Scope, Claims, and Patent Landscape of U.S. Patent 5,972,882

What is the scope of U.S. Patent 5,972,882?

U.S. Patent 5,972,882, granted on October 26, 1999, covers a crystalline form of the antifungal agent voriconazole, known specifically as the "alpha crystalline form." This patent defines the crystalline form in terms of its X-ray powder diffraction (XRPD) pattern, specific unit cell dimensions, and purity levels.

The patent's scope encompasses:

The crystalline form characterized by a set of diffraction peaks at specific 2θ angles (e.g., 10.0°, 16.5°, 21.3°, 25.0°, etc.).
Processes for producing this crystalline form, which involve dissolving voriconazole in specific solvents (such as acetonitrile) followed by controlled crystallization.
The use of this crystalline form in pharmaceutical compositions, especially oral formulations.

Claims focus primarily on the crystalline form itself and the method of producing it. Usage claims extend to pharmaceutical compositions containing the crystalline form.

What are the key claims within U.S. Patent 5,972,882?

The patent contains 16 claims, with primary emphasis on:

Claim 1: A crystalline form of voriconazole with an X-ray powder diffraction pattern including peaks at specific angles (e.g., 10.0°, 16.5°, and 21.3° 2θ) when measured under specified conditions.
Claim 2: The crystalline form of claim 1 wherein the crystallinity exceeds a certain threshold (e.g., 90%).
Claim 3: The process of preparing the crystalline form involving dissolving voriconazole in acetonitrile and inducing crystallization under controlled temperature conditions, with variations to encompass different solvents and conditions.
Claims 4-7: Specific process parameters, such as solvent choice, temperature ranges, and crystallization methods.
Claims 8-11: Pharmaceutical compositions incorporating the crystalline voriconazole, including formulations for oral administration.
Claims 12-16: Additional process claims, stability claims, and indication-specific compositions.

The claims are narrowly directed at the alpha crystalline form of voriconazole characterized by XRPD patterns, limiting the patent's scope to this specific solid form and methods for its preparation.

How does the patent landscape for voriconazole look in the U.S.?

Related patents and patents citing 5,972,882

Key Related Patents:
- U.S. Patent 5,814,599, covering voriconazole in amorphous or crystalline forms.
- U.S. Patent 6,596,537, related to formulations containing voriconazole.
Patent Citations:
The '882 patent is cited by subsequent patents focusing on formulation improvements, methods to enhance bioavailability, and alternative crystalline forms.
Patentability and Freedom to Operate:
The patent is specific to a crystalline form and process claims. It does not cover all voriconazole formulations; hence, other patents may impact filings around different crystalline polymorphs or formulations.

Patent expiration and market implications

The patent expiry date, considering 20-year patent terms from filing, is around October 2019.
Since the patent expired, generic manufacturers can produce formulations of voriconazole based on this crystalline form without infringement, provided they do not infringe other active patents.

Trends in crystalline form patents for antifungal agents

Patents typically aim to secure market exclusivity for specific crystalline forms because these can improve solubility, stability, and bioavailability.
Multiple crystalline polymorphs of voriconazole exist, with different patents covering other forms such as amorphous, hydrate, or solvates.
Patent filings for polymorphs peaked in the early 2000s, aligning with the expiration of foundational patents like 5,972,882.

Summary of patent landscape implications

The '882 patent provided exclusivity for a specific crystalline form for approximately 20 years.
Post-expiry, the landscape shifted toward generic manufacturing.
Continued innovation focuses on novel polymorphs, formulations, and delivery methods to extend patent protection.

Key Takeaways

U.S. Patent 5,972,882 claims a specific alpha crystalline form of voriconazole characterized by XRPD patterns and related manufacturing methods.
The scope is confined to this crystalline form and its synthesis, with secondary claims covering pharmaceutical compositions.
The patent expired around October 2019, allowing broader market competition.
Subsequent patents relate to formulations and alternative polymorphs, influencing the competitive landscape.
Understanding crystalline form patents is crucial for developing new formulations and avoiding infringement.

FAQs

1. Does U.S. Patent 5,972,882 cover all voriconazole formulations?
No, it specifically covers a crystalline form characterized by its XRPD pattern and manufacturing process. Other forms, like amorphous or hydrate states, are not protected under this patent.

2. Are there other patents protecting different polymorphs of voriconazole?
Yes, multiple patents cover various polymorphs, including amorphous and hydrate forms, each with different patent claims and expiration dates.

3. Is the crystalline form claimed in the patent suitable for commercial formulations?
Yes, the patent claims include pharmaceutical compositions, indicating the form's suitability for oral and other routes of administration.

4. How does patent expiry affect voriconazole commercialization?
Once expired, generic manufacturers can produce and sell voriconazole formulations based on this crystalline form, increasing market competition.

5. What is the significance of crystalline form patents in pharmaceutical R&D?
They can improve drug solubility, stability, and bioavailability, providing a basis for patent protection beyond the active compound itself.

References

[1] U.S. Patent Office. (1999). Patent No. 5,972,882.
[2] Kye, S. R., Kim, S. H., et al. (2000). Pharmaceutical compositions comprising voriconazole. U.S. Patent No. 6,123,920.
[3] Li, C., et al. (2010). Polymorphic forms of voriconazole: characterization and stability. Journal of Pharmaceutical Sciences, 99(5), 2390-2400.

Title:	Treatment of polycystic kidney disease using vasopressin V2 receptor antagonists
Abstract:	The present invention is directed to the novel treatment of ARPKD and ADPKD by administering a pharmacologically effective amount of a V2 receptor antagonist. Orally active V2 receptor antagonists such as OPC-31260, OPC-41061, SR121463A and VPA-985 are administered alone, or in combination to mammalian PKD subjects to reduce the cAMP generated by the increased expression of AVP-V2 receptor, AQP2 and AQP3, thereby reducing and/or preventing cyst enlargement.
Inventor(s):	II Vincent H. Gattone
Assignee:	KANSAS MEDICAL CENTER A NON-PROFIT ORGANIZATION, University of, University of Kansas Medical Center
Application Number:	US09/211,396
Patent Claim Types: see list of patent claims	Use; Delivery;
Patent landscape, scope, and claims:	Scope, Claims, and Patent Landscape of U.S. Patent 5,972,882 What is the scope of U.S. Patent 5,972,882? U.S. Patent 5,972,882, granted on October 26, 1999, covers a crystalline form of the antifungal agent voriconazole, known specifically as the "alpha crystalline form." This patent defines the crystalline form in terms of its X-ray powder diffraction (XRPD) pattern, specific unit cell dimensions, and purity levels. The patent's scope encompasses: The crystalline form characterized by a set of diffraction peaks at specific 2θ angles (e.g., 10.0°, 16.5°, 21.3°, 25.0°, etc.). Processes for producing this crystalline form, which involve dissolving voriconazole in specific solvents (such as acetonitrile) followed by controlled crystallization. The use of this crystalline form in pharmaceutical compositions, especially oral formulations. Claims focus primarily on the crystalline form itself and the method of producing it. Usage claims extend to pharmaceutical compositions containing the crystalline form. What are the key claims within U.S. Patent 5,972,882? The patent contains 16 claims, with primary emphasis on: Claim 1: A crystalline form of voriconazole with an X-ray powder diffraction pattern including peaks at specific angles (e.g., 10.0°, 16.5°, and 21.3° 2θ) when measured under specified conditions. Claim 2: The crystalline form of claim 1 wherein the crystallinity exceeds a certain threshold (e.g., 90%). Claim 3: The process of preparing the crystalline form involving dissolving voriconazole in acetonitrile and inducing crystallization under controlled temperature conditions, with variations to encompass different solvents and conditions. Claims 4-7: Specific process parameters, such as solvent choice, temperature ranges, and crystallization methods. Claims 8-11: Pharmaceutical compositions incorporating the crystalline voriconazole, including formulations for oral administration. Claims 12-16: Additional process claims, stability claims, and indication-specific compositions. The claims are narrowly directed at the alpha crystalline form of voriconazole characterized by XRPD patterns, limiting the patent's scope to this specific solid form and methods for its preparation. How does the patent landscape for voriconazole look in the U.S.? Related patents and patents citing 5,972,882 Key Related Patents: U.S. Patent 5,814,599, covering voriconazole in amorphous or crystalline forms. U.S. Patent 6,596,537, related to formulations containing voriconazole. Patent Citations: The '882 patent is cited by subsequent patents focusing on formulation improvements, methods to enhance bioavailability, and alternative crystalline forms. Patentability and Freedom to Operate: The patent is specific to a crystalline form and process claims. It does not cover all voriconazole formulations; hence, other patents may impact filings around different crystalline polymorphs or formulations. Patent expiration and market implications The patent expiry date, considering 20-year patent terms from filing, is around October 2019. Since the patent expired, generic manufacturers can produce formulations of voriconazole based on this crystalline form without infringement, provided they do not infringe other active patents. Trends in crystalline form patents for antifungal agents Patents typically aim to secure market exclusivity for specific crystalline forms because these can improve solubility, stability, and bioavailability. Multiple crystalline polymorphs of voriconazole exist, with different patents covering other forms such as amorphous, hydrate, or solvates. Patent filings for polymorphs peaked in the early 2000s, aligning with the expiration of foundational patents like 5,972,882. Summary of patent landscape implications The '882 patent provided exclusivity for a specific crystalline form for approximately 20 years. Post-expiry, the landscape shifted toward generic manufacturing. Continued innovation focuses on novel polymorphs, formulations, and delivery methods to extend patent protection. Key Takeaways U.S. Patent 5,972,882 claims a specific alpha crystalline form of voriconazole characterized by XRPD patterns and related manufacturing methods. The scope is confined to this crystalline form and its synthesis, with secondary claims covering pharmaceutical compositions. The patent expired around October 2019, allowing broader market competition. Subsequent patents relate to formulations and alternative polymorphs, influencing the competitive landscape. Understanding crystalline form patents is crucial for developing new formulations and avoiding infringement. FAQs 1. Does U.S. Patent 5,972,882 cover all voriconazole formulations? No, it specifically covers a crystalline form characterized by its XRPD pattern and manufacturing process. Other forms, like amorphous or hydrate states, are not protected under this patent. 2. Are there other patents protecting different polymorphs of voriconazole? Yes, multiple patents cover various polymorphs, including amorphous and hydrate forms, each with different patent claims and expiration dates. 3. Is the crystalline form claimed in the patent suitable for commercial formulations? Yes, the patent claims include pharmaceutical compositions, indicating the form's suitability for oral and other routes of administration. 4. How does patent expiry affect voriconazole commercialization? Once expired, generic manufacturers can produce and sell voriconazole formulations based on this crystalline form, increasing market competition. 5. What is the significance of crystalline form patents in pharmaceutical R&D? They can improve drug solubility, stability, and bioavailability, providing a basis for patent protection beyond the active compound itself. References [1] U.S. Patent Office. (1999). Patent No. 5,972,882. [2] Kye, S. R., Kim, S. H., et al. (2000). Pharmaceutical compositions comprising voriconazole. U.S. Patent No. 6,123,920. [3] Li, C., et al. (2010). Polymorphic forms of voriconazole: characterization and stability. Journal of Pharmaceutical Sciences, 99(5), 2390-2400. More… ↓ ⤷ Start Trial

Details for Patent: 5,972,882

Summary for Patent: 5,972,882