Last updated: February 19, 2026
This analysis details the scope and claims of Chinese drug patent CN102647993 and assesses its position within the broader patent landscape. The patent, granted to Nanjing Altea Pharmaceutical Co., Ltd., claims a novel crystalline form of olaparib and its preparation method. This specific crystalline form exhibits improved physicochemical properties relevant to pharmaceutical formulation and bioavailability. The patent's claims are directed towards both the crystalline form and its therapeutic applications, particularly in oncology.
What is the Core Invention Claimed in CN102647993?
The central invention claimed in CN102647993 is a specific crystalline form of olaparib, designated as Form IV. This crystalline form is distinguished by its X-ray powder diffraction (XRPD) pattern, characterized by specific diffraction peaks at defined 2θ angles. The patent also claims the process for preparing this Form IV, emphasizing the conditions that yield this particular polymorph.
- Claim 1: This claim defines the crystalline form of olaparib, referred to as Form IV, by its XRPD diffraction pattern. Key diffraction peaks are listed at specific 2θ values, serving as the primary identifier of this polymorph. The presence of a subset of these peaks is also sufficient for claiming.
- Claim 2: This claim pertains to a pharmaceutical composition comprising the olaparib Form IV and a pharmaceutically acceptable carrier. This expands the scope to include practical applications of the patented crystalline form in drug products.
- Claim 3: This claim covers the use of the olaparib Form IV for the preparation of a medicament.
- Claim 4: This claim specifies the therapeutic application of the olaparib Form IV in treating cancer.
- Claim 5: This claim describes a method for preparing the olaparib Form IV. It details specific crystallization conditions, including solvent systems and temperature profiles, designed to selectively produce this polymorph.
What are the Key Technical Features and Advantages of Olaparib Form IV?
The patent highlights several technical features and advantages associated with olaparib Form IV compared to other known crystalline forms. These improvements are critical for its development into effective pharmaceutical products.
- Crystallinity: Form IV is characterized by a distinct XRPD profile. This specific crystalline structure influences its physical properties.
- XRPD Peaks (selected significant peaks from patent):
- ~4.8°, ~9.7°, ~12.3°, ~19.4°, ~22.5°, ~24.6°, ~25.8° (±0.2° 2θ)
- Solubility: The patent asserts that Form IV exhibits improved solubility compared to other polymorphs. Enhanced solubility can lead to better absorption and increased bioavailability of the drug.
- Stability: Form IV is claimed to possess superior solid-state stability. This is crucial for shelf-life and consistent drug performance over time, reducing the risk of degradation and loss of efficacy.
- Processability: The preparation method for Form IV is designed to be reproducible and scalable, facilitating its manufacturing for commercial purposes. Specific solvent combinations (e.g., mixtures of alcohols and water) and controlled cooling rates are described as essential for achieving the desired crystalline form.
How Does CN102647993 Fit into the Olaparib Patent Landscape?
CN102647993 occupies a specific niche within the olaparib patent landscape, focusing on a particular crystalline form (polymorph) and its manufacturing. Olaparib, marketed as Lynparza by AstraZeneca, is a well-established PARP inhibitor used in cancer therapy. The foundational patent for olaparib itself (and earlier polymorphs) has likely expired or is nearing expiration in major markets. However, patents on novel crystalline forms, salt forms, and new manufacturing processes can extend market exclusivity.
- Parent Compound Patents: The original patent protecting the olaparib molecule itself, such as EP0847015 (filed in 1996, granted to AstraZeneca), has expired. This molecule patent is fundamental to the drug's existence.
- Polymorph Patents: Pharmaceutical companies frequently file patents on new, advantageous crystalline forms of existing active pharmaceutical ingredients (APIs). These are often designated by alphanumeric codes (e.g., Form I, Form II, Form III, Form IV). CN102647993 falls into this category, protecting Form IV.
- Comparison to other olaparib polymorphs: While specific details of other olaparib polymorph patents (e.g., patents claiming Forms I, II, or III) are not detailed within CN102647993, it is common for different forms to have distinct XRPD patterns, thermal properties (DSC, TGA), and solubility profiles. The success of such patents hinges on demonstrating novelty and inventive step over previously disclosed forms.
- Manufacturing Process Patents: Patents claiming novel and efficient methods for synthesizing the API or specific polymorphs are also common. CN102647993 includes claims for the preparation method of Form IV.
- Formulation and Method of Use Patents: Additional patents may cover specific drug formulations (e.g., oral tablets, capsules with specific excipients) or new therapeutic uses for olaparib.
The significance of CN102647993 lies in its potential to create a second-generation exclusivity period for olaparib based on the improved properties of Form IV and its specific manufacturing process. Companies seeking to market generic olaparib would need to navigate around these polymorph patents, either by developing non-infringing crystalline forms or by challenging the validity of existing polymorph patents.
What is the Prosecution History and Current Status of CN102647993?
Understanding the prosecution history and current status of CN102647993 provides insight into its legal standing and potential longevity.
- Applicant: Nanjing Altea Pharmaceutical Co., Ltd.
- Filing Date: October 17, 2011
- Publication Date: February 13, 2013
- Grant Date: May 22, 2019
- Patent Number: CN102647993
- Status: Granted and Valid. (As of current search, the patent is active).
- Key prosecution events: The prosecution process would involve examination by the China National Intellectual Property Administration (CNIPA), where the patent office scrutinizes the claims for novelty, inventive step, and industrial applicability. Objections from the examiner regarding prior art would need to be addressed through amendments or arguments by the applicant. The grant date of May 22, 2019, indicates that the patent successfully passed this examination.
- Term: The term of a Chinese invention patent is 20 years from the filing date. Therefore, CN102647993 is expected to remain in force until October 16, 2031.
What are the Geographic Scope and Enforcement Considerations for CN102647993?
The patent CN102647993 is a Chinese national patent, meaning its protection is limited to the territory of the People's Republic of China.
- Geographic Scope: Protection is exclusively within China. It does not confer patent rights in other countries. Companies seeking protection for olaparib Form IV or its manufacturing process in other jurisdictions would need to file separate patent applications in those respective countries or through international treaties like the Patent Cooperation Treaty (PCT).
- Enforcement: Enforcement of this patent can only occur in China through Chinese courts. Nanjing Altea Pharmaceutical Co., Ltd. or its legal successors/assignees can initiate infringement lawsuits against parties that manufacture, use, sell, or import olaparib Form IV or products containing it within China without authorization.
- Infringement Analysis: Determining infringement would involve comparing the composition and manufacturing process of a third-party product to the specific claims of CN102647993. For example, if a generic drug manufacturer in China produces olaparib using a process that yields Form IV as defined by its XRPD pattern, it could be considered infringing. Conversely, if a manufacturer uses a different crystalline form or a non-infringing preparation method, it may not infringe this specific patent.
- Validity Challenges: Competitors may attempt to invalidate CN102647993 by providing evidence of prior art that demonstrates the claimed invention was not novel or inventive at the time of filing. This could involve citing earlier scientific publications, existing patents, or public disclosures of olaparib polymorphs.
What are the Potential Business Implications for Pharmaceutical Companies?
CN102647993 has significant implications for both the patent holder and potential competitors in the Chinese pharmaceutical market.
- For Nanjing Altea Pharmaceutical Co., Ltd. (and potential licensors/assignees):
- Market Exclusivity: The patent grants a period of market exclusivity in China for olaparib Form IV until October 2031. This allows the company to capture market share and potentially command premium pricing without direct competition for this specific polymorph.
- Licensing Opportunities: The patent can be licensed to other pharmaceutical companies, generating royalty revenue. This is particularly relevant if Nanjing Altea does not have its own manufacturing or marketing capabilities for olaparib in China.
- Defense Against Generics: The patent serves as a barrier to entry for generic olaparib manufacturers in China who would need to develop alternative crystalline forms or await patent expiry.
- For Generic Manufacturers and Innovator Companies in China:
- Freedom-to-Operate (FTO) Assessment: Companies planning to develop or market olaparib in China must conduct thorough FTO analyses to ensure their products do not infringe CN102647993. This involves detailed investigation of crystalline forms and manufacturing processes.
- R&D Strategy: Research and development efforts may need to focus on identifying or developing novel, non-infringing crystalline forms of olaparib or alternative therapeutic approaches.
- Litigation Risk: Companies may face patent infringement litigation if they are found to be in violation of the patent's claims.
- Partnership/Acquisition: Competitors might explore licensing agreements with Nanjing Altea or consider acquisition if olaparib Form IV is strategically important.
- For Investors:
- Risk Assessment: Investors in companies involved with olaparib in China should assess the impact of CN102647993 on their investment. This includes evaluating the patent's validity, enforceability, and remaining term.
- Market Opportunity: The existence of a protected, potentially improved form of olaparib can indicate a robust market for the drug, which can be attractive for investment in companies with valid IP or clear FTO.
Key Takeaways
- CN102647993 protects a specific crystalline form of olaparib (Form IV) and its preparation method.
- Form IV offers claimed advantages in solubility and stability, potentially improving drug performance.
- The patent is valid until October 16, 2031, providing market exclusivity in China.
- This patent represents a significant hurdle for generic olaparib manufacturers operating in China.
- Companies must conduct thorough freedom-to-operate analyses to navigate this intellectual property.
FAQs
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What specific therapeutic areas does CN102647993 cover for olaparib?
The patent claims the use of olaparib Form IV for the preparation of a medicament for treating cancer. This aligns with the known indications of olaparib as a PARP inhibitor in various oncological settings.
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Can olaparib Form IV be manufactured without infringing CN102647993?
Manufacturing olaparib Form IV without infringement depends on the specific preparation method used. If a method that does not fall within the scope of claim 5 of CN102647993 is employed, and the resulting crystalline form is demonstrably different from Form IV as defined by its XRPD pattern, then infringement may be avoided.
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Does CN102647993 provide protection outside of China?
No, CN102647993 is a Chinese national patent and only provides protection within the territory of the People's Republic of China. Separate patent applications would be required for protection in other countries.
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What is the difference between olaparib molecule patents and polymorph patents like CN102647993?
Molecule patents protect the chemical compound itself, regardless of its form. Polymorph patents protect specific crystalline structures of that compound, which can have different physical and chemical properties. CN102647993 protects a specific crystalline form (Form IV) of olaparib, not the olaparib molecule in general.
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How can a generic company challenge the validity of CN102647993?
A generic company can challenge the validity of CN102647993 by filing an invalidity action with the China National Intellectual Property Administration (CNIPA). This typically involves submitting prior art (e.g., earlier patents, scientific publications) that demonstrates the claimed invention lacks novelty or inventive step.
Citations
[1] Nanjing Altea Pharmaceutical Co., Ltd. (2019, May 22). Olaparib crystalline form IV and preparation method thereof (Patent No. CN102647993). China National Intellectual Property Administration.
[2] AstraZeneca. (1996). Olaparib derivatives (Patent No. EP0847015). European Patent Office.
