专利号:US-8138346-B2 优先权日:2006-08-16 标题 :Method for synthesis of 8-alkoxy-9H-isothiazolo[5,4-B]quinoline-3,4-diones 发明人:BRADBURY BARTON JAMES; WILES JASON ALLAN; HASHIMOTO AKIHIRO; WANG QIUPING; LUCIEN EDLAINE; PAIS GODWIN; KIM HA YOUNG 权利人:BRADBURY BARTON JAMES; WILES JASON ALLAN; HASHIMOTO AKIHIRO; WANG QIUPING; LUCIEN EDLAINE; PAIS GODWIN; KIM HA YOUNG; ACHILLION PHARMACEUTICALS INC 摘要:The present invention provides process for synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones of the Formula A. n nThe substituents R, R 5 , R 6 , R 7 , R 8 and R 9 are defined herein. The invention also provides novel synthetic intermediates useful in the synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones.
专利号:WO-2021161084-A1 优先权日:2020-02-16 标题 :N-(4-fluorophenyl)-5-phenyl-[1,2,4] triazolo [1,5-a] pyridine-2-carboxamide derivatives and their synthesis thereof 发明人:NINGEGOWDA RAGHU; BANUPRAKASH GOVINDAPPA; CHANDRASHEKHARAPPA SANDEEP 权利人:NINGEGOWDA RAGHU; BANUPRAKASH GOVINDAPPA; CHANDRASHEKHARAPPA SANDEEP 摘要:The present invention relates to the development of novel N-(4-fluorophenyl)-5-phenyl- [1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives for their different pharmacological activities. It particularly relates to the development of N-(4-fluorophenyl)-5-phenyl- [1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives as antiviral, anticancer, antifungal, hypoglycemic, anti-tubercular, sedative, anti-type 2 diabetes activity. It specifically relates to the N-(4-fluorophenyl)-5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives for treatment of H37Rv and multidrug-resistant (MDR) strains of Mycobacterium tuberculosis (MTB). The present invention also relates to the process for synthesis of N-(4-fluorophenyl)- 5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives. The invention further relates to method for treatment of method for treatment of diseases such as tuberculosis, type 2 diabetes, bacterial, viral and fungal infections. Invention addresses the challenges in working with chemical processes and products by inventing novel reaction methodology that can maximize the desired products and minimize by-products, designing new synthetic schemes that can simplify operations in chemical productions and seeking nontoxic reagent that are inherently environmentally and ecologically benign. Synthesis of novel N-(4- fluorophenyl)-5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives is being employed to develop a novel synthetic methodology and their pharmacological applications. Novel series of N-(4-fluorophenyl)-5-phenyl-[1,2,4]triazolo[l,5-a]pyridine-2-carboxamide derivatives were designed synthesized evaluated for their in vitro anti-mycobacterial activity against H37Rv and multi-drug-resistant (MDR) strains of mycobacterium tuberculosis (MTB). All the synthesized compounds were characterized by spectroscopic methods like Mass, NMR and elemental analysis.
专利号:US-9346851-B2 优先权日:2008-02-22 标 题 :Chemical modification of proteins 发明人:BERNARDES GONCALO; CHALKER JUSTIN; DAVIS BENJAMIN 权利人:BERNARDES GONCALO; CHALKER JUSTIN; DAVIS BENJAMIN; RP SCHERER TECHNOLOGIES LLC 摘要:The invention relates to methods for selectively converting a cysteine residue in a peptide or protein to the dehydroalanine (Dha) residue. The method also works on selenocysteine and substituted cysteine and selenocysteine residues, resulting in the Dha residue which may be converted to any natural or unnatural amino acid residue desired without the alteration of the remainder of the peptide or protein. The invention also allows ligation of a desired peptide at any point rather than at a point where there should be a naturally occurring cysteine, thereby allowing native chemical ligation to be used in the synthesis of peptides that do not contain cysteine. The methodology allows for the synthesis of very large peptides.
专利号:US-9243002-B2 优先权日:2013-02-07 标题 :Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C 发明人:DAI XING; LIU HONG; PALANI ANANDAN; HE SHUWEN; BROCKUNIER LINDA L; NARGUND RAVI; MARCANTONIO KAREN; ZORN NICOLAS; XIAO DONG; PENG XUANJIA; LI PENG; GUO TAO 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
专利号:US-5684195-A 优先权日:1994-07-14 标 题:Method of preparing sulfmonamides from sulfones 发明人:HUANG HORNG-CHIH; HARRING SCOTT R 权利人:SEARLE & CO 摘要:A one-pot synthesis of sulfonamides from sulfones has been developed. Conversion of sulfones to the corresponding sulfinic acid salts is followed by oxidative-amination to give the sulfonamides.
专利号:US-2008071086-A1 优先权日:2006-08-16 标 题 :Method for synthesis of 8-alkoxy-9h-isothiazolo[5,4-b]quinoline-3,4-diones
摘要:Sainsbury, M., Science of Synthesis Knowledge Updates, (2010) 1, 223. 摘要:Ochoa, C. I.; Tambar, U. K., Science of Synthesis Knowledge Updates, (2020) 2, 337. 参考文献:10.1007/s41061-017-0111-1 摘要:Marmelstein AM, Moreno J, Fiedler D. Chemical Approaches to Studying Labile Amino Acid Phosphorylation. Top Curr Chem (Cham). 2017 Apr;375(2):22. doi: 10.1007/s41061-017-0111-1.