Substituted pyrazolo[1,5-a]pyrimidines as TYK2 inhibitors

• US 11,414,431 B2
• Filed: 10/15/2019
• Issued: 08/16/2022
• Est. Priority Date: 10/15/2018
• Status: Active Grant

• Current Assignee: Takeda Pharmaceutical Company Limited
• Original Assignee: Nimbus Lakshmi Inc. (Takeda Pharmaceutical Company Limited)
• Inventors: Masse, Craig E., Greenwood, Jeremy Robert, Mondal, Sayan
• Primary Examiner(s): Willis, Douglas M
• Application Number:
  US16/602,000
• Publication Number:
  US 20200131201A1
• Time in Patent Office: 1,036 Days
• Field of Search: 5142593, 544281
• CPC Class Codes: C07D 487/04 Ortho-condensed systems
• CPC Class Codes: C07D 519/00 Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

The present invention provides compounds of Formula I′:

compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.

Claims

1. A compound of Formula I′

;

2. The compound of claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R^1A is selected from the group consisting of:

3. The compound of claim 2, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein each R^2A is independently selected from the group consisting of:

4. The compound of claim 1, wherein the compound is of Formula II:

5. The compound of claim 1, wherein the compound is of Formula III:

6. The compound of claim 1, wherein the compound is of Formula VI:

7. The compound of claim 1, wherein the compound is of Formula VIII:

8. A pharmaceutical composition comprising a pharmaceutically acceptable carrier, adjuvant, or vehicle and a compound of claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof.

9. The A compound, or a stereoisomer thereof, wherein the compound, or stereoisomer thereof, is selected from the group consisting of: