Crystalline form of Olaparib

Patent metadata

Field	Value
Publication number	US-10662178-B2
Application number	US-201916261901-A
Country	US
Kind code	B2
Filing date	Jan 30, 2019
Priority date	Jan 31, 2018
Publication date	May 26, 2020
Grant date	May 26, 2020

Abstract

The present invention provides a novel crystalline form of Olaparib comprising Olaparib and benzyl alcohol, compositions thereof, and the use of this crystalline form in the treatment of cancers, such as germline BRCA-mutated (gBRCAm) advanced ovarian cancer.

First claim

What is claimed is:

1. A crystalline form of Olaparib comprising Olaparib and benzyl alcohol.

2. The crystalline form of claim 1 , wherein the molar ratio of Olaparib to benzyl alcohol is between approximately 1:0.25 and approximately 1:1.25.

3. The crystalline form of claim 1 , wherein the molar ratio of Olaparib to benzyl alcohol is between approximately 1:0.25 and approximately 1:0.75.

4. The crystalline form of claim 1 , wherein the molar ratio of Olaparib to benzyl alcohol is between approximately 1:0.4 and approximately 1:0.6.

5. The crystalline form of claim 1 , characterized by a PXRD diffractogram comprising peaks, expressed in degrees 2θ (±0.2°), at 10.1°, 12.5° and 20.7°.

6. The crystalline form of claim 5 , wherein the PXRD diffractogram further comprises at least three peaks, expressed in degrees 2θ (±0.2°), selected from the group consisting of: 7.1°, 11.8°, 13.5°, 15.2°, 17.0°, 18.4°, 19.0°, 21.6°, 24.5° and 26.6°.

7. The crystalline form of claim 5 , wherein the PXRD diffractogram further comprises peaks, expressed in degrees 2θ (±0.2°), at 7.1°, 11.8°, 13.5°, 15.2°, 17.0°, 18.4°, 19.0°, 21.6°, 24.5° and 26.6°.

8. The crystalline form of claim 7 , providing a PXRD diffractogram comprising peaks in substantially the same positions (±0.2° 2θ) as those shown in FIG. 1 .

9. The crystalline form of claim 5 , wherein the molar ratio of Olaparib to benzyl alcohol is between approximately 1:0.25 and approximately 1:0.75.

10. The crystalline form of claim 6 , wherein the molar ratio of Olaparib to benzyl alcohol is between approximately 1:0.25 and approximately 1:0.75.

11. A pharmaceutical composition comprising the crystalline form of Olaparib of claim 5 , and one or more pharmaceutically acceptable excipients.

12. The pharmaceutical composition of claim 11 , wherein the pharmaceutical composition is a capsule.

13. The pharmaceutical composition of claim 11 , wherein the pharmaceutical composition is a tablet.

14. The pharmaceutical composition of claim 13 , wherein the pharmaceutical composition comprises an amount of the crystalline form of Olaparib equivalent to 100 mg or 150 mg Olaparib.

Assignees

• Apotex Inc

Inventors

• Rey Allan W
• Souza Fabio E S
• Bhattacharyya Annyt
• Khalili Bahareh

Classifications

• C07D403/12 Primary

  linked by a chain containing hetero atoms as chain links · CPC title

• A61K9/20

  Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} · CPC title

• A61K31/502

  ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine · CPC title

• A61K9/48

  Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)} · CPC title

• A61K31/497

  containing further heterocyclic rings · CPC title