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Details for Patent: 6,093,383

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Details for Patent: 6,093,383

Title: Bisamine bisthiol radiolabel binding moieties
Abstract:This invention relates to bisamine bisthiol radiolabel binding moieties and synthetic methods therefor. Specifically, the invention provides radiolabel binding moieties that form an electrically neutral complex with technetium-99m.
Inventor(s): Dean; Richard T. (Bedford, NH), Buttram; Scott (Derry, NH), McBride; William (Manchester, NH), Lister-James; John (Bedford, NH), Civitello; Edgar R. (Londonderry, NH)
Assignee: Diatide, Inc. (Londonderry, NH)
Filing Date:Jun 06, 1995
Application Number:08/467,791
Claims:1. A composition of matter comprising a bisamino bisthiol radiolabel binding moiety having a formula selected from the group consisting of: ##STR7## wherein each R is independently H, CH.sub.3 or C.sub.2 H.sub.5 but if X=H, one R=Y;

(pgp).sup.N =an amine protecting group or H;

each (pgp).sup.S is independently a thiol protecting group or H;

m, n and p are independently 2 or 3;

X=H or --A--COOH, but if X=H, one R=Y and (pgp).sup.N is not H;

Y=--A--COOH;

A=linear or cyclic lower alkyl, aryl, heterocyclyl, combinations or substituted derivatives thereof, ##STR8## wherein each R is independently H, CH.sub.3 or C.sub.2 H.sub.5 but if Z=H, one R=Y;

each (pgp).sup.N is an amine protecting group or H;

each (pgp).sup.S is independently a thiol protecting group or H;

m, n and p are independently 2 or 3;

Z=H or --A--CH(V)NH(pgp).sub.2.sup.N, but if Z=H, one R=Y;

Y=--A--CH(V)NH(pgp).sub.2.sup.N ;

A=linear or cyclic lower alkyl, aryl, heterocyclyl, combinations or substituted derivatives thereof;

V=H or COOH;

and wherein if (pgp).sup.N and V are H, then (pgp).sup.S is not H and if (pgp).sup.S and V are H, then (pgp).sup.N is not H, and if V is H, (pgp).sub.1.sup.N is not H; and ##STR9## wherein each R is independently H, CH.sub.3 or C.sub.2 H.sub.5 and one R=Y;

each (pgp).sup.N is an amine protecting group or H;

each (pgp).sup.S is independently a thiol protecting group or H;

m, n and p are independently 2 or 3;

Y=--A--CH(V)NH(pgp).sub.2.sup.N ;

A=linear or cyclic lower alkyl, aryl, heterocyclyl, combinations or substituted derivatives thereof;

V=H or COOH;

and wherein if (pgp).sub.2.sup.N and V are H, then (pgp).sup.S is not H and if (pgp).sup.S and V are H, then (pgp).sub.2.sup.N is not H, and at least one (pgp).sub.1.sup.N moiety is not H;

wherein the radiolabel-binding moiety is capable of forming an electrically neutral complex with a technetium-99m.
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