专利号:US-7678789-B2 优先权日:2005-02-11 标 题 :[1,2,4]-dithiazoli(di)ne derivatives, inducers of gluthathione-S-transferase and NADPH quinone oxido-reductase, for prophylaxis and treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular 发明人:FEENSTRA ROELOF W; KEIZER HISKIAS G; PRAS-RAVES MARIA L; VAN VLIET BERNARD J; VAN SCHARRENBURG GUSTAAF J M 权利人:SOLVAY PHARM BV 摘要:The present invention relates to 5-imino-5H-[1,2,4]-dithiazol-3-yl-amine and [1,2,4]-dithiazolidine-3,5-diylidene-diamine derivatives as inducers of gluthathione-S-transferase (GST) and NADPH quinone oxidoreductase (NQO), to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said [1,2,4]-dithiazoli(di)ne derivatives. The invention also relates to the use of a compound disclosed herein for the treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular. The invention relates to compounds of the general formula (I): n nwhereinn nwherein the symbols have the meanings given in the specification.
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:EP-1851209-B1 优先权日:2005-02-11 标题:[1,2,4]-dithiazoli(di)ne derivatives, inducers of gluthathione-s-transferase and nadph quinone oxido-reductase, for prophylaxis and treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular 发明人:FEENSTRA ROELOF W; KEIZER HISKIAS G; PRAS-RAVES MARIA L; VAN VLIET BERNARD J; VAN SCHARRENBURG GUSTAAF J 权利人:ABBOTT HEALTHCARE PRODUCTS BV 摘要:The present invention relates to 5-imino-5H-[1,2,4]-dithiazol-3-yl-amine and [1,2,4]- dithiazolidine-3,5-diylidene-diamine derivatives as inducers of glutha-thione-S- transferase (GST) and NADPH quinone oxidoreductase (NQO), to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said [1,2,4]-dithiazoli(di)ne derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament useful in the for prophylaxis and treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular. The invention relates to compounds of the general formula (I): wherein the symbols have the meanings given in the specification.
专利号:US-7147856-B2 优先权日:1996-08-28 标题 :Stable radioiodine conjugates and methods of their synthesis 发明人:GOVINDAN SERENGULAM V 权利人:IMMUNOMEDICS INC 摘要:Methods are described for conjugating radioiodinated peptides or carbohydrate structures to proteins with improved yields and qualities of conjugates. In one method, specially designed radioiodinated bifunctional peptides containing nonmetabolizable amide bonds are coupled to antibodies. In a second method, radioiodinated nonmetabolizable bifunctional peptides, which also contain aminopolycarboxylates, are coupled to antibodies. In a third method, radioiodinated bifunctional aminopolycarboxylates are coupled to antibodies. In a fourth method, a hydrazide-appended antibody is coupled to a radioiodinated carbohydrate or a thiolated antibody is coupled to a hydrazide-appended and radioiodinated carbohydrate. In a fifth method a monoderivatized cyanuric chloride is used to conjugate thiolated antibody. Radioiodinated residualizing antibody conjugates made by these methods are particularly stable in vivo and are suitable for radioimmunodetection and radioimmunotherapy.
专利号:WO-0051976-A1 优先权日:1999-03-03 标 题 :Regioselective synthesis of dtpa derivatives
专利号:US-6663866-B1 优先权日:1996-08-28 标题:Stable radioiodine conjugates and methods for their synthesis 发明人:GOVINDAN SERENGULAM V 权利人:IMMUNOMEDICS INC 摘要:Methods are described for conjugating radioiodinated peptides to non-metabolizable carbohydrates with improved yields and qualities of conjugates. Radioiodinated residualizing antibody conjugates comprising a carbohydrate-appended peptide are also provided. The instant radioiodinated residualizing antibody conjugates are particularly stable in vivo and are suitable for radioimmunodetection and radioimmunotherapy.
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, 419. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 366. 摘要:Aitken, R. A., Science of Synthesis Knowledge Updates, (2018) 3, 327. 摘要:Braverman, S.; Cherkinsky, M., Science of Synthesis Knowledge Updates, (2014) 3, 290. 参考文献:10.1007/s11418-020-01443-4 摘要:Kurimoto S, Fujita H, Kawaguchi S, Sasaki YF, Nakamura T, Kubota T. Kamiohnoyneosides A and B, two new polyacetylene glycosides from flowers of edible Chrysanthemum "Kamiohno". Journal of Natural Medicines. 2020 Aug 17;75(1):167–72. doi: 10.1007/s11418-020-01443-4.