Abstract: The present invention relates to an improved process for the preparation of 4H-pyranone structured CYP11A1 inhibitors such as 5-((1-(methylsulfonyl)-piperidin-4-yl)methoxy)-2-((5-(trifluoromethyl)isoindolin-2-yl)methyl)-4H-pyran-4-one (1A) and key intermediates thereof including 5-(trifluoromethyl)isoindoline (V) and 5-hydroxy-2-((5-(trifluoromethyl)isoindolin-2-yl)methyl)-4H-pyran-4-one (III). CYP11A1 inhibitors are useful in the treatment of hormonally regulated cancers, such as prostate cancer and breast cancer.
| # | Name | Date |
|---|---|---|
| 1 | 202317086957-STATEMENT OF UNDERTAKING (FORM 3) [19-12-2023(online)].pdf | 2023-12-19 |
| 2 | 202317086957-NOTIFICATION OF INT. APPLN. NO. & FILING DATE (PCT-RO-105-PCT Pamphlet) [19-12-2023(online)].pdf | 2023-12-19 |
| 3 | 202317086957-FORM 1 [19-12-2023(online)].pdf | 2023-12-19 |
| 4 | 202317086957-DECLARATION OF INVENTORSHIP (FORM 5) [19-12-2023(online)].pdf | 2023-12-19 |
| 5 | 202317086957-COMPLETE SPECIFICATION [19-12-2023(online)].pdf | 2023-12-19 |
| 6 | 202317086957-Proof of Right [10-01-2024(online)].pdf | 2024-01-10 |
| 7 | 202317086957-FORM-26 [10-01-2024(online)].pdf | 2024-01-10 |
| 8 | 202317086957-FORM 3 [17-06-2024(online)].pdf | 2024-06-17 |
| 9 | 202317086957-FORM 18 [18-06-2025(online)].pdf | 2025-06-18 |