IP Library Patent Application 14478519
Patent Application
App. No. 14/478,519

USE OF LIPID CONJUGATES IN THE TREATMENT OF DISEASES OR DISORDERS OF THE EYE

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Patent No.
US None
App. No.
14/478,519
Abstract

In one embodiment, the invention provides a method of treating, reducing the incidence, reducing the severity or pathogenesis of an eye disease or disorder in a subject, including, inter alia, retinal detachment, macular degeneration, glaucoma or retinopathy, comprising the step of administering an effective amount of a lipid or phospholipid moiety bound optionally via a spacer to a physiologically acceptable monomer, dimer, oligomer, or polymer via an ester or amide bond, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof. This invention also provides a contact lens solution comprising a lipid or phospholipid moiety bound optionally via a spacer to a physiologically acceptable monomer, dimer, oligomer, or polymer via an ester or amide bond, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof.

Claims (53)

1 . A method of treating a disease or disorder of the eye in a subject comprising the step of contacting said subject with a compound comprising a lipid or phospholipid moiety bound optionally via a spacer to a physiologically acceptable polymer, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof.

2 . The method according to claim 1 , wherein said phospholipid moiety is phosphatidylethanolamine.

3 . The method according to claim 2 , wherein said phosphatidylethanolamine is dipalmitoyl phosphatidylethanolamine.

4 . The method according to claim 2 , wherein said phosphatidylethanolamine is dimyristoyl phosphatidylethanolamine

5 . The method according to claim 1 , wherein said physiologically acceptable monomer, dimer, oligomer, or polymer is polygeline.

6 . The method according to claim 1 , wherein said physiologically acceptable monomer, dimer, oligomer, or polymer is a polypyranose.

7 . The method according to claim 6 , wherein said polypyranose is carboxymethylcellulose.

8 . The method according to claim 6 , wherein said polypyranose is alginate.

9 . The method according to claim 6 , wherein said polypyranose is hydroxyethyl starch.

10 . The method according to claim 1 , wherein the lipid or phospholipid moiety bound optionally via a spacer to a physiologically acceptable monomer, dimer, oligomer, or polymer via an ester or amide bond, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof is represented by the structure of the general formula (A):

wherein

L is a lipid or a phospholipid;

Z is either nothing, ethanolamine, serine, inositol, choline, phosphate, or glycerol;

Y is either nothing or a spacer group ranging in length from 2 to 30 atoms;

X is a physiologically acceptable polymer; and

n is a number from 2 to 1000.

11 . The method of claim 10 , wherein L is phosphatidyl, Z is ethanolamine, Y is nothing, and X is carboxymethylcellulose or a glycosaminoglycan.

12 . The method of claim 10 , wherein the phosphatidylethanolamine moiety is dipalmitoyl or dimyristoyl phosphatidylethanolamine.

13 . The method of claim 10 , wherein the lipid or phospholipid moiety bound optionally via a spacer to a physiologically acceptable monomer, dimer, oligomer, or polymer via an ester or amide bond, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof is represented by the structure of the general formula (I):

wherein

R 1 is a linear, saturated, mono-unsaturated, or poly-unsaturated, alkyl chain ranging in length from 2 to 30 carbon atoms;

R 2 is a linear, saturated, mono-unsaturated, or poly-unsaturated, alkyl chain ranging in length from 2 to 30 carbon atoms; and

Y is either nothing or a spacer group ranging in length from 2 to 30 atoms;

X is a physiologically acceptable polymer; and

n is a number from 1 to 1000.

14 . The method of claim 13 , wherein n is a number from 2 to 100.

15 . The method of claim 10 , wherein the lipid or phospholipid moiety bound optionally via a spacer to a physiologically acceptable monomer, dimer, oligomer, or polymer via an ester or amide bond, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof is represented by the structure of the general formula (III):

wherein

R 1 is a linear, saturated, mono-unsaturated, or poly-unsaturated, alkyl chain ranging in length from 2 to 30 carbon atoms;

R 2 is a linear, saturated, mono-unsaturated, or poly-unsaturated, alkyl chain ranging in length from 2 to 30 carbon atoms;

Z is either nothing, inositol, choline, or glycerol;

Y is either nothing or a spacer group ranging in length from 2 to 30 atoms;

X is a glycosaminoglycan; and

n is a number from 1 to 1000.

16 . The method of claim 15 , wherein n is a number from 2 to 100.

17 . The method of claim 10 , wherein the lipid or phospholipid moiety bound optionally via a spacer to a physiologically acceptable monomer, dimer, oligomer, or polymer via an ester or amide bond, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof is represented by the structure of the general formula (IV):

wherein

R 1 is either hydrogen or a linear, saturated, mono-unsaturated, or poly-unsaturated, alkyl chain ranging in length from 2 to 30 carbon atoms;

R 2 is a linear, saturated, mono-unsaturated, or poly-unsaturated, alkyl chain ranging in length from 2 to 30 carbon atoms;

Z is either nothing, inositol, choline, or glycerol;

Y is either nothing or a spacer group ranging in length from 2 to 30 atoms;

X is a glycosaminoglycan; and

n is a number from 1 to 1000.

18 . The method of claim 17 , wherein n is a number from 2 to 100.

19 . The method of claim 10 , wherein the lipid or phospholipid moiety bound optionally via a spacer to a physiologically acceptable monomer, dimer, oligomer, or polymer via an ester or amide bond, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof is represented by the structure of the general formula (V):

wherein

R 1 is a linear, saturated, mono-unsaturated, or poly-unsaturated, alkyl chain ranging in length from 2 to 30 carbon atoms;

R 2 is either hydrogen or a linear, saturated, mono-unsaturated, or poly-unsaturated, alkyl chain ranging in length from 2 to 30 carbon atoms;

Z is either nothing, inositol, choline, or glycerol;

Y is either nothing or a spacer group ranging in length from 2 to 30 atoms;

X is a glycosaminoglycan; and

n is a number from 1 to 1000.

20 . The method of claim 19 , wherein n is a number from 2 to 100.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 6, 2018
From: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM, LTD
To: YEDGAR, SAUL
Reel/Frame 046006/0942 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 18, 2014
From: YEDGAR, SAUL; COHEN, YUVAL
To: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD; CELSUS THERAPEUTICS PLC
Reel/Frame 034201/0545 →