IP Library Granted Patent US 11,529,359
Granted Patent B2
US 11,529,359 · App. 16/994,146 · Granted Dec 20, 2022

Use of GABA

Inventors: Hanns Ulrich Zeilhofer (Zurich, CH); William Ralvenius (Somerville, MA)
Assignee: UNIVERSITAT ZURICH
A61K31/5517A61K31/4184A61K31/4188A61K31/437A61K31/5025A61K31/519A61K31/53A61K31/5513A61P17/04
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Quick Facts
Patent No.
US 11,529,359
App. No.
16/994,146
Granted
Dec 20, 2022
Kind
B2
Abstract

A compound for use in the treatment of itch is provided, wherein the compound comprises the general formula (1a), general formula (1b) or general formula (1c). The compounds of the invention are positive allosteric α2 and/or α3 GABA A receptor modulators.

Claims (16)

1. A method of treating a pruritic condition in a subject, comprising administering to the subject a compound that comprises the general formula (5a),

wherein,

R 1 is an unsubstituted biphenyl or a substituted biphenyl comprising at least one —CN as a substituent; and

R 7 is an unsubstituted C 1 -C 6 alcohol,

wherein the compound is a positive, allosteric a2 or a3 GABA A receptor modulator.

2. The method of claim 1 , wherein R 7 is an unsubstituted C 3 alcohol.

3. The method of claim 1 , wherein R 7 is an unsubstituted isopropanol.

4. The method of claim 1 , wherein the —CN is on the phenyl moiety not connected to the parent moiety.

5. The method of claim 1 , wherein R 1 is a substituted biphenyl, and wherein one phenyl moiety of the biphenyl comprises at least one —F as a substituent.

6. The method of claim 1 , wherein R 1 is a substituted biphenyl, and wherein each phenyl moiety of the biphenyl comprises one —F as a substituent.

7. The method of claim 1 , wherein the subject is an animal.

8. The method of claim 1 , wherein the pruritic condition is associated with atopic dermatitis, kidney disease, liver disease, or treatment with opioids.

9. The method of claim 1 , further comprising administering a corticosteroid, gabapentinoide, an opioid-receptor antagonist, capsaicin, or a local anesthetic to the subject.

10. The method of claim 1 , wherein the compound is administered to the subject at a dose of at least 0.01 mg/kg of the subject's bodyweight.

11. The method of claim 1 , wherein the compound is administered to the subject at a dose of at least 0.03 mg/kg of the subject's bodyweight.

12. The method of claim 1 , wherein the compound is

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 7, 2021
From: ZEILHOFER, HANNS ULRICH; RALVENIUS, WILLIAM
To: UNIVERSITAT ZURICH
Reel/Frame 055856/0074 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 1, 2020
From: ZEILHOFER, HANNS ULRICH; RALVENIUS, WILLIAM
To: UNIVERSITAT ZURICH
Reel/Frame 053661/0938 →
Priority Claims (2)
EP 16153035 · Jan 27, 2016 · regional
EP 16178824 · Jul 11, 2016 · regional
Continuity (3)
Continuation 16045193 · Jul 25, 2018
Continuation PCTEP2017051866 · Jan 27, 2017
Related Publication 20210100814A1 · Apr 8, 2021