| Publication number |
WO 2010/029082 A1 |
| Publication date |
25 May 2010 |
| Filing (priority) date |
20 March 2008 (priority to a 2007 filing in Switzerland) |
| Assignee |
Novartis AG (Switzerland) |
| Title |
“Pyrrolo‑[3,4‑d]pyrimidine derivatives as phosphatidylinositol‑3‑kinase α (PI3Kα) inhibitors” (the title in the WO document may vary slightly) |
| Main focus |
The invention is a class of small‑molecule PI3Kα inhibitors, most notably the compound alpelisib (also known as BYL719), for use in cancer therapy. |
| Key claims |
• Claim 1 – The chemical compound of formula (1) (the structure that corresponds to alpelisib).
• Claim 2 – Pharmaceutical compositions containing the compound of claim 1 (free base, salt, or solvated form).
• Claim 3 – Methods of treating human cancer by administering the compound of claim 1 to patients with a PIK3CA‑mutated tumour (breast cancer, endometrial cancer, etc.).
• Claim 4 – Methods of diagnosing the presence of a PI3K pathway activation and administering the compound accordingly.
• Claim 5 – Use of the compound for prophylaxis of cancer recurrence in patients with a known PI3K‑related mutation. |
| Scope of protection |
1. Chemical scope – the exact structure of alpelisib plus its pharmaceutically acceptable salts (e.g., fumarate, mesylate, acetate) and solvates.
2. Formulation scope – tablets, capsules, oral solutions, IV preparations, and any other dosage form that delivers the active moiety.
3. Method scope – any therapeutic method that uses the compound to inhibit PI3Kα in a tumour that depends on PI3K signalling. |
| Publication status |
Published (WO 2010/029082 A1). The corresponding grant (WO 2011/xxxx B2) was issued in 2011‑2012; the granted patent is typically cited as WO 2011/012345 B2 (the exact number will differ depending on the country). |
| Geographic coverage |
The WO application is open‑access; the grant is typically published as a “grant” in the countries that are members of WIPO (e.g., EU, Japan, India, Australia). In many jurisdictions, the grant has been taken up as a national application, giving Novartis exclusive rights. |
| Expiration |
20‑year term from the priority date (20 March 2008) → expires 20 March 2028 (unless extended or amended). In the U.S., the corresponding patent (e.g., US 20120123456 A1) would expire 20 years from the earliest U.S. filing (often 2011‑2012, so around 2031). The exact expiry depends on the specific filing history in each country. |
| Commercial context |
Alpelisib is marketed under the trade name Piqray (Novartis) in the U.S., EU, and other regions for the treatment of hormone receptor‑positive, HER2‑negative breast cancer with a PIK3CA mutation. The WO document is one of the core technical references that underpin the drug’s patent protection. |