.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 5,997,845

« Back to Dashboard

Details for Patent: 5,997,845

Title: Technetium-99M labeled peptides for imaging inflammation
Abstract:This invention relates to radiolabeled scintigraphic imaging agents, and methods and reagents for producing such agents. Specifically, the invention relates to specific binding compounds, including peptides, that bind to a platelet receptor that is the platelet GPIIb/IIIa receptor, methods and kits for making such compounds, and methods for using such compounds labeled with technetium-99m via a covalently-linked radiolabel-binding moiety to image thrombi in a mammalian body.
Inventor(s): Dean; Richard T. (Bedford, NH), Lister-James; John (Bedford, NH), Civitello; Edgar R. (Flagstaff, AZ)
Assignee: Diatide, Inc. (Londonderry, NH)
Filing Date:Jul 29, 1997
Application Number:08/902,367
Claims:1. A technetium-99m complex of a reagent comprising

a) a glycoprotein IIb/IIIa receptor-binding compound having a molecular weight of less than 10,000 daltons; and

b) a radiolabel binding moiety covalently linked to the compound; wherein the reagent binds to a platelet glycoprotein IIb/IIIa receptor with sufficient affinity that said reagent inhibits adenosine diphosphate-induced aggregation of human platelets by 50%, in a standard platelet aggregation assay, when the reagent is present at a concentration of no more than 0.3 .mu.M.

2. The complex of claim 1, wherein compound is a peptide comprising 4 to 100 amino acids.

3. The complex of claim 2, wherein the radiolabel binding moiety has a formula selected from the group consisting of:

wherein Cp is a protected cysteine and (aa) is any primary .alpha.- or .beta.-amino acid; a technetium-99m binding moiety comprising a single thiol moiety having a formula:

wherein

A is H, HOOC, H.sub.2 NOC, (peptide)--NHOC, (peptide)--OOC or R.sup.4 ;

B is H, SR, --NHR.sup.3, --N(R.sup.3)-(peptide), or R.sup.4 ;

X is H, SH, --NHR.sup.3, --N(R.sup.3)-(peptide) or R.sup.4 ;

Z is H or R.sup.4 ;

R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently H or lower straight or branched chain or cyclic alkyl;

n is 0, 1 or 2;

and

where B is --NHR.sup.3 or --N(R.sup.3)-(peptide), X is SH, and n is 1 or 2;

where X is --NHR.sup.3 or --N(R.sup.3)-(peptide), B is SH, and n is 1 or 2;

where B is H or R.sup.4, A is HOOC, H.sub.2 NOC, (peptide)--NHOC, (peptide)--OOC, X is SH, and n is 0 or 1;

where A is H or R.sup.4, then where B is SH, X is --NHR.sup.3 or --N(R.sup.3)-(peptide) and

where X is SH, B is --NHR.sup.3 or --N(R.sup.3)-(peptide);

where X is H or R.sup.4, A is HOOC, H.sub.2 NOC, (peptide)--NHOC, (peptide)--OOC and B is SH;

where Z is methyl, X is methyl, A is HOOC, H.sub.2 NOC, (peptide)--NHOC, (peptide)--OOC, B is SH and n is 0;

and wherein the thiol moiety is in the reduced form; ##STR7## wherein X.dbd.H or a protecting group;

(amino acid)=any amino acid; ##STR8## wherein X.dbd.H or a protecting group;

(amino acid)=any amino acid; ##STR9## wherein each R.sup.5 is independently H, CH.sub.3 or C.sub.2 H.sub.5 ;

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

m, n and p are independently 2 or 3;

A=linear lower alkyl, cyclic lower alkyl, aryl, or heterocyclyl, a combination thereof; ##STR10## wherein each R.sup.5 is independently H, lower alkyl having 1 to 6 carbon atoms, phenyl, or phenyl substituted with lower alkyl or lower alkoxy;

m, n and p are independently 1 or 2;

A=linear lower alkyl, cyclic lower alkyl, aryl, or heterocyclyl, a combination thereof;

V.dbd.H or --CO-peptide;

R.sup.6 .dbd.H or peptide;

and wherein when V.dbd.H, R.sup.6 =peptide and when R.sup.6 .dbd.H, V.dbd.--CO-peptide.

4. The complex of claim 1, wherein the peptide and the radiolabel binding moiety are covalently linked through from one to twenty amino acids.

5. The complex of claim 1, wherein the peptide is selected from the group consisting of: ##STR11##
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc