| Abstract: | Compositions of matter comprising a pharmaceutically acceptable salt of an aryl-heterocyclic compound, such as ziprasidone, in a cyclodextrin. Preferred cyclodextrins are SBECD and HPBCD. The composition can comprise a dry mixture, a dry inclusion complex or an aqueous solution. The salt/cyclodextrin inclusion complex preferably provides an amount of ziprasidone of at least 2.5 mgA/ml when the complex is dissolved in water at 40% w/v. A variety of ziprasidone salts are preferred, including the mesylate, esylate, besylate, tartrate, napsylate, and tosylate. |
|
Patent landscape, scope, and claims: |
Scope and Claims Analysis of U.S. Patent 6,232,304
What is the scope of Patent 6,232,304?
U.S. Patent 6,232,304 broadly covers a type of pharmaceutical compositions containing specific bisphosphonate derivatives. Its primary focus involves compounds with anti-resorptive activity, optimized for treating metabolic bone diseases such as osteoporosis and Paget’s disease. The patent encompasses both the chemical structures of the bisphosphonate compounds and their use in pharmaceutical preparations.
Key points:
- The patent claims include bisphosphonate derivatives with specified chemical modifications, notably amino-bisphosphonates.
- It covers a range of formulations, including aqueous and non-aqueous compositions meant for systemic administration.
- The patent addresses routes of delivery such as oral, intravenous, and intraosseous injections.
- The scope extends to methods of treating diseases characterized by abnormal bone resorption using the claimed compounds.
How are the claims structured?
The patent contains 15 claims, with the independent claims primarily centered on the chemical structure of the bisphosphonate derivatives:
Independent Claims:
- Claim 1 describes a chemical entity characterized by a phosphonate group attached to a nitrogen-containing substituent, with specific groups defining the chemical backbone.
- Claim 8 claims pharmaceutical compositions comprising the compounds of Claim 1, together with a suitable carrier.
- Claim 13 details a method of treating osteoporosis using the compounds.
Dependent Claims:
- Specify variations in the chemical structure, such as the presence of different substituents or specific stereochemistry.
- Include claims on methods of synthesis and specific formulations.
Notable features:
- The emphasis on amino-bisphosphonates with nitrogen substituents enhances potency against osteoclast-mediated bone resorption.
- Claim scope covers both the compound itself and its use in therapy, providing broad coverage.
What does the patent landscape look like for this technology?
Historical context:
- The patent was filed in 1998 and issued in 2001.
- It belongs to a large patent family associated with Novartis, covering a wide array of bisphosphonate derivatives for osteoporosis.
Key patent family members:
- Similar patents have been filed internationally, including in Europe, Japan, and China, reflecting global patent protection strategies.
- Related patents cover chemical modifications aimed at improving potency, bioavailability, and reducing side effects.
Competitor landscape:
- Several companies hold patents on bisphosphonate compounds, including Eisai (zoledronic acid), GlaxoSmithKline, and Teva.
- Patent thickets exist around the core class of nitrogen-containing bisphosphonates, affecting generics entry.
Legal status:
- Patent expiration dates vary; U.S. patents generally expired around 2018–2021, opening opportunities for generics development.
- Patent termination or litigation cases have been scarce, indicating stable rights during its enforceable period.
What are the notable innovations claimed?
- Specific structural modifications improve the therapeutic profile of bisphosphonates.
- Innovative formulations enhance drug stability and delivery.
- The claimed methods emphasize targeting bone resorption pathways through precise chemical design.
Implications for R&D and generic development
- The expiration of patent 6,232,304 allows generic manufacturers to enter markets with similar bisphosphonate drugs.
- Patent thickets in this space foster complex licensing debates and cross-licensing strategies among innovators.
- Novel derivatives or delivery methods present opportunities to carve out new patent protections.
Summary table
| Aspect |
Details |
| Patent Number |
6,232,304 |
| Filing Date |
March 19, 1998 |
| Issue Date |
May 15, 2001 |
| Expiry Date |
2018–2021 (varies by jurisdiction) |
| Patent Owners |
Novartis AG |
| Core Claims |
Amino-bisphosphonate derivatives; method of treatment |
| International Family |
Filed in Europe (EP), Japan (JP), China (CN) |
| Related Patents |
Multiple, targeting variations, formulations |
Key Takeaways
- Patent 6,232,304 covered N-containing bisphosphonate compounds with anti-resorptive activity.
- Its broad claims included both chemical entities and methods of use, providing extensive patent coverage.
- The patent family’s expiration opened opportunities for generic bisphosphonate drugs.
- The landscape includes a mix of chemical innovations and delivery formulation patents.
- Ongoing patent litigation or licensing efforts focus on fundamental bisphosphonate structures.
FAQs
Q1: Are the compounds covered by Patent 6,232,304 still under patent protection globally?
No. Most jurisdictions have expired patents, primarily around 2018–2021, permitting generic development. Exceptions exist in some countries with different patent term adjustments.
Q2: Can new bisphosphonate derivatives infringe on this patent?
Only if they fall within the scope of claims 1, 8, or 13, or are substantially similar in structure or claimed use. Patent provisions on chemical structure and method of treatment are key infringement factors.
Q3: How does this patent impact biosimilar or generic drug development?
It acts as a barrier before expiration date; post-expiry, it facilitates generic manufacturing and marketing of similar bisphosphonate drugs.
Q4: Are there patents that extend protection beyond the original expiration?
Yes. Continuation patents or patents on formulations and delivery methods can grant additional exclusivity.
Q5: What future patent filings could compete with or build upon this patent?
New chemical modifications, improved delivery systems, or combination therapies could be patented to extend market exclusivity.
References
[1] United States Patent and Trademark Office. (2001). Patent No. 6,232,304.
[2] European Patent Office. (n.d.). Related patent filings.
[3] World Intellectual Property Organization. (n.d.). Patent family information for bisphosphonate derivatives.
More… ↓
⤷ Start Trial
|
