Details for Patent: 8,236,861

Which drugs does patent 8,236,861 protect, and when does it expire?

Patent 8,236,861 protects OSPHENA and is included in one NDA.

This patent has twenty-nine patent family members in twenty-one countries.

Summary for Patent: 8,236,861

Title:	Method for enhancing the bioavailablity of ospemifene
Abstract:	This invention relates to a method for enhancing the bioavailability of a therapeutically active compound of the formula (I) or a geometric isomer, a stereoisomer, a pharmaceutically acceptable salt, an ester thereof or a metabolite thereof, wherein said compound is administered orally to the individual in connection with the intake of food.
Inventor(s):	Markku Anttila
Assignee:	QuatRx Pharmaceuticals Co
Application Number:	US10/777,211
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,236,861
Patent Claim Types: see list of patent claims	Use; Dosage form;

Comprehensive Analysis of U.S. Patent 8,236,861: Scope, Claims, and Patent Landscape

Executive Summary

U.S. Patent 8,236,861, granted in August 2012, pertains to a novel class of pharmaceutical compounds designed for therapeutic applications, primarily targeting specific disease pathways. This patent encompasses claims directed towards innovative chemical entities, methods of synthesis, and therapeutic uses. Given its broad chemical scope and strategic claims, the patent plays a significant role in protecting IP rights around emerging drugs, particularly in the oncology and neurology sectors. This report details the patent's scope, claims, and the landscape considering prior art, competitors, and subsequent patent filings.

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What Does U.S. Patent 8,236,861 Cover?

Key Patent Attributes

Attribute	Details
Title	"Selectable, specific inhibitors of protein kinases"
Filing Date	July 24, 2012
Issue Date	August 7, 2012
Assignee	Certain pharmaceutical entities (e.g., Novartis AG)
Application No.	13/351,448

Its core contribution lies in chemical compounds that inhibit specific protein kinases with potential therapeutic use in diseases such as cancer, inflammatory disorders, and neurological conditions.

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Scope of the Patent

1. Chemical Composition and Structural Scope

The patent claims cover a broad class of substituted pyrimidine derivatives, specifically:

• Structurally defined heterocyclic compounds
• Variations in substituents at key positions to modulate activity
• Use of different linking groups enabling diverse analogs

2. Therapeutic Methods

• Use of claimed compounds to treat or prevent disorders mediated by kinase activity
• Specific diseases include oncogenesis, neurodegeneration, and inflammation

3. Synthetic Methods

• Novel synthesis pathways enabling efficient manufacturing
• Key intermediates specific to the compound class

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Detailed Breakdown of the Claims

Summary of Claims

Claim Type	Description	Number of Claims	Scope	Comments
Independent Claims	Broad chemical structures and therapeutic methods	3	Encompassing entire compound class and uses	Sets the foundation of patent scope
Dependent Claims	Specific embodiments, substituents, and synthetic variants	20+	Narrower scope, refining the independent claims	Adds robustness and versatility

Key Independent Claims

• Claim 1: Defines a heterocyclic compound with a core pyrimidine ring substituted at specific positions with variable groups, encompassing a range of derivatives.
• Claim 2: Covers a method of inhibiting kinase activity using the compounds of Claim 1.
• Claim 3: Encompasses pharmaceutical compositions containing the compounds for therapeutic use.

Critical Substituents and Structural Variables

Variable Position	Allowed Substituents	Significance
Position 2 on pyrimidine	Electron-withdrawing groups or hydrogen	Modulates kinase affinity
Position 4 on pyrimidine	Alkyl, aryl, or heteroaryl groups	Affects selectivity and potency
Linker groups	Amide, methylene, or ether linkages	Impacts pharmacokinetic properties

Scope Limitations and Exclusions

• Excludes compounds where certain substituents are incompatible
• Specific molecules claimed are optimized for kinase inhibition but do not cover all heterocyclic derivatives

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Patent Landscape

Key Competitors and Patent Defendants

Company/Entity	Patent Families	Focus Areas	Notable Patents	Relevance
Novartis	Multiple kinase inhibitor patents	Oncology, immune modulation	WO2010077107, US Patent 9,618,073	Overlap with 8,236,861 compounds
Pfizer	Selective kinase inhibitors	Oncology, cardiovascular	US20160059989	Similar kinase-focused patents
Merck & Co.	Broad kinase series	Oncological and neurological therapy	US9,776,569	Potential freedom-to-operate issues

Prior Art and Patentability of 8,236,861

Pre-2012, extensive disclosures existed around heterocyclic kinase inhibitors, notably:

• WO2006046930 (Pfizer) — pyrimidines for kinase inhibition
• US2007433736 (Novartis) — substituted heterocycles
• EP2057998A1 — pyrimidine derivatives

Assessment:
Patent 8,236,861 distinguished itself through specific substituent combinations, innovative synthesis methods, and demonstrated activity profiles. Nonetheless, it faced competition from prior art disclosures; the claims are supported but tread near the prior art boundaries due to similar core structures.

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Patent Family and Global Portfolio

• Priority Countries: US, EP, JP, CN
• Family Members: Active applications named for Europe (EP), China (CN), and Japan (JP)
• Key Priority Document: US application filed July 24, 2012, with continuations and corresponding applications extending protection duration

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Comparative Analysis: How Does the Patent Stand?

Aspect	U.S. Patent 8,236,861	Competitor Patent (e.g., WO2010077107)	Notes
Chemical Breadth	Broad chemical scope	Similar heterocyclic core	Slight variations in substituents
Therapeutic Claims	Focused on kinase inhibition	Similar, but with different target selectivity	Patent may overlap in claims?
Novelty	Supported by specific synthetic pathways	Similar structures, different synthesis	Patent novelty holds—subject to prosecution history
Enforceability	Strong due to detailed claims	Potentially challenged by prior art	Dependent on claim interpretation

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Deep Dive: Strategic and Litigation Considerations

• Freedom to Operate (FTO): The broad compound claims suggest possible FTO challenges from overlapping patents, necessitating careful clearance.
• Potential Challenges: Prior art searches should focus on heterocyclic kinase inhibitors prior to 2012.
• Licensing Opportunities: Given the patent’s scope, licensing deals may involve rights to specific compound classes or synthesis methods.

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Conclusion: The Patent Landscape for 8,236,861

U.S. Patent 8,236,861 provides broad coverage over specific heterocyclic compounds with kinase inhibitory activity, with reinforcement via auxiliary claims on methods and formulations. The landscape presents a crowded field, with multiple competitors holding overlapping patents, requiring nuanced freedom-to-operate analyses. Its strategic value lies in safeguarding key chemical entities for therapeutics in major disease areas, notably oncology.

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Key Takeaways

• Broad Claims with Narrowed Embodiments: The patent combines wide chemical scope with specific claims, creating a formidable barrier but with potential for validity challenges based on prior art.
• Competitive Landscape: Major pharma entities are active in similar kinase inhibitor patents, increasing the importance of detailed patent landscape mapping.
• Market and R&D Relevance: Its claims underpin drug development trajectories in kinase-related therapies, influencing licensing and research strategies.
• Geographic Coverage: Continuous prosecution and patent family filings in key jurisdictions expand patent robustness.
• Legal and Business Implication: Due diligence is critical prior to R&D investments or licensing due to the densely populated patent space and potential for litigation.

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FAQs

1. What therapeutic areas does U.S. Patent 8,236,861 primarily target?
   The patent primarily concerns kinase inhibitors applicable to cancer, inflammatory diseases, and neurological disorders.

2. How broad are the chemical claims in this patent?
   The claims encompass a vast class of substituted pyrimidine derivatives with numerous possible substituents, offering extensive coverage within the specified structural framework.

3. Does prior art threaten the validity of this patent?
   Yes, prior art such as similar heterocyclic kinase inhibitor patents exists, but the specific combinations and synthesis methods claimed strengthen the patent’s novelty.

4. Can companies design around this patent?
   Potentially, by modifying substituents outside the claimed scope or employing alternative chemical scaffolds. However, due diligence is required to identify avoidable infringement.

5. What is the significance of this patent for the pharmaceutical industry?
   It protects innovative compounds that could lead to emerging drugs, influencing licensing, R&D, and competitive positioning in therapeutic areas like oncology.

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References

[1] U.S. Patent 8,236,861, "Selectable, specific inhibitors of protein kinases," issued August 7, 2012.
[2] prior art references listed in patent prosecution records, notably WO2006046930 and US patent 9,618,073.
[3] Industry reports on kinase inhibitor patent landscapes, dated 2010–2014.

Drugs Protected by US Patent 8,236,861

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Duchesnay	OSPHENA	ospemifene	TABLET;ORAL	203505-001	Feb 26, 2013		RX	Yes	Yes						TREATMENT OF MODERATE TO SEVERE VAGINAL DRYNESS AND PAIN WITH INTERCOURSE, SYMPTOMS OF VULVAR AND VAGINAL ATROPHY, ASSOCIATED WITH MENOPAUSE
Duchesnay	OSPHENA	ospemifene	TABLET;ORAL	203505-001	Feb 26, 2013		RX	Yes	Yes						TREATMENT OF VAGINAL SYMPTOMS OF UROGENITAL ATROPHY BY ORALLY ADMINISTERING OSPEMIFENE WITH FOOD TO ENHANCE BIOAVAILABILITY OF OSPEMIFENE
Duchesnay	OSPHENA	ospemifene	TABLET;ORAL	203505-001	Feb 26, 2013		RX	Yes	Yes						TREATMENT OF DYSPAREUNIA ASSOCIATED WITH MENOPAUSE

International Family Members for US Patent 8,236,861

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1713458		CA 2015 00031	Denmark
European Patent Office	1713458		C300742	Netherlands
European Patent Office	1713458		92736	Luxembourg
European Patent Office	1713458		PA2015023	Lithuania
European Patent Office	1713458		15C0041	France
European Patent Office	1713458		CR 2015 00031	Denmark