IP Library Granted Patent US 10,676,473
Granted Patent B2
US 10,676,473 · App. 14/973,180 · Granted Jun 9, 2020

Solid state forms of fused heteroaromatic pyrrolidinones

Inventors: Rongliang Chen (San Diego, CA); Tomonori Ichibakase (Osaka, JP); Chunrong Ma (San Diego, CA); Christopher F. Matthews (San Diego, CA); Hajime Motoyoshi (Osaka, JP); Colin O'Bryan (San Diego, CA); Kentaro Yaji (Osaka, JP); Naoki Yoshikawa (Osaka, JP)
Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
C07D471/04A61K9/20A61K9/48
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Quick Facts
Patent No.
US 10,676,473
App. No.
14/973,180
Granted
Jun 9, 2020
Kind
B2
Abstract

Disclosed are chemical entities which are inhibitors of spleen tyrosine kinase (SYK), namely, chemical entities comprising 6-((1R,2S)-2-aminocyclohexylamino)-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,4-c]pyridine-3(2H)-one and certain solid state forms thereof. Also disclosed are methods of using the chemical entities to treat disorders such as a cancer.

Claims (8)

1. A crystal form of 6-((1R,2S)-2-aminocyclohexylamino)-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,4-c]pyridine-3(2H)-one citrate, which is in substantially crystalline form, and is characterized by an X-ray powder diffraction (XRPD) pattern using Cu Kα radiation comprising peaks at 2θ angles of 9.4, 16.6, 17.4, 18.9, 19.2, and 20.7°±0.2 degrees.

2. The crystal form of claim 1 , characterized by an XRPD pattern using Cu Kα radiation comprising peaks at 2θ angles of 4.7, 9.4, 16.6, 17.4, 18.9, 19.2, 20.7, and 23.0°±0.2 degrees.

3. The crystal form of claim 1 , characterized by an XRPD pattern using Cu Kα radiation comprising peaks at 2θ angles of 4.7, 9.4, 13.0, 13.8, 14.1, 16.6, 17.4, 18.4, 18.9, 19.2, 20.7, 23.0, 23.3, 23.6, and 25.0°±0.2 degrees.

4. The crystal form of claim 1 , wherein the crystal form is not hygroscopic.

5. A pharmaceutical composition comprising the crystal form of claim 1 and one or more pharmaceutically acceptable carriers.

6. The pharmaceutical composition of claim 5 , which is suitable for oral administration.

7. The pharmaceutical composition of claim 6 , which is a dosage form selected from a capsule and a tablet.

8. The pharmaceutical composition of claim 7 , wherein the dosage form is a tablet.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 2, 2023
From: CALITHERA BIOSCIENCES, INC.
To: WELLS THERAPEUTICS, INC.
Reel/Frame 063837/0942 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 5, 2021
From: TAKEDA PHARMACEUTICAL COMPANY LIMITED
To: CALITHERA BIOSCIENCES, INC.
Reel/Frame 058289/0027 →
CORRECTIVE ASSIGNMENT TO CORRECT THE LIST OF ASSIGNORS PREVIOUSLY RECORDED ON REEL 039644 FRAME 0825. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Sep 8, 2016
From: ICHIBAKASE, TOMONORI; MOTOYOSHI, HAJIME; YAJI, KENTARO; YOSHIKAWA, NAOKI
To: TAKEDA PHARMACEUTICAL COMPANY LIMITED
Reel/Frame 039970/0223 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 6, 2016
From: CHEN, RONGLIANG; MA, CHUNRONG; MATTHEWS, CHRISTOPHER F.; O'BRYAN, COLIN
To: TAKEDA CALIFORNIA, INC.
Reel/Frame 039644/0724 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 6, 2016
From: TAKEDA CALIFORNIA, INC.
To: TAKEDA PHARMACEUTICAL COMPANY LIMITED
Reel/Frame 039644/0765 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 6, 2016
From: ICHIBAKASE, TOMONORI; MOTOYOSHI, HAJIME; YAJI, KENTARO; YOSHIKAWA, NAOKI; OKUMURA, YOICHI
To: TAKEDA PHARMACEUTICAL COMPANY LIMITED
Reel/Frame 039644/0825 →