Synthesis of halichondrin analogs and uses thereof
US10556910B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jun 30, 2015 |
| Grant date | Feb 11, 2020 |
| Priority date | — |
| Expiry date | Jun 30, 2035 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D493/14
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting microtubule dynamics. Also provided are methods of synthesis, pharmaceutical compositions, kits, methods of treatment, and uses that involve the compounds for treatment of a proliferative disease (e.g., cancer). Compounds of the present invention are particularly useful for the treatment of metastatic breast cancer, non-small cell lung cancer, prostate cancer, and sarcoma. The included methods of synthesis are useful for the preparation of compounds of Formula (I)-(III) along with naturally occurring halicondrins (e.g., halichondrin B & C, norhalichondrin A, B, & C, and homohalichondrin A, B, & C). Also included are methods for interconverting between the halichondrins, norhalichondrins, and homohalichondrins and their unnatural epimers at the C38 ketal stereocenter through the use of an acid-mediated equilibration.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.