Compositions, methods, and systems for the synthesis and use of imaging agents

Patent metadata

Field	Value
Publication number	US-11174223-B2
Application number	US-201715593540-A
Country	US
Kind code	B2
Filing date	May 12, 2017
Priority date	May 11, 2010
Publication date	Nov 16, 2021
Grant date	Nov 16, 2021

Abstract

The present invention generally relates to novel synthetic methods, systems, kits, salts, and precursors useful in medical imaging. In some embodiments, the present invention provides compositions comprising an imaging agent precursor, which may be formed using the synthetic methods described herein. An imaging agent may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 18F. In some cases, an imaging agent including salt forms (e.g., ascorbate salt) may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.

First claim

The invention claimed is:

1. An ascorbate salt of formula (VII):

wherein X ⊖ is ascorbate, optionally, wherein the fluorine is isotopically enriched with 18 F.

2. A pharmaceutically acceptable composition comprising the salt of claim 1 , and optionally a pharmaceutically acceptable excipient.

3. A composition comprising the salt of claim 1 for imaging a portion of a subject.

4. A method of imaging a subject, comprising:
administering a dose of a pharmaceutically acceptable composition comprising the salt of claim 1 and optionally a pharmaceutically acceptable excipient; and
acquiring at least one image of a portion of the subject.

5. The method of claim 4 , wherein the maximum dose of the salt is approximately 13 mCi or less.

6. The method of claim 4 , wherein the dose is between 8 mCi and 13 mCi.

7. The method of claim 4 , wherein the portion of the subject is at least a portion of the cardiovascular system, at least a portion of the heart, or at least a portion of a tumor.

8. A method for detecting norepinephrine transporter (NET) in a portion of a subject, the method comprising:
administering a dose of a pharmaceutically acceptable composition comprising the salt of claim 1 and optionally a pharmaceutically acceptable excipient; and
acquiring at least one image of the portion of the subject, wherein the image detects NET in the subject.

Assignees

• Lantheus Medical Imaging Inc

Inventors

• Purohit Ajay
• Benites Pedro
• Radeke Heike S
• Lazewatsky Joel
• Lee L Veronica

Classifications

• C07D307/58

  One oxygen atom, e.g. butenolide · CPC title

• C07C309/04

  containing only one sulfo group · CPC title

• C07C53/06

  Salts thereof · CPC title

• C07C309/73 Primary

  to carbon atoms of non-condensed six-membered aromatic rings · CPC title

• C07C277/08

  of substituted guanidines · CPC title