IP Library Granted Patent US 9,403,875
Granted Patent B2
US 9,403,875 · App. 12/695,125 · Granted Aug 2, 2016

Cage-like bifunctional chelators, copper-64 radiopharmaceuticals and PET imaging using the same

Inventors: Peter S. Conti (Pasadena, CA); Hancheng Cai (Alhambra, CA); Zibo Li (Logan, UT); Shuanglong Liu (Alhambra, CA)
Assignee: UNIVERSITY OF SOUTHERN CALIFORNIA
C07K7/086A61K51/0482A61K51/082A61K51/088C07D487/08C07K5/1021
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Quick Facts
Patent No.
US 9,403,875
App. No.
12/695,125
Granted
Aug 2, 2016
Kind
B2
Abstract

Disclosed is a class of versatile Sarcophagine based bifunctional chelators (BFCs) containing a hexa-aza cage for labeling with metals having either imaging, therapeutic or contrast applications radiolabeling and one or more linkers (A) and (B). The compounds have the general formula where A is a functional group selected from group consisting of an amine, a carboxylic acid, an ester, a carbonyl, a thiol, an azide and an alkene, and B is a functional group selected from the group consisting of hydrogen, an amine, a carboxylic acid, and ester, a carbonyl, a thiol, an azide and an alkene. Also disclosed are conjugate of the BFC and a targeting moiety, which may be a peptide or antibody. Also disclosed are metal complexes of the BFC/targeting moiety conjugates that are useful as radiopharmaceuticals, imaging agents or contrast agents.

Claims (9)

1. A chemical composition comprising:

wherein A is a carboxylic acid having the formula:

and wherein R 1 , R 2 , R 3 , and R 4 are independently selected from the group consisting of H, halogen, alkyl, alkoxy or alkene, and a salt or an ester thereof, and

B is a functional group selected from the group consisting of hydrogen, and amine, a carboxylic acid, an ester, a carbonyl, a thiol, an azide and alkene.

2. The chemical composition according to claim 1 , wherein R 1 , R 2 , R 3 , and R 4 are hydrogen.

3. A chemical composition comprising a molecule selected from the group consisting of:

and a salt or an ester thereof.

4. A radiopharmaceutical comprising a compound having the formula:

5. The radiopharmaceutical according to claim 4 , further comprising a carrier.

Assignments (3)
CONFIRMATORY LICENSE Recorded Apr 25, 2023
From: UNIVERSITY OF SOUTHERN CALIFORNIA
To: UNITED STATES DEPARTMENT OF ENERGY
Reel/Frame 063443/0493 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 7, 2016
From: LIU, SHUANGLONG
To: UNIVERSITY OF SOUTHERN CALIFORNIA
Reel/Frame 040593/0851 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 19, 2010
From: CONTI, PETER S.; CAI, HANCHENG; LI, ZIBO
To: UNIVERSITY OF SOUTHERN CALIFORNIA
Reel/Frame 024255/0264 →
Continuity (2)
Provisional Application 61147709 · Jan 27, 2009
Related Publication 20100196271A1 · Aug 5, 2010