IP Library Granted Patent US 10,336,752
Granted Patent B2
US 10,336,752 · App. 15/914,074 · Granted Jul 2, 2019

TYK2 inhibitors, uses, and methods for production thereof

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Quick Facts
Patent No.
US 10,336,752
App. No.
15/914,074
Filed
Mar 7, 2018
Granted
Jul 2, 2019
Kind
B2
Art Unit
1626
USPC
514/210.18
Abstract

The present invention provides compounds useful as inhibitors of Tyrosine Kinase 2 (Tyk2), solid forms and compositions thereof, methods of producing the same, and methods of using the same in the treatment of Tyk2-mediated diseases.

Claims (25)

1. A compound of Formula I:

or a pharmaceutically acceptable salt thereof,

wherein each of X, Y, and Z is independently hydrogen or deuterium.

2. The compound of claim 1 of the formula:

or a pharmaceutically acceptable salt thereof.

3. The mesylate salt of the compound of claim 2 .

4. The free base of the compound of claim 2 .

5. The compound of claim 1 , wherein said compound is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

6. A solid form of a compound of claim 1 .

7. A crystalline form of a compound according to claim 4 having a powder X-ray diffraction (XRPD) pattern as depicted in FIG. 1 .

8. A crystalline form of a compound according to claim 3 having a powder X-ray diffraction (XRPD) pattern as depicted in FIG. 2 .

9. A crystalline form of a compound according to claim 3 having a powder X-ray diffraction (XRPD) pattern as depicted in FIG. 3 .

10. A crystalline form of a compound according to claim 3 having a powder X-ray diffraction (XRPD) pattern as depicted in FIG. 4 .

11. A crystalline form of a compound according to claim 3 having a powder X-ray diffraction (XRPD) pattern as depicted in FIG. 5 .

12. A crystalline form of a compound according to claim 3 having a powder X-ray diffraction (XRPD) pattern as depicted in FIG. 6 .

13. A process for producing a compound of the formula:

comprising contacting a compound of the formula:

with an acid.

14. A process for producing a compound of the formula:

comprising contacting a compound of the formula:

with a compound of formula:

 under aryl amination conditions.

15. A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier, adjuvant, or diluent.

16. A method of inhibiting a Tyk2 enzyme in a patient or biological sample comprising contacting said patient or biological sample with a compound according to claim 1 .