Details for Patent: 6,093,383
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| 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. |
