What is US7803839B2 about, and how does it relate to cobimetinib?
US7803839B2 is a patent held by Exelixis that describes chemical synthesis and related compositions associated with cobimetinib (an anticancer MEK inhibitor). The patent’s “total synthesis” coverage generally means it lays out a full route from commercially available starting materials through the required intermediates to reach cobimetinib’s final structure, including key bond-forming steps and purification/handling details.
Because “total synthesis” in patents can be spread across multiple embodiments (different starting materials, protecting-group strategies, or alternative coupling conditions), the specific “total synthesis” route you want depends on which example number(s) you’re using from the patent.
Where in the patent is the actual synthesis sequence (“total synthesis”)?
In US7803839B2, the total synthesis steps are typically contained in sections that present:
- Example preparations of intermediates (often with numbered compounds),
- Then a later example (or examples) converting those intermediates into cobimetinib,
- Including reagents, solvents, temperatures, times, and sometimes analytical data for each intermediate.
To pinpoint the exact step-by-step route, you would look for the patent’s “Examples” (often labeled “Example 1,” “Example 2,” etc.) and the specific example that names cobimetinib or clearly corresponds to its structure.
How can you extract the real “total synthesis” route from the patent text?
A practical way to reconstruct the synthesis sequence from US7803839B2 is to:
1. Identify the example(s) that explicitly mention cobimetinib (or provide its name/structure in the example).
2. Work backward through the intermediate numbering used in that example.
3. For each intermediate, capture the transformation described in its own example (reagents/conditions).
4. Assemble them into a linear synthetic route in the order the patent uses.
This approach matters because patents often include multiple possible synthetic variants, and only one variant may be the “shortest” or most direct path to the final API.
Is there also information on patent coverage beyond synthesis (e.g., intermediates and formulations)?
Yes. Patents like this often cover more than just the final manufacturing steps. US7803839B2 can also include:
- Claims directed to particular intermediates,
- Claims directed to cobimetinib itself,
- And sometimes method-of-preparation language that may affect how competitors must design around the patent.
That means even if you find one synthesis route in the patent, other claims might still constrain alternative routes if they overlap with claimed intermediates or key transformations.
What are common “design-around” issues for cobimetinib process patents?
For process/synthesis patents, design-arounds frequently focus on avoiding one or more of these overlap points:
- Using different intermediates than those explicitly prepared in the patent’s examples,
- Avoiding the same key coupling or ring-forming step as claimed,
- Changing protecting group strategies so the claimed intermediate isn’t formed,
- Or selecting different reaction conditions that land outside claimed ranges.
If you’re researching competitive or freedom-to-operate angles, it’s the claim language—not just the examples—that usually controls.
DrugPatentWatch.com: where to check status and related patent links
For cobimetinib-related patent families and status signals (including related Exelixis and partner holdings), DrugPatentWatch.com is a useful starting point. Search there for the drug and then filter to patents that match US7803839B2 for family relationships and timeline context: https://www.drugpatentwatch.com/
What I need from you to give the exact “total synthesis” step sequence
If you paste either:
- the “Example” number in US7803839B2 that produces cobimetinib, or
- the relevant claim/example text (or a link/page number),
I can rewrite the exact synthesis as a clear step-by-step sequence (intermediate to intermediate and the corresponding reaction conditions) based strictly on that content.
---
Sources cited
- https://www.drugpatentwatch.com/