IP Library › Granted Patent US 10,869,933
Granted Patent B2
US 10,869,933 · App. 16/599,605 · Granted Dec 22, 2020

Oligomer-phenothiazine conjugates

Inventors: Xuyuan Gu (Foster City, CA); Jennifer Riggs-Sauthier (Huntsville, AL)
Assignee: Nektar Therapeutics
A61K47/60
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Quick Facts
Patent No.
US 10,869,933
App. No.
16/599,605
Granted
Dec 22, 2020
Kind
B2
Abstract

The invention relates to (among other things) oligomer-phenothiazine conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over un-conjugated phenothiazine compounds.

Claims (23)

1. A method of treating allergic reactions, anaphylaxis, motion sickness, nausea, or visceral pain comprising administering to a subject in need thereof a therapeutically effective amount of a compound having the formula:

R 1 , R 2 , R 3 , and R 4 , each independently are selected from the group consisting of hydrogen, unsubstituted alkyl, and substituted alkyl; or R 3 and R 4 together with the nitrogen form a heterocycle;

n is an integer equal to or greater than one;

X is a spacer moiety; and

POLY is a poly(ethylene oxide) polymer.

2. The method of claim 1 , wherein said administering is selected from parenteral, oral, transdermal, and rectal.

3. The method of claim 2 , wherein said parenteral administering is selected from intravenous and intramuscular injection.

4. The method of claim 1 , wherein said administering is orally administering.

5. The method of claim 1 , wherein administering comprises administering about 0.001 mg/day to 1000 mg/day.

6. The method of claim 1 , wherein administering comprises administering about 0.10 mg/day to 500 mg/day.

7. The method of claim 1 , wherein administering comprises administering on a dosing schedule selected from five times a day, four times a day, three times a day, twice daily, once daily, three times weekly, and twice weekly.

8. The method of claim 1 , wherein the poly(ethylene oxide) is a poly(ethylene glycol) polymer.

9. The method of claim 1 , wherein the poly(ethylene oxide) is made of from about 1 to about 30 monomers.

10. The method of claim 9 , wherein the poly(ethylene oxide) is made of from about 1 to about 10 monomers.

11. The method of claim 1 , wherein an alkoxy or hydroxy end-capping moiety is attached to the poly(ethylene oxide) polymer.

12. The method of claim 1 , wherein a single poly(ethylene oxide) polymer is attached to the phenothiazine residue.

13. The method of claim 1 , wherein more than one poly(ethylene oxide) polymer is attached to the phenothiazine residue.

14. The method of claim 1 , wherein the linkage is selected from an ether linkage and an ester linkage.

15. The method of claim 1 , wherein POLY is —(CH 2 CH 2 O) n Y, wherein Y is selected from H and —CH 3 ; and

n is 1 to 30.

16. The method of claim 1 , wherein X is —O— or a bond.

17. The method of claim 1 , having the formula:

18. The method of claim 1 , having the formula: