IP Library Granted Patent US 11,154,513
Granted Patent B2
US 11,154,513 · App. 15/280,411 · Granted Oct 26, 2021

Semifluorinated compounds

Inventors: Dieter Scherer (Laufen, CH); Ralf Grillenberger (Nuremberg, DE); Frank Löscher (Schriesheim, DE); Hartmut Voss (Schriesheim, DE)
Assignee: NOVALIQ GMBH
A61K31/02A61F9/0008A61K9/0048A61K9/08A61K47/02C07C17/266
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Quick Facts
Patent No.
US 11,154,513
App. No.
15/280,411
Granted
Oct 26, 2021
Kind
B2
Abstract

The present invention is directed to certain semifluorinated compounds and to compositions comprising such compounds. The invention further provides the use of the compounds and of the compositions as medicaments for topical administration to the eye.

Claims (25)

1. An ophthalmic composition comprising

CF 3 —(CF 2 ) 3 —CH(CH 3 )—(CH 2 ) 2 —CH 3 and CF 3 —(CF 2 ) 3 —(CH 2 ) 4 —CH 3 .

2. The composition according to claim 1 , wherein the composition consists of the CF 3 —(CF 2 ) 3 —CH(CH 3 )—(CH 2 ) 2 —CH 3 and the CF 3 —(CF 2 ) 3 —(CH 2 ) 4 —CH 3 .

3. The composition according to claim 1 , being in liquid form and comprising at least 1 wt % of said compound CF 3 —(CF 2 ) 3 —CH(CH 3 )—(CH 2 ) 2 —CH 3 or from 1 wt % to 5 wt % of said compound CF 3 —(CF 2 ) 3 —CH(CH 3 )—(CH 2 ) 2 —CH 3 , based on the total weight of the composition.

4. The composition according to claim 1 , being formulated as a clear liquid solution.

5. The composition according to claim 1 being substantially free of:

(a) a polymer,

(b) a perfluorinated compound, and/or

(c) a dissolved pharmacologically active ingredient which is not a semifluorinated alkane.

6. The composition of according to claim 1 , wherein the composition is in liquid form and consists essentially of the compound CF 3 —(CF 2 ) 3 —CH(CH 3 )—(CH 2 ) 2 —CH 3 in an amount from 1 wt % to 5 wt % and the compound CF 3 —(CF 2 ) 3 —(CH 2 ) 4 —CH 3 in an amount up to 95 wt %, based on the total weight of the composition.

7. The composition according to claim 1 , being in liquid form and comprising from 1 wt % to 5 wt % of CF 3 —(CF 2 ) 3 —CH(CH 3 )—(CH 2 ) 2 —CH 3 and up to 95 wt % of CF 3 —(CF 2 ) 3 —(CH 2 ) 4 —CH 3 , based on the total weight of the composition.

8. The composition according to claim 7 , being formulated as a clear liquid solution.

9. The composition according to claim 8 being substantially free of:

(a) a polymer,

(b) a perfluorinated compound, and/or

(c) a dissolved pharmacologically active ingredient which is not a semifluorinated alkane.

10. The composition of according to claim 9 , wherein the composition consists essentially of the CF 3 —(CF 2 ) 3 —CH(CH 3 )—(CH 2 ) 2 —CH 3 and the CF 3 —(CF 2 ) 3 —(CH 2 ) 4 —CH 3 , and optionally one or more lipophilic liquid constituents.

11. A kit comprising an ophthalmic composition according to claim 1 and a container for holding the composition, wherein said container comprises a dropper which dispenses droplets having a volume of 8 to 15 μL topically to a lacrimal sac, lower eyelid, eye surface, or other ophthalmic tissue.

12. A method of treating a disease or condition of a patient in need of such treatment, comprising administering the composition according to claim 1 to the patient.

13. The method according to claim 12 , wherein the disease or condition is dry eye disease (keratoconjunctivitis sicca) or a symptom or condition associated therewith; and/or Meibomian Gland Dysfunction (MGD), or a symptom or condition associated therewith.

14. The method according to claim 13 , wherein the composition is topically administered into the lacrimal sac, into the lower eyelid, to an eye surface or to an ophthalmic tissue.

15. The method according to claim 12 , wherein the disease or condition is corneal damage.

16. A method of treating a disease or condition of a patient in need of such treatment, comprising administering the composition according to claim 10 to the patient.

17. The method according to claim 16 , wherein the disease or condition is dry eye disease (keratoconjunctivitis sicca) or a symptom or condition associated therewith; and/or Meibomian Gland Dysfunction (MGD), or a symptom or condition associated therewith.

18. The method according to claim 16 , wherein the disease or condition is corneal damage.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 27, 2017
From: SCHERER, DIETER; GRILLENBERGER, RALF; LÖSCHER, FRANK; VOSS, HARTMUT
To: NOVALIQ GMBH
Reel/Frame 041820/0860 →
Priority Claims (2)
EP 15187760 · Sep 30, 2015 · regional
EP 15192429 · Oct 30, 2015 · regional
Continuity (1)
Related Publication 20170087101A1 · Mar 30, 2017
Cited By (6)
US 12,226,422 US 12,397,039 US 12,419,933 US 12,496,326 US 12,569,452 US 12,599,607