Patent ID: 6054303
Filing Date: 2000-04-25
Classification: C07K,G01N,Y02A,Y10S

Abstract:
A cyclosporin compound conjugated to an organic radical at an alanine nitrogen atom of said cyclosporin, wherein said compound is useful in an immunological determination, and further wherein,said organic radical is an immunogenic carrier comprising a poly(amino acid) having a molecular weight greater than 2000; a ligand; a residue of a small organic compound, wherein said small organic compound has a molecular weight less than about 2000; or a label;said organic radical is conjugated to the cyclosporin through a linking group selected from the group consisting of:(A) an alkyleneoxide chain of the formula --(CH.sub.2).sub.n O--, wherein an alanine nitrogen atom of cyclosporin is conjugated to a carbon atom of the alkyleneoxide, n is an integer of 1 to 6, the alkyleneoxide oxygen atom is bound to a first end of from 1 to 3 carboxamide groups linked together by alkylene chains, and the organic radical is bound to a second end of the from 1 to 3 carboxamide groups; or(B) a carbonyloxybenzyl group of the formula: ##STR18## wherein an alanine nitrogen atom of cyclosporin is conjugated to the benzylic carbon atom, an oxygen atom of the carbonyloxy group is bound to a first end of from 1 to 3 carboxamide groups linked together by alkylene chains, and the organic radical is bound to a second end of the from 1 to 3 carboxamide groups;such that if the linking group is the carboxamide extended alkyleneoxide chain, then the alanine nitrogen is part of cyclosporin amino acid residue no. 7, and if the linking group is the carboxamide extended carbonyloxybenzyl group, then the alanine nitrogen is part of cyclosporin amino acid residue no. 7, 8, or nos. 7 and 8.