IP Library Granted Patent US 11,155,544
Granted Patent B2
US 11,155,544 · App. 16/523,979 · Granted Oct 26, 2021

Heterocycle comprising tyrosine kinase inhibitors

Inventors: David M. Goldstein (Redwood City, CA); Timothy D. Owens (Redwood City, CA)
Assignee: Principia Biopharma Inc.
C07D471/04A61P19/02C07D487/04
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 11,155,544
App. No.
16/523,979
Granted
Oct 26, 2021
Kind
B2
Abstract

The present disclosure provides compounds of formula (I) that are tyrosine kinase inhibitors, in particular Bruton tyrosine kinase (“BTK”) inhibitors, and are therefore useful for the treatment of diseases treatable by inhibition of BTK such as cancer, autoimmune, inflammatory, and thromboembolic diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Claims (25)

1. A compound chosen from:

Name

Structure

(R)-2-(3-(8-amino-1- (2-fluoro-4- phenoxyphenyl) imidazo[1,5-a] pyrazin-3- yl)piperidine-1- carbonyl)-4-methyl- 4-(4-(oxetan- 3-yl)piperazin-1-yl) pent-2-enenitrile;

(S)-2-(2-((8-amino- 1-(2-fluoro-4- phenoxyphenyl) imidazo[1,5-a] pyrazin-3- yl)methyl) pyrrolidine- 1-carbonyl)-4,4- dimethylpent-2- enenitrile;

(S)-2-(2-((8-amino- 1-(2-fluoro-4- phenoxyphenyl) imidazo[1,5-a] pyrazin-3- yl)methyl) pyrrolidine-1- carbonyl)-4- methyl-4- morpholinopent- 2-enenitrile;

(S)-2-(2-((8- amino-1-(2- fluoro-4- phenoxyphenyl) imidazo[1,5-a] pyrazin-3- yl)methyl) pyrrolidine- 1-carbonyl)-4- methyl-4- (methyl(oxetan- 3-yl) amino)pent-2- enenitrile;

(S)-2-(2-((8-amino- 1-(2-fluoro-4- phenoxyphenyl) imidazo[1,5-a] pyrazin-3- yl)methyl) pyrrolidine-1- carbonyl)-4- methyl-4-(4- (oxetan-3-yl) piperazin-1-yl) pent-2-enenitrile; and

(R)-2-(3-(8-amino- 1-(4- phenoxyphenyl) imidazo[1,5-a] pyrazin-3- yl)piperidine- 1-carbonyl)-4- methyl-4-(4- (oxetan- 3-yl)piperazin- 1-yl)pent-2- enenitrile,

or a stereoisomer of any of the above compounds,

or an E or Z isomer thereof,

or a pharmaceutically acceptable salt of any of the above compounds.

2. The compound of claim 1 chosen from:

Name

Structure

(R)-2-(3-(8-amino-1-(2-fluoro-4- phenoxyphenyl)imidazo[1,5-a]pyrazin-3- yl)piperidine-1-carbonyl)-4-methyl-4-(4- (oxetan-3-yl)piperazin-1-yl)pent-2-enenitrile;

or a stereoisomer,

or an E or Z isomer thereof,

or a pharmaceutically acceptable salt thereof.

3. A pharmaceutical composition comprising:

a compound of claim 1 or a pharmaceutically acceptable salt thereof; and

a pharmaceutically acceptable excipient.

4. A pharmaceutical composition comprising:

a compound of claim 2 or a pharmaceutically acceptable salt thereof; and

a pharmaceutically acceptable excipient.

Assignments (2)
ASSIGNEE CHANGE OF ADDRESS Recorded Sep 16, 2025
From: PRINCIPIA BIOPHARMA INC.
To: PRINCIPIA BIOPHARMA INC.
Reel/Frame 072881/0270 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 22, 2021
From: GOLDSTEIN, DAVID; OWENS, TIMOTHY D.
To: PRINCIPIA BIOPHARMA INC.
Reel/Frame 056616/0972 →
Continuity (4)
Continuation 15738051
Provisional Application 62183969 · Jun 24, 2015
Provisional Application 62271715 · Dec 28, 2015
Related Publication 20190345159A1 · Nov 14, 2019