29083-18-9Relevant academic research and scientific papers
Preparation method and medical application of benzisothiazole and benzothiophene
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Paragraph 0166; 0170; 0171, (2021/08/19)
The invention discloses a preparation method and medical application of benzisothiazole and benzothiophene, and telates to the field of pharmaceutical chemistry. According to the invention, benzisothiazole and benzothiophene are the first type of HIF-2 agonists; compared with a compound M1001 found by the applicant in the earlier stage, the invention has better HIF-2 agonist activity, and has remarkable enhancement activity on expression of mRNA and protein of EPO, VGEF, Glut1, NDRG1 and the like at the downstream of HIF-2, so that the invention can be used for preparing drugs for treating and/or preventing chronic kidney diseases/chronic renal anemia, dyslipidemia and high cholesterol caused by abnormal expression of HIF-2; and the method has a good industrialization prospect.
Oxidative cyclization of N-alkyl-o-methyl-arenesulfonamides to biologically important saccharin derivatives
Xu, Liang,Shu, Hong,Liu, Ying,Zhang, Suhong,Trudell, Mark L.
, p. 7902 - 7910 (2007/10/03)
Various biologically important saccharin skeletons and their N-alkyl derivatives have been efficiently prepared by chromium(VI) oxide catalyzed H5IO6 oxidation of N-alkyl-o-methyl-arenesulfonamides in acetonitrile. N-tert-Butyl saccharin skeletons were easily prepared by H5IO6-CrO3 oxidation of N-tert-butyl-o-methyl arenesulfonamides in the presence of acetic anhydride. The method that furnished the novel fluoro and trifluoromethyl substituted saccharin skeletons is characterized by two steps, a simple work-up procedure, a single purification and good overall yields from substituted toluene derivatives.
INDOLE ACETIC ACIDS EXHIBITING CRTH2 RECEPTOR ANTAGONISM AND USES THEREOF
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Page/Page column 64-65, (2008/06/13)
The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metab
Synthesis of fused sulfonamide (1,1-dioxoisothiazole)substituted 1,5-diarylpyrazoles as cyclooxygenase inhibitors
Pal, Manojit,Veeramaneni, Venugopal Rao,Kumar, Sanjeev,Lohray, Vidya B.,Yeleswarapu, Koteswar Rao
, p. 1095 - 1101 (2007/10/03)
First synthesis of novel 1,1-dioxo-2,3-dihydrobenzo[d] isothiazolyl substituted 1,5-diarylpyrazoles has been accomplished via oxidative cyclization of 4-fluoro-2-methyl benzenesulfonamide followed by the treatment with hydrazine and then with 1,3-dicarbon
