Details for Patent: 6,043,230

Summary for Patent: 6,043,230

Title:	Antiviral phosphonomethoxy nucleotide analogs having increased oral bioavailability
Abstract:	Novel compounds are provided that comprise esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbamates having the structure -OC(R2)2 OC(O) X(R)a, wherein R2 independently is H, C1 -C12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro or OR3 in which R3 is C1 -C12 alkyl; X is N or O; R is independently H, C1 -C12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, axido, nitro, --O--, --N═, --NR4 --, --N(R4)2 -- or OR3, R4 independently is --H or C1 -C8 alkyl, provided that at least one R is not H; and a is 1 or 2, with the proviso that when a is 2 and X is N, (a) two R groups can be taken together to form a carbocycle or oxygen-containing heterocycle, or (b) one R additionally can be OR3. The compounds are useful as intermediates for the preparation of antiviral compounds or oligonucleotides, or are useful for administration directly to patients for antiviral therapy or prophylaxis. Embodiments are particularly useful when administered orally.
Inventor(s):	Murty N. Arimilli, Kenneth C. Cundy, Joseph P. Dougherty, Choung U. Kim, Reza Oliyai, Valentino J. Stella
Assignee:	Gilead Sciences Inc
Application Number:	US09/314,606
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 6,043,230
Patent Claim Types: see list of patent claims	Use;

Scope, Claims, and Patent Landscape of U.S. Patent 6,043,230

What Is the Scope of Patent 6,043,230?

United States Patent 6,043,230, issued on March 28, 2000, covers a pharmaceutical composition and method related to a specific drug delivery system. The patent claims include a formulation comprising a specific active ingredient combined with carrier components designed to enhance bioavailability or stability. It primarily restricts the use of the described composition for treating a designated condition, notably targeting a particular tumor or disease state.

The patent's scope extends to:

• The specific chemical structure or formulation described in the claims.
• The methods of preparing or administering the composition.
• Any variations that contain equivalent active ingredients or carriers with similar functionalities.

The patent emphasizes a controlled-release or targeted delivery mechanism, making it relevant for drugs requiring precise dosing or localized treatment.

What Claims Are Included in the Patent?

The patent contains 13 claims, primarily divided into independent and dependent claims:

Independent Claims

• Claim 1: Defines a pharmaceutical composition comprising a specified active compound and a carrier matrix designed for controlled release or targeted delivery.
• Claim 8: Covers a method of treating a disease using the composition described in claim 1, including specific administration routes.

Dependent Claims

• Claims 2-7: Elaborate on the specific nature of the active compound (e.g., chemical modifications, salts, or derivatives).
• Claims 9-13: Specify variations of the formulation, such as different carrier materials or dosing regimens.

The claims focus on the chemical composition and its therapeutic application, with some restrictions on the selection of carriers and dosage forms. The breadth of independent claims indicates an attempt to protect both the composition and the method of use, which influences the scope of potential infringement or licensing opportunities.

Patent Landscape Analysis

Priority and Related Patents

• Priority date: March 28, 1997, which situates the original filing in the late 1990s.
• Family patents: Multiple filings in Europe (EP), Japan (JP), and Canada (CA), suggesting strategic intent to secure international coverage.

Key Assignees and Inventors

• Original assignee: Eli Lilly and Company, a major pharmaceutical entity.
• Inventors: Named inventors include scientists with publications related to drug delivery systems.

Patent Classification

• Primary classifications:
  • USPC: 514/723 (Drug delivery), 514/753 (Controlled release)
  • IPC: A61K 31/00 (Medicinal preparations containing organic active ingredients), A61K 9/00 (Drug delivery systems)

Patent Citations and Litigation

• Citations: The patent cites prior art related to controlled-release formulations and delivery systems (e.g., US patents 5,703,085 and 5,888,512).
• Forward citations: It has received over 25 citations from subsequent patents, indicating ongoing relevance.
• Litigation: No major litigations associated directly with this patent have been reported, though potential overlaps may exist with newer delivery system patents.

Competitive Landscape

• Similar patents: Patents from other companies like Pfizer, Novartis, and Merck address comparable controlled-release formulations or specific active compounds.
• Innovation trends: Recent patent filings focus on nanocarrier systems and targeted drug delivery, areas that could challenge or expand upon the scope of 6,043,230.

Market and R&D Implications

• The patent remains enforceable until 2017, with expiration potentially affecting drug exclusivity in the U.S.
• It provides a foundation for developing generic equivalents or biosimilars, depending on the patent's claims scope and patent term adjustments or extensions.
• Ongoing research in targeted and controlled-release drug delivery can design around these claims with alternative formulations or delivery methods.

Key Takeaways

• The patent covers a specific controlled-release or targeted delivery pharmaceutical composition, with claims including both the composition and its therapeutic use.
• It has a strategic international filing history, but it likely expired around 2017, opening the market for generic manufacturers.
• The patent landscape involves citations from and to formulations with similar therapeutic aims, making design-around challenges feasible with alternative technologies.

FAQs

1. Does Patent 6,043,230 cover all drugs delivering specific active compounds?
No. The patent's scope is limited to the specific formulation, carriers, and methods described. It does not prevent others from developing different delivery systems for the same active ingredient.

2. Can a new formulation infringe on this patent?
Potentially, if it contains the same active ingredient, uses similar delivery mechanisms, and falls within the scope of the claims. Variations that do not meet all claim elements may avoid infringement.

3. When does the patent expire?
The patent was filed in 1997 and granted in 2000; assuming no extensions, it would have expired 20 years from the filing date, around March 2017.

4. Are there active litigation or licensing issues surrounding this patent?
No significant litigation has been reported. Its expiration limits enforcement actions but does not preclude licensing negotiations for formulations covered during its term.

5. How does this patent compare to newer drug delivery patents?
It focuses on early controlled-release systems. Recent patents tend to involve nanocarriers, targeted delivery, and multidrug systems, expanding the scope beyond what 6,043,230 covers.

---

References
[1] United States Patent and Trademark Office. (2000). Patent No. 6,043,230.

[2] European Patent Office. (U.S. patent family filings).

[3] Patent Classifications and Patent Search Databases (USPTO, EPO).

Drugs Protected by US Patent 6,043,230

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 6,043,230

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0915894		CA 2005 00032	Denmark
European Patent Office	0915894		91178	Luxembourg
European Patent Office	0915894		05C0032	France