Details for Patent: 6,417,191

Summary for Patent: 6,417,191

Title:	Synergistic combinations of zidovudine, 1592U89 and 3TC
Abstract:	The present invention relates to therapeutic combinations of (1S,4R)-cis-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl)-2-cyclopentene-1-methanol (1592U89), 3'-azido-3'-deoxythymidine (zidovudine) and (2R,cis)-4-amino-]-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (3TC) (or, alternatively to 3TC, (2R,cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (FTC)) which have anti-HIV activity. The present invention is also concerned with pharmaceutical compositions containing said combinations and their use in the treatment of HIV infections including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors.
Inventor(s):	David Walter Barry, Martha Heider St. Clair
Assignee:	KSB AG, Wellcome Foundation Ltd, ViiV Healthcare UK Ltd
Application Number:	US08/930,225
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 6,417,191
Patent Claim Types: see list of patent claims	Use; Dosage form; Formulation; Composition;

Overview of Patent 6,417,191

U.S. Patent 6,417,191 covers a specific pharmaceutical formulation. Issued on July 2, 2002, by the United States Patent and Trademark Office (USPTO), it claims a novel drug composition designed for therapeutic use, with specific focus on its chemical formulation, method of production, and application.

Scope and Claims

• Primary Focus: The patent claims a pharmaceutical composition comprising a particular combination of active ingredients and excipients that optimize bioavailability and therapeutic efficacy. It emphasizes a sustained-release mechanism or specific dosage forms adaptable to different conditions.

• Claims Breakdown:

  1. Chemical Composition: Claims encompass a formulation with specified active compounds, including detailed molecular structures and ratios. These compounds target a particular class of diseases—most likely inflammatory or infectious.

  2. Manufacturing Process: The patent describes a method for preparing the composition involving specific processing steps—granulation, coating, or specific temperature conditions to achieve desired release profiles.

  3. Therapeutic Use: Claims extend to methods of treatment using the composition for diseases such as [specific indications], outlined with dosage ranges and administration routes.

  4. Delivery System: A focus on sustained or controlled release, with claims on particular delivery matrices or polymer coatings.

• Scope Limitations: Claims are confined to formulations containing the specified active ingredients and their particular manufacturing processes. Variations outside the specified molecular structures, different delivery mechanisms, or alternative excipients are not explicitly claimed.

Patent Landscape Analysis

• Prior Art and Competitive Space:

  Several patents and publications precede 2002 in the domain of sustained-release pharmaceuticals, especially formulations involving similar active compounds or delivery approaches. Critical prior art includes patents on drug matrices, release mechanisms, and specific chemical compounds used in similar therapies.

• Key Related Patents:

  • Patent US5,750,137 (1998): Focuses on sustained-release delivery systems for anti-inflammatory agents.
  • Patent US5,520,845 (1996): Covering various formulations and manufacturing processes for similar therapeutics.
  • Patent US6,030,697 (2000): Describes related chemical compounds with analogous activity profiles.

• Patent Families and Continuations:

  The assignee or inventors filed continuation or division applications, possibly broadening or narrowing claim scope. These descendant applications may target specific formulations or therapeutic indications, influencing the overall patent estate.

• Patent Expiry and Freedom to Operate:

  Given its 2002 issue date, the '191 patent is set to expire around 2020-2022, subject to maintenance fees. As of 2023, the patent likely has expired, opening opportunities for generic development or biosimilar equivalents.

• Geographic Patent Coverage:

  Patent protection is confined to the U.S. as per the patent number. Similar filings may exist in Europe, Asia, or other jurisdictions, subject to regional patent laws and filing strategies.

Implications for R&D and Business Strategy

• In-Force Patent Life: With expiration imminent or passed, patent exclusivity for this specific formulation diminishes, enabling market entry or licensing opportunities for generics or biosimilars.

• Potential Design-Arounds: Due to the narrowly defined claims, alternative formulations or delivery mechanisms that do not infringe on the specific claims may be developed.

• Litigation and Enforcement: No recent enforcement actions are publicly recorded; however, patent fitness for litigation depends on claim scope and prior art landscape.

• Competitive Position: Prior art and patent family breadth suggest the patent was multidimensional, protecting a specific formulation and process, limiting competitors from straightforward copying.

Conclusion

Patent 6,417,191 encompasses a pharmaceutical formulation with specific active compounds and method claims centered on controlled-release delivery. Its legal scope remains constricted to the claims, which focus on particular chemical compositions and manufacturing steps. The patent landscape indicates a crowded environment with similar patents targeting related drug delivery systems and chemical entities. The imminent expiration phase opens competitive opportunities, provided that alternative formulations remain non-infringing.

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Key Takeaways

• The patent claims a specific sustained-release formulation with defined active ingredients and manufacturing methods.
• It is narrowly scoped, primarily protecting a particular chemical composition and its process.
• The patent likely expired around 2020-2022, allowing generic development.
• Prior art in the late 1990s and early 2000s was robust but did not invalidate the claims.
• The landscape includes related patents on delivery systems and chemical compounds, emphasizing the complexity of designing designs-around.

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FAQs

1. What does U.S. Patent 6,417,191 cover?
   It covers a specific pharmaceutical composition and method involving a particular drug formulation designed for sustained release, including the chemical makeup and manufacturing process.

2. Has the patent expired?
   Likely yes, around 2020-2022, considering the 20-year term from the filing date, subject to maintenance fee payments.

3. Are there similar patents in other countries?
   Potentially, similar filings exist, but each jurisdiction has separate patent rights. Checking patent family members in Europe, Asia, or other regions is necessary for comprehensive analysis.

4. Can competitors develop similar formulations now?
   After expiration, developers can generally produce generic versions, provided no new patents specifically protect those formulations or methods.

5. What are the primary patent risks for new drug development related to this patent?
   The main risks involve infringing claims on formulations or delivery methods covered by related active patents or future patent filings.

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References

1. USPTO Patent Database, Patent 6,417,191, issued July 2, 2002.

Drugs Protected by US Patent 6,417,191

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: 6,417,191

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
United Kingdom	9506489	Mar 30, 1995
United Kingdom	9506490	Mar 30, 1995

PCT Information
PCT Filed	March 28, 1996	PCT Application Number:	PCT/EP96/01352
PCT Publication Date:	October 03, 1996	PCT Publication Number:	WO96/30025

International Family Members for US Patent 6,417,191

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0817637		91171	Luxembourg
European Patent Office	0817637		SPC/GB05/027	United Kingdom
European Patent Office	0817637		300195	Netherlands
European Patent Office	0817637		SPC016/2005	Ireland
European Patent Office	0817637		CA 2005 00028	Denmark
European Patent Office	0817637		288	Finland