference to the X-ray crystal structure of an example. The series was optimised rapidly to a compound showing oral activity in an in vivo disease model.
BIPHENYL DERIVATIVES AND THEIR USE IN TREATING HEPATITIS C
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Page/Page column 110, (2008/06/13)
A compound which is a biphenyl derivative of formula (I), or a pharmaceutically acceptable salt thereof wherein: R1 is a C1-C6 alkyl group or a moiety -A1, -L1-A1, -A1-A1′, -L1-A1-A1′, -A1-L1-A1′, -A1-Y1-A1′, -A1-Het1-A1′, -L1-A1-Y1-A1′, -L1-A1-Het1-A1′, -L1-Het1-A1, -L1-Y1-A1, -L1-Y1-Het1-A1, -L1-Het1-Y1-A1, -L1-Y1-Het1-L1′, -A1-Y1-Het1-A1′, -A1-Het1-Y1-A1′, -A1-Het1-L1-A1′, -A1-L1-Het1-A1′ or -L1-Het1-L1′; - A and B are the same or different and each represent a direct bond or a -CO- NR′-, -NR′-CO-, -NR′-CO2-, -CO-, -NR′-CO-NR′′-, -NR′-S(O)2-, -S(O)2-NR′-, -SO2-, -NR′-, -NR′-CO-CO-, -CO-O-, -O-CO-, -(C1-C2 alkylene)-NR′- or -(C1-C2 hydroxyalkylene)-NR′ - moiety, wherein R′ and R′′ are the same or different and each represent hydrogen or C1-C4 alkyl; - R2 and R3 are the same or different and each represent C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy or halogen; n and m are the same or different and each represent 0 or 1 ; R4 is a C1-C6 alkyl group or a moiety -A4, -L4-A4, -A4-A4′, -L4-A4-A4′ , -A4-L4-A4′, -A4-Y4-A4′, -A4-Het4-A4′, -L4-A4-Y4-A4′, -L4-A4-Het4-A4′, -L4-Het4-A4, -L4-Y4-A4, -L4-Y4-Het4-A4, -L4-Het4-Y4-A4, -L4-Y4-Het4-L4′, -A4-Y4-Het4-A4′, -A4-Het4-Y4-A4′, -A4-Het4-L4-A4′, -A4-L4-Het4-A4′ or -L4-Het4-L4′, each A1, A4, A1′ and A4′ are the same or different and represent a phenyl, 5- to 10- membered heteroaryl, 5- to 10- membered heterocyclyl or C3-C8 carbocyclyl moiety; each L1 and L4 is the same or different and represents a C1-C4 alkylene or a C1-C4 hydroxyalkylene group; each Y1 and Y4 is the same or different and represents -CO-, -SO- or -S(O)2-; each L1′ and L4′ is the same or different and represents hydrogen or a C1-C4 alkyl group; and each Het1 and Het4 is the same or different and represents -O-, -S- or -NR′-, wherein R′ is hydrogen or a C1-C4 alkyl group, the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R1 and R4 being optionally fused to a phenyl, 5- to 10- membered heteroaryl or 5- to 10- membered heterocyclyl ring; and the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R1 and R4 being unsubstituted or substituted by (a) a single unsubstituted substituent selected from -(C1-C4 alkyl)-X1, -CO2R′, -SO2NR′R′′, -S(O)2-R′, -CONR′R′′, -NR′-CO-R′′′, -NR′-S(O)2-R′′′, -CO-NR′-(C1-C4 alkyl)-NR′R′′ and -CO-O-(C1-C4 alkyl)-NR′R′′ and/or (b) 1, 2 or 3 unsubstituted substituents selected from -(C1-C4 alkyl)-X2, halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C4 hydroxyalkyl, hydroxy, cyano, nitro and -NR′R′′, wherein X1 is -CO2R′, -SO2-R′, -NR′-CO2-R′′, -NR′-S(O)2-R′′′, -CONR′R′′ or -SO2-NR′R′′, each X2 is the same or different and is cyano, nitro or -NR′R′′, each R′ and R′′ is the same or different and represents hydrogen or C1-C4 alkyl and each R′′′ is the same or different and represents C1-C4 alkyl.
