IP Library › Granted Patent US 12,544,463
Granted Patent B2
US 12,544,463 · App. 17/384,998 · Granted Feb 10, 2026

Deuterium substituted positron emission tomography (PET) imaging agents and their pharmacological application

Inventors: Zehui Wu (Philadelphia, PA); Zhihao Zha (Philadelphia, PA); Futao Liu (Philadelphia, PA); Karl Ploessl (Wilmington, DE); Seok Rye Choi (Aston, PA); Hank F. Kung (Springfield, PA)
Assignee: Five Eleven Pharma Inc.
A61K51/0455A61B6/037A61K51/04A61K51/0419A61K51/0431A61K51/0453C07B59/001C07B59/002C07B59/004C07C217/80C07C323/37C07D213/64C07D221/06C07D405/04C07D471/04C07B2200/05C07D277/66
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Quick Facts
Patent No.
US 12,544,463
App. No.
17/384,998
Granted
Feb 10, 2026
Kind
B2
Abstract

The present invention relates to deuterated compounds according to Formula I-A, Formula II-A, Formula II-D, and Formula III-A. These compounds can be used as PET imaging agents for evaluating Parkinson's Disease, Alzheimer Disease, and for determining specific serotonin reuptake inhibitor (SSRIi) activity for treatment of depression. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I-A, Formulae II-A, Formula II-D, or Formula III-A, or a pharmaceutically acceptable salt thereof.

Claims (26)

1 . A compound of Formula I-A:

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is methyl and is optionally substituted with one or more deuterium atoms;

X is —OTs; and

Y is (CD 2 ) 3 .

2 . The compound of claim 1 , having Formula I-B:

or a pharmaceutically acceptable salt thereof.

3 . The compound of claim 1 , having Formula I-C:

or a pharmaceutically acceptable salt thereof.

4 . The compound of claim 1 , wherein R 1 is CD 3 .

5 . A compound having Formula II-B:

or a pharmaceutically acceptable salt thereof, wherein:

Y is —[O(CR a R b ) 2 ] m —, wherein R a and R b are each independently hydrogen or deuterium atoms;

X is —OTs;

R 2 is CD 3 ;

m is 3; and

A 1 is N or CH.

6 . The compound of claim 5 , or a pharmaceutically acceptable salt thereof, wherein:

A 1 is N.

7 . The compound of claim 5 , or a pharmaceutically acceptable salt thereof, wherein A 1 is CH.

8 . The compound of claim 6 , or a pharmaceutically acceptable salt thereof, wherein Y is —[OCD 2 CD 2 ] 3 —.

9 . The compound of claim 5 , having Formula II-C:

or a pharmaceutically acceptable salt thereof, wherein:

A 1 is N or CH.

10 . The compound of claim 9 , or a pharmaceutically acceptable salt thereof, wherein A 1 is N.

11 . The compound of claim 9 , or a pharmaceutically acceptable salt thereof, wherein A 1 is CH.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 7, 2025
From: WU, ZEHUI; ZHA, ZHIHAO; LIU, FUTAO; PLOESSL, KARL; CHOI, SEOK RYE; KUNG, HANK F.
To: FIVE ELEVEN PHARMA INC.
Reel/Frame 072832/0954 →
Continuity (4)
Continuation 16824139 · Mar 19, 2020
Division 15994474 · May 31, 2018
Provisional Application 62513217 · May 31, 2017
Related Publication 20210346526A1 · Nov 11, 2021
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