Compositions and methods for assessing eye vasculature

Patent metadata

Field	Value
Publication number	US-10898591-B2
Application number	US-201916694994-A
Country	US
Kind code	B2
Filing date	Nov 25, 2019
Priority date	May 12, 2015
Publication date	Jan 26, 2021
Grant date	Jan 26, 2021

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.

First claim

The invention claimed is:

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.

Assignees

• Medibeacon Inc

Inventors

• Dorshow Richard B
• Rogers Thomas E

Classifications

• A61B5/0071

  by measuring fluorescence emission · CPC title

• C07K5/06139

  with the first amino acid being heterocyclic · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P11/00

  Drugs for disorders of the respiratory system · CPC title

• A61K49/0021 Primary

  the fluorescent group being a small organic molecule · CPC title