专利号:WO-9740025-A1 优先权日:1996-04-19 标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA 摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-5135737-A 优先权日:1986-11-10 标 题:Amplifier molecules for enhancement of diagnosis and therapy 发明人:KEANA JOHN F W 权利人:OREGON STATE 摘要:Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines. Via such chemistry, the amplifiers are attachable to monoclonal antibodies for concentration of pharmacologically active groups at a desired site in the body.
专利号:WO-9403593-A1 优先权日:1992-08-04 标题 :Amplifier molecules for enhancement of diagnosis and therapy 发明人:KEANA JOHN F W 权利人:OREGON STATE 摘要:Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines. Via such chemistry, the amplifiers are attachable to monoclonal antibodies for concentration of pharmacologically active groups at a desired site in the body.
专利号:WO-2019081972-A1 优先权日:2017-08-09 标题:PROCESS FOR THE PREPARATION OF 4-NITROPHENYL ETHYLAMIDE MANDELIC ACID FROM 4-NITROBENZYL CYANIDE 发明人:HORAK RADIM; GREPL MARTIN; FUNK PETR; KORISTRK KAMIL; KVAPIL LUBOMIR; URBASEK MIROSLAV; HRADIL PAVEL 权利人:SANECA PHARMACEUTICALS A S 摘要:The invention relates to the preparation of a salt of 4-nitrophenylethylamine with (R) -mandelic acid and its use for the synthesis of mirabegron. The invention relates to the preparation of 4-nitrophenylethylamine (1) by reduction of 4-nitrobenzyl cyanide (7) in a solvent with the use of a borane generated in situ in a reaction mixture from NaBH 4 and BF 3 .And 2 O. the 4-nitrophenyl ethylamine (1) according to the present invention is isolated from the solution as a mandelate 3.
专利号:US-5412148-A 优先权日:1986-11-10 标题:Amplifier molecules derived from diethylene triaminepentaacetic acid for enhancement of diagnosis and therapy 发明人:KEANA JOHN F W 权利人:OREGON STATE 摘要:Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines. Via such chemistry, the amplifiers are attachable to monoclonal antibodies for concentration of pharmacologically active groups at a desired site in the body.
专利号:EP-1476197-B1 优先权日:2002-02-22 标题 :Synthesis of lipopolysaccharide-protein conjugate vaccines via the lipid a region following removal of the glycosidic phosphate residue 发明人:JENNINGS HAROLD; MIESZALA MALGORZATA; KOGAN GRIGORIJ; ZOU WEI; RICHARDS JAMES C; COX ANDREW; MOXON RICHARD 权利人:CA NAT RESEARCH COUNCIL 摘要:This invention relates to lipopolysaccharide-protein conjugate vaccines with appropriate presentation of conserved inner core oligosaccharide epitopes having improved immunogenic properties. These are based upon antigenic, detoxified bacterial lipopolysaccharides which optimally present an inner core oligosaccharide epitope following removal of at least a glycosidic phosphate of the lipid A region. These partially or completely dephosphorylated antigenic, detoxified bacterial lipopolysaccharides are linkable to an immunologically acceptable carrier and can be used in polyvalent or multivalent vaccines.
摘要:J.W. Eastes, M.H. Aldridge and M.J. Kamlet. J. Chem. Soc., B 1969, 922. 参考文献:10.1007/s10517-006-0011-9 摘要:Dovedova EL, Khrustalev DA, Khudoerkov RM. Effect of Delta-Sleep-Inducing Peptide on Activity of Enzymes of Biogenic Amine Metabolism in the Brain of Wistar and August Rats. Bulletin of Experimental Biology and Medicine. 2005 Nov;140(5):514–6. doi: 10.1007/s10517-006-0011-9.