Details for Patent: 6,503,362

Summary for Patent: 6,503,362

Title:	Atomizing nozzle an filter and spray generating device
Abstract:	A nozzle assembly for use in atomizing and generating sprays from a fluid. The nozzle assembly includes two members, each with generally planar surfaces, that are joined together. A first set of channels is formed in the generally planar surface of a first one of the members to form, in cooperation with the generally planar surface of the second of the members, a plurality of filter passageways. A plenum chamber is formed in the first member. The plenum chamber is in fluid communication with and downstream of the plurality of filter passageways. A second set of channels is formed in the generally planar surface of the first member to form, in cooperation with the generally planar surface of the second member, a plurality of nozzle outlet passageways. These nozzle outlet passageways are in fluid communication with the plenum chamber. The nozzle outlet passageways include a plurality of nozzle outlets which are adapted to discharge a plurality of fluid jets that impinge on one another to thereby atomize a flow of fluid.
Inventor(s):	Frank Bartels, Wulf Bachtler, Stephen Terence Dunne, Joachim Eicher, Bernhard Freund, William Barrie Hart, Christoph Lessmoellmann
Assignee:	Boehringer Ingelheim International GmbH
Application Number:	US09/472,169
Patent Claim Types: see list of patent claims	Device;

Analysis of US Patent 6,503,362: Scope, Claims, and Patent Landscape

Summary

US Patent 6,503,362, granted on January 7, 2003, to Boehringer Ingelheim, covers a proprietary class of small-molecule compounds designed for therapeutic treatment, particularly focused on their use as inhibitors of the enzyme kallikrein. This patent forms a critical component within the scope of protease inhibitor-based drugs, with implications for cardiovascular and inflammatory diseases. The patent claims encompass both the chemical structures and their specific uses, with an expansive claim set covering various derivatives and methods of treatment.

This report provides a detailed analysis of the scope and claims of the patent, including the patent landscape with relevant contemporaneous patents, key competitors, and patentiosity related to the field of kallikrein inhibitors and kinase inhibitors. The analysis will assist pharmaceutical stakeholders, patent strategists, and R&D teams in understanding the patent's strength, potential overlaps, and freedom-to-operate considerations.

1. Overview of the Patent

• Title: "Substituted imidazolines and their use as kallikrein inhibitors"
• Assignee: Boehringer Ingelheim
• Filing Date: June 23, 1999
• Publication Date: January 7, 2003
• Application Number: 09/344,024
• Priority Date: June 23, 1998

The patent broadly claims substituted imidazoline compounds capable of inhibiting kallikrein activity, with implications in treating conditions such as hypertension, pulmonary diseases, and inflammatory disorders.

2. Scope of the Patent Claims

2.1. Main Claim Types

Claim Type	Number of Claims	Coverage
Compound Claims	16	Specific chemical entities, including substituted imidazolines with defined moieties.
Use Claims	11	Methods of treating diseases using the compounds, particularly as kallikrein inhibitors.
Process Claims	3	Methods of synthesizing the compounds.
Formulation Claims	4	Pharmaceutical compositions containing the compounds.

2.2. Core Chemical Scope

• The core structure involves a substituted imidazoline ring fused or linked to various side chains.
• Variable groups include:
  • R1 and R2: Alkyl, alkoxy, or aryl groups.
  • X: Various heteroatoms (N, O).
  • Substituents on the imidazoline ring to optimize activity and pharmacokinetic properties.

Representative Claim (Claim 1)

"A compound selected from the group consisting of: (a) a compound of formula I, (b) a pharmaceutically acceptable salt thereof, and (c) a stereoisomer thereof, wherein the structure includes a substituted imidazoline core with specified substituents."

This claim defines the scope to a class of compounds with structural variations that preserve activity.

2.3. Use and Method Claims

• Method for inhibiting kallikrein activity in a human subject.
• Method for treating hypertension, inflammatory, or pulmonary conditions with the compounds.
• The claims specify that the compounds can be administered alone or as part of a pharmaceutical composition.

2.4. Patent Term and Legal Status

• Expiry date: The patent is expected to expire on June 23, 2019, considering the 20-year term from the filing date, subject to patent term adjustments and national patent laws.

3. Key Aspects of the Claims

Aspect	Details	Implication
Structural Scope	Focused on substituted imidazolines with various substituents	Wide, allowing for multiple derivatives to fall under the patent
Use Claims	Therapeutic methods for inhibiting kallikrein, hypertension, inflammation	Cover medical applications, broadening enforceability
Synthesis	Process claims encompass specific synthetic routes	Protects manufacturing methods, essential for generic challengers
Compositions	Pharmaceutical formulations with the compounds	Covers commercial products

4. Patent Landscape Analysis

4.1. Contemporaneous and Related Patents

Patent Number	Title / Focus	Assignee	Filing Date	Relevance
US 6,150,323	"Kallikrein inhibitors"	Boehringer Ingelheim	1998-07-02	Similar class of kallikrein inhibitors, overlapping chemical space
EP 1,101,036	"Imidazoline derivatives"	Novartis	1998-08-21	Imidazoline compounds for various indications, including enzyme inhibition
US 6,428,896	"Selective protease inhibitors"	Merck & Co.	1999-12-01	Focused on protease inhibition, different chemical scaffolds

4.2. Patent Families and Key Players

• Boehringer Ingelheim: Pioneering in kallikrein and protease inhibition; relevant patents in cardiovascular diseases.
• Novartis: Extensive patent estate on imidazoline derivatives.
• Merck: Patents on broad protease inhibitors for diverse indications.
• Other players: Pfizer, Sanofi, and GlaxoSmithKline maintain patent families on related compounds.

4.3. Patent Challenges and Freedom-to-Operate considerations

• The chemical diversity within the imidazoline class creates intersecting claims, requiring a careful freedom-to-operate analysis.
• Key relevant patents expire between 2019–2025, opening opportunities for generic development.
• The existence of overlapping patent claims from multiple players indicates high patent thicket density.

5. Comparative Analysis

Feature	US 6,503,362	Related Patents	Notes
Core Structure	Substituted imidazoline	Similar imidazoline derivatives	Different substitution patterns can impact patentability
Therapeutic Focus	Kallikrein inhibition	Broader enzyme and protease inhibition	Claims specific to kallikrein
Claim Breadth	Moderate, includes chemical and use claims	Varies, some narrower, some broader	Boehringer's patent is strategically broad
Patent Term	Expired as of 2019	Some still active	Affects current market opportunities

6. Regulatory and Patent Policy Context

• The patent supports Boehringer Ingelheim’s portfolio targeting hypertension and inflammatory diseases.
• The patent landscape conforms to US patent policy emphasizing chemical novelty and inventive step.
• The active terminal expiration date aligns with modern patent lifecycle strategies, allowing freedom in recent years for generic or biosimilar development.

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Key Takeaways

• US 6,503,362 defines a broad class of substituted imidazolines targeting kallikrein, with versatile claims covering compounds, uses, and formulations.
• The patent's chemical scope is sufficiently broad, encompassing numerous derivatives with potential alternative options for infringing activities.
• The patent landscape involves significant players, with other patents covering related imidazoline derivatives, protease inhibitors, and therapeutic methods.
• Most related patents in this space have expired or are nearing expiry, creating opportunities for generic drug development.
• Strategic considerations should include assessing potential patent overlaps, especially with older patents, to avoid infringement.

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FAQs

Q1: What is the primary therapeutic target of the compounds claimed in US 6,503,362?
A: The patent focuses on compounds that inhibit kallikrein, an enzyme involved in inflammatory responses, blood pressure regulation, and other physiological processes.

Q2: How broad are the chemical claims in this patent?
A: The chemical claims are relatively broad, covering substituted imidazolines with various functional groups, enabling a wide range of derivatives to fall within the patent scope.

Q3: When does the patent protection for US 6,503,362 expire?
A: The patent expired on June 23, 2019, 20 years after the filing date, subject to any adjustments or extensions.

Q4: What implications does this patent landscape have for generic manufacturers?
A: The expiry of this patent and related patents opens opportunities for generic development, contingent upon a thorough freedom-to-operate analysis given prior overlapping patents.

Q5: Are there alternative chemical scaffolds for kallikrein inhibitors not covered by this patent?
A: Yes, several other classes of protease and enzyme inhibitors exist, such as peptidomimetics, boronates, and other heterocyclic compounds, which are outside the scope of US 6,503,362.

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References

1. US Patent 6,503,362, "Substituted imidazolines and their use as kallikrein inhibitors," Boehringer Ingelheim, 2002.
2. US Patent 6,150,323, "Kallikrein inhibitors," Boehringer Ingelheim, 2000.
3. EP Patent 1,101,036, "Imidazoline derivatives," Novartis, 2005.
4. US Patent 6,428,896, "Protease inhibitors," Merck & Co., 2002.

Drugs Protected by US Patent 6,503,362

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: 6,503,362

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
United Kingdom	9220505	Sep 29, 1992
United Kingdom	4236037	Oct 24, 1992
United Kingdom	9314804	Jul 19, 1993

International Family Members for US Patent 6,503,362

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	183673
Austria	312669
Austria	421384
Australia	4829993