489471-57-0Relevant articles and documents
Preparation of unsymmetrical sulfonylureas from N,N′-sulfuryldiimidazoles
Beaudoin, Serge,Kinsey, Kenneth E.,Burns, James F.
, p. 115 - 119 (2003)
The synthetic methods reported in the literature for the preparation of sulfonylureas tend to be restricted in scope or unsuitable for use in parallel synthesis. We have developed a method for preparing sterically congested sulfonylureas based on N,N′-sul
Evaluation of WO2017018805: 1,3,4-oxadiazole sulfamide derivatives as selective HDAC6 inhibitors
Liang, Yuan-Yuan,Zhang, Cheng-Mei,Liu, Zhao-Peng
, p. 647 - 651 (2018)
Introduction: There are great potential in the development of selective HDAC6 inhibitors for the treatment of infectious diseases, neoplasms, endocrine diseases, and other diseases associated with HDAC6 activity. Areas covered: The application claims 1,3,4-oxadiazole sulfamide derivatives as selective HDAC6 inhibitors for the treatment of infectious diseases, neoplasms, endocrine, nutritional, and metabolic diseases; mental and behavioral disorders; neurological diseases; diseases of the eye and adnexa; cardiovascular diseases; respiratory diseases; digestive diseases; diseases of the skin and subcutaneous tissue; disease of the musculoskeletal system and connective tissue; or congenital malformations, deformations and chromosomal abnormalities. Many of the exemplified compounds showed nanomole potency against HDAC6 and were more than 5000-fold selectivity for HDAC6 over HDAC1. Expert opinion: These 1,3,4-oxadiazole sulfamide derivatives have a unique zinc-binding group (ZBG) that provide good leads for the discovery of potent selective HDAC6 inhibitors for the treatment of a variety of diseases associated with HDAC6 activity.
1,3,4-OXADIAZOLE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Paragraph 383-385, (2021/09/03)
The present invention relates to a novel compound having a histone deacetylase 6 (HDAC6) inhibitory activity, an isomer thereof or a pharmaceutically acceptable salt thereof, the use thereof for preparing a therapeutic medicament; a pharmaceutical composition containing the same, and a treatment method using the composition; and a preparation method thereof. The novel compound, the isomer thereof, or the pharmaceutically acceptable salt thereof according to the present invention has the HDAC6 inhibitory activity, which is effective in the prevention or treatment of HDAC6-mediated diseases including cancer, inflammatory diseases, autoimmune diseases, neurological or neurodegenerative diseases.
5- OR 7-AZAINDAZOLES AS BETA-LACTAMASE INHIBITORS
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Page/Page column 116; 117, (2020/09/19)
The present invention relates to β-lactamase inhibitors having the following general formula (I): wherein R1-R4 and X1-X2 are defined in the specification, pharmaceutical composition thereof, and use thereof for the treatment of a bacterial infection, alone or in combination with β-lactam antibiotics and/or other antibiotics and/or other β-lactamase inhibitors.
Sulfuryl Fluoride Mediated Conversion of Aldehydes to Nitriles
Gurjar, Jitendra,Bater, Jorick,Fokin, Valery V.
supporting information, p. 1906 - 1909 (2019/01/24)
Aliphatic, aromatic, and heteroaromatic aldehydes were readily converted to corresponding nitriles in a one-pot reaction sequence with hydroxylamine and sulfuryl fluoride. The reaction proceeds at room temperature, does not require metal catalysts and special precautions, and produces nitriles in excellent yields. It is compatible with a variety of functional groups, can be performed in aqueous and organic solvents, and is readily scalable to multigram quantities. Mild conditions and high selectivity of the reaction enabled the construction of polyfunctional probes containing nitrile, alkyne, azide, and fluorosulfate groups for further orthogonal derivatization.
1,3,4-OXADIAZOLE SULFAMIDE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Paragraph 159-161, (2017/02/24)
The present invention relates to novel compounds having histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical c
HETEROCYCLICALKYL DERIVATIVE COMPOUNDS AS SELECTIVE HISTONE DEACETYLASE INHIBITORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
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Paragraph 219; 220; 221, (2016/12/22)
The present invention relates to novel heterocyclicalkyl derivatives having histone deacetylase (HDAC) inhibitory activity, optical isomers thereof or pharmaceutically acceptable salts thereof, the use thereof for the preparation of medicaments, pharmaceutical compositions containing the same, a method for treating diseases using the composition, and methods for preparing the novel heterocyclicalkyl derivatives. The novel heterocyclicalkyl derivatives according to the present invention are selective histone deacetylase (HDAC) inhibitors, and may be effectively used for the treatment of histone deacetylase-mediated diseases, such as cell proliferative diseases, inflammatory diseases, autosomal dominant diseases, genetic metabolic diseases, autoimmune diseases, acute/chronic neurological disease, hypertrophy, heart failure, ocular diseases, or neurodegenerative diseases.
SMALL MOLECULE INHIBITORS OF MCL-1 AND USES THEREOF
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Page/Page column 86-87, (2016/11/14)
This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having benzoic acid structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
SYNTHETIC N-ACETYL-MURAMIC ACID DERIVATIVES AND USES THEREOF
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Page/Page column 8; 9, (2016/11/17)
The present invention provides N-acetyl-muramic acid (NAM) derivatives having Formula I, wherein Xa is selected from the group consisting of X1-X59, Ya is selected from the group consisting of H, monophosphate, uridine diphosphate and ethyl azide linker prepared from 2-azido-ethanol, and Za is selected from the group consisting of OH, an ethylene diamine coupled fluorophore, a peptide and a peptide with an ethylene diamine coupled fluorophore, wherein the peptide is selected from the group consisting of a monopeptide, a dipeptide, a tripeptide and a pentapeptide. Also provided are methods for synthesizing NAM derivatives and methods for modulating Nod2 in cells, modifying bacterial cell wall or modulating innate immune response by a subject to bacterial cells upon exposure to NAM derivatives.
A safe and facile route to imidazole-1-sulfonyl azide as a diazotransfer reagent
Ye, Hui,Liu, Ruihua,Li, Dongmei,Liu, Yonghui,Yuan, Haixin,Guo, Weikang,Zhou, Lifei,Cao, Xuefeng,Tian, Hongqi,Shen, Jie,Wang, Peng George
supporting information, p. 18 - 21 (2013/03/29)
A facile approach to the diazotransfer reagent of imidazole-1-sulfonyl azide was reported. The procedure was well optimized to clarify potential explosion risks. A high production yield as well as small batch variation was achieved even without careful pretreatment of reagents and solvents. HPLC and NMR methods to monitor the process were provided. These features made this protocol suitable for large scale preparation in academia and industry as well.
