You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 29, 2024

Claims for Patent: 8,293,207


✉ Email this page to a colleague

« Back to Dashboard


Summary for Patent: 8,293,207
Title:Radiometal-labeled amino acid analogs, imaging and therapeutic agents incorporating the same, and methods using the same
Abstract: An amino acid analog is provided, in syn-stereoisomeric form, anti-stereoisomeric form, or a combination thereof. The amino acid analog includes a cyclobutane ring with at least one of an amine group and a carboxyl group attached to one carbon node of the cyclobutane ring. A chain of moieties X, Y, and Z attached to one of remaining three carbon nodes of the cyclobutane ring. X is a chelating agent selected from a group comprising DCTA, DOTA, DTPA, EDTA, NOTA, PCTA, and TETA. Y is a linking moiety selected from a group comprising --NH--CO-- and --NH-p-CHSN-Bn- where the linking moiety facilitates incorporation of the chelating agent into the amino acid analog. Z is a metal radioisotope selected from a group comprising Cu-60, Cu-61, Cu-62, Cu-64, Cu-67, Ga-67, Ga-68, Y-86, Y-88, Y-90, Sr-85, Sr-89, Gd-153, Gd-157, Sm-153, Lu-177, W-185, Re-186, Re-188, and Ir-192.
Inventor(s): Zavarzin; Valery (Newton, MA), Weinberg; Irving (Besthesda, MD)
Assignee:
Application Number:12/562,788
Patent Claims:1. An amino acid analog, in at least one of syn-stereoisomeric form, anti-stereoisomeric form, or a combination thereof, comprising: a cyclobutane ring with at least an amine group and a carboxyl group attached to one carbon node of the cyclobutane ring and a chain of moieties Y-X-Z attached to one of remaining three carbon nodes of the cyclobutane ring, wherein X is 1,4,7-triazacyclononane, wherein Y is --NH-p-CHSN-benzene, and wherein Z is a metal radioisotope selected from the group consisting of Cu-61, Cu-62, Cu-64, and Ga-68.

2. The amino acid analog of claim 1, further comprising at least one moiety R selected from the group consisting of of CH.sub.3, C.sub.2H.sub.5, C.sub.3H.sub.8, and C.sub.4H.sub.10, wherein R is attached to one of the remaining two carbon nodes on the cyclobutane ring.

3. A diagnostic composition for tumor imaging comprising the amino acid analog of claim 1 and a carrier.

4. A kit for production of a radiopharmaceutical, comprising: a septum closed vial containing at least one of a lyophilized or freeze-dried amino acid analog according to claim 1; an excipient; at least one compound providing pH adjustment to the range 5.0-7.8 and additionally providing adjustment to physiological isotonicity for injection when admixed with a volume of sterile water, wherein the at least one compound reconstitutes the vial contents by bringing the vial contents into solution.

5. A method of tumor imaging by at least one of positron emission tomography (PET) or single photon emission tomography (SPECT), comprising: (a) administering to a subject, a tumor-revealing amount of the amino acid analog of claim 1; (b) allowing sufficient time for biodistribution in the subject; and (c) measuring distribution of the amino acid analog by means of PET or SPECT.

6. A method of tumor radiotherapy comprising administering an effective amount of the amino acid analog of claim 1 and a radioisotope to a subject having a tumor.

7. An amino acid analog, in at least one of syn-stereoisomeric form, anti-stereoisomeric form, or a combination thereof, comprising: cyclobutane ring of the formula ##STR00010## wherein X is 1, 4, 7-triazacyclononane wherein Y is --NH-p-CHSN-benzene, and wherein Z is a metal radioisotope selected from the group consisting of Cu-61, Cu-62, Cu-64, and Ga-68.

8. The amino acid analog of claim 7 further comprising at least one moiety R selected wherein the cyclobutane ring has the formula ##STR00011## and R is selected from the group consisting of CH.sub.3, C.sub.2H.sub.5, C.sub.3H.sub.8, or C.sub.4H.sub.10.

Make Better Decisions: Try a trial or see plans & 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 verification 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.