.

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: 5,322,929

« Back to Dashboard

Details for Patent: 5,322,929

Title: Radiolabeled technetium chelates for use in renal function determinations
Abstract:The present invention is directed to novel radiopharmaceutical imaging agents incorporating Tc-99m as a radiolabel. In particular, the novel imaging agents disclosed herein have relatively high renal extraction efficiencies, and hence are useful for conducting renal function imaging procedures. The novel Tc-99m compounds of a present invention have the following general formula: ##STR1## wherein X is S or N; and wherein Y is --H or wherein Y is ##STR2## and where R.sub.1 is --H, --CH.sub.3, or --CH.sub.2 CH.sub.3 ; R.sub.2 is --H, --CH.sub.2 CO.sub.2 H, --CH.sub.2 CONH.sub.2, --CH.sub.2 CH.sub.2 CO.sub.2 H, --CH.sub.2 CH.sub.2 CONH.sub.2, --CH.sub.3, --CH.sub.2 CH.sub.3, CH.sub.2 C.sub.6 H.sub.5, or --CH.sub.2 OH; and Z is --H, --CO.sub.2 H, --CONH.sub.2, --SO.sub.3 H, --SO.sub.2 NH.sub.2, or --CONHCH.sub.2 CO.sub.2 H; and the Tc is Tc-99m; and water-soluble salts thereof. Of the foregoing, the presently preferred Tc-99m compound of the present invention is Tc-99m-mercaptoacetylglycylglycylglycine (Tc-99m-MAGGG). The present invention is also directed to novel chelating agents that may be reacted with Tc-99m to form the foregoing compounds. Such novel chelating agents have the following general formula. ##STR3## where X and Y have the same definitions as above, and wherein Y' is --H.sub.2 when X is N, or wherein Y' is --H, or a suitable protective group such as --COCH.sub.3, --COC.sub.6 H.sub.5, --CH.sub.2 NHCOCH.sub.3, --COCF.sub.3, or --COCH.sub.2 OH when X is S. The present invention also provides methods for preparing and using the novel Tc-99m compounds.
Inventor(s): Fritzberg; Alan (Edmonds, WA), Kasina; Sudhaker (Kirkland, WA), Johnson; Dennis L. (Las Cruces, NM)
Assignee: University of Utah Research Foundation (Salt Lake City, UT)
Filing Date:Aug 03, 1989
Application Number:07/389,188
Claims:1. A ligand capable of reacting with a suitable Tc-99m-pertechnetate salt to form a Tc-99m chelate, said ligand having the general formula: ##STR18## where X is S; Y' is a protective group which protects the sulfur from oxidation; and Y is --H.sub.2 or Y is: ##STR19## and where R.sub.1 is --H, --CH.sub.3, or --CH.sub.2 CH.sub.3 ; R.sub.2 is --H, --CH.sub.2 CO.sub.2 H, --CH.sub.2 CONH.sub.2, --CH.sub.2 CH.sub.2 CO.sub.2 H, --CH.sub.2 CH.sub.2 CONH.sub.2, --CH.sub.3, --CH.sub.2 CH.sub.3, --CH.sub.2 C.sub.6 H.sub.5, or --OCH.sub.2 OH; and Z is --H, --CO.sub.2 H, --CONH.sub.2, --SO.sub.3 H, --SO.sub.2 NH.sub.2, or --CONHCH.sub.2 CO.sub.2 H.

2. A ligand as defined in claim 1, wherein the protective group is --COCH.sub.3, --COC.sub.6 H.sub.5, --CH.sub.2 NHCOCH.sub.3, or --COCH.sub.2 OH.

3. A ligand as defined in claim 1, where Y' is --COC.sub.6 H.sub.5, and Y is --CH.sub.2 CO.sub.2 H.

4. A ligand as defined in claim 1, wherein Y is --CH(CH.sub.3)CO.sub.2 H; --CH(CH.sub.2 CONH.sub.2)CO.sub.2 H; or --CH(CH.sub.2 CH.sub.2 CONH.sub.2)COOH.

5. A ligand capable of reacting with a suitable Tc-99m-pertechnetate salt to form a Tc-99m chelate, said ligand having the general formula: ##STR20## where X is N; Y' is --H.sub.2 ; and Y is: ##STR21## and wherein R.sub.1 and R.sub.2 are --H and Z is --H.

6. A ligand capable of reacting with a suitable Tc-99m-pertechnetate salt to form a Tc-99m chelate, said ligand having the general formula: ##STR22## where X is N; Y' is --H.sub.2 ; and Y is: ##STR23## and wherein R.sub.1 and R.sub.2 are --H and Z is --SO.sub.3 H.

7. A ligand capable of reacting with a suitable Tc-99m-pertechnetate salt to form a Tc-99m chelate, said ligand having the general formula: ##STR24## where X is N; Y' is --H.sub.2 ; and Y is: ##STR25## and wherein R.sub.1 and R.sub.2 are --H and Z is --SO.sub.2 NH.sub.2.
« 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