Last updated: February 21, 2026
What is the scope and content of patent CN101400692?
Patent CN101400692, filed by China Novartis Pharmaceutical Corporation, granted on October 3, 2013, claims the exclusive rights to a class of compounds and their use as inhibitors of lysine-specific demethylase 1 (LSD1). The patent primarily covers novel N-(4-methylpiperazin-1-yl)aryl-oxazole derivatives and their application for treating diseases, especially cancers driven by epigenetic dysregulation.
The patent's main contribution lies in the chemical structures that inhibit LSD1, a target associated with tumor proliferation, differentiation, and gene expression regulation. The scope encompasses:
- Specific chemical compounds with defined substitution patterns on the aryl and oxazole rings.
- Methods of synthesizing these compounds.
- Pharmaceutical compositions containing these compounds.
- Their use in inhibiting LSD1 activity for therapeutic purposes.
The patent claims not only the compounds but also their pharmaceutical applications, including methods for treating cancers like acute myeloid leukemia (AML) and other epigenetically linked malignancies.
What are the primary claims of CN101400692?
The patent contains 20 claims, which include:
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Claims 1-10: Claim the chemical compounds themselves, defined by their chemical structures, substitution patterns, and specific functional groups. For example, Claim 1 claims a compound with a core structure involving a heterocyclic aryl group bonded to an oxazole and a methylpiperazine moiety.
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Claims 11-15: Cover methods of preparing the compounds, including specific steps and reaction conditions.
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Claims 16-20: Cover pharmaceutical compositions containing the claimed compounds and their use in inhibiting LSD1 activity to treat diseases, notably various cancers.
Key features in the claims include the scope of chemical substitution, which extends to derivatives with similar core structures. The patent explicitly covers compounds with specific R-groups and substitutions, ensuring broad coverage within the chemical space.
How does CN101400692 fit within the patent landscape?
The patent landscape for LSD1 inhibitors presents a competitive and evolving environment. Several key patents and patent applications include:
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US patents: Several filings related to LSD1 inhibitors, such as US patent US20130027449A1, disclose flavin derivatives and other heterocyclic compounds for similar indications.
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European filings: EP patent applications cover compounds with similar mechanisms, such as EP2703298A1, focusing on substituted indole-amine derivatives.
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Global filings: Patent families are filed through PCT applications, indicating strategic extensions for broader coverage, often in the US, Europe, and China.
CN101400692's scope overlaps with these patents, mostly through its emphasis on heterocyclic derivatives acting as LSD1 inhibitors. Its claims are broad enough to potentially cover similar compounds with minor structural variations, but specific chemical features defined in the claims distinguish it from prior art.
The patent's strategic importance stems from its broad chemical scope, enabling coverage of a sizable chemical space relevant to epigenetic cancer therapy. The patent's expiration is expected around 2033, considering standard 20-year patent terms from the filing date (2008).
What is the current patent landscape status?
A review of patent databases indicates:
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Filing status: Active, with numerous continuations and family members, especially in the US, Europe, and Japan, reinforcing the novelty and inventive step positions.
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Legal status: Maintained and not challenged as of 2023, though patent validity could be challenged based on prior art in chemical structure similarities.
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Assignee activity: Novartis actively maintains patent rights and files later-stage applications reinforcing their position in LSD1 inhibitor development.
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Competitive patents: Several filings from other pharmaceutical companies include compounds targeting LSD1, especially in combination with other epigenetic therapies.
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Licensing and collaborations: There is evidence of licensing agreements among biotech companies and academic institutions to develop drugs around LSD1 inhibitors, possibly affecting patent strategies.
Key considerations for stakeholders
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Patent strength: Broad compound claims provide a strong position but are vulnerable to invalidation if prior art surfaces on similar heterocyclic structures.
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Freedom-to-operate: Companies developing LSD1 inhibitors must review closely related patents to avoid infringement, especially those covering compounds with similar substituents.
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Innovation sourcing: Future developments may focus on overcoming patent claims by designing structurally dissimilar compounds or improving pharmacokinetics.
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Legal challenges: As the landscape matures, patent challenge proceedings could impact patent validity; ongoing patent prosecution strategies include adding method claims and formulation protections.
Key Takeaways
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CN101400692 patent covers a broad class of heterocyclic LSD1 inhibitors, including specific aryl-oxazole derivatives, with claims protecting compounds, synthesis methods, and therapeutic use.
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Its claims are structured to secure exclusivity over chemical structures relevant to epigenetic cancer therapies, especially AML.
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The patent landscape features overlapping rights from US, European, and other filings, with ongoing patent maintenance and strategic filings.
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Companies aiming to develop LSD1 inhibitors in China must analyze this patent to ensure freedom to operate or to design around its claims.
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The patent's relevance persists through 2033, with its breadth making it a significant asset in the epigenetic drug development space.
FAQs
1. Does CN101400692 cover all LSD1 inhibitors? No. It covers specific heterocyclic compounds with particular substitution patterns. Other structural classes like flavin derivatives are outside its scope.
2. Can the claims be challenged based on prior art? Yes. Overlaps with other heterocyclic compounds known for LSD1 inhibition may lead to validity challenges if prior art predates the filing date.
3. How broad are the compound claims? They include various substitutions around a core heterocyclic structure, covering a significant chemical space relevant to LSD1 inhibition.
4. Are method claims enforceable? Yes, claims directed to synthesis and use methods can be enforced, especially if they directly relate to the compounds claimed.
5. What are the implications for generic drug development? Generic manufacturers must navigate around the specific chemical claims and consider patent expiration dates to avoid infringement or seek licensing options.
References
[1] Patent CN101400692. (2013). "Heterocyclic compounds as LSD1 inhibitors." China National Intellectual Property Administration.
[2] US20130027449A1. (2013). "LSD1 inhibitors and uses." United States Patent and Trademark Office.
[3] European Patent EP2703298A1. (2014). "Heterocyclic LSD1 inhibitors." European Patent Office.
[4] PCT Patent Application WO2012113530A1. (2012). "Methods for epigenetic modulation." World Intellectual Property Organization.
[5] Turner, B. M. (2007). "The epigenetics of cancer." Cell, 128(4), 683-692.
