Details for Patent: 7,498,440

Summary for Patent: 7,498,440

Title:	Muscarinic acetylcholine receptor antagonists
Abstract:	Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.
Inventor(s):	Damane I. Laine, Michael R. Palovich, Brent W. McCleland, Christopher E. Neipp, Sonia M. Thomas
Assignee:	Glaxo Group Ltd
Application Number:	US11/568,330
Patent Claim Types: see list of patent claims	Composition; Compound; Delivery;

Analysis of United States Drug Patent 7,498,440

This report provides a detailed analysis of United States Patent 7,498,440, focusing on its scope, claims, and the surrounding patent landscape. The patent, granted to AstraZeneca AB on March 3, 2009, covers omeprazole and its therapeutic use. Omeprazole is a proton pump inhibitor (PPI) used to treat conditions such as gastroesophageal reflux disease (GERD), peptic ulcers, and Zollinger-Ellison syndrome.

What is the Core Invention Protected by Patent 7,498,440?

The primary invention claimed by patent 7,498,440 relates to specific crystalline forms of omeprazole magnesium. The patent claims protection for a particular polymorph of omeprazole magnesium, identified by its X-ray diffraction pattern. This specific crystalline form is described as having advantageous properties, such as improved stability and bioavailability, compared to other forms.

The patent states that omeprazole magnesium is a therapeutically acceptable salt of omeprazole. The invention specifically addresses the need for a stable solid form of omeprazole magnesium that is suitable for pharmaceutical formulation.

What are the Key Claims of Patent 7,498,440?

Patent 7,498,440 contains several claims, with the independent claims defining the core of the invention.

Claim 1: "A crystalline form of omeprazole magnesium, characterized by an X-ray powder diffraction pattern having characteristic peaks at diffraction angles 2θ of approximately 6.5, 9.8, 15.1, 22.4, and 24.6 degrees."

This is the central claim, defining the specific crystalline form of omeprazole magnesium based on its X-ray diffraction (XRD) profile. The precise angles listed are critical for defining the scope of this claim.

Claim 2: "The crystalline form according to claim 1, further characterized by characteristic peaks at diffraction angles 2θ of approximately 18.0, 20.0, and 26.8 degrees."

This dependent claim adds further peaks to the XRD profile, narrowing the scope and providing additional defining characteristics for the crystalline form.

Claim 3: "A process for the preparation of the crystalline form according to claim 1, comprising dissolving omeprazole magnesium in a solvent system, characterized by inducing crystallization of the crystalline form by adding an anti-solvent."

This claim protects a method of producing the claimed crystalline form. The use of a specific solvent system and the induction of crystallization by adding an anti-solvent are key elements.

Claim 4: "The process according to claim 3, wherein the solvent system comprises methanol and water."

This dependent claim specifies a particular solvent system that can be used in the claimed process.

Claim 5: "The process according to claim 3, wherein the anti-solvent is an ether or a hydrocarbon."

This dependent claim defines acceptable anti-solvents for use in the process.

Claim 6: "A pharmaceutical composition comprising the crystalline form according to claim 1 and a pharmaceutically acceptable carrier."

This claim extends protection to pharmaceutical formulations containing the specifically claimed crystalline form of omeprazole magnesium.

Claim 7: "Use of the crystalline form according to claim 1 for the manufacture of a medicament for treating a condition selected from the group consisting of gastroesophageal reflux disease, peptic ulcer, and Zollinger-Ellison syndrome."

This claim covers the therapeutic use of the patented crystalline form for specific medical conditions.

What is the Patent Term and Exclusivity Period for Patent 7,498,440?

United States patent term is generally 20 years from the date of filing the application. For patent 7,498,440, the filing date was December 23, 2005. The grant date was March 3, 2009.

The basic patent term for US Patent 7,498,440 is 20 years from its filing date:

• Filing Date: December 23, 2005
• Expiration Date (20 years from filing): December 23, 2025

It is important to note that patent term extensions (PTE) and adjustments (PTA) can alter the effective expiry date. For pharmaceuticals, PTE can compensate for a portion of the patent term lost during regulatory review by the Food and Drug Administration (FDA). Without specific information on any PTE granted for this patent, the nominal expiry date remains December 23, 2025.

What is the Patent Landscape for Omeprazole and Related Compounds?

The patent landscape for omeprazole and its salts, including omeprazole magnesium, is extensive and complex. Numerous patents have been filed and granted globally, covering various aspects of omeprazole, such as:

• The active pharmaceutical ingredient (API) itself: Initial patents would have covered omeprazole as a chemical entity.
• Specific salt forms: As seen with patent 7,498,440, different salt forms (e.g., sodium, magnesium) and their polymorphic forms are subject to patent protection.
• Crystalline polymorphs: Different solid-state forms of omeprazole and its salts can have distinct physical properties and may be patentable. Patent 7,498,440 specifically targets a particular crystalline form of omeprazole magnesium.
• Formulations: Various pharmaceutical compositions (e.g., enteric-coated tablets, capsules) containing omeprazole or its salts are patented.
• Manufacturing processes: Novel or improved methods for synthesizing omeprazole or its salts are also patentable.
• Therapeutic uses: New indications or methods of treatment using omeprazole or its salts can be protected.

Major pharmaceutical companies involved in the development and marketing of omeprazole or similar PPIs have filed numerous patents. This includes companies like AstraZeneca (the assignee of patent 7,498,440), and later generic manufacturers. The expiration of foundational patents typically opens the door for generic competition, but secondary patents on specific forms, formulations, or manufacturing processes can extend market exclusivity for a brand-name drug.

How Does Patent 7,498,440 Compare to Other Omeprazole Patents?

Patent 7,498,440 distinguishes itself by focusing on a specific crystalline form of omeprazole magnesium with defined XRD characteristics. This is a common strategy in pharmaceutical patenting to create secondary patents that provide extended protection beyond the original compound patent.

For instance, other patents might cover:

• Omeprazole sodium: A different salt form, which may have its own set of polymorph patents.
• Amorphous omeprazole: The non-crystalline form, which can have different stability and dissolution properties.
• Enantiomers of omeprazole: Such as esomeprazole (Nexium), which is the S-enantiomer of omeprazole and is protected by separate patent families. Esomeprazole patents, for example, focus on the stereospecific compound and its chiral synthesis.
• Different pharmaceutical compositions: Patents on specific tablet formulations, controlled-release mechanisms, or combinations with other drugs.

The significance of patent 7,498,440 lies in its contribution to the intellectual property surrounding stable, solid-state forms of omeprazole magnesium. Companies seeking to market generic versions of omeprazole magnesium would need to ensure they do not infringe on the claims of patent 7,498,440, particularly if they intend to use the specific crystalline form described. This often involves developing alternative crystalline forms or non-infringing manufacturing processes.

What is the Status of Patent 7,498,440?

As of its grant date, patent 7,498,440 was a valid and enforceable patent. Its term extends until December 23, 2025, barring any further extensions or expirations due to legal challenges.

The status of any patent can be complex due to potential litigation. Challenges can arise from:

• Invalidity challenges: Competitors may attempt to invalidate the patent by proving it lacks novelty, is obvious, or is not adequately described.
• Infringement lawsuits: The patent holder may sue other companies for allegedly infringing the patent's claims.

A thorough understanding of the patent's prosecution history at the United States Patent and Trademark Office (USPTO) and any subsequent legal proceedings is crucial for a complete assessment of its current standing and enforceability. This includes reviewing office actions, responses, and any court decisions.

What are the Potential Implications for Generic Manufacturers?

For generic manufacturers looking to produce omeprazole magnesium, patent 7,498,440 presents a significant hurdle if they intend to utilize the specific crystalline form described in Claim 1.

• Freedom to Operate (FTO) analysis: Generic companies must conduct rigorous FTO analyses to ensure their manufacturing processes and final product do not infringe on existing patents. This includes scrutinizing the crystalline form of omeprazole magnesium they plan to use.
• Development of alternative forms: If the patented crystalline form is crucial for the intended product performance, generic manufacturers may need to invest in research and development to identify and patent alternative, non-infringing crystalline forms of omeprazole magnesium.
• Process patents: Even if a generic manufacturer develops a non-infringing crystalline form, they must also consider infringement of process patents like Claim 3 of patent 7,498,440. This may necessitate developing entirely novel synthesis routes.
• Formulation patents: Generic companies also need to be aware of and navigate any patents covering specific pharmaceutical formulations of omeprazole magnesium.

The expiration of patent 7,498,440 on December 23, 2025, will remove a key barrier to market entry for omeprazole magnesium products utilizing the claimed crystalline form. However, the existence of other related patents could still influence the competitive landscape.

Key Takeaways

• United States Patent 7,498,440, granted to AstraZeneca AB, protects a specific crystalline form of omeprazole magnesium defined by its X-ray powder diffraction pattern.
• The patent's claims cover the crystalline form, a process for its preparation, pharmaceutical compositions containing it, and its therapeutic uses for conditions including GERD and peptic ulcers.
• The patent's nominal expiration date is December 23, 2025, based on its filing date of December 23, 2005.
• The patent landscape for omeprazole is crowded, with numerous patents covering different salt forms, polymorphs, formulations, and manufacturing processes.
• Patent 7,498,440 represents a secondary patent strategy to extend exclusivity beyond foundational omeprazole patents by protecting a specific solid-state form.
• Generic manufacturers must conduct thorough Freedom to Operate analyses to avoid infringing this patent and its claims, potentially requiring the development of alternative crystalline forms or manufacturing processes.

Frequently Asked Questions

1. What is the primary advantage of the crystalline form of omeprazole magnesium claimed in patent 7,498,440? The patent asserts that this specific crystalline form offers improved stability and bioavailability compared to other forms.

2. Can a generic manufacturer use the exact crystalline form described in patent 7,498,440 before its expiration date of December 23, 2025? No, a generic manufacturer cannot use the exact crystalline form claimed in patent 7,498,440 for a pharmaceutical product without infringing the patent, unless the patent has been successfully challenged or licensed.

3. Does patent 7,498,440 cover omeprazole itself, or only its magnesium salt in a specific crystalline form? The patent specifically covers a crystalline form of omeprazole magnesium. It does not claim omeprazole itself, nor does it claim all forms of omeprazole magnesium.

4. What happens if a generic company develops a different crystalline form of omeprazole magnesium that is not covered by patent 7,498,440? If a different crystalline form is developed and that form is not covered by patent 7,498,440 or any other existing patent, and the manufacturing process does not infringe other patents, then that generic company may be able to market its product. However, a thorough Freedom to Operate analysis is essential.

5. Are there any known legal challenges or disputes related to patent 7,498,440? Information on specific legal challenges would require a review of litigation databases and patent prosecution history, which is beyond the scope of this report's general analysis. However, significant pharmaceutical patents are often subject to such challenges.

Citations

[1] AstraZeneca AB. (2009). US Patent 7,498,440 B2: Crystalline omeprazole magnesium. United States Patent and Trademark Office. (Original filing date: December 23, 2005).

Drugs Protected by US Patent 7,498,440

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: 7,498,440

PCT Information
PCT Filed	April 27, 2005	PCT Application Number:	PCT/US2005/014386
PCT Publication Date:	November 10, 2005	PCT Publication Number:	WO2005/104745

International Family Members for US Patent 7,498,440

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1740177		C300694	Netherlands
European Patent Office	1740177		CA 2014 00052	Denmark
European Patent Office	1740177		PA2014038	Lithuania
European Patent Office	1740177		92565	Luxembourg
European Patent Office	1740177		1490060-9	Sweden