专利号:US-2016194279-A1 优先权日:2012-12-09 标 题 :One pot process for the conversion of aroyl chlorides to acyl thioureas 发明人:CHEPURI VENKATA RAMANA; BEERAN SENTHILKUMAR 权利人:COUNCIL SCIENT IND RES 摘要:The present invention disclose an improved one pot process for synthesis of acyl thioureas of formula (I), with yield greater than 80%, from aroyl chlorides of formula (I) wherein, R′ is an aryl or a heteroarylene group substituted with one or more groups selected from hydrogen, alkyl, alkylene, alkynyl, alkoxy, alkenyloxy, halo, hydroxyl, nitro, amino, carboxyl, ester, halogenated hydrocarbon or an aryl or heteroaryl; R″ and R′″ are selected independently from hydrogen, alkyl, alkylene, alkynyl, alkoxy, alkenyloxy, halo, hydroxyl, nitro, amino or halogenated hydrocarbon.
专利号:US-7179918-B2 优先权日:2001-06-11 标 题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis 发明人:CANAN KOCH STACIE S; ALEXANDER THERESE N; BURKE BENJAMIN J; JEWELL TANYA M; KUCERA DAVID J; LINTON MARIA ANGELICA; MITCHELL JR LENNERT J; REICH SIEGFRIED H; SKALITZKY DONALD J; TATLOCK JOHN H; VARNEY MICHAEL D; VIRGIL SCOTT C; WEBBER STEPHEN E; WORLAND STEPHEN T; BARVIAN MARK; BOLTON GARY; BOYER JR FREDERICK EARL; MACHAK JEFFREY J; HOLLER TOD; MURPHY SEAN T; MELNICK MICHAEL; JOSYULA VARA PRASAD 权利人:AGOURON PHARMA 摘要:Compounds of the formula: n nwhere the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.
专利号:WO-9948868-A9 优先权日:1998-03-26 标 题 :Heterocyclic classes of compounds for the modulating tyrosine protein kinase 发明人:FONG ANNIE; HANNAH ALISON; HARRIS G DAVIS; HIRTH PETER; HUBBARD STEVEN R; LANGECKER PETER; LIANG CONGXIN; MCMAHON GERALD; MOHAMMADI MOOSA; SCHLESSINGER JOSEPH; SHAWVER LAURA K; SUN LI; TANG PENG C; ULLRICH AXEL 权利人:SUGEN INC; UNIV NEW YORK; MAX PLANCK INST FUR BIOCHEMIE; FONG ANNIE; HANNAH ALISON; HARRIS G DAVIS; HIRTH PETER; HUBBARD STEVEN R; LANGECKER PETER; LIANG CONGXIN; MCMAHON GERALD; MOHAMMADI MOOSA; SCHLESSINGER JOSEPH; SHAWVER LAURA K; SUN LI; TANG PENG C; ULLRICH AXEL 摘要:The invention relates to certain indolinone-based and pyrazolylamide-based compounds, their method of synthesis, and combinatorial libraries consisting of the compounds. The invention also relates to methods of modulating the function of protein kinases using these compounds and methods of treating diseases by modulating the function of protein kinases and related signal transduction pathways.
专利号:EP-4630405-A1 优先权日:2022-12-06 标题 :Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels
专利号:WO-2012014114-A1 优先权日:2010-07-30 标 题:Matrix metalloproteinase inhibitors 发明人:KHERA MANOJ KUMAR; SATTIGERI JITENDRA; SATTIGERI VISWAJANANI; YADAV NEERAJ KUMAR; KUMAR KEWAL; RAUF ABDUL REHMAN ABDUL; CLIFFE IAN A; BHATNAGAR PRADIP KUMAR; RAY ABHIJIT; SRIVASTAVA PUNIT; DASTIDAR SUNANDA GHOSH 权利人:RANBAXY LAB LTD; KHERA MANOJ KUMAR; SATTIGERI JITENDRA; SATTIGERI VISWAJANANI; YADAV NEERAJ KUMAR; KUMAR KEWAL; RAUF ABDUL REHMAN ABDUL; CLIFFE IAN A; BHATNAGAR PRADIP KUMAR; RAY ABHIJIT; SRIVASTAVA PUNIT; DASTIDAR SUNANDA GHOSH 摘要:The present invention relates to certain hydroxy propionic acid derivatives and the processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, dry eye, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by over-expression and over activation of a matrix metalloproteinase using the compounds.
专利号:WO-2012094334-A1 优先权日:2011-01-04 标题 :One-step 18f labeling of biological substrates and uses of 18f labeled biological substrates 发明人:CHEN XIAOYUAN; JACOBSON WEISS ORIT 权利人:US HEALTH; CHEN XIAOYUAN; JACOBSON WEISS ORIT 摘要:Disclosed is a rapid one-step 18 F radiolabeling method for biological substrates that contain a specific arene group activated for nucleophilic aromatic substitution with 18 F. The method involves reacting a biological substrate having at least one 4-nitro-3-trifluorobenzamide moiety covalently bonded thereto with a 18 F anion in the presence of a cryptand. The method of the present invention has one or more advantages: significantly shortens reaction and overall synthesis time; requires low amount of precursor; and provides acceptable yields of high specific activity product. Also disclosed are methods of identifying a cell or population of cells expressing a protein or peptide of interest and methods for diagnosing a disease in a subject. Further disclosed are 18 F labeled compounds of formula (I): wherein X, n, R 1 , R 2 , and R 3 are as described herein.
[参考文献]: D Rouquié, Et Al. Thyroid Tumor Formation In The Male Mouse Induced By Fluopyram Is Mediated By Activation Of Hepatic Car/pxr Nuclear Receptors. Regul Toxicol Pharmacol. 2014 Dec;70(3):673-80.
合成参考文献
摘要:Glushkov, V. A.; Shklyaev, Yu. V., Science of Synthesis Knowledge Updates, (2018) 3, 254. 摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 286.