IP Library Granted Patent US 10,308,606
Granted Patent B2
US 10,308,606 · App. 15/699,124 · Granted Jun 4, 2019

PSMA-targeted NIR dyes and their uses

Inventors: Sumith A. Kularatne (West Lafayette, IN); Pravin Gagare (West Lafayette, IN)
Assignee: On Target Laboratories, LLC
C07D209/20A61K49/00A61K49/0032A61K49/0052A61K49/0054A61K49/0056G01N21/6428G01N33/57434G01N33/57492C07D209/24G01N2021/6439
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Quick Facts
Patent No.
US 10,308,606
App. No.
15/699,124
Granted
Jun 4, 2019
Kind
B2
Abstract

The present disclosure relates to prostate specific membrane antigen (PSMA) targeted compounds conjugated to near-infra red (NIR) dyes and methods for a method for synthesizing a compound of the formula:

Claims (27)

1. A method for synthesizing a compound of the formula:

wherein n is 0, 1, 2, 3, or 4;

further wherein R 3 , R 4 , and R 5 are independently selected from the group consisting of H + , Na + , K + , and NH 4 + ; R 6 , R 7 , R 8 , and R 9 are independently selected from the group consisting of H + , Na + , K + , and NH 4 + ; and R 10 H + ;

comprising the steps of:

(a) reacting a compound of formula I:

with a compound of formula:

in the presence of a polar organic solvent, 1-[Bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium 3-oxid hexafluorophosphate and N,N-Diisopropylethylamine under argon and

(b) reacting the resulting compound with sodium carbonate and a dye compound of the formula

2. The method of claim 1 , wherein the polar organic solvent is selected from the group consisting of dimethyl sulfoxide, dimethylformamide, and water.

3. A method for synthesizing an isotopic form of a compound of the formula:

wherein said isotopic form comprises one or more carbon and/or hydrogen isotopes selected from the group consisting of H 2 , H 3 , C 13 and C 14 ;

further wherein n is 0, 1, 2, 3, or 4;

further wherein R 3 , R 4 , and R 5 are independently selected from the group consisting of H + , Na + , K + , and NH 4 + ; R 6 , R 7 , R 8 , and R 9 are independently selected from the group consisting of H + , Na + ,K + , and NH 4 + ;and R 10 H + ;

comprising the steps of:

(a) reacting an isotopic form of a compound of formula:

wherein said isotopic form comprises one or more carbon and/or hydrogen isotopes selected from the group consisting of H 2 , H 3 , C 13 and C 14 ,

with an isotopic form of a compound of formula:

wherein said isotopic form comprises one or more carbon and/or hydrogen isotopes selected from the group consisting of H 2 , H 3 , C 13 and C 14 ,

in the presence of a polar organic solvent, 1-[Bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium 3-oxid hexafluorophosphate and N,N-Diisopropylethylamine under argon to provide an isotopic form of a compound that comprises one or more carbon and/or hydrogen isotopes selected from the group consisting of H 2 , H 3 , C 13 and C 14 ,

(b) reacting the isotopic form of the compound obtained in step (a) with sodium carbonate and an isotopic form of a dye compound of the formula:

wherein said isotopic form comprises one or more carbon and/or hydrogen isotopes selected from the group consisting of H 2 , H 3 , C 13 and C 14 .

4. A method for synthesizing a compound of the formula:

wherein n is 0, 1, 2, 3, or 4

(a) reacting a compound of formula

with a compound of formula:

in the presence of a polar organic solvent, 1-[Bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium 3-oxid hexafluorophosphate and N,N -Diisopropylethylamine under argon

(b) reacting the resulting compound thereof with sodium carbonate and a dye compound of the formula:

Assignments (2)
CHANGE OF NAME Recorded May 15, 2024
From: ON TARGET LABORATORIES, LLC
To: ON TARGET LABORATORIES, INC.
Reel/Frame 067419/0833 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 16, 2017
From: KULARATNE, SUMITH A.; GAGARE, PRAVIN
To: ON TARGET LABORATORIES, LLC
Reel/Frame 044150/0665 →
Continuity (2)
Provisional Application 62385528 · Sep 9, 2016
Related Publication 20180099934A1 · Apr 12, 2018
Cited By (3)
US 12,208,102 US 12,473,265 US 12,655,115