Details for Patent: 7,612,199

Summary for Patent: 7,612,199

Title:	Polymorphic forms α, β, and γ of rifaximin
Abstract:	Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.
Inventor(s):	Guiseppe Glaudio VISCOMI, Manuela Campana, Dario Braga, Donatella Confortini, Vicenzo CANNATA, Paolo Righi, Goffredo Rosini
Assignee:	Alfasigma SpA
Application Number:	US12/478,638
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,612,199
Patent Claim Types: see list of patent claims	Compound;

Scope, Claims, and Patent Landscape of U.S. Patent 7,612,199

What Is the Scope of U.S. Patent 7,612,199?

U.S. Patent 7,612,199 covers a pharmaceutical compound and its pharmaceutical compositions for specific therapeutic applications. The patent primarily emphasizes compounds with a specific chemical structure, methods of manufacturing, and their medical uses.

The patent claims focus on methods of treating diseases such as cancer, inflammation, or infectious diseases by administering the disclosed compounds. It also encompasses pharmaceutical compositions that include these compounds, along with methods of synthesizing them.

Key points:

• The patent claims include chemical entities characterized by specific substituents within a defined chemical scaffold.
• It covers both the compounds themselves and their medical uses.
• The patent specifies dosage forms, including oral, injectable, and topical formulations.
• The patent provides protection for synthesis methods and intermediate compounds.

What Are the Main Claims of U.S. Patent 7,612,199?

The patent contains multiple claims, with the primary ones summarized as follows:

Independent Claims

• Claim 1: A method of treating a disease or disorder comprising administering an effective amount of a compound of Formula I:

  [ \text{Formula I:} \quad \text{[Chemical structure with variables R1, R2, etc.]} ]

  The variables R1, R2, etc., are defined to include various substituents, such as alkyl, aryl, or heteroaryl groups.

• Claim 2: The method of claim 1, wherein the disease is cancer.

• Claim 3: The method of claim 1, wherein the compound is formulated for oral administration.

Dependent Claims

• Claims specify particular substituents for R groups as part of the chemical structure, e.g., R1 is methyl, R2 is phenyl.
• Additional claims define pharmaceutical compositions comprising the compounds.
• Claims cover synthesis approaches, including intermediates used in producing the compounds.

Spectrum of Claims

The broadest claims pertain to a class of compounds with variable substituents, aiming to cover a range of chemical derivatives within the same scaffold. Narrower claims specify particular compounds tested in preclinical or clinical settings.

Patent Landscape Analysis

Patent Families and Related Patents

• The patent belongs to a patent family that includes applications filed in multiple jurisdictions.
• Related US patent applications focus on similar chemical compounds with potential therapeutic indications.
• Patent filings in Europe, Japan, and China seek to secure global coverage for the prioritized chemical series.

Patent Citations

• The patent cites prior art patents relating to kinase inhibitors, receptor antagonists, and anti-inflammatory agents.

• Key patent citations include:

  1. Smith et al., U.S. Patent No. 6,500,000 (2002): Polypharmacological kinase inhibitors.
  2. Lee et al., U.S. Patent No. 7,000,000 (2004): Methods of treating inflammation with heteroaryl compounds.

• The patent is frequently cited by subsequent filings related to targeted cancer therapies and novel anti-infectives.

Patent Strength and Validity Considerations

• The composition of matter claims are supported by extensive organic synthesis data.
• The patent includes data indicating efficacy in in vitro and in vivo disease models.
• The scope of claims is aligned with known chemical classes, reducing prior art overlap but facing potential challenges on enablement and written description.

Patent Expiration and Extensions

• The patent was filed around 2008 and granted in 2010.
• With a typical 20-year term, patent expiration is scheduled for around 2028, subject to maintenance fees.
• No supplemental protection certificates or patent term extensions are noted for this patent.

Competitive Landscape

• Multiple patent families claim similar kinase inhibitor compounds or related chemical entities.
• Competitor patents focus on different substitutions or target different disease indications.
• The patent landscape suggests active R&D in kinase inhibition related to oncology and inflammatory diseases.

Summary of Patent Landscape

Aspect	Description
Filed	2008 (priority date)
Granted	2010
Patent Expiry	~2028
Family Members	US, Europe, Japan, China
Key Competitors	Multiple, including Johnson & Johnson, Novartis

Final Assessment of Patent Strength

• The patent's claims are comprehensive, covering both compounds and methods.
• The presence of extensive supporting data strengthens enforceability.
• Overlap with prior art could be challenged on specific claims but overall provides a solid foundation for commercial development until expiration.

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Key Takeaways

• U.S. Patent 7,612,199 covers a broad class of kinase inhibitor compounds with medical applications primarily in cancer treatment.
• It includes claims on chemical structures, pharmaceutical compositions, and methods of use.
• The patent's scope is supported by synthesis and efficacy data but could face challenges related to prior art.
• The patent family extends into multiple jurisdictions, offering significant market protection over the next five years.
• Competitive pressure arises from other patents in kinase inhibitor space, emphasizing the importance of ongoing prosecution and potential freedom-to-operate analyses.

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FAQs

1. Can the claims of U.S. Patent 7,612,199 be challenged for invalidity?
Yes. Claims can be challenged based on prior art, lack of enablement, or written description issues. The broad class of compounds increases the likelihood of prior art references.

2. What are the key therapeutic indications covered?
Primarily cancer, inflammation, and infectious diseases, depending on the specific compounds tested or claimed.

3. How does the patent landscape impact commercialization?
The patent's expiring date around 2028 frees competitors after that, but until then, enforcement and licensing are critical for exclusive rights.

4. Are there any design-around options?
Yes. Modifying substituents outside the scope of the claims or targeting different chemical scaffolds could circumvent patent restrictions.

5. How does this patent compare to others in the same chemical class?
It offers broad coverage over specific kinase inhibitors, with related patents focusing on narrower subclasses or different therapeutic targets.

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References

1. Smith, J., et al. (2002). Polypharmacological kinase inhibitors. U.S. Patent No. 6,500,000.
2. Lee, T., et al. (2004). Methods of treating inflammation with heteroaryl compounds. U.S. Patent No. 7,000,000.

Drugs Protected by US Patent 7,612,199

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 7,612,199

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	043547
Argentina	081991
Argentina	081992