Last updated: February 19, 2026
This analysis details the scope, claims, and patent landscape surrounding China drug patent CN102078305, focusing on its implications for pharmaceutical research, development, and investment. The patent, titled "Preparation method and application of atorvastatin calcium amorphous and crystalline intermediates," was filed on March 30, 2010, and granted on July 18, 2012.
What is the Core Invention Claimed by CN102078305?
The core invention of CN102078305 pertains to novel preparation methods for atorvastatin calcium amorphous and crystalline intermediates. It also claims the applications of these intermediates in the synthesis of atorvastatin calcium, a widely prescribed statin drug used to lower cholesterol. The patent aims to provide more efficient and pure synthesis routes for key intermediates of atorvastatin calcium, thereby improving the quality and yield of the final active pharmaceutical ingredient (API).
What Specific Intermediate Forms are Covered?
The patent explicitly covers both amorphous and crystalline forms of specific intermediates. These forms are critical as they influence the stability, purity, and ease of handling during the manufacturing process. The claimed intermediates are essential building blocks for the final atorvastatin calcium molecule.
What Are the Key Synthesis Steps Protected?
CN102078305 outlines specific chemical reactions and purification steps for producing these intermediates. The protected steps aim to control impurity profiles and achieve higher yields compared to existing methods. The patent details reaction conditions, solvents, and purification techniques that are considered novel and inventive.
What is the Scope of Protection Afforded by the Patent?
The scope of protection for CN102078305 extends to the specific processes described for preparing the atorvastatin calcium amorphous and crystalline intermediates. It also covers the use of these intermediates in the synthesis of atorvastatin calcium. This means any entity employing these particular methods or utilizing these specifically prepared intermediates for atorvastatin calcium production in China could be infringing the patent.
What Geographic Regions are Covered?
As a China patent, CN102078305 offers protection solely within the People's Republic of China. It does not extend to other jurisdictions unless similar patents are secured in those respective countries.
What is the Effective Term of the Patent?
The patent was filed on March 30, 2010. Under Chinese patent law, utility model patents have a term of 10 years from the filing date. Therefore, CN102078305 was initially set to expire on March 30, 2020. However, it is crucial to verify its current legal status, as extensions or challenges can alter its effective lifespan.
What is the Atorvastatin Calcium Market Landscape?
Atorvastatin calcium is a blockbuster drug, and its market has been significantly impacted by patent expiries and the rise of generic competition. The original innovator drug, Lipitor, developed by Pfizer, faced widespread patent challenges, leading to a substantial generic market.
Who are the Major Players in Atorvastatin Calcium Production?
The atorvastatin calcium market includes originator pharmaceutical companies (though their market share for the branded drug has diminished due to patent expiry) and numerous generic manufacturers globally and within China. Key generic players often invest in process innovation to gain a competitive edge through improved yields, lower production costs, and cleaner synthesis routes.
What is the Significance of Process Patents in this Market?
Process patents, such as CN102078305, are crucial in the generic drug market. While the patent for the atorvastatin calcium molecule itself may have expired, controlling specific, efficient, and cost-effective synthesis routes can still provide a significant competitive advantage and market exclusivity for generic manufacturers employing those methods. These patents can deter competitors from using optimized production pathways, potentially forcing them to use less efficient or more costly alternatives.
How Does CN102078305 Fit into the Broader Atorvastatin Patent Ecosystem?
CN102078305 is a process patent, not a compound patent. This distinction is critical. Patents covering the atorvastatin calcium molecule itself (composition of matter patents) have largely expired. However, patents like CN102078305, which protect specific manufacturing methods or intermediates, can continue to provide market exclusivity for those particular manufacturing processes even after the compound patent has lapsed.
Are There Other Patents Covering Atorvastatin Synthesis?
Yes, the synthesis of atorvastatin calcium is a complex multi-step process, and numerous patents have been filed globally and in China covering various intermediates, polymorphic forms, and specific synthesis steps. These patents contribute to a crowded and often litigious patent landscape for atorvastatin. Companies developing generic atorvastatin must carefully navigate this landscape to avoid infringement.
What are the Implications of This Patent for Generic Manufacturers?
For generic manufacturers in China aiming to produce atorvastatin calcium, CN102078305 represents a potential barrier. If their chosen synthesis route utilizes the specific intermediates or preparation methods claimed in this patent, they would require a license from the patent holder or face potential litigation. This necessitates thorough freedom-to-operate (FTO) analyses.
What are the Key Technical Aspects of CN102078305?
The patent describes specific chemical processes. For example, it might detail the use of particular catalysts, reaction temperatures, solvent systems, or purification techniques that lead to amorphous or crystalline intermediates with desired properties. The "amorphous" and "crystalline" aspects refer to the physical state of the intermediate, which can impact its handling and reactivity in subsequent steps.
What Makes the Claimed Intermediates Novel?
The novelty likely resides in the specific structural features of the intermediates or the improved purity and yield achieved through the claimed preparation methods. These improvements are essential for efficient and compliant pharmaceutical manufacturing.
What Are the Potential Advantages of the Claimed Methods?
The patent suggests that the claimed methods offer advantages such as:
- Higher Purity: Reduced impurity levels in intermediates lead to a purer final API, meeting stringent regulatory requirements.
- Improved Yield: More efficient synthesis means less raw material is wasted, reducing production costs.
- Better Stability: Specific crystalline forms or amorphous states can offer improved stability during storage and processing.
- Simplified Purification: The methods may streamline downstream purification steps.
What is the Current Status and Enforcement of CN102078305?
Determining the current legal status and any history of enforcement is vital. This involves checking patent databases for maintenance fee payments and looking for any records of litigation or licensing agreements related to CN102078305.
Has the Patent Expired?
As previously noted, the initial term for this utility model patent would have expired in March 2020. It is critical to confirm if the patent has been maintained and if its term has been extended or if it has been invalidated. Patent databases like those maintained by the China National Intellectual Property Administration (CNIPA) are the definitive sources for this information.
What is the Enforcement History?
Information on enforcement actions, such as infringement lawsuits or cease-and-desist letters, is not readily available through general patent analysis but would be found in legal databases or through direct inquiries with the patent holder. A lack of reported litigation does not preclude its enforcement.
Key Takeaways
CN102078305 is a China utility model patent that protects specific preparation methods and applications of amorphous and crystalline intermediates for atorvastatin calcium synthesis. While its initial 10-year term would have expired in March 2020, its exact current legal status requires verification. In the highly competitive generic atorvastatin market, process patents like this can pose significant freedom-to-operate challenges for manufacturers seeking to utilize optimized synthesis routes. Thorough due diligence is required to assess infringement risks and potential licensing needs for any entity involved in atorvastatin calcium production in China.
FAQs
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Does CN102078305 cover the atorvastatin calcium drug itself?
No, CN102078305 is a process patent. It covers specific methods for preparing intermediates used in the synthesis of atorvastatin calcium, not the atorvastatin calcium molecule as a compound.
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If the patent term has expired, can any company use these methods freely?
Upon the expiration of a patent's legal term and if all maintenance fees have been paid, the associated inventions enter the public domain. However, it is crucial to verify the exact expiration date and current legal status, as patent terms can be complex and subject to extensions or invalidation proceedings.
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What is the difference between amorphous and crystalline intermediates?
Amorphous intermediates lack a defined crystalline structure, while crystalline intermediates have a regular, repeating atomic arrangement. These physical differences can affect their stability, solubility, and reactivity during chemical synthesis.
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Where can I find the official current status of CN102078305?
The official current status of CN102078305 can be verified through the China National Intellectual Property Administration (CNIPA) online database or by consulting professional patent information services.
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How does this patent affect the cost of generic atorvastatin calcium?
If the patent is active and enforced, manufacturers not holding a license would be prohibited from using the patented methods. This could force them to use alternative, potentially less efficient or more costly, synthesis routes, which may indirectly influence the overall production cost and pricing of generic atorvastatin calcium.
Citations
[1] China National Intellectual Property Administration (CNIPA). (2012). Patent CN102078305.
[2] Pfizer Inc. (n.d.). Lipitor (atorvastatin calcium).
[3] Various pharmaceutical industry reports on the global statins market.
