专利号:US-5635157-A 优先权日:1992-04-13 标 题 :Synthesis of 4-substituted-trans-1,2-diaminocyclohexyl polyaminocarboxylate metal chelating agents for the preparation of stable radiometal antibody immunoconjugates for therapy and spect and pet imaging 发明人:MEASE RONNIE C; KOLSKY KATHRYN L; MAUSNER LEONARD F; SRIVASTAVA SURESH C 摘要:Cyclohexyl chelating agents useful in forming antibody-metal conjugates useful for diagnostic and therapeutic purposes. New compounds and processes of forming these compounds are disclosed including 4-haloacetamido-trans-1,2-diaminocyclohexyl polyaminocarboxylate and 4-isothiocyanato-trans-1,2-diamino cyclohexane-N, N, N', N'-tetra acetic acid.
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: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: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.
专利号:US-5292938-A 优先权日:1992-04-13 标题 :Synthesis of 4-substituted-trans-1, 2-diaminocyclohexyl polyaminocarboxylate metal chelating agents for the preparation of stable radiometal antibody immunoconjugates for therapy and spect and pet imaging
专利号:DD-294021-A5 优先权日:1990-05-02 标题 :PROCESS FOR SYNTHESIS OF 1- (4,7-DIMETHYL-2-OXO-2H-CHROMEN-6-YLOXYACETYL) -4-SUBSTITUTED -THIOSEMICARBAZIDES