IP Library Granted Patent US 12,060,343
Granted Patent B2
US 12,060,343 · App. 17/713,646 · Granted Aug 13, 2024

Substituted 1,2,4-triazoles as intermediates in the synthesis of TYK2 inhibitors

Inventors: Bohan Jin (San Francisco, CA); Qing Dong (San Francisco, CA); Gene Hung (San Francisco, CA); Stephen W. Kaldor (San Francisco, CA)
Assignee: Alumis Inc.
C07D401/14C07D401/12C07D403/12
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Quick Facts
Patent No.
US 12,060,343
App. No.
17/713,646
Granted
Aug 13, 2024
Kind
B2
Abstract

Described herein are compounds, for example, 1,2,4-triazole-substituted N-heteroaryl amines, that are useful in treating a TYK2-mediated disorder. In some embodiments, the TYK2-mediated disorder is an autoimmune disorder, an inflammatory disorder, a proliferative disorder, an endocrine disorder, a neurological disorder, or a disorder associated with transplantation.

Claims (18)

1. A compound of Formula (I):

wherein the compound of Formula (I) is prepared by a process comprising the following steps:

(1) reducing a compound of the following formula:

in the presence of H 2 and a palladium catalyst, to provide a compound of the following formula:

and

(2) coupling the compound provided in step (1) above with a compound of Formula (II):

in the presence of a palladium catalyst, to provide the compound of Formula (I):

2. A process for preparing a compound of Formula (I):

wherein the process comprises the following steps:

(1) reducing a compound of the following formula:

in the presence of H 2 and a palladium catalyst, to provide a compound of the following formula:

and

(2) coupling the compound provided in step (1) above with a compound of Formula (II):

in the presence of a palladium catalyst, to provide the compound of Formula (I):

3. The process of claim 2 , wherein reducing comprises hydrogenating in the presence of Pd—C.

4. The process of claim 2 , wherein coupling comprises palladium-catalyzed cross coupling with Pd 2 (dba) 2 .

5. A compound:

6. A compound:

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 21, 2023
From: JIN, BOHAN; DONG, QING; HUNG, GENE; KALDOR, STEPHEN W.
To: ESKER THERAPEUTICS, INC.
Reel/Frame 062753/0802 →
CHANGE OF NAME Recorded Feb 21, 2023
From: ESKER THERAPEUTICS, INC.
To: ALUMIS INC.
Reel/Frame 062813/0382 →
Continuity (10)
Continuation 17243508 · Apr 28, 2021
Continuation 16938183 · Jul 24, 2020
Continuation PCTUS2019057485 · Oct 22, 2019
Provisional Application 62907354 · Sep 27, 2019
Provisional Application 62893721 · Aug 29, 2019
Provisional Application 62875449 · Jul 17, 2019
Provisional Application 62839459 · Apr 26, 2019
Provisional Application 62756942 · Nov 7, 2018
Provisional Application 62749003 · Oct 22, 2018
Related Publication 20220235035A1 · Jul 28, 2022