专利号:US-2005119332-A1 优先权日:1998-03-12 标 题 :Substituted thiophene compounds as modulators of protein tyrosine phosphatases (PTPases) 发明人:JEPPESEN LONE; ANDERSEN HENRIK S; OLSEN OLE H; JUDGE LUKE M; HOLSWORTH DANIEL D; BAKIR FARID; AXE FRANK U; GE YU 摘要:The present invention provides novel compounds of formula 1a, n nnovel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
专利号:US-2002165398-A1 优先权日:1998-03-12 标题:Modulators of protein tyrosine phosphatases (PTPases) 发明人:JEPPESEN LONE; ANDERSEN HENRIK SUNE; OLSEN OLE HVILSTED; JUDGE LUKE MILBURN; HOLSWORTH DANIEL DALE; BAKIR FARID; AXE FRANK URBAN; GE YU 摘要:The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. n The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimers disease and schizophrenia, and infectious diseases.
专利号:WO-9635659-A1 优先权日:1995-05-12 标 题 :Amination of electrophilic aromatic compounds by vicarious nucleophilic substitution 发明人:MITCHELL ALEXANDER R; PAGORIA PHILLIP F; SCHMIDT ROBERT D 权利人:UNIV CALIFORNIA; MITCHELL ALEXANDER R; PAGORIA PHILLIP F; SCHMIDT ROBERT D 摘要:The present invention relates to a process to aminate electrophilic aromatic compounds by vicarious nucleophilic substitution of hydrogen using quaternary hydrazinium salts. The use of trimethylhydrazinium iodide, as well as hydroxylamine, alkoxylamines, and 4-amino-1,2,4-triazole to produce aminated aromatic structures, such as 1,3-diamino-2,4,6-trinitrobenzene (DATB), 1,3,5-triamino-2,4,6-trinitrobenzene (TATB) and 3,5-diamino-2,4,6-trinitrotoluene (DATNT), is described. DATB and TATB are useful insensitive high explosives. TATB is also used for the preparation of benzenehexamine, a starting material for the synthesis of novel materials (optical imaging devices, liquid crystals, ferromagnetic compounds).
专利号:US-6069277-A 优先权日:1995-05-12 标 题 :Amination of electrophilic aromatic compounds by vicarious nucleophilic substitution 发明人:MITCHELL ALEXANDER R; PAGORIA PHILIP F; SCHMIDT ROBERT D 权利人:UNIV CALIFORNIA 摘要:The present invention relates to a process to aminate electrophilic aromatic compounds by vicarious nucleophilic substitution of hydrogen using quaternary hydrazinium salts. The use of trialkylhydrazinium halide, e.g., trimethylhydrazinium iodide, as well as hydroxylamine, alkoxylamines, and 4-amino-1,2,4-triazole to produce aminated aromatic structures, such as 1,3-diamino-2,4,6-trinitrobenzene (DATB), 1,3,5-triamino-2,4,6-trinitrobenzene (TATB) and 3,5-diamino-2,4,6-trinitrotoluene (DATNT), is described. DATB and TATB are useful insensitive high explosives. TATB is also used for the preparation of benzenehexamine, a starting material for the synthesis of novel materials (optical imaging devices, liquid crystals, ferromagnetic compounds).
专利号:US-5569783-A 优先权日:1995-05-12 标 题:Vicarious nucleophilic substitution to prepare 1,3-diamino-2,4,6-trinitrobenzene or 1,3,5-triamino-2,4,6-trinitrobenzene 发明人:MITCHELL ALEXANDER R; PAGORIA PHILIP F; SCHMIDT ROBERT D 权利人:UNIV CALIFORNIA 摘要:The present invention relates to a process to produce 1,3-diamino-2,4,6-trinitrobenzene (DATB) or 1,3,5-triamino-2,4,6,-trinitrobenzene (TATB) by: n (a) reacting at ambient pressure and a temperature of between about 0° and 50° C. for between about 0.1 and 24 hr, a trinitroaromatic compound of structure V: ##STR1## wherein X, Y, and Z are each independently selected from --H, or --NH 2 , with the proviso that at least 1 or 2 of X, Y, and Z are hydrogen, n with an amount effective to produce DATB or TATB of 1,1,1-trialkylhydrazinium halide wherein alkyl is selected from methyl, ethyl, propyl or butyl and halide is selected from chloride, bromide or iodide. n in the presence of a strong base selected from sodium butoxide, potassium butoxide, potassium propoxide, sodium propoxide, sodium ethoxide, potassium ethoxide, sodium methoxide, potassium methoxide, and combinations thereof; n in a solvent selected from the group consisting of methanol, ethanol, propanol, butanol, dimethylsulphoxide, N-methylpyrrolidone, hexamethylphosphoramide, dimethylformide, dimethylacetamide and mixtures thereof, provided that when alcohols are present primarily DATB and picramide is formed; and (b) isolating the DATB or TATB produced. DATB and TATB are useful specialty explosives. TATB is also used for the preparation of benzenehexamine, a starting material for the synthesis of novel materials (optical imaging devices, liquid crystals, ferromagnetic compounds).
专利号:US-2013267712-A1 优先权日:2012-04-02 标题 :Aromatic ketone synthesis with amide reagents and related reactions 发明人:KLUMPP DOUGLAS A; RAJA ERUM K 权利人:KLUMPP DOUGLAS A; RAJA ERUM K; UNIV NORTHERN ILLINOIS 摘要:A method of preparing an aryl carbonyl or aryl thiocarbonyl compound, comprises reacting an N-(nitroaryl)-amide or N-(nitroaryl)-thioamide with an aromatic ring, with a superacid catalyst, to produce the aryl carbonyl or aryl thiocarbonyl compound. The superacid is present in an amount of at most 8 equivalents in proportion to the N-(nitroaryl)-amide or N-(nitroaryl)-thioamide. A method of preparing aryl amide or aryl thioamide, comprises reacting an N-(nitroaryl)-carbamide or N-(nitroaryl)-thiocarbamide with an aromatic ring, with a superacid catalyst, to produce the aryl amide or aryl thioamide.
[参考文献]: Dirk Volkmer, Et Al. Dinuclear Nickel(Ii) Complexes As Models For The Active Site Of Urease. Inorg Chem. 1996 Jun 19;35(13):3792-3803. [参考文献]: E Heymann, Et Al. Hydrolysis Of Aromatic Amides As Assay For Carboxylesterases-Amidases. Methods Enzymol. 1981:77:405-9. [参考文献]: Glendon B Hunsinger, Et Al. Improved Accuracy In High-Temperature Conversion Elemental Analyzer δ18O Measurements Of Nitrogen-Rich Organics. Rapid Commun Mass Spectrom. 2012 Mar 15;26(5):554-62. [参考文献]: R S Markin, Et Al. Short-Column Liquid Chromatographic Assay For Caffeine And Chloramphenicol In Serum. J Chromatogr. 1990 Feb 23;525(2):464-70. [参考文献]: Ross L Stein, Et Al. Enzymatic Hydrolysis Of P-Nitroacetanilide: Mechanistic Studies Of The Aryl Acylamidase From Pseudomonas Fluorescens. Biochemistry. 2002 Jan 22;41(3):991-1000.
合成参考文献
摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 281. 摘要:Cormier, M.; Goddard, J.-P., Science of Synthesis, (2020) , 132. 摘要:Tang, R.-Y., Science of Synthesis: Knowledge Updates, (2024) 1, 413. 摘要:Li, Y.; Fang, X.; Wang, Y., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 70. 参考文献:10.1385/mb:33:2:103 摘要:Martins S, Karmali A, Andrade J, Serralheiro ML. Immobilized metal affinity chromatography of monoclonal immunoglobulin M against mutant amidase from Pseudomonas aeruginosa. Mol Biotechnol. 2006 Jun;33(2):103–14. doi: 10.1385/mb:33:2:103.