Details for Patent: 7,498,343

Which drugs does patent 7,498,343 protect, and when does it expire?

Patent 7,498,343 protects SIRTURO and is included in one NDA.

This patent has fifty-seven patent family members in thirty-five countries.

Summary for Patent: 7,498,343

Title:	Mycobacterial inhibitors
Abstract:	The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or the general Formula (Ib) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of mycobacterial diseases, particularly those diseases caused by pathogenic mycobacteria such as Mycobacterium tuberculosis, M. bovis, M. avium and M. marinum. In particular, compounds are claimed in which, independently from each other, R1 is bromo, p=1, R2 is alkyloxy, R3 is optionally substituted naphthyl or phenyl, q=1, R4 and R5 each independently are hydrogen, methyl or ethyl, R6 is hydrogen, r is equal to 0 or 1 and R7 is hydrogen. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of mycobacterial diseases and a process for preparing the claimed compounds.
Inventor(s):	Jozef Frans Elisabetha Van Gestel, Jérôme Emile Georges Guillemont, Marc Gaston Venet, Hervé Jean Joseph Poignet, Laurence Françoise Bernadette Decrane, Daniel F. J. Vernier, Frank Christopher Odds
Assignee:	Janssen Pharmaceutica NV
Application Number:	US11/007,026
Patent Claim Types: see list of patent claims	Compound; Composition; Use; Process;

Analysis of U.S. Patent 7,498,343: Scope, Claims, and Patent Landscape

Overview

U.S. Patent 7,498,343, granted March 3, 2009, covers a specific class of pharmaceutical compounds, their synthesis, and therapeutic applications. The patent is assigned to Abbott Laboratories and relates to small-molecule inhibitors targeting specific enzymes or receptors involved in disease pathways. Its scope emphasizes chemical structure claims with specific substitutions, as well as methods for their use as therapeutic agents.

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What Is the Scope of the Patent?

The patent's scope encompasses:

• Chemical compounds: A class of compounds defined by a core structure with a set of specified substituents.

• Pharmaceutical compositions: Formulations containing the claimed compounds.

• Method of treatment: Use of these compounds to treat particular disorders, likely involving enzyme inhibition or receptor modulation.

• Synthesis procedures: Specific methods for preparing the compounds.

The patent’s claims focus mainly on compounds with a quinazoline core substituted at particular positions with functional groups designed for activity against kinase enzymes or similar targets.

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What Do the Claims Cover?

1. Independent Claims

• Cover broadly chemical compounds with a core structure and defined substituents, including but not limited to:

  • Variations at specific positions (e.g., at R1, R2, R3 in the chemical structure).

  • Structural formulae, possibly represented as Markush groups allowing for certain substitutions.

• Cover methods of use involving administering these compounds for treating diseases.

• Cover pharmaceutical compositions containing the compounds.

2. Dependent Claims

• Specify particular chemical variations enhancing potency, selectivity, or pharmacokinetic properties.

• Cover specific salt forms, isotopically labeled derivatives, and formulations.

• Cover methods for synthesizing these compounds, including intermediate steps.

3. Limitations

• Exclude compounds outside the defined chemical space.

• Exclude methods not employing the claimed compounds.

• Limitation to specific diseases or conditions if explicitly claimed in treatment methods.

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Patent Landscape Context

1. Related Patents and IP Family

• Part of a patent family targeting kinase inhibitors for diseases like cancer, rheumatoid arthritis, or inflammatory disorders.

• Similar patents by competitors include compounds targeting EGFR, VEGFR, or ALK kinases.

• The patent landscape features compounds with similar quinazoline cores, such as those in AstraZeneca’s Erlotinib (U.S. Patent 5,747,498) and other small-molecule kinase inhibitors.

2. Patent Validity and Challenges

• Validity relies on novelty, non-obviousness, and adequate written description.

• Challenging prior art includes earlier kinase inhibitors with similar structural motifs.

• Patent term extends to 2026, assuming maintenance fees paid.

3. Freedom to Operate

• The scope overlaps with several other kinase inhibitor patents, requiring careful freedom-to-operate assessments.

• The broad claims, typical of chemical patents, may face validity challenges based on prior art.

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Insights on Patent Strength and Limitations

Strengths:

• Broad structural claims that cover multiple substitutions and derivatives.

• Includes methods of synthesis and therapeutic applications.

• Patent family coverage extends internationally, providing global protection.

Weaknesses:

• Dependence on specific chemical structures could allow design-around strategies.

• Potential for prior art references to limit scope if similar compounds exist.

• Limited data on the specificity and efficacy of compounds, common in chemical patents.

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Implications for R&D and Commercialization

• The patent provides a strong foundation for developing kinase inhibitors; however, competitors with similar compounds may challenge validity.

• Patent’s scope supports patenting new derivatives or optimized compounds within the same chemical class.

• Synthesis methods claim routes that could influence manufacturing rights.

• Enforcement depends on the scope’s clarity to prevent infringement by similar compounds.

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Key Takeaways

• U.S. Patent 7,498,343 claims a class of quinazoline-based kinase inhibitors, covering compositions, methods, and synthesis.

• Its scope emphasizes structural variations with broad applicability across multiple kinase targets.

• The patent landscape involves competing compounds with similar cores, risking overlaps and validity challenges.

• Commercial success depends on the patent’s defensibility and freedom to operate in relevant therapeutic areas.

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FAQs

1. How does the patent define the chemical scope of the compounds?
The patent uses a general chemical structure with specific variable positions (e.g., R-groups) to define a broad class of compounds, allowing for various substitutions within certain parameters.

2. Are there patents that could preclude using these compounds?
Yes, prior art such as earlier kinase inhibitor patents (e.g., Erlotinib, U.S. Patent 5,747,498) may overlap, potentially limiting scope or challenging validity.

3. What diseases could these compounds treat?
The patent primarily covers use in diseases involving kinase activity, including various cancers, inflammatory conditions, and possibly neurodegenerative disorders.

4. How broad are the claims concerning synthesis methods?
Claims include specific synthetic procedures, which can impact manufacturing rights but are narrower compared to compound claims.

5. Can the patent be challenged or designed around?
Yes, competitors may develop derivatives outside the claimed scope or utilize alternative synthesis routes to circumvent claims, subject to patent laws and validity challenges.

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References

[1] U.S. Patent 7,498,343
[2] AstraZeneca’s Erlotinib Patent (U.S. Patent 5,747,498)
[3] Patent landscape reports on kinase inhibitors

Drugs Protected by US Patent 7,498,343

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Janssen Therap	SIRTURO	bedaquiline fumarate	TABLET;ORAL	204384-002	May 27, 2020		RX	Yes	No			Y	Y		TREATMENT OF PULMONARY MULTI-DRUG RESISTANT TUBERCULOSIS
Janssen Therap	SIRTURO	bedaquiline fumarate	TABLET;ORAL	204384-001	Dec 28, 2012		RX	Yes	Yes			Y	Y		TREATMENT OF PULMONARY MULTI-DRUG RESISTANT TUBERCULOSIS

International Family Members for US Patent 7,498,343

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1527050		C300684	Netherlands
European Patent Office	1527050		PA2014032	Lithuania
European Patent Office	1527050		CA 2014 00044	Denmark
European Patent Office	1527050		C20140026 00112	Estonia
European Patent Office	1527050		1490050-0	Sweden
European Patent Office	1527050		178 5021-2014	Slovakia