2516-37-2Relevant academic research and scientific papers
NOVEL HYDRAZONE DERIVATIVE WITH ARYL OR HETEROARYL GROUP SUBSTITUTED AT TERMINAL AMINE GROUP THEREOF AND USE THEREOF
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Paragraph 0300, (2021/11/04)
The present invention relates to novel hydrazone derivatives in which a terminal amine group is substituted with an aryl group or a heteroaryl group, and uses thereof.
NOVEL HETEROCYCLIC DERIVATIVES WITH CARDIOMYOCYTE PROLIFERATION ACTIVITY FOR TREATMENT OF HEART DISEASES
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Page/Page column 20; 21; 54; 55, (2021/06/22)
Provided are novel heterocyclic derivatives with cardiomyocyte proliferation activity for treatment of heart diseases. Specifically, provided are the compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs, prepa
METHODS AND MATERIALS FOR INCREASING TRANSCRIPTION FACTOR EB POLYPEPTIDE LEVELS
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Page/Page column 110, (2020/07/21)
This document provides methods and materials for increasing TFEB polypeptide levels. For example, compounds (e.g., organic compounds) having the ability to increase TFEB polypeptide levels within cells and/or within a nucleus of cells, formulations containing compounds having the ability to increase TFEB polypeptide levels within cells and/or within a nucleus of cells, methods for making compounds having the ability to increase TFEB polypeptide levels within cells and/or within a nucleus of cells, methods for making formulations containing compounds having the ability to increase TFEB polypeptide levels within cells and/or within a nucleus of cells, methods for increasing TFEB polypeptide levels within cells and/or within a nucleus of cells, and methods for treating mammals (e.g., humans) having a condition responsive to an increase in TFEB polypeptide levels are provided.
Novel hydrazone derivatives comprising aryl or heteroaryl group substituted at terminal amine and use thereof
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Paragraph 1403; 1405-1407, (2020/08/28)
The present invention relates to novel hydrazone derivatives with an aryl or heteroaryl group substituted at a terminal amine group thereof and a use thereof.
Derivatives with uracil-benzothiazole structure, preparation method of derivatives, and application of anti-HCV drugs
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Paragraph 0042-0044, (2019/12/02)
According to the invention, a new series of uracil-benzothiazole NS5B RdRp inhibitors are designed and synthesized; the compounds have the structure shown in a general formula (1), wherein the uracil-benzothiazole NS5B RdRp inhibitor provided by the inven
HETEROARYL COMPOUNDS AND USES THEREOF
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Paragraph 0185; 0188-0189, (2019/11/28)
Described herein are compounds of formula (I), and pharmaceutically acceptable salts, solvates, hydrates, isotopically labeled derivatives and radiolabeled derivative thereof, and pharmaceutical compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for detecting and imaging Tau aggregates in the brain for detection of Alzheimer's disease (AD) in a subject.
Nitrogen-containing bicyclic compounds and preparation method and use thereof
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Paragraph 0719; 0721-0722, (2018/11/04)
The present invention relates to nitrogen-containing bicyclic compounds and a preparation method and use thereof. The compounds or pharmaceutical compositions can be used as an inhibitor of retinoic acid-related orphan receptor gamma t (ROR gamma t). The invention also relates to the preparation method of the compounds and pharmaceutical compositions, and use of the in the compounds and pharmaceutical compositions in treatment or prevention of RORyt-mediated inflammatation or autoimmune diseases in mammals, particularly humans.
Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis
Patrick, Donald A.,Gillespie, J. Robert,McQueen, Joshua,Hulverson, Matthew A.,Ranade, Ranae M.,Creason, Sharon A.,Herbst, Zackary M.,Gelb, Michael H.,Buckner, Frederick S.,Tidwell, Richard R.
supporting information, p. 957 - 971 (2017/02/19)
A previous publication from this lab (Patrick, et al. Bioorg. Med. Chem. 2016, 24, 2451-2465) explored the antitrypanosomal activities of novel derivatives of 2-(2-benzamido)ethyl-4-phenylthiazole (1), which had been identified as a hit against Trypanosoma brucei, the causative agent of human African trypanosomiasis. While a number of these compounds, particularly the urea analogues, were quite potent, these molecules as a whole exhibited poor metabolic stability. The present work describes the synthesis of 65 new analogues arising from medicinal chemistry optimization at different sites on the molecule. The most promising compounds were the urea derivatives of 2-aryl-benzothiazol-5-amines. One such analogue, (S)-2-(3,4-difluorophenyl)-5-(3-fluoro-N-pyrrolidylamido)benzothiazole (57) was chosen for in vivo efficacy studies based upon in vitro activity, metabolic stability, and brain penetration. This compound attained 5/5 cures in murine models of both early and late stage human African trypanosomiasis, representing a new lead for the development of drugs to combat this neglected disease.
Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)- thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors
Malmstroem, Jonas,Viklund, Jenny,Slivo, Can,Costa, Ana,Maudet, Mickael,Sandelin, Catrin,Hiller, Goesta,Olsson, Lise-Lotte,Aagaard, Anna,Geschwindner, Stefan,Xue, Yafeng,Vasaenge, Mervi
, p. 5919 - 5923 (2012/11/07)
4-(1,3-Benzothiazol-2-yl)thiophene-2-sulfonamide (4a) was found to be a moderately potent inhibitor of cyclin-dependent kinase 5 (cdk5) from a HTS screen. The synthesis and SAR around this hit is described. The X-ray coordinates of ligand 4a with cdk5 are also reported, showing an unusual binding mode to the hinge region via a water molecule.
New Compounds Useful for Treating CNS Disorders
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Page/Page column 10, (2011/05/05)
The present invention provides new compounds of formula (I) as well as a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds
