IP Library Granted Patent US 10,888,562
Granted Patent B1
US 10,888,562 · App. 16/376,452 · Granted Jan 12, 2021

AXL kinase inhibitors and use of the same

Inventors: Adam Siddiqui-Jain (South Jordan, UT); Paul Flynn (Citrus Heights, CA); Akihito Nonoyama (Hyogo, JP); Akihito Kiguchiya (Nara, JP)
Assignee: Sumitomo Dainippon Pharma Oncology, Inc.
A61K31/506A61K31/519A61P35/02C07D403/12C07B2200/13
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Quick Facts
Patent No.
US 10,888,562
App. No.
16/376,452
Granted
Jan 12, 2021
Kind
B1
Abstract

Tartrate salts of the compound of structure (I), crystalline forms thereof, and therapeutic applications thereof for treating solid tumors (e.g., advanced solid tumor) or hematopoietic cancers. Also provided herein are methods for synthesizing the tartrate salts and the crystalline forms thereof.

Claims (11)

1. A crystalline form of a tartrate salt of the compound of structure (I):

2. The crystalline form of claim 1 , which is crystalline Form A, having a molar ratio of tartaric acid to the compound of structure (I) of about 2:1.

3. The crystalline form of claim 2 , characterized by an x-ray powder diffraction (XRPD) pattern comprising peaks, in units 2-theta, at 11.2±0.2, 17.1±0.2, and 19.9±0.2.

4. The crystalline form of claim 2 , characterized by an XRPD pattern comprising three or more peaks, in units of 2-theta, selected from 7.0±0.2, 11.2±0.2, 15.4±0.2, 16.3±0.2, 17.1±0.2, 19.9±0.2, 21.6±0.2, and 25.5±0.2.

5. A composition comprising the crystalline form of claim 2 .

6. The composition of claim 5 , comprising crystalline Form A in substantially pure form.

7. The pharmaceutical composition of claim 5 , wherein the pharmaceutical composition is formulated for oral administration.

8. A unit dose comprising the pharmaceutical composition of claim 5 , wherein the unit dose comprises about 1-100 mg of the tartrate salt.

9. The crystalline form of claim 1 , wherein the tartrate salt is a salt of L-(+)-tartaric acid.

10. The crystalline form of claim 2 , wherein Form A is in substantially pure form.

11. The crystalline form of claim 4 , wherein the XRPD pattern is substantially identical to the XRPD pattern shown in FIG. 61A .

Assignments (6)
CHANGE OF NAME Recorded Apr 27, 2022
From: SUMITOMO DAINIPPON PHARMA ONCOLOGY, INC.
To: SUMITOMO PHARMA ONCOLOGY, INC.
Reel/Frame 059809/0557 →
MERGER Recorded Jul 10, 2020
From: TOLERO PHARMACEUTICALS, INC.
To: BOSTON BIOMEDICAL, INC.
Reel/Frame 053172/0424 →
CHANGE OF NAME Recorded Jul 10, 2020
From: BOSTON BIOMEDICAL, INC.
To: SUMITOMO DAINIPPON PHARMA ONCOLOGY, INC.
Reel/Frame 053184/0684 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 17, 2019
From: SIDDIQUI-JAIN, ADAM; WARNER, STEVEN L.; FLYNN, PAUL; BEARSS, DAVID J.; FOULKS, JASON MARC
To: TOLERO PHARMACEUTICALS, INC.
Reel/Frame 049775/0391 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 17, 2019
From: TOMIMATSU, NOZOMI; FUJIMURA, KEN; UMEHARA, HIROKI; NONOYAMA, AKIHITO; KIGUCHIYA, AKIHITO
To: SUMITOMO DAINIPPON PHARMA COMPANY, LIMITED
Reel/Frame 049775/0543 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 17, 2019
From: SUMITOMO DAINIPPON PHARMA COMPANY, LIMITED
To: TOLERO PHARMACEUTICALS, INC.
Reel/Frame 049775/0631 →