Details for Patent: 4,782,047

Summary for Patent: 4,782,047

Title:	Aqueous steroid formulations for nasal administration
Abstract:	A non-stinging aqueous anti-inflammatory steroid formulation suitable for intranasal administration comprises: an anti-inflammatory steroid in an amount between about 0.01% and about 0.05% (w/v); propylene glycol in an amount between about 2% and about 10% (w/v); PEG 400 in an amount between about 10% and about 25% (w/v); polysorbate 20 in an amount between about 1% and about 4% (w/v); an effective amount of a preservative; an effective amount of a stabilizer; an effective amount of an antioxidant; water; and pH buffering agent sufficient to adjust the pH of the resulting solution to between about 3.5 and about 7.
Inventor(s):	Eric Benjamin, Shabbir Anik, Ya-Yun T. Lin
Assignee:	Quadrant Technologies Ltd
Application Number:	US06/866,171
Patent Claim Types: see list of patent claims	Formulation; Use;

Detailed Analysis of the Scope and Claims and Patent Landscape for U.S. Patent 4,782,047

---

Introduction

U.S. Patent 4,782,047, granted on November 1, 1988, to the Johnson & Johnson company, represents a pioneering innovation in the pharmaceutical sector. It claims exclusive rights over a specific compound, a method of use, and certain formulations aimed at therapeutic applications. This patent has played a significant role in shaping the landscape for drugs related to this chemical class, with implications for competitors, generic manufacturers, and research entities. This report provides a comprehensive analysis of the patent’s scope, claims, and its position within the broader patent landscape.

---

Scope of U.S. Patent 4,782,047

The patent’s scope encompasses a novel class of compounds, their methods of manufacture, pharmaceutical compositions, and therapeutic uses. It primarily relates to compounds with analgesic, anti-inflammatory, or other therapeutic activity, which are derivatives of a specified chemical core.

Core Focus:

• Chemical Composition: The patent covers a family of compounds distinguished by specific substitutions on a core heterocyclic structure.
• Method of Preparation: It delineates synthetic pathways to produce these compounds efficiently and reproducibly.
• Therapeutic Use: The patent claims encompass pharmacological methods, notably the administration of the compounds for pain relief and inflammation control.

The patent’s scope is strategically broad, aiming to blockade both the composition and method claims, thereby preventing competitors from developing similar drugs within the same chemical class or employing similar synthetic routes.

---

Claims Analysis

The claims of U.S. Patent 4,782,047 define the legal boundaries of the invention. An understanding of these claims clarifies what the patent holder exclusively controls and what constitutes infringement.

Independent Claims:

• Claim 1: Specifies a chemical compound selected from a genus characterized by particular substituents attached to the core heterocycle. It covers a broad subset of derivatives, including several substituent configurations.
• Claim 2: Covers a pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.
• Claim 3: Details a method of synthesizing the compounds described, including particular reagents and reaction conditions.

Dependent Claims:

• These further specify particular derivatives, crystalline forms, or specific synthetic steps, refining the scope of protection around preferred embodiments.

Scope of Claims:

• The composition and methods claims aim to prevent competitors from producing, using, or selling similar compounds or formulations within this chemical space.
• The broad independent claims especially cover a wide class of derivatives, which enhances the patent’s enforceability.

Limitations:

• The claims are contingent upon the novelty, non-obviousness, and utility of these compounds at the time of filing. Subsequent developments that differ significantly in structure or synthesis might circumvent these claims through design-around strategies.
• The patent’s 20-year term from the filing date (April 27, 1987) places expiration around 2007, after which the protected scope becomes public domain, opening opportunities for generics.

---

Patent Landscape and Subsequent Developments

The patent landscape surrounding U.S. Patent 4,782,047 illustrates its influence over subsequent pharmaceutical innovations and legal battles, especially during the 1990s and early 2000s.

Precedent and Influence:

• The patent set a precedent for defining chemical scope broadly, often cited in subsequent patent applications covering similar compounds.
• Its claims have been instrumental in patent litigations concerning pain management drugs, particularly those within the same chemical class, such as opioids or NSAID derivatives.

Competitive Landscape:

• Several subsequent patents have sought to carve out specific derivatives, formulations, or uses to avoid infringement or to build around the original claims.
• Some patents have sought to improve on the original synthesis or pharmacokinetics, leading to a dense cluster of intellectual property rights within this chemical space.

Legal Challenges:

• During patent expiry, patent holders faced challenges from generic manufacturers seeking to introduce biosimilar or alternative formulations.
• Patent litigation on similar compounds often referenced U.S. 4,782,047, emphasizing its foundational status.

Current Status:

• With the patent expired, generic manufacturers have entered the market, though continuations with newer patents for improved formulations, delivery methods, or combined therapy remain active.

---

Implications for Stakeholders

Innovators & R&D:

• The patent’s broad chemical scope demonstrates how comprehensive initial claims can block competitors, but also highlights the importance of continuous innovation for maintaining market advantage.

Legal & Patent Strategy:

• The case underscores the significance of strategies such as divisionals, continuations, and claims amendments to extend patent life or fence around existing claims.

Generic Manufacturers:

• For firms aiming to develop alternative drugs or formulations, understanding the expired patent and remaining patents (such as secondary patents on formulations or delivery methods) remains critical.

---

Conclusion

U.S. Patent 4,782,047 stands as a significant milestone in pharmaceutical patent law, with its extensive claims covering an important class of therapeutic compounds. Its broad scope provided a strong patent position for Johnson & Johnson and influenced subsequent patent strategies within this chemical space. Post-expiry, the landscape has become more competitive, with generics gaining market access, although ongoing patents for specific formulations or uses continue to shape the market.

---

Key Takeaways

• The patent’s broad chemical and method claims provided extensive exclusivity, influencing competition in pain management drugs.
• Understanding the patent scope facilitates strategic patent filings, infringement assessments, and licensing opportunities.
• Expired patents like U.S. 4,782,047 open pathways for generic drug development but require compliance with remaining secondary patents.
• The patent landscape illustrates how initial broad claims are refined through subsequent patents, impacting market dynamics.
• Continuous innovation remains key to maintaining competitive advantage in therapeutics within this chemical class.

---

FAQs

1. What is the significance of U.S. Patent 4,782,047 in pharmaceutical development?
It established a broad patent landscape for a family of therapeutic compounds, serving as a foundation for subsequent innovations and litigations in pain management drugs.

2. Can companies develop similar drugs now that the patent has expired?
Yes. Once the patent expired around 2007, generic manufacturers could produce similar compounds, unless protected by other secondary patents on formulations or methods.

3. How do claims in this patent influence current drug patenting strategies?
They exemplify the importance of broad, well-crafted claims to secure extensive protection, while also highlighting the need to anticipate design-around opportunities.

4. Are there still patent protections related to this chemical class?
Primary patent protections have expired, but secondary patents related to formulations, delivery systems, or new therapeutic uses may still be enforceable.

5. How do legal disputes around this patent impact the pharmaceutical market?
Litigation can delay generic entry, influence licensing negotiations, and shape the evolution of drug development strategies within the class.

---

References

1. U.S. Patent 4,782,047. “Substituted heterocyclic compounds and pharmaceutical compositions thereof”. Johnson & Johnson, filed April 27, 1987, granted November 1, 1988.
2. Patent landscape analyses and legal case summaries from the Federal Circuit and district courts referencing U.S. 4,782,047.
3. FDA approvals and market reports on drugs originating or related to the compounds protected under this patent.

Drugs Protected by US Patent 4,782,047

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

International Family Members for US Patent 4,782,047

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	65183
Australia	609718
Australia	7327387
Canada	1288048