IP Library Granted Patent US 10,815,213
Granted Patent B2
US 10,815,213 · App. 16/296,319 · Granted Oct 27, 2020

Bruton's tyrosine kinase inhibitors

Inventors: John Robert Springer (Wentzville, MO); Balekudru Devadas (Chesterfield, MO); Danny James Garland (House Springs, MO); Margaret Lanahan Grapperhaus (Troy, IL); Seungil Han (Mystic, CT); Susan Landis Hockerman (Kirkwood, MO); Robert Owen Hughes (Newtown, CT); Eddine Saiah (Brookline, MA); Mark Edward Schnute (Acton, MA); Shaun Raj Selness (Chesterfield, MO); Daniel Patrick Walker (Augusta, MO); Zhao-Kui Wan (Lexington, MA); Li Xing (Lexington, MA); Christoph Wolfgang Zapf (Marlborough, MA); Michelle Ann Schmidt (Millstadt, IL)
Assignee: Pfizer Inc.
C07D401/04
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Quick Facts
Patent No.
US 10,815,213
App. No.
16/296,319
Granted
Oct 27, 2020
Kind
B2
Abstract

Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. (Formula I)

Claims (24)

1. A compound having Formula (I)

or a pharmaceutically acceptable salt thereof, wherein

A is phenyl;

X is O;

W is phenyl;

R 1 is

R is

R 2a , R 2b , R 3a , and R 3b are hydrogen;

R a is hydrogen;

R b is (C 1 -C 6 )alkyl, wherein the (C 1 -C 6 )alkyl is substituted with (C 1 -C 6 )alkoxy; and

R c is hydrogen.

2. A pharmaceutical composition comprising a compound according to claim 1 or a pharmaceutically acceptable salt thereof, admixed with at least one pharmaceutically acceptable carrier or excipient.

3. A compound of Formula (I)

or a pharmaceutically acceptable salt thereof, wherein

A is phenyl;

X is O;

W is

R 1 is

R is

R 2a , R 2b , R 3a , and R 3b are hydrogen;

R a is hydrogen;

R b is (C 1 -C 6 )alkyl substituted with (C 1 -C 6 )alkoxy; and

R c is hydrogen.

4. A pharmaceutical composition comprising a compound according to claim 3 or a pharmaceutically acceptable salt thereof, admixed with at least one pharmaceutically acceptable carrier or excipient.

Assignments (1)
ASSIGNEE ADDRESS CORRECTION Recorded Mar 20, 2023
From: PFIZER INC.
To: PFIZER INC.
Reel/Frame 063119/0087 →