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-9700244-A1 优先权日:1995-06-19 标题 :Process for parallel synthesis of a non-peptide library 发明人:FRITZ JAMES E; KALDOR STEPHEN W 权利人:LILLY CO ELI; FRITZ JAMES E; KALDOR STEPHEN W 摘要:A process for the sequential preparation of a library of compounds having pharmaceutical usage. The process involves the sequential mixing of solution phase reagents, followed by scavenging of excess unreacted reagents with solid phase scavenging agents. The process is highly iterative and applicable for producing various ureas, thiureas, amides, carbonates and tertiary amines.
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:US-5585487-A 优先权日:1995-05-26 标题:Method for the preparation of β-thiolactam compound 发明人:OISHI AKIHIRO; TAGUCHI YOICHI; SHIBUYA ISAO; TSUCHIYA TOHRU 权利人:AGENCY IND SCIENCE TECHN 摘要:Disclosed is a method for the preparation of a beta -thiolactam compound, i.e. a 7-substituted-2-oxa-7-azabicyclo [3.2.0]-heptan-6-thione, represented by the general formula in which R is an alkyl or aryl group, having usefulness as an intermediate for the synthesis of various biologically active compounds. The compound can be prepared by the reaction of an isothiocyanate compound R-NCS, R being the same as above, and 2,3-dihydrofuran, preferably, under pressurization up to 2000 atmospheres or higher at an elevated temperature.
专利号:WO-2024177606-A1 优先权日:2023-02-24 标 题:Quinazolinone derivative compounds showing anti-cancer activity and the synthesis methods of these compounds 发明人:EVREN ASAF EVRIM; YURTTAS LEYLA; AKALIN CIFTCI GULSEN; SAGLIK BEGUM NURPELIN 权利人:BILECIK SEYH EDEBALI UNIV; ANADOLU UNIV 摘要:The invention relates to quinazolinone-derived compounds that show anticancer activity on the adenocarcinoma human alveolar basal epithelial cell line (A549) by inducing apoptosis in lung cancer cells through inhibition of the epidermal growth factor receptor (EGFR), and at the same time do not have any cytotoxic effects on healthy cells, and to the synthesis methods of these compounds The general structure of the compounds of the invention is shown by Formula (X).
摘要:Merino, P., Science of Synthesis, (2010) 45, 138. 摘要:Merino, P., Science of Synthesis, (2010) 45, 261. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2018) 2, 255. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2018) 2, 159. 摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 305.