IP Library Granted Patent US 10,828,307
Granted Patent B2
US 10,828,307 · App. 16/596,611 · Granted Nov 10, 2020

Salts and solid form of a BTK inhibitor

Inventors: Mohammad Reza Masjedizadeh (San Jose, CA); Steven Gourlay (San Francisco, CA)
Assignee: Principia Biopharma Inc.
A61K31/519A61K31/5395A61K45/06A61P25/00C07D487/04
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Quick Facts
Patent No.
US 10,828,307
App. No.
16/596,611
Granted
Nov 10, 2020
Kind
B2
Abstract

Disclosed herein are processes for preparing 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile free base (compound (I)), salts of compound (I) and solid state form of said salts. Also disclosed herein are pharmaceutical compositions comprising such salts and solid state form thereof and methods of treating cancer, autoimmune, and inflammatory diseases using compound (I) or a pharmaceutically acceptable salt thereof.

Claims (8)

1. A method of treating pemphigus foliaceus in a mammal comprising administering to the mammal a pharmaceutical composition comprising:

a compound selected from (E) isomer, (Z) isomer, and a mixture of (E) and (Z) isomer of 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile; or

a pharmaceutically acceptable salt of any of the foregoing compounds.

2. The method of claim 1 , wherein the mammal is a human.

3. The method of claim 1 , wherein the pharmaceutical composition comprises at least one compound which is a substantially pure (E) or (Z) isomer of 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile, and/or

at least one pharmaceutically acceptable salt of the compound; and

at least one pharmaceutically acceptable carrier or excipient.

4. The method of claim 3 , wherein at least about 85% w/w of 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile or at least about 85% w/w of a pharmaceutically acceptable salt of 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile is the (E) isomer.

Assignments (3)
ASSIGNEE CHANGE OF ADDRESS Recorded Sep 16, 2025
From: PRINCIPIA BIOPHARMA INC.
To: PRINCIPIA BIOPHARMA INC.
Reel/Frame 072881/0270 →
ASSIGNEE CHANGE OF ADDRESS Recorded Oct 13, 2020
From: PRINCIPIA BIOPHARMA INC.
To: PRINCIPIA BIOPHARMA INC.
Reel/Frame 054059/0410 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 20, 2019
From: MASJEDIZADEH, MOHAMMAD REZA; GOURLAY, STEVEN
To: PRINCIPIA BIOPHARMA INC.
Reel/Frame 051064/0454 →
Continuity (6)
Continuation 16116425 · Aug 29, 2018
Continuation 15120293
Provisional Application 62096468 · Dec 23, 2014
Provisional Application 61946480 · Feb 28, 2014
Provisional Application 61943262 · Feb 21, 2014
Related Publication 20200038405A1 · Feb 6, 2020
Cited By (3)
US 12,336,999 US 12,410,176 US 12,673,953