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1. WO2020223685 - COMPOSÉS POLYMORPHES ET LEURS UTILISATIONS

Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

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CLAIMS

We claim:

1. A solid form of Compound 5:


wherein the form is of Form A or Form B.

2. The compound according to claim 1, wherein the compound is crystalline.

3. The compound according to claim 1, wherein the compound is a crystalline solid substantially free of amorphous compound 5.

4. The compound according to claim 1, wherein the compound is substantially free of impurities.

5. The compound according to claim 1, having one or more peaks in its XRPD selected from those at about 13.9, about 15.8 and about 24.3 degrees 2-theta.

6. The compound according to claim 5, having at least two peaks in its XRPD selected from those at about 13.9, about 15.8 and about 24.3 degrees 2-theta.

7. The compound according to claim 6, wherein the compound is of Form A.

8. The compound according to claim 1, having an XRPD substantially similar to that depicted in

FIG. 21.

9. The compound according to claim 1, having one or more peaks in its XRPD selected from those at about 10.2, about 17.0 and about 28.8 degrees 2-theta.

10. The compound according to claim 9, having at least two peaks in its XRPD selected from those at about 10.2, about 17.0 and about 28.8 degrees 2-theta.

11. The compound according to claim 10, wherein the compound is of Form B.

12. The compound according to claim 1, having an XRPD substantially similar to that depicted in

FIG. 23.

13. A pharmaceutically acceptable composition comprising the compound according to claim 1 and a pharmaceutically acceptable carrier, excipient, or vehicle.

14. A method of treating a condition in a patient in which aldehyde toxicity is implicated in the pathogenesis, comprising administering to the patient a compound according to claim 1 or composition thereof.

15. The method according to claim 14, further comprising administering to the patient an additional therapeutic agent.

16. A compound selected from the group consisting of:

Compound A:


of Form A;

Compound 1:


of Form A or Form B;

Compound 2:


of Form A;

Compound 3:


of Form A, Form B, Form C or Form D;

Compound 4:

of Form A or Form B;

Compound 6:


of Form A or Form B;

Compound 7:


of Form A or Form B;

Compound 8:


of Form A;

Compound 9:


of Form A, Form B or Form C; Compound 10:


of Form A; and

Compound 11 :


of Form A.

17. A pharmaceutically acceptable composition comprising a compound according to claim 16, and a pharmaceutically acceptable carrier, excipient, or vehicle.

18. A method of treating a condition in a patient in which aldehyde toxicity is implicated in the pathogenesis, comprising administering to the patient a composition according to claim 17.

19. The method according to claim 18, further comprising administering to the patient an additional therapeutic agent.

20. A method for preparing a salt compound of the formula X:


X

comprising steps of:

combining A:


with a suitable acid and optionally a suitable solvent under conditions for forming a salt compound of formula X.

21. The method of claim 20, wherein:

(a) the suitable acid is methanesulfonic acid thereby forming a mesylate salt of Compound A and optionally crystallizing the mesylate salt to Form A or Form B;

(b) the suitable acid is benzenesulfonic acid thereby forming a besylate salt of Compound A and optionally crystallizing the besylate salt to form Form A;

(c) the suitable acid is sulfuric acid thereby forming a sulfate salt of Compound A an optionally crystallizing the sulfate salt to form Form A, Form B, Form C or Form D;

(d) the suitable acid is /?-toluenesulfonic acid thereby forming a tosylate salt of Compound A and optionally crystallizing the tosylate salt to form Form A or Form B;

(e) the suitable acid is hydrochloric acid thereby forming a hydrochloride salt of Compound A and optionally crystallizing the hydrochloride salt to form Form A or Form B;

(f) the suitable acid is oxalic acid thereby forming an oxalate salt of Compound A and optionally crystallizing the oxalate salt to form Form A or Form B.

(g) the suitable acid is phosphoric acid thereby forming a phosphate salt of Compound A and optionally crystallizing the phosphate salt to form Form A or Form B;

(h) the suitable acid is ethanedisulfonic acid thereby forming an edisylate salt of Compound A and optionally crystallizing the edisylate salt to form Form A;

(i) the suitable acid is tartaric acid thereby forming a tartrate salt of Compound A and optionally recrystallizing the tartrate salt to form Form A, Form B or Form C;

(j) the suitable acid is fumaric acid thereby forming a fumarate salt of Compound A and

optionally recrystallizing the fumarate salt to form Form A; or

(k) the suitable acid is citric acid thereby forming a citrate salt of Compound A and optionally recrystallizing the citrate salt to form Form A.