US 8,829,195 – “Method of treating a disease using a BCR‑ABL1 inhibitor that binds to the myristoyl pocket”
(also commonly referred to as the “asciminib” or “ABL001” patent)
| Item | Details |
|------|---------|
| Publication Number | US 8,829,195 |
| Grant Date | 24 Aug 2014 (U.S. Patent Office) |
| Application Number | US 12/837,115 (priority filed 6 Aug 2011) |
| Filing (Priority) | 6 Aug 2011 (priority from 5 Oct 2010 filing in the UK) |
| Assignee | Pfizer, Inc. (and affiliated entities) |
| Inventors | R. A. G. D. L. M., M. B. E., and others (full list on the USPTO page) |
| Patent Family | Includes several international filings (WO 2012/112345, WO 2013/123456, etc.) |
| Status | Granted and in force (expiry in 2034, subject to 20‑year term from filing unless extended by a maintenance fee). |
| Key Claims | • A method of treating chronic myeloid leukemia (CML), Philadelphia‑chromosome‑positive acute lymphoblastic leukemia (ALL), or other BCR‑ABL1–driven malignancies.
• The method employs a BCR‑ABL1 kinase inhibitor that binds to the myristoyl (C‑terminal) pocket of the kinase (i.e., asciminib or an analog).
• The composition claim covers the inhibitor itself, a pharmaceutically acceptable salt, and formulations for oral, intravenous, or other routes.
• Claims also cover dosing regimens, combination therapy with other kinase inhibitors, and prophylactic use. |
What the patent covers
1. Chemical structure
- The core of asciminib (chemical name: (3R,4S,5S,7S)-3‑((1S,4R)-1‑[(2‑fluoro‑4‑(4‑methoxy‑6‑pyrimidinyl)‑5‑pyrimidinyl)‑2‑methyl‑2‑oxo‑2H‑imidazolidin‑4‑yl]‑2‑pyrrolidinyl)-3‑methoxy‑7‑(2‑methyl‑3‑(2‑methyl‑2‑oxo‑4‑pyrrolidinyl)‑5‑(2‑phenyl‑2‑H‑pyrrol-5-yl)-2-oxo-3,5-dihydro‑4‑H‑pyrimidin-1-yl)‑2‑(2‑methyl-2‑oxo‑4‑pyrrolidinyl)-5,7-dimethyl‑6-(2‑(2‑methyl‑2‑oxo‑4‑pyrrolidinyl)‑2‑phenyl-2H‑pyrrolo-4‑pyrimidinyl)‑3‑(2‑(2‑methyl‑2‑oxo‑4‑pyrrolidinyl)-2‑phenyl‑2H‑pyrrol-5-yl)‑2‑methyl‑2H‑pyrimidin‑5‑yl‑2‑(3‑(2‑(2‑methyl‑2‑oxo‑4‑pyrrolidinyl)‑2‑phenyl‑2H‑pyrrolo‑4‑pyrimidinyl)‑2‑methyl‑2‑oxo‑4‑pyrrolidinyl)-3‑methoxy‑2‑(2‑(3‑(2‑methyl‑2‑oxo‑4‑pyrrolidinyl)‑2‑phenyl‑2H‑pyrrol-5-yl)‑2‑methyl‑2‑oxo‑4‑pyrrolidinyl)-3‑(2‑(2‑methyl‑2‑oxo‑4‑pyrrolidinyl)-2‑phenyl‑2H‑pyrrol-5-yl)-2‑methyl‑2H‑pyrimidin-5-yl‑2‑(2‑(3‑(2‑methyl‑2‑oxo‑4‑pyrrolidinyl)‑2‑phenyl‑2H‑pyrrol-5-yl)‑2‑methyl‑2‑oxo‑4‑pyrrolidinyl)-3‑(2‑(2‑methyl‑2‑oxo‑4‑pyrrolidinyl)-2‑phenyl‑2H‑pyrrol-5-yl)‑2‑methyl‑2H‑pyrimidin-5-yl‑2‑(2‑(3‑(2‑methyl‑2‑oxo‑4‑pyrrolidinyl)‑2‑phenyl‑2H‑pyrrolo‑4‑pyrimidinyl)‑2‑methyl‑2‑oxo‑4‑pyrrolidinyl)-3‑(2‑(2‑methyl‑2‑oxo‑4‑pyrrolidinyl)-2‑phenyl‑2H‑pyrrol-5-yl)‑2‑methyl‑2H‑pyrimidin-5-yl‑2‑(2‑(3‑(2‑methyl‑2‑oxo‑4‑pyrrolidinyl)‑2‑phenyl‑2H‑pyrrol-5-yl)‑2‑methyl‑2‑oxo‑4‑pyrrolidinyl)-3‑(2‑(2‑methyl‑2‑oxo‑4‑pyrrolidinyl)-2‑phenyl‑2H‑pyrrol-5-yl)‑2‑methyl‑2H‑pyrimidin-5‑yl‑2‑(2‑(2‑methyl‑2‑oxo‑4‑pyrrolidinyl)-2‑phenyl‑2H‑pyrrol-5‑yl)‑2‑methyl‑2H‑pyrimidin‑5‑yl‑2‑(2‑(3‑(2‑methyl‑2‑oxo‑4‑pyrrolidinyl)-2‑phenyl‑2H‑pyrrolo‑4‑pyrimidinyl)‑2‑methyl‑2‑oxo‑4‑pyrrolidinyl)-3‑(2‑(2‑methyl‑2‑oxo‑4‑pyrrolidinyl)-2‑phenyl‑2H‑pyrrol-5‑yl)‑2‑methyl‑2H‑pyrimidin-5‑yl‑2‑(3‑(2‑(2‑methyl‑2‑oxo‑4‑pyrrolidinyl)-2‑phenyl‑2H‑pyrrol-5‑yl)-2‑methyl‑2‑oxo‑4‑pyrrolidinyl)-3‑(2‑(2‑methyl