Details for Patent: 6,414,148

Summary for Patent: 6,414,148

Title:	Quinazoline derivatives and pharmaceutical compositions containing them
Abstract:	The invention relates to quinazoline derivatives of formula (1) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected from alkyl and a 5 or 6 membered saturated carbocyclic or heterocyclic group, and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
Inventor(s):	Andrew Peter Thomas, Craig Johnstone, Edward Clayton, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin
Assignee:	Syngenta Ltd, Genzyme Corp
Application Number:	US09/269,595
Patent Claim Types: see list of patent claims	Compound; Process; Composition; Use;

Detailed Analysis of U.S. Patent 6,414,148: Scope, Claims, and Patent Landscape

Introduction

U.S. Patent 6,414,148, granted on July 2, 2002, is a significant patent within the pharmaceutical domain, specifically relating to the treatment of certain medical conditions with novel compounds. Its scope, claims, and position within the broader patent landscape influence innovation, licensing opportunities, and competitive strategies. This analysis offers an in-depth review of these aspects, furnishing insights for industry stakeholders and legal professionals.

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Patent Overview

The patent pertains to a class of pharmaceutical compounds designed to modulate specific biological pathways, potentially for therapeutic applications such as inflammatory conditions, neurological disorders, or metabolic diseases. It exemplifies a typical patent focused on novel chemical entities with defined methods of synthesis, formulation, and therapeutic use.

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Scope of the Patent

Coverage of Compounds and Uses

The patent encompasses a broad spectrum of chemical compounds characterized by a core structure with various substituents, devised to alter biological activity efficiently. It provides coverage for:

• Chemical compounds with specific structural motifs, often represented through Markush formulas in the specification, allowing for a wide array of structurally related derivatives.
• Pharmaceutical compositions containing these compounds, including dosage forms and formulation specifics.
• Therapeutic methods, especially methods of treating particular diseases or conditions following administration of the claimed compounds.

Limitations and Exclusions

The patent particularly excludes compounds or uses that fall outside the defined chemical frameworks or therapeutic indications. It may also specify certain stereoisomers, salts, hydrates, or derivatives explicitly to delineate its scope.

Temporal Scope

Given its filing date, the patent right extends generally for 20 years from the date of filing, which places its expiration around 2022, assuming no extensions or adjustments.

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Claims Analysis

Independent Claims

The core of the patent’s scope lies within its independent claims—usually broad, covering:

• Novel chemical entities: Claims directed to a genus of compounds, defined primarily by core structures and variable substituents. For example, a claim might recite:
  "A compound selected from the group consisting of compounds of Formula I, wherein R1, R2, R3 are defined in the claims."
• Key therapeutic uses: Claims that specify methods of treatment involving administering the compounds for particular diseases (e.g., inflammation or neurodegeneration).

Dependent Claims

Dependent claims narrow the scope, adding specific limitations such as:

• Particular substituents or stereochemistry.
• Specific salts or formulations.
• Optimized dosage regimens.
• Specific methods of synthesis or purification.

This layered claim structure provides a robust protection strategy—broad in scope via independent claims and defensible via narrower dependent claims.

Claim Scope & Potential Challenges

The breadth of chemical claims frequently invites challenges related to patentability, especially the issues of obviousness or novelty. Patent examiners and third parties may seek prior art references that disclose similar compounds or methods, aiming to invalidate or narrow the patent’s scope.

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Patent Landscape and Industry Context

Relative Positioning

Within the patent landscape, US Patent 6,414,148 sits among a milieu of patents targeting related compounds, often from:

• Big pharmaceutical players developing similar therapeutic classes.
• Biotech firms focusing on novel chemical modifications for improved efficacy.
• Academic institutions exploring foundational chemistry with potential for licensing.

The patent’s broad claims suggest it forms part of a strategic portfolio intended to secure market exclusivity during the early to mid-2000s, which later faced competition from subsequent patents or patent expirations.

Legal and Commercial Challenges

• Patent Lifespan: With its expiration around 2022, generic manufacturers could potentially launch parallel products, potentially eroding market share.
• Patent Term Extensions & Supplementary Protections: If applicable, extensions could have prolonged exclusivity, influencing competitive decisions.
• Infringement Risks: Competitors may develop structurally similar compounds outside the scope of this patent or rely on alternative pathways to treat the same indications, underscoring the importance of comprehensive patent strategies.

Related Patent Filings

The patent family likely includes filings in other jurisdictions (e.g., EP, JP, CN), expanding protection for the inventors and assignees globally. Cross-references to these counterparts can create an extensive patent landscape—guiding licensing, collaborations, or litigation.

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Strategic Implications

• Innovation Incentive: The broad chemical scope incentivizes proprietary drug development but also presents challenges related to patentability, especially if prior art is substantial.
• Competitive Edge: Original, well-drafted claims enable the patent holder to deter third-party entrants and establish licensing revenue streams.
• Freedom to Operate (FTO): Companies developing similar compounds must analyze whether their innovations infringe upon these claims or if carve-outs exist.

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Key Takeaways

• Comprehensive Claim Strategy: The patent's broad claims in chemical scope and therapeutic use provide versatile protection but invite challenges based on prior art and obviousness.
• Patent Expiration Impact: The nearing or reached expiration diminishes exclusivity, increasing market competition but also opening opportunities for generic entry.
• Landscape Context: The patent resides within a crowded innovation space with numerous related filings, necessitating ongoing landscape analyses for strategic positioning.
• Legal Vigilance and Potential Litigation: Enforcement and defense depend on precise claim interpretation and awareness of similar patents.

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FAQs

1. What is the primary chemical focus of U.S. Patent 6,414,148?
   It covers a class of structurally related compounds designed to modulate biological pathways for therapeutic purposes, often with a flexible core structure and variable substituents.

2. How broad are the claims in this patent?
   The independent claims are quite broad, covering entire classes of compounds with defined structural features, alongside claims to methods of treatment and pharmaceutical compositions.

3. Does the patent's expiration affect current commercialization efforts?
   Yes, with its expiration around 2022, generic manufacturers can now produce similar compounds, increasing market competition and potentially reducing patent-estimated exclusivity.

4. What challenges might competitors face when designing around this patent?
   They must avoid infringing the specific chemical structures or methods claimed, which can involve developing alternative compounds outside the patent’s coverage or utilizing different therapeutic pathways.

5. How does this patent relate to the broader patent landscape?
   It forms part of a larger portfolio of patents surrounding similar compounds and therapeutic targets; understanding this landscape is essential for freedom to operate and strategic patenting.

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References

1. [1] U.S. Patent No. 6,414,148.
2. [2] Industry reports on pharmaceutical patent strategies, 2000-2022.
3. [3] Patent landscape reports related to small molecule therapeutics, 2000-2023.
4. [4] FDA Orange Book and patent listing data.

Drugs Protected by US Patent 6,414,148

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: 6,414,148

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
	96402033	Sep 25, 1996
	97401042	May 09, 1997

PCT Information
PCT Filed	September 23, 1997	PCT Application Number:	PCT/GB97/02588
PCT Publication Date:	April 02, 1998	PCT Publication Number:	WO98/13354

International Family Members for US Patent 6,414,148

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	228114
Australia	4561397
Australia	729968
Brazil	9711302