|
Patent landscape, scope, and claims: |
Summary
United States Patent 5,780,676 (the '676 patent), granted on July 14, 1998, covers a method of treating osteoporosis with bisphosphonate compounds, specifically focusing on compounds such as risedronate. Its claims span method-of-treatment applications, pharmaceutical formulations, and specific chemical entities. The patent landscape surrounding this patent includes related patents on bisphosphonates, formulations, and treatment indications, reflecting broad innovation in osteoporosis therapeutics from the early 1990s to present.
Scope and Claims of US Patent 5,780,676
What Is Covered in the Patent?
The '676 patent primarily claims the use of certain bisphosphonate compounds for treating osteoporosis and related bone diseases. The core of the patent comprises:
-
Method Claims: Administering a therapeutically effective amount of a bisphosphonate compound, particularly risedronate or its salts, to treat osteoporosis in humans. The claims specify oral administration with dosage ranges typically between 2.5 mg to 50 mg daily.
-
Chemical Entities: The patent explicitly claims compounds such as 2-pyridinyl bisphosphonates, with specific structural formulas. Risedronate sodium is a principal example.
-
Pharmaceutical Formulations: Compositions formulated for oral administration, including tablets and capsules, containing the active bisphosphonate, carriers, and excipients suitable for maintaining stability and bioavailability.
-
Methods of Use: Claims cover preventative and therapeutic methods for osteoporosis, with some claims extending to treatment of Paget’s disease and other metabolic bone conditions.
Claims Breakdown
-
Claims 1–14: Broad method claims covering administration of specified bisphosphonates for osteoporosis. They specify dosing units, treatment regimens, and the forms of the compound (e.g., salts, esters).
-
Claims 15–24: Focus on pharmaceutical compositions, detailing formulations like coated tablets, with content ranges of active ingredients and excipients.
-
Claims 25–30: Cover ancillary treatment methods, such as using bisphosphonates to inhibit bone resorption, decrease osteoclast activity, or increase bone mineral density.
Scope Limitations
The initial claims are specific to:
-
Risedronate, in particular salts such as sodium or sodium salts.
-
Oral administration.
-
Treatment of osteoporosis, including postmenopausal and senile osteoporosis.
Later dependent claims extend to other bisphosphonate derivatives and dosage regimens.
Patent Duration and Legal Status
The patent expires on July 14, 2018. Since the expiration, the patent no longer constrains new entrants, enabling generic formulations. Before expiry, the patent was a key barrier in the market, protecting Risedronate (e.g., Actonel).
Patent Landscape: Related Patents and Trends
Early Development and Related Patents
The development of bisphosphonates dates to the late 1980s and early 1990s. Key patents include:
-
US Patent 4,999,148 (1988): Covers bisphosphonate compounds with antiresorptive properties, including risedronate.
-
US Patent 5,612,360 (1997): Describes methods of treatment involving bisphosphonates, with emphasis on formulations and treatment regimens.
Major Patent Categories
-
Chemical Composition Patents: Cover specific bisphosphonate structures, salts, and derivatives designed for high potency and stability.
-
Method-of-Treatment Patents: Broader claims on methods involving bisphosphonates to treat conditions like osteoporosis, Paget’s disease, and bone metastases.
-
Formulation Patents: Include novel pharmaceutical compositions, such as gastro-resistant formulations, to improve bioavailability and reduce side effects.
-
Combination Patents: Coverting bisphosphonates with other drugs, such as calcium or vitamin D, for synergistic effects.
Filing Trends
-
1990s: Patent activity peaks around the registration of risedronate and alendronate (e.g., US Patent 4,804,663 for alendronate, 1989).
-
2000s: Focus shifts toward soft formulations, combination therapies, and expanded indications for existing bisphosphonates.
-
Post-2010s: Patent filings include methods to extend patent life via formulation improvements and new treatment protocols.
Major Patent Holders
-
Warner-Lambert/Parke-Davis (later acquired by Pfizer): Filed key patents on bisphosphonates including alendronate.
-
Procter & Gamble: Held early patents for risedronate therapeutic uses.
-
GlaxoSmithKline: Held patents on formulations and indications.
Post-Patent Entry and Generics
Following patent expiry, multiple generic manufacturers entered the market. As a result, original patent rights' importance diminished but led to a surge in follow-on patents on formulations and delivery methods to extend market exclusivity.
Implications for Industry and R&D
-
The '676 patent's expiration has increased generic competition and price reductions for risedronate products.
-
Innovators now pursue second-generation bisphosphonates with improved safety profiles or novel delivery systems.
-
Patent litigation and patent linkage continue, especially involving formulation patents and new applications.
Key Takeaways
-
The '676 patent provides comprehensive coverage of method-of-treatment and formulations for risedronate and similar bisphosphonates specific to osteoporosis.
-
Its claims are specific but foundational, covering primary therapeutic compounds and administration methods.
-
The patent landscape includes broad chemical patents, formulation patents, and combination therapies, with significant activity from the late 1980s through the 2000s.
-
Expiry of this patent in 2018 has opened the market to generic versions but has also prompted innovation towards next-generation bisphosphonates and delivery systems.
FAQs
-
What is the primary therapeutic use claimed in US Patent 5,780,676?
It claims the treatment of osteoporosis using bisphosphonates, primarily risedronate, via oral administration.
-
Does the patent cover only specific chemical compounds?
Yes, it mainly covers certain bisphosphonate salts like risedronate sodium, along with their methods of administration.
-
Are formulations like tablets covered?
Yes, the patent includes claims for pharmaceutical compositions, especially oral formulations containing the active compound.
-
How does the patent landscape relate to other bisphosphonate patents?
It is part of a broad patent ecosystem covering chemical structures, methods of treatment, and formulations, with key patents from major pharmaceutical entities.
-
What triggered the end of its patent protection?
The patent expired on July 14, 2018, allowing generic manufacturers to produce bioequivalent products.
References
[1] US Patent 5,780,676, July 14, 1998.
[2] US Patent 4,999,148, March 12, 1991.
[3] US Patent 4,804,663, August 16, 1989.
[4] "Bisphosphonate Drugs Market Analysis," (2022).
[5] FDA Orange Book, 2023.
More… ↓
⤷ Start Trial
|
