Bruton's tyrosine kinase inhibitors

Patent metadata

Field	Value
Publication number	US-10815213-B2
Application number	US-201916296319-A
Country	US
Kind code	B2
Filing date	Mar 8, 2019
Priority date	Nov 2, 2012
Publication date	Oct 27, 2020
Grant date	Oct 27, 2020

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)

First claim

We claim:

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.

Assignees

• Pfizer

Inventors

• Springer John Robert
• Devadas Balekudru
• Garland Danny James
• Grapperhaus Margaret Lanahan
• Han Seungil
• Hockerman Susan Landis
• Hughes Robert Owen
• Saiah Eddine
• Schnute Mark Edward
• Selness Shaun Raj
• Walker Daniel Patrick
• Wan Zhao-Kui
• Xing Li
• Zapf Christoph Wolfgang
• Schmidt Michelle Ann

Classifications

• A61P37/02

  Immunomodulators · CPC title

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P35/02

  specific for leukemia · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• C07D401/04 Primary

  directly linked by a ring-member-to-ring-member bond · CPC title