200440-13-7Relevant academic research and scientific papers
Synthesis of thiazole analogues of the immunosuppressive agent (1R,25,3A)-2-acetyl-4(5)-(1,2,3,4-tetrahydroxybutyl)imidazole
Jeoffreys, George R.,Ung, Alison T.,Pyne, Stephen G.,Skelton, Brian W.,White, Allan H.
, p. 2281 - 2291 (1999)
The synthesis of four of the diastereoisomers of 2-acetyl-5-(l ,2,3,4-tetrahydroxybutyl)thiazole and two of the diastereoisomers of 2-acetyl-5-( 1,2,3,4,5-pentahydroxypentyl)thiazole and 2-acetyl-4-( 1,2,3,4,5-pentahydroxypentyl)thiazole are reported. These syntheses involve the condensation of 5- or 4-metallated 2-( 1,1 -dimethoxyethyl)thiazoles with 2,3-O-isopropylidene-D-erythrono-l,4-lactone or 5-O-(tert-butyldimethylsilyl)-2,3-O-isopropylideneD-ribonolactone followed by reductive ring-opening of the resulting lactols. The stereochemistries and structures of some key compounds have been determined by single crystal X-ray structural analysis.
Synthesis of 2-acetyl-5-(1,2,3,4,5,6-hexahydroxyhexyl)thiazoles
Ung, Alison T.,Pyne, Stephen G.,Jeoffreys, George R.,Skelton, Brian W.,White, Allan H.
, p. 297 - 303 (2011)
The syntheses of two diastereoisomers of 2-acetyl-5-(1,2,3,4,5,6- hexahydroxyhexyl)thiazole are reported. The synthesis of these diastereoisomers involved the coupling of 5-metallated 2-(1,1-dimethoxyethyl)thiazole with a Weinreb amide derived from d-gluconolactone, followed by asymmetric reduction of the ketone thus prepared. The stereochemistries and structures of some key compounds were determined by single-crystal X-ray structural analysis.
NLRP3 INHIBITORS
-
Page/Page column 74, (2020/06/10)
The present application relates to compounds with NLRP3inhibitory activity and to associated salts, solvates, prodrugs and pharmaceutical compositions. The present application further relates to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP3inhibition.
Synthesis and biological evaluation of thiazole derivatives as novel USP7 inhibitors
Chen, Chao,Song, Jiemei,Wang, Jinzheng,Xu, Chang,Chen, Caiping,Gu, Wei,Sun, Hongbin,Wen, Xiaoan
supporting information, p. 845 - 849 (2017/02/18)
Herpesvirus-associated Ubiquitin-Specific Protease (HAUSP, also called USP7) interacts with and stabilizes Mdm2, and represents one of the first examples that deubiquitinases oncogenic proteins. USP7 has been regarded as a potential drug target for cancer therapy. Inhibitors of USP7 have been recently shown to suppress tumor cell growth in vitro and in vivo. Based on leading USP7 inhibitors P5091 and P22077, we designed and synthesized a series of thiazole derivatives. The results of in vitro assays showed that the thiazole compounds exhibited low micromolar inhibition activity against both USP7 enzyme and cancer cell lines. The compounds induced cell death in a p53-dependent and p53-independent manner. Taken together, this study may provide thiazole compounds as a new class of USP7 inhibitors.
FUSED TRICYCLIC SILYL COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
-
Paragraph 0298; 0299, (2015/12/08)
no abstract published
ANTIVIRAL COMPOUNDS COMPOSED OF THREE LINKED ARYL MOIETIES TO TREAT DISEASES SUCH AS HEPATITIS C
-
Page/Page column 92-93, (2010/12/26)
The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56
ALKYNYL ALCOHOLS AS KINASE INHIBITORS
-
Page/Page column 178, (2010/01/30)
Selected compounds are effective for prophylaxis and treatment of inflammation and inflammatory disorders, such as NIK-mediated disorders. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, inflammation and the like.
THIAZOLES USEFUL AS INHIBITORS OF PROTEIN KINASES
-
Page 65; 82-83, (2010/02/08)
The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
