Granted Patent B2

US 12,521,370 · App. 18/252,949 · Granted Jan 13, 2026

Inventors: Peter Rands (London, GB); Ellen James (London, GB); Tiffanie Benway (London, GB); Zelah Joel (London, GB); Marie Layzell (London, GB)

Assignee: Cybin UK Ltd

A61K31/4045A61K9/007A61K47/10

Abstract

Claims (34)

1 . A parenteral formulation suitable for inhalation comprising a freebase of a deuterium-substituted dimethyltryptamine compound of Formula IA or of Formula IB:

wherein:

one xa H is D and the other is H or D;

each Ya H is independently selected from H and D; and

R 4a and R 5a are both H;

wherein:

R 1 is independently selected from 5-methoxy and 5-bromo;

n is selected from 0, and 1;

R 2 is CD 3 ;

R 3 is CD 3 or H; and

each yb H is independently protium or deuterium; and a biocompatible excipient;

wherein the concentration of the freebase is from about 1 mg/mL to about 1000 mg/mL.

2 . The formulation of claim 1 wherein the compound is of Formula IA and both Xa H or both Ya H are D and/or both Ya H are H or both Ya H are D.

3 . The formulation of claim 1 , wherein the compound is of Formula IB and n is 0; or n is 1 and R 1 is selected from 5-methoxy and 5-bromo.

4 . The formulation of claim 1 , wherein the compound is of Formula IB and R 2 and R 3 are both CD 3 .

5 . The formulation of claim 1 wherein the freebase has a purity of greater than or equal to 99% when measured by HPLC.

6 . The formulation of claim 1 , wherein the biocompatible excipient comprises a solvent.

7 . The formulation of claim 6 , wherein the solvent is selected from any one or a combination of two or more of propylene glycol, glycerine, polyethylene glycol, water, ethanol and triacetin.

8 . The formulation of claim 6 , wherein the solvent is selected from propylene glycol, glycerine and polyethylene glycol, or a mixture thereof.

9 . The formulation of claim 6 , wherein the solvent is a mixture of propylene glycol and glycerine in a ratio of from about 50:50 to about 30:70 by weight.

10 . The formulation of claim 1 , wherein the biocompatible excipient comprises a taste-masking agent.

11 . The formulation of claim 1 , having an oxygen content of less than 2 ppm.

12 . The formulation of claim 1 , stored in a container adapted to prevent penetration of ultraviolet light.

13 . A kit suitable for preparing a parenteral formulation suitable for inhalation of claim 1 , said kit comprising a freebase of a deuterium- substituted dimethyltryptamine compound, and a biocompatible excipient, which is separate to the freebase.

14 . The kit of claim 13 further comprising a container adapted to prevent penetration of ultraviolet light.

15 . A method of preparing a parenteral formulation suitable for inhalation as defined in claim 1 , comprising contacting a freebase of a deuterium-substituted dimethyltryptamine compound, with a biocompatible excipient.

16 . The method of claim 15 wherein the freebase is dissolved in a solvent selected from propylene glycol, glycerine and polyethylene glycol, or a mixture thereof to form a solution.

17 . The method of claim 16 wherein the solvent is a mixture of propylene glycol and glycerine in a ratio of from about 50:50 to about 30:70 by weight.

18 . The method of claim 16 comprising the step of stirring the freebase in the solvent at a temperature of from about 25° C to about 50° C.

19 . The method of claim 16 further comprising sparging the solution with an inert gas.

20 . The method of claim 16 comprising adding a taste-masking agent.

21 . A method of treating a psychiatric or neurological disorder comprising pulmonary administration to a patient in need thereof of a parenteral formulation suitable for inhalation as defined in claim 1 .

22 . The method of claim 21 wherein the psychiatric or neurological disorder is selected from the group consisting of (i) an obsessive compulsive disorder, (ii) a depressive disorder, (iii) an anxiety disorder, (iv) substance abuse, and (v) an avolition disorder.

23 . The method of claim 21 , wherein the parenteral formulation is prepared by contacting a freebase of a deuterium-substituted dimethyltryptamine compound with a biocompatible excipient.

Assignments (2)

Priority Claims (9)

Continuity (5)

References Cited (127)