IP Library Granted Patent US 12,011,442
Granted Patent B2
US 12,011,442 · App. 16/948,893 · Granted Jun 18, 2024

Solid-state forms of Abemaciclib, their use and preparation

Inventor: Clifton R. Hamilton (Devens, MA)
Assignee: Macfarlan Smith Limited
A61K31/506C07B2200/13
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Quick Facts
Patent No.
US 12,011,442
App. No.
16/948,893
Granted
Jun 18, 2024
Kind
B2
Abstract

The invention relates to a crystalline methanol solvate or hydrate form of ABC, and an anhydrous form of ABC, that reversibly forms a hydrate of ABC. The invention is also directed to the preparation of the aforesaid solvate, hydrate, and anhydrous solid-state forms of ABC. Furthermore, the invention relates to pharmaceutical compositions comprising at least one of the aforesaid crystalline forms of ABC according to the invention, and the pharmaceutical use of at least one of the aforesaid crystalline forms of ABC according to the invention for treatment of a patient in need thereof.

Claims (6)

1. A compound which is crystalline Form II of anhydrous abemaciclib.

2. The compound of claim 1 having at least 2 or more X-ray powder diffraction peaks selected from 5.1, 6.2 and 16.8° 2⊖ measured by CuKα radiation +/−0.2⊖.

3. The compound of claim 1 having a TGA plot showing onset of decomposition at about 320° C.

4. The compound of claim 1 having a thermal event at about 180-182° C.

5. A process for the preparation of solid-state Form II of anhydrous abemaciclib, comprising:

(a) vacuum drying Form I of variable methanol solvate of abemaciclib at an elevated temperature for about 8 hours or more to yield solid-state Form II of anhydrous abemaciclib.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 7, 2022
From: JOHNSON MATTHEY PUBLIC LIMITED COMPANY
To: MACFARLAN SMITH LIMITED
Reel/Frame 061888/0166 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 3, 2022
From: HAMILTON, CLIFTON
To: JOHNSON MATTHEY PUBLIC LIMITED COMPANY
Reel/Frame 058529/0313 →