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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 (26)
1. A method for treating a pruritic condition in a subject, wherein the method comprises administering to the subject a compound with the general formula (2a″)
with
R 1 being
a substituted phenyl comprising C 1 -C 4 -alkyl, F, Cl, Br, I, —CN as substituents, wherein in particular said substituted phenyl comprises at least one —F as a substituent,
R 7 being
tert-butyl,
a C 4 -cycloalkyl,
R 8 being
—O—CH 2 —R 4 , with R 4 being an C 1 -C 6 substituted or unsubstituted 5-membered heteroaryl.
2. The method according to claim 1 , with R 8 being
—O—CH 2 —R 4 , with R 4 being an C 1 -C 6 substituted or unsubstituted triazole.
3. The method according to claim 1 , wherein the pruritic condition is Serotonin-, Histamine-, Chloroquine-, Compound 48/80 induced itch and bile acid-induced itch.
4. The method according to claim 1 , wherein the compound is an α1, α2, α3 or α5 GABA A receptor modulator.
5. The method according to claim 4 , wherein the compound is a positive allosteric α2 or α3 GABA A receptor modulator.
6. The method according to claim 1 , wherein the subject is a dog.
7. The method according to claim 1 , wherein the pruritic condition is Serotonin-, Histamine-, Chloroquine-, Compound48/80 induced itch and bile acid-induced itch.
8. The method according to claim 1 , wherein the pruritic condition is associated with atopic dermatitis, kidney disease, liver disease, or treatment with opioids.
9. The method according to claim 1 , wherein the compound is to be administered with a corticosteroid, a gabapentinoide, an opioid-receptor antagonist, capsaicin, or a local anaesthetic to the subject.
10. A method for treating an itch in a subject, wherein the method comprises administering to the subject a compound
thereby treating the itch.
11. The method of claim 10 , wherein the itch is associated with kidney disease, liver disease, or treatment with opioids.
12. The method of claim 10 , wherein the compound is to be administered at a dose of from about 0.01 mg/kg per day to about 10 mg/kg per day when administered to a dog.
13. A pharmaceutical composition comprising
wherein the compound is in the form of a suspension in a saline solution, and wherein said pharmaceutical composition is formulated to provide a dose of at least 0.01 mg/kg of a subject's bodyweight when administered to the subject.
14. The pharmaceutical composition of claim 13 , wherein the pharmaceutical composition is formulated to provide a dose of at least 0.03 mg/kg of a subject's bodyweight when administered to the subject.
15. The pharmaceutical composition of claim 13 , wherein the suspension comprises polysorbate 80.
Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Sep 2, 2022
From: ZEILHOFER, HANNS ULRICH; RALVENIUS, WILLIAM
To: UNIVERSITAT ZURICH
Reel/Frame 060975/0299 →
Priority Claims (2)
EP 16153035
· Jan 27, 2016
· regional
EP 16178824
· Jul 11, 2016
· regional
Continuity (4)
Continuation
PCTEP2017051866
· Jan 27, 2017
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