IP Library Granted Patent US 10,898,591
Granted Patent B2
US 10,898,591 · App. 16/694,994 · Granted Jan 26, 2021

Compositions and methods for assessing eye vasculature

Inventors: Richard B. Dorshow (St. Louis, MO); Thomas E. Rogers (Ballwin, MO)
Assignee: MediBeacon Inc.
A61K49/0021A61B5/0071C07D241/20C07K5/06139A61B1/042A61B5/0082A61B5/0261
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Quick Facts
Patent No.
US 10,898,591
App. No.
16/694,994
Granted
Jan 26, 2021
Kind
B2
Abstract

Compositions and methods for assessing blood vessels and organs of the body are disclosed herein, specifically methods for assessing the vasculature of the eye.

Claims (22)

1. A composition comprising a compound of structural Formula I

or a salt thereof; wherein

X 1 and X 2 are independently —CO(AA);

Y 1 and Y 2 are independently chosen from —OR 10 , —SR 11 , —NR 12 R 13 , —N(R 14 )COR 15 , —CONH(PS); —P(R 16 ) 2 , —P(OR 17 ) 2 and

each Z 1 is independently chosen from a bond, —CR 18 R 19 —, —O—, —NR 20 —, —NCOR 21 —, —S—, —SO—, and —SO 2 —;

each R 1 to R 21 are independently chosen from hydrogen, C 1 -C 10 alkyl, C 1 -C 10 alkyl substituted with hydroxyl and carboxylic acid, C 3 -C 6 polyhydroxylated alkyl, C 5 -C 10 aryl, C 5 -C 10 heteroaryl, C 3 -C 5 heterocycloalkyl, C 3 -C 5 heterocycloalkyl substituted with C(O), —(CH 2 ) a CO 2 H, —(CH 2 ) a CO 2 H substituted with C 5 -C 10 heteroaryl, —(CH 2 ) a CONR 30 R 31 , —(CH 2 ) a NHSO 3 − , —(CH 2 ) a NHSO 3 H, —(CH 2 ) a OH, —(CH 2 ) a OPO 3 = , —(CH 2 ) a OPO 3 H 2 , —(CH 2 ) a OPO 3 H − , —(CH 2 ) a OR 22 , —(CH 2 ) a OSO 3 − , —(CH 2 ) a OSO 3 H, —(CH 2 ) a PO 3 = , —(CH 2 ) a PO 3 H 2 , —(CH 2 ) a PO 3 H − , —(CH 2 ) a SO 3 − , —(CH 2 ) a SO 3 H, —(CH 2 ) d CO(CH 2 CH 2 O) c R 23 , (CHCO 2 H) a CO 2 H, —CH 2 (CHNH 2 ) a CH 2 NR 25 R 26 , —CH 2 (CHOH) a CO 2 H, —CH 2 (CHOH) a R 27 , —CH[(CH 2 ) b NH 2 ] a CH 2 OH, —CH[(CH 2 ) b NH 2 ] a CO 2 H, and —(CH 2 ) a NR 28 R 29 ;

each R 22 to R 31 are independently chosen from hydrogen, C 1 -C 10 alkyl, and C 1 -C 5 -dicarboxylic acid;

(AA) is a polypeptide chain comprising one or more natural or unnatural β-amino acids or γ-amino acids linked together by peptide bonds;

(PS) is a sulfated or non-sulfated polysaccharide chain comprising one or more monosaccharide units connected by glycosidic linkages; and

each ‘a’, ‘b’, and ‘d’ are independently chosen from 0 to 10, ‘c’ is chosen from 1 to100 and each of ‘m’ and ‘n’ independently is an integer from 1 to 3.

2. The composition of claim 1 , wherein Y 1 and Y 2 are each —NR 12 R 13 wherein one of R 12 and R 13 is hydrogen and the other of R 12 and R 13 is chosen from hydrogen and C 1 -C 10 alkyl.

3. The composition of claim 2 , wherein Y 1 and Y 2 are each —NR 12 R 13 wherein each of R 12 and R 13 is hydrogen.

4. The composition of claim 1 , wherein the compound of formula I is

(2R,2′R)-3,3′-(3,6-diaminopyrazine-2,5-dicarbonyl)bis(azanediyl))bis(2-(hydroxymethyl)propanoic acid.

5. The composition of claim 1 , wherein the composition is administered intravenously, intraperitoneally, subcutaneously or by infusion.

6. The composition of claim 5 , wherein the composition is administered intravenously.

7. The composition of claim 1 , wherein the compound fluoresces upon irradiation with non-ionizing radiation.

8. The composition of claim 7 , wherein the non-ionizing radiation has a wavelength of at least 350 nm.

9. The composition of claim 1 , wherein the compound of structural Formula I is hydrophilic or has rigid functionality.

10. The composition of claim 1 , wherein the compound of structural Formula I is at least partially renally excretable.

11. The composition of claim 1 , wherein the compound of structural Formula I is completely renally excretable.

12. The composition of claim 1 , wherein the composition further comprises a pharmaceutically acceptable carrier.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 28, 2020
From: DORSHOW, RICHARD B.; ROGERS, THOMAS E.
To: MEDIBEACON INC.
Reel/Frame 054195/0426 →
Cited By (1)
US 12,303,570