# US 11,440,908 B2 · Crystalline forms of dasatinib

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- Number: US 11,440,908 B2
- Document ID: US11440908B2
- Status: Granted
- Kind: B2
- Application number: 16/949,260
- Filed: 2020-10-22
- Published: 2021-02-04
- Granted: 2022-09-13
- Earliest claimed: 2018-04-25
- Assignees: Johnson Matthey Public Limited Company
- Applicants: Johnson Matthey Public Limited Company
- Inventors: Padmini Kavuru
- Web page: https://patentgrep.com/patent/US11440908B2

## CPC

- C07D 417/12: linked by a chain containing hetero atoms as chain links
- A61P 35/02: specific for leukemia
- C07B 2200/13: Crystalline forms, e.g. polymorphs
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)

## Abstract

The present disclosure relates to a dasatinib co-crystal form comprising dasatinib and a second compound, also referred to as a co-crystal former, wherein the second compound is selected from butyl paraben, propyl paraben and ethyl vanillin. The present disclosure is also related to an ethyl formate solvate form of dasatinib. The present disclosure is also related to processes for the preparation of the dasatinib co-crystal and solvate forms of dasatinib. Further, the present disclosure also relates to pharmaceutical compositions comprising the dasatinib co-crystal and solvate forms of dasatinib and methods for treating disease using the dasatinib co-crystal and solvate forms of dasatinib.

## Claims

### Claim 1

A dasatinib co-crystal comprising dasatinib and a second compound, wherein the second compound is ethyl vanillin, characterized by having at least 2 or more X-ray powder diffraction peaks selected from about 5.7, 10.9, 13.5, 17.1, 18.4, 19.4, 23.7 and 26.3° 2θ.

### Claim 2 (depends on 1)

The dasatinib co-crystal according to claim 1, wherein a molar ratio of the dasatinib to the ethyl vanillin is about 1:1.

### Claim 3 (depends on 1)

The dasatinib co-crystal according to claim 1, which is Form II co-crystal of dasatinib and ethyl vanillin.

### Claim 4 (depends on 3)

The dasatinib co-crystal according to claim 3, characterized by one or more thermal events selected from about 140° C., about 181° C., and about 293° C., as measured by differential scanning calorimetry.

### Claim 5 (depends on 3)

The dasatinib co-crystal of claim 3 which is monoclinic, P2l/n.

### Claim 6 (depends on 3)

The dasatinib co-crystal d of claim 3 which has single crystal parameters
a=18.452 (1) Å
b=9.441 (6) Å
c=19.377 (1) Å
α=γ=90°, η=108.78 (1°).

### Claim 7 (depends on 3)

The dasatinib co-crystal of claim 3 which has a cell volume of about 3195.71 Å3.