IP Library Granted Patent US 8,859,524
Granted Patent B2
US 8,859,524 · App. 13/283,020 · Granted Oct 14, 2014

Lipid conjugates in the treatment of chronic rhinosinusitis

Inventor: Saul Yedgar (Jerusalem, IL)
Assignee: Yissum Research Development Company of The Hebrew University of Jerusalem
A61K31/728A61K31/727A61K31/685A61K31/717
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Quick Facts
Patent No.
US 8,859,524
App. No.
13/283,020
Granted
Oct 14, 2014
Kind
B2
Abstract

This invention provides a method of treating, suppressing, inhibiting, or preventing chronic rhinosinusitis in a subject comprising the step of administering to a subject a compound comprising a lipid or phospholipid moiety bond to a physiologically acceptable monomer, dimer, oligomer, or polymer, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof. This invention also provides a method of treating, suppressing, inhibiting, or preventing nasal polyps in a subject comprising the step of administering to a subject a compound comprising a lipid or phospholipid moiety bond to a physiologically acceptable monomer, dimer, oligomer, or polymer, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof.

Claims (44)

1. A method of treating or preventing chronic rhinosinusitis in a subject, comprising the step of administering to said subject a compound represented by the structure of the general formula (A):

wherein

L is a phospholipid;

Z is nothing;

Y is nothing;

X is a glycosaminoglycan; and

n is a number from 1 to 1000.

2. The method according to claim 1 wherein said glycosaminoglycan is selected from the group consisting of hyaluronic acid, heparin, heparin sulfate, chondroitin, chondroitin sulfate, keratan, keratan sulfate, and dermatan sulfate or a derivative thereof.

3. The method according to claim 1 , wherein L is phosphatidylethanolamine.

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

5. The method according to claim 1 , wherein said chronic rhinosinusitis is chronic rhinosinusitis with polyps.

6. A method of treating or preventing nasal polyps in a subject, comprising the step of administering to said subject a compound represented by the structure of the general formula (A):

wherein

L is a phospholipid;

Z is nothing;

Y is nothing;

X is a glvcosaminoglycan; and

n is a number from 1 to 1000.

7. The method according to claim 6 , wherein said glycosaminoglycan is selected from the group consisting of hyaluronic acid, heparin, heparin sulfate, chondroitin, chondroitin sulfate, keratan, keratan sulfate, and dermatan sulfate or a derivative thereof.

8. The method according to claim 6 , wherein L is a phosphatidylethanolamine.

9. The method according to claim 8 , wherein said phosphatidylethanolamine is dipalmitoyl phosphatidylethanolamine.

10. The method according to claim 1 , wherein said compound 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;

Y is nothing;

X is glycosaminoglycan; and

n is a number from 1 to 1,000.

11. The method of claim 10 , wherein said glycosaminoglycan is selected from the group consisting of hyaluronic acid, heparin, heparin sulfate, chondroitin, chondroitin sulfate, keratan, keratan sulfate, dermatan sulfate or a derivative thereof.

12. The method of claim 1 , wherein said glycosaminoglycan has a molecular weight of between 5 kD and 90 kD.

13. The method of claim 1 , wherein said glycosaminoglycan has a molecular weight of between 5 kD and 20 kD.

14. The method according to claim 6 , wherein said compound 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;

Y is nothing;

X is glycosaminoglycan; and

n is a number from 1 to 1,000.

15. The method of claim 14 , wherein said glycosaminoglycan is selected from the group consisting of hyaluronic acid, heparin, heparin sulfate, chondroitin, chondroitin sulfate, keratan, keratan sulfate, dermatan sulfate or a derivative thereof.

16. The method of claim 14 , wherein said glycosaminoglycan has a molecular weight of between 5 kD and 20 kD.

17. The method of claim 10 , wherein n is a number from 2 to 500.

18. The method of claim 14 , wherein n is a number from 2 to 500.

19. The method of claim 1 , wherein the step of administering comprises nasal administration.

20. The method of claim 6 , wherein the step of administering comprises nasal administration.

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 14, 2011
From: YEDGAR, SAUL
To: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD.
Reel/Frame 027218/0978 →
Continuity (7)
Continuation In Part 11285375 · Nov 23, 2005
Continuation In Part PCTIL2005001225 · Nov 17, 2005
Continuation In Part 13283020
Continuation In Part 12463792 · May 11, 2009
Continuation In Part 12997014
Provisional Application 61177083 · May 11, 2009
Related Publication 20120071442A1 · Mar 22, 2012