Polymorphic compounds and uses thereof

Patent metadata

Field	Value
Publication number	US-10414732-B2
Application number	US-201815924005-A
Country	US
Kind code	B2
Filing date	Mar 16, 2018
Priority date	Mar 16, 2017
Publication date	Sep 17, 2019
Grant date	Sep 17, 2019

Abstract

The present invention provides freebase and salt forms, and compositions and methods thereof, useful for treating various conditions, in which aldehyde toxicity is implicated in the pathogenesis, by the administration of small molecule therapeutics acting as a scavenger for toxic aldehydes.

First claim

We claim:

1. A solid form of compound 1:

having one or more peaks in its XRPD selected from those at about 9.3, about 16.9, and about 26.4 degrees 2-theta; or having one or more peaks in its XRPD selected from those at about 9.6, about 19.1, and about 28.8 degrees 2-theta.

2. The solid form according to claim 1 , wherein said compound is crystalline.

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

4. The solid form according to claim 1 , wherein said compound is substantially free of impurities.

5. The solid form according to claim 1 , having at least two peaks in its XRPD selected from those at about 9.3, about 16.9, and about 26.4 degrees 2-theta.

6. The solid form according to claim 5 , wherein said compound is of Form A.

7. The solid form according to claim 1 , having an XRPD substantially similar to that depicted in FIG. 5 .

8. The solid form according to claim 1 , having at least two peaks in its XRPD selected from those at about 9.6, about 19.1, and about 28.8 degrees 2-theta.

9. The solid form according to claim 8 , wherein said compound is of Form B.

10. The solid form according to claim 1 , having an XRPD substantially similar to that depicted in FIG. 7 .

11. A pharmaceutically acceptable composition comprising the solid form according to claim 1 and a pharmaceutically acceptable carrier, excipient, or vehicle.

12. A compound selected from:
Compound A:

of Form A or B, wherein Form A has one or more peaks in its XRPD selected from those at about 5.4, about 10.8, and about 16.6 degrees 2-theta and Form B has one or more peaks in its XRPD selected from those at about 11.6, about 23.3, and about 35.3 degrees 2-theta;
Compound 2:

of Form A or B, wherein Form A has one or more peaks in its XRPD selected from those at about 8.4, about 14.0, and about 25.4 degrees 2-theta and Form B has one or more peaks in its XRPD selected from those at about 8.4, about 26.8, and about 29.3 degrees 2-theta;
Compound 3:

of Form A, wherein Form A has one or more peaks in its XRPD selected from those at about 17.2, about 23.8, and about 25.5 degrees 2-theta;
Compound 4:

of Form A, wherein Form A has one or more peaks in its XRPD selected from those at about 13.4, about 17.0, and about 25.9 degrees 2-theta;
Compound 5:

of Form A, wherein Form A has one or more peaks in its XRPD selected from those at about 17.0, about 22.6, and about 26.1 degrees 2-theta;
Compound 6:

of Form A, wherein Form A has one or more peaks in its XRPD selected from those at about 16.9, about 19.8, and about 25.3 degrees 2-theta;
Compound 7:

of Form A, wherein Form A has one or more peaks in its XRPD selected from those at about 16.8, about 24.3, and about 27.8 degrees 2-theta;
Compound 8:

of Form A, wherein Form A has one or more peaks in its XRPD selected from those at about 7.1, about 17.2, and about 18.4 degrees 2-theta;
or
Compound 9:

of Form A, wherein Form A has one or more peaks in its XRPD selected from those at about 7.2, about 8.1, and about 16.1 degrees 2-theta.

13. A pharmaceutically acceptable composition comprising a compound according to claim 12 , and a pharmaceutically acceptable carrier, excipient, or vehicle.

14. The compound according to claim 12 , wherein said compound is crystalline.

15. The compound according to claim 12 , wherein said compound is substantially free of impurities.

Assignees

• Aldeyra Therapeutics Inc

Inventors

• Buist Amanda
• Fucci Eden
• Machatha Stephen G
• Suleiman Osama
• Wittering Kate

Classifications

• C07C309/30

  of six-membered aromatic rings substituted by alkyl groups · CPC title

• C07C309/20

  of an acyclic unsaturated carbon skeleton · CPC title

• C07C2602/42

  the bicyclo ring system containing seven carbon atoms · CPC title

• C07B2200/13

  Crystalline forms, e.g. polymorphs · CPC title

• A61K31/47

  Quinolines; Isoquinolines · CPC title