IP Library Granted Patent US 8,865,129
Granted Patent B2
US 8,865,129 · App. 13/464,718 · Granted Oct 21, 2014

Lanthanoid complex capsule and particle contrast agents, methods of making and using thereof

Inventor: Marc Anton Walters (New Rochelle, NY)
Assignee: New York University
C07D257/02A61K49/106A61K49/1809C07K5/003A61K9/5176A61K49/124A61K49/1881
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Quick Facts
Patent No.
US 8,865,129
App. No.
13/464,718
Granted
Oct 21, 2014
Kind
B2
Abstract

The invention relates to compositions of DOTA derivative compounds, lanthanoid-DOTA derivative molecular complex, and lanthanoid-complex encapsulated solid lipid particles or capsules, and methods of making and using the compositions. The solid lipid particles or capsules contain micelle cores stabilized by a hyperbranched polymer shell based from a crosslinked DOTA derivative compound or crosslinked lanthanoid-DOTA derivative complex. These solid lipid particles or capsules can be used in various applications, such as contrast agents or drug delivery vehicles.

Claims (22)

1. A compound of formula (I):

wherein R is H or a cation; R′ is mercaptoalkyl or radical of mercaptoalkyl, or alkylthioalkyl.

2. The compound of claim 1 , wherein R′ is C 2 H 4 —SH, —C 2 H 4 —S., or —C 2 H 4 —S—CH 3 .

3. The compound of claim 1 , wherein R is H, Li + , Na + , K + or NH 4 + .

4. A molecular complex comprising a molecule of formula (III):

and optionally a balancing counterion,

wherein M is a chelating metal ion and R′ is a polymer precursor group that is able to self-crosslink or crosslink in presence of one or more crosslinking agents.

5. The molecular complex of claim 4 , wherein the metal ion is a lanthanoid.

6. The molecular complex of claim 4 , wherein the metal ion is La, Eu, Tb, Gd, Ga, or In.

7. The molecular complex of claim 4 , wherein R′ is or substituted alkyl group.

8. The molecular complex of claim 4 , wherein R′ is hydroxyalkyl, mercaptoalkyl or radical of mercaptoalkyl, or alkylthioalkyl.

9. The molecular complex of claim 8 , wherein R′ is —CH 2 —OH, —C 2 H 4 —OH, —C 2 H 4 —S—CH 3 , —C 2 H 4 —SH, or —C 2 H 4 —S.

10. A hyperbranched polymeric nanoparticle or nanocapsule formed from the molecular complex of claim 4 .

11. A compound of formula (I):

wherein R is H or a cation; R′ is a polymer precursor group which is able to self-crosslink or crosslink in presence of one or more crosslinking agents, and

wherein the compounds of formula (I) are chiral.

12. The compound of claim 11 , wherein R′ is substituted alkyl group.

13. The compound of claim 11 , wherein R′ is hydroxyalkyl, mercaptoalkyl or radical of mercaptoalkyl, or alkylthioalkyl.

14. The compound of claim 11 , wherein R′ is —CH 2 —OH, —C 2 H 4 —OH, —C 2 H 4 —SH, —C 2 H 4 —S., or —C 2 H 4 —S—CH 3 .

15. The compound of claim 11 , wherein R is H, Li + , Na + , K + or NH 4 + .

16. The compound of claim 11 , wherein the compound is:

17. A compound of formula (II):

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 3, 2012
From: WALTERS, MARC ANTON
To: NEW YORK UNIVERSITY
Reel/Frame 028722/0914 →
Continuity (3)
Provisional Application 61482950 · May 5, 2011
Provisional Application 61604770 · Feb 29, 2012
Related Publication 20120294809A1 · Nov 22, 2012