IP Library Granted Patent US 12,043,620
Granted Patent B2
US 12,043,620 · App. 17/687,826 · Granted Jul 23, 2024

Benzazole compounds and methods for making and using the compounds

Inventors: Rose Yen (San Francisco, CA); Yan Chen (Foster City, CA); Rajinder Singh (Belmont, CA); Vanessa Taylor (San Francisco, CA)
Assignee: Rigel Pharmaceuticals, Inc.
C07D413/14A61K31/454A61K31/4545A61K31/496A61K31/5377A61K45/06A61P9/00A61P11/00A61P17/00A61P21/00A61P25/00A61P29/00A61P35/00C07D417/14C07D471/04
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Quick Facts
Patent No.
US 12,043,620
App. No.
17/687,826
Granted
Jul 23, 2024
Kind
B2
Abstract

Disclosed are novel benzazole compounds and compositions comprising the compounds. The compounds are useful as kinase inhibitors including interleukin receptor associated kinases (IRAK) inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition.

Claims (26)

1. A compound having a formula

or a pharmaceutically acceptable salt, solvate, hydrate, or N-oxide thereof, wherein:

X is O or S;

Y is S;

Z is N;

Het-1 is

R 1 and R 2 independently are H, aliphatic, heteroaliphatic, heterocyclyl, aryl, araliphatic, or together with the nitrogen to which they are attached, form a heterocyclic ring;

each R 8 independently is aliphatic, halo, heteroaliphatic, —O-aliphatic, heterocyclyl, aryl, araliphatic, —O-heterocyclyl, hydroxyl, nitro, cyano, carboxyl, carboxyl ester, acyl, amide, amino, sulfonyl, sulfonamide, sulfanyl, sulfinyl or haloalkyl;

R 10 and R 23 are selected from H, aliphatic, heteroaliphatic, —O-aliphatic, heterocyclyl, aryl, araliphatic, —O-heterocyclyl, hydroxyl, cyano, carboxyl, carboxyl ester, acyl, amide, amino, sulfonyl, sulfonamide, or haloalkyl; and

R and R′ are each independently aliphatic, or R and R′ together with the nitrogen attached thereto form a heterocyclic ring.

2. The compound of claim 1 , wherein:

each R 8 independently is selected from halo, C 1-6 haloalkyl, C 1-6 alkyl, -OC1-6 alkyl, amino or —CH 2 OP(O)(OR 24 ) 2 ; and

each R 24 independently is H, C 1-6 alkyl or a counterion forming a pharmaceutically acceptable base addition salt with the phosphate moiety.

3. The compound of claim 1 , wherein at least one R 8 is —NH 2 , —CH 3 , —CF 3 , —CF 2 H or —CH 2 CF 3 .

4. The compound of claim 1 , wherein R and R′ independently are aliphatic.

5. The compound of claim 1 , wherein R and R′ together with the nitrogen attached thereto form a heterocyclic ring.

6. The compound of claim 1 , wherein NRR′ is selected from

7. The compound of claim 1 , wherein R 1 is H or alkyl, and R 2 is aliphatic or heteroaliphatic.

8. The compound of claim 1 , wherein R 1 and R 2 , together with the nitrogen attached thereto, are selected from

R a is aliphatic, haloalkyl or acyl;

n is 1 or 2; and

p is 0, 1 or 2.

9. The compound of claim 8 , wherein:

R a is CH 3 , CF 3 , CF 2 H, or R b C(O)—; and

R b is aliphatic or haloalkyl.

10. A composition, comprising a compound of claim 1 , and a pharmaceutically acceptable excipient.

Assignments (3)
SECURITY INTEREST Recorded May 8, 2026
From: RIGEL PHARMACEUTICALS, INC.
To: MIDCAP FUNDING IV TRUST
Reel/Frame 075576/0880 →
SECURITY INTEREST Recorded Aug 25, 2022
From: RIGEL PHARMACEUTICALS, INC.
To: MIDCAP FINANCIAL TRUST
Reel/Frame 061327/0712 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 16, 2022
From: YEN, ROSE; CHEN, YAN; TAYLOR, VANESSA; SINGH, RAJINDER
To: RIGEL PHARMACEUTICALS, INC.
Reel/Frame 059287/0056 →
Continuity (5)
Continuation 16928413 · Jul 14, 2020
Continuation 16057687 · Aug 7, 2018
Division 15226625 · Aug 2, 2016
Provisional Application 62200778 · Aug 4, 2015
Related Publication 20220185804A1 · Jun 16, 2022