| 摘要 |
PROBLEM TO BE SOLVED: To solve such a problem that none gives useful suggestions for solving the problem represented by the need of administering to the patient pharmaceutical formulations containing, as active ingredients, Fab fragments which are selectively and quantitatively functionalized only at desired specific sites of the molecule, thus showing a predefined precise substitution stoichiometry. SOLUTION: The invention provides chemical conjugates between an immunoglobulin Fab fragment and molecular compounds imparting diagnostic or therapeutic utility, whereby the only sites of conjugation on the Fab fragment are one or both of the sulfhydryl groups deriving from the selective and quantitative reduction of the inter-chain disulfide bond of the Fab fragment and whereby the molecular compounds imparting diagnostic or therapeutic utility have at least one free sulfhydryl-reactive group and are characterized in that the conjugation stoichiometric molar ratio of molecular compound to Fab fragment is in the range from 0.95 to 1.05 or in the range from 1.95 to 2.05. COPYRIGHT: (C)2011,JPO&INPIT
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