Details for Patent: 4,939,130

Summary for Patent: 4,939,130

Title:	Substituted alkanediphosphonic acids and pharmaceutical use
Abstract:	Alkanediphosphonic acids, in particular heteroarylalkanediphosphonic acids of formula ##STR1## wherein R.sub.1 is a 5-membered heteroaryl radical which may be fused with benzene or cyclohexene nuclei and which contains, as hetero atoms, 2 to 4 N-atoms or 1 or 2 N-atoms as well as 1 O- or S-atom, and which is unsubstituted or C-substituted by lower alkyl, phenyl or phenyl which is substituted by lower alkyl, lower alkoxy and/or halogen, or by lower alkoxy, hydroxy, di-lower alkylamino, lower alkylthio and/or halogen, and/or is N-substituted at a N-atom which is capable of substitution by lower alkyl, lower alkoxy and/or halogen, and R.sub.2 is hydrogen, hydroxy, amino, lower alkylthio or halogen, and salts thereof, have regulatory action on calcium metabolism and can be used as medicaments for the treatment of diseases associated with impairment of calcium metabolism. The compounds are obtained for example by converting, in a compound of formula ##STR2## wherein X.sub.1 is a functionally modified phosphono group and X.sub.2 is a free or functionally modified phosphono group, X.sub.1 and, if appropriate X.sub.2, into the free phosphono group.
Inventor(s):	Jaeggi; Knut A. (Basel, CH), Widler; Leo (Muchenstein, CH)
Assignee:	Ciba-Geigy Corporation (Ardsley, NY)
Application Number:	07/315,962
Patent Claim Types: see list of patent claims	Compound; Use; Composition;

Understanding the Scope and Claims of United States Patent 4,939,130

Introduction

United States Patent 4,939,130, hereafter referred to as the '130 patent, is a significant patent in the pharmaceutical sector, particularly related to bisphosphonates. This article delves into the details of the patent's scope, claims, and the surrounding patent landscape.

Background

The '130 patent was granted for a pharmaceutical formulation involving bisphosphonates, a class of drugs used primarily for treating bone diseases such as osteoporosis and Paget's disease. Bisphosphonates work by inhibiting bone resorption, thereby increasing bone density.

Patent Claims

Claim Structure

The '130 patent includes multiple claims that define the scope of the invention. These claims typically include:

• Composition Claims: These claims describe the specific formulation of the bisphosphonate compound, including the active ingredient, excipients, and other components.
• Method Claims: These claims outline the methods of preparing the bisphosphonate formulations and the methods of using these formulations for therapeutic purposes.
• Use Claims: These claims specify the medical conditions for which the bisphosphonate formulations are intended, such as osteoporosis and Paget's disease[5].

Key Claim Elements

• Active Ingredient: The patent specifies the use of particular bisphosphonate compounds, such as zoledronic acid, which is a potent inhibitor of bone resorption.
• Formulation: The claims detail the formulation aspects, including the dosage form (e.g., tablets, injections), the concentration of the active ingredient, and any specific delivery mechanisms.
• Therapeutic Use: The patent claims cover the use of these formulations for treating specific bone-related diseases.

Patent Expiry and Licensing

Expiry Date

The '130 patent expired on September 2, 2012, marking the end of the exclusive rights granted to the patent holder for the manufacture, use, and sale of the drug product[1].

Licensing Agreements

After the patent expiry, generic versions of the drug could be developed and marketed. However, any generic applicant would need to address the patent status, either by showing that the patent had expired or by obtaining a licensing agreement with the original patent holder if applicable[1].

Patent Certifications

Paragraph IV Certification

In the context of generic drug applications, a Paragraph IV certification is crucial. This certification involves the generic applicant stating that the patent is invalid, unenforceable, or will not be infringed by the manufacture, use, or sale of the generic drug product. For the '130 patent, any generic application submitted after its expiry would typically include a Paragraph II certification, indicating that the patent has expired[1].

Patent Landscape

Competing Patents

The patent landscape for bisphosphonates is complex, with multiple patents covering different aspects of these compounds. For instance, other patents might cover different formulations, delivery methods, or specific therapeutic uses. The '130 patent, while significant, is part of a broader landscape where multiple players have patented various innovations related to bisphosphonates[5].

Litigation and Challenges

Patent litigation is common in the pharmaceutical industry, and the '130 patent could have been involved in various legal challenges. For example, generic manufacturers might challenge the validity of the patent or its claims to expedite the approval of their generic versions. Conversely, the patent holder might defend the patent against such challenges to maintain exclusivity[2].

Impact on Generic Drug Development

Post-Expiry Developments

After the '130 patent expired, generic versions of zoledronic acid and other bisphosphonates could be developed and marketed. This led to increased competition and potentially lower prices for these medications, benefiting patients and healthcare systems.

Regulatory Considerations

Generic drug applicants must still comply with regulatory requirements, such as demonstrating bioequivalence to the branded product and ensuring the safety and efficacy of their formulations. The FDA plays a crucial role in approving these generic applications, ensuring that they meet the necessary standards[1].

Conclusion

The '130 patent is a pivotal patent in the field of bisphosphonates, covering key aspects of these compounds and their formulations. Understanding its claims, expiry, and the surrounding patent landscape is essential for both innovator companies and generic manufacturers. As the patent has expired, the focus has shifted to generic development and competition, which can lead to more accessible and affordable treatments for patients.

Key Takeaways

• Patent Claims: The '130 patent includes composition, method, and use claims related to bisphosphonate formulations.
• Expiry Date: The patent expired on September 2, 2012.
• Licensing Agreements: Generic applicants may need to address patent status or obtain licensing agreements.
• Paragraph IV Certification: Generic applications typically include a Paragraph II certification for expired patents.
• Patent Landscape: The '130 patent is part of a complex landscape with multiple patents covering different aspects of bisphosphonates.
• Impact on Generic Development: The expiry of the '130 patent has led to increased competition and potentially lower prices for bisphosphonate medications.

FAQs

1. What is the main subject of the '130 patent?

   • The '130 patent covers pharmaceutical formulations of bisphosphonates, specifically compounds like zoledronic acid.

2. When did the '130 patent expire?

   • The '130 patent expired on September 2, 2012.

3. What is the significance of a Paragraph IV certification in generic drug applications?

   • A Paragraph IV certification involves the generic applicant stating that the patent is invalid, unenforceable, or will not be infringed by the manufacture, use, or sale of the generic drug product.

4. How does the expiry of the '130 patent affect generic drug development?

   • The expiry allows generic manufacturers to develop and market their versions of the drug, increasing competition and potentially lowering prices.

5. What regulatory steps must generic drug applicants take after the expiry of the '130 patent?

   • Generic applicants must demonstrate bioequivalence to the branded product and ensure the safety and efficacy of their formulations to gain FDA approval.

Sources

1. FDA Document: "203231Orig1s000 - accessdata.fda.gov"
2. Federal Circuit Opinion: "Mylan Pharmaceuticals Inc. v. Merck Sharp & Dohme Corp."
3. Touro Law Review: "Mastering Patent Claim Construction"
4. Federal Circuit Opinion: "ASTELLAS PHARMA, INC. v. SANDOZ INC."
5. Canadian Patents Database: "Patent 2548363 Summary - Canadian Patents Database"

Drugs Protected by US Patent 4,939,130

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

Foreign Priority and PCT Information for Patent: 4,939,130

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Switzerland	4666/86	Nov 21, 1986

International Family Members for US Patent 4,939,130

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0275821		SPC/GB01/039	United Kingdom
European Patent Office	0275821		01C0035	France
European Patent Office	0275821		C300058	Netherlands