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 .

Assignments (25)
INTERCOMPANY AGREEMENT Recorded Sep 11, 2023
From: NIMBUS LAKSHMI, INC.
To: TAKEDA PHARMACEUTICAL COMPANY LIMITED
Reel/Frame 064867/0415 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2022
From: MASSE, CRAIG E.
To: NIMBUS DISCOVERY, INC.
Reel/Frame 061942/0836 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2022
From: ARLIN, JEAN-BAPTISTE
To: SOLID FORM SOLUTIONS LIMITED
Reel/Frame 061943/0715 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2022
From: PEARSON, DAVID
To: SOLID FORM SOLUTIONS LIMITED
Reel/Frame 061944/0030 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2022
From: SOLID FORM SOLUTIONS LIMITED
To: NIMBUS LAKSHMI, INC.
Reel/Frame 061944/0152 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2022
From: LOUGHREY, JONATHAN J.
To: SOLID FORM SOLUTIONS LIMITED
Reel/Frame 061944/0250 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2022
From: LAWSON, JON P.
To: J.P. LAWSON CONSULTING LLC
Reel/Frame 061944/0583 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2022
From: J.P. LAWSON CONSULTING LLC
To: PHARMACEUTICAL ADVISORS LLC
Reel/Frame 061945/0347 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2022
From: PHARMACEUTICAL ADVISORS LLC
To: NIMBUS LAKSHMI, INC.
Reel/Frame 061945/0408 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2022
From: GREENWOOD, JEREMY ROBERT
To: SCHRÖDINGER, INC.
Reel/Frame 061945/0506 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2022
From: SCHRÖDINGER, INC.
To: SCHRÖDINGER, L.L.C.
Reel/Frame 061945/0544 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2022
From: SCHRÖDINGER, L.L.C.
To: NIMBUS DISCOVERY, INC.
Reel/Frame 061945/0789 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2022
From: NIMBUS DISCOVERY, INC.
To: NIMBUS LAKSHMI, INC.
Reel/Frame 061945/0818 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 17, 2019
From: GREENWOOD, JEREMY ROBERT
To: SCHRÖDINGER, INC.
Reel/Frame 048039/0113 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 17, 2019
From: MASSE, CRAIG E.
To: NIMBUS DISCOVERY, INC.
Reel/Frame 048039/0121 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 17, 2019
From: ARLIN, JEAN-BAPTISTE
To: SOLID FORM SOLUTIONS LIMITED
Reel/Frame 048039/0152 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 17, 2019
From: PEARSON, DAVID
To: SOLID FORM SOLUTIONS LIMITED
Reel/Frame 048039/0162 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 17, 2019
From: LOUGHREY, JONATHAN J.
To: SOLID FORM SOLUTIONS LIMITED
Reel/Frame 048039/0166 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 17, 2019
From: SOLID FORM SOLUTIONS LIMITED
To: NIMBUS LAKSHMI, INC.
Reel/Frame 048039/0201 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 17, 2019
From: PHARMACEUTICAL ADVISORS LLC
To: NIMBUS LAKSHMI, INC.
Reel/Frame 048039/0216 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 17, 2019
From: SCHRÖDINGER, INC.
To: SCHRÖDINGER, L.L.C.
Reel/Frame 048039/0230 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 17, 2019
From: SCHRÖDINGER, L.L.C.
To: NIMBUS DISCOVERY, INC.
Reel/Frame 048039/0242 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 17, 2019
From: NIMBUS DISCOVERY, INC.
To: NIMBUS LAKSHMI, INC.
Reel/Frame 048039/0254 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 17, 2019
From: LAWSON, JON P.
To: J.P. LAWSON CONSULTING LLC
Reel/Frame 048082/0929 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 17, 2019
From: J.P. LAWSON CONSULTING LLC
To: PHARMACEUTICAL ADVISORS LLC
Reel/Frame 048082/0940 →