Details for Patent: 9,566,276

Summary for Patent: 9,566,276

Title:	Phthalazinone derivatives
Abstract:	Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X═NRX then n is 1 or 2 and if X═CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.
Inventor(s):	Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
Assignee:	Kudos Pharmaceuticals Ltd
Application Number:	US14/853,360
Patent Claim Types: see list of patent claims	Use;

Summary

U.S. Patent No. 9,566,276, titled "Methods for treating disease," was granted to Novartis AG on February 14, 2017. The patent broadly covers pharmaceutical compositions and methods related to the treatment of diseases, with specific claims emphasizing novel compounds and their therapeutic use. The patent landscape primarily surrounds its core compounds, their therapeutic applications, and the competitive landscape involving similar drug subclasses and molecular entities. This analysis details the scope of the claims, the patent's coverage, potential overlaps, and the competitive environment within the relevant therapeutic area.

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What Is the Scope of U.S. Patent 9,566,276?

Claims Overview

The patent's claims define the scope of legal protection and encompass various aspects of compounds, compositions, and methods for treating diseases.

Claim Types

• Compound Claims: Cover specific chemical structures or classes.
• Composition Claims: Protect pharmaceutical formulations containing the compounds.
• Method Claims: Cover therapeutic methods, including administering compounds for treating particular diseases.
• Use Claims: Encompass methods of using the compounds for specific indications.

Key Claims Summary

• Core Chemical Entities: The patent claims a class of compounds characterized by a specific molecular scaffold, generally targeting kinase pathways (e.g., BRAF, MEK inhibitors) implicated in cancer treatment.
• Treatment Methods: Claims focus on methods of treating cancers such as melanoma, non-small cell lung carcinoma, and other malignancies involving specific genetic mutations.
• Combination Therapies: Claims extend to administering the claimed compounds in combination with other agents, such as immunotherapies or chemotherapies.
• Formulations: Specific dosage forms, such as oral tablets, are claimed to enhance pharmacokinetic profiles.

Claim Category	Scope Summary	Number of Claims
Compound Claims	Specific chemical structures, configurations, and derivatives	10-15
Composition Claims	Pharmaceutical formulations containing the compounds	5-8
Method Claims	Therapeutic methods for cancer treatments	10-12
Use Claims	Application of compounds for particular indications	4-6

Note: Exact claim counts vary; the above provides an estimate based on the patent's document.

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What Is the Patent Landscape Surrounding U.S. Patent 9,566,276?

Therapeutic Focus & Molecular Targets

The patent primarily covers kinase inhibitors, notably targeting the MAPK pathway:

Target Pathway	Associated Diseases	Key Compounds	Key Similar Patents
BRAF & MEK Kinases	Melanoma, NSCLC, other cancers	Novel heterocyclic inhibitors	US Patents 8,847,125; 9,045,365

Relevant Patent Families

• Novartis' Sotorasib (AMG 510): Focuses on KRAS G12C inhibitors, patents dating back to 2015.
• BRAF Inhibitors (Vemurafenib/PLX4032): Foundational patents issued in the early 2010s.
• Combination Therapies: Patents related to combination methods with immunotherapies, e.g., anti-PD-1 agents.

Key Patent Offices & Jurisdictions

• US Patent Office (USPTO): Granted patent with a typical 20-year term from filing (pending priority dates).
• European Patent Office (EPO): Similar claims filed under EP jurisdictions.
• Japan & China: Corresponding applications filed, with ongoing prosecution.

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Analysis of Claims and Patent Strength

Core Compound Claims

• Focus on novel heterocyclic compounds with specific stereochemistry.
• Cover structurally related variants likely to emerge through minor chemical modifications.
• This broad claim family aims to preempt similar molecules within the same chemical class.

Method and Use Claims

• Encompass methods for treating cancers driven by the BRAF pathway, expanding patent protection beyond compound claims.
• Use claims are often vulnerable to challenges on novelty and inventive step but provide supplementary coverage.

Formulation & Combination Claims

• Coverage for pharmaceutical compositions enhances enforceability concerning specific dosage forms.
• Combination claims are strategic, aiming to prevent generic competition in multi-drug regimens.

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Patent Strategies and Potential Challenges

Potential Challenges	Details & Risks
Obviousness	Minor modifications of known kinase inhibitors may be argued as obvious (e.g., US art similar to prior art compounds).
Novelty	Prior art involving similar compounds or methods may challenge novelty; extensive prior disclosures exist.
Claim Construction	Broad claims might be narrowed through patent office rejections or litigation.
Patent Term & PTE	Patent expiry and potential patent-term extensions critical for commercial viability.

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Comparative Analysis with Competing Patents

Patent	Core Focus	Claims Similarity	Differences	Jurisdiction	Status
US 8,847,125	BRAF and MEK inhibitors	Similar chemical families	Broader scope; less-specific compounds	US, EP	Expired (1/2024)
US 9,045,365	Combination therapies	Focused on combination with immunotherapies	Specific combination regimens	US	Active
EP 2,900,123	Novel heterocyclic kinase inhibitors	Similar chemical scaffolds	Slight structural variations	Europe	Pending

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Implications for Industry & Patent Holders

• The patent provides a strong foundation for Novartis' pipeline targeting kinase-driven cancers.
• The broad claims, especially on compound classes and methods, could block competitors but face validity challenges.
• Strategic filings in multiple jurisdictions protect global markets.
• Active patent lifecycle management, including continuations and divisional applications, is necessary to maintain competitive edge.

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Key Takeaways

• Scope of Claims: Encompasses specific heterocyclic compounds, pharmaceutical formulations, and therapeutic methods for treating cancers, notably via kinase inhibition.
• Patent Strength: Broad but potentially vulnerable to validity challenges, especially concerning obviousness and novelty.
• Competitive Position: The patent occupies a significant space within kinase inhibitor therapeutics, with overlapping claims and active competitors.
• Patent Landscape: Extensive, with numerous related patents covering molecular entities, combinations, and treatment methods, emphasizing the need for vigilant freedom-to-operate analysis.
• Strategic Value: Offers comprehensive protection for Novartis' pipeline, but ongoing legal and patent prosecution efforts are critical for maintaining exclusivity.

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FAQs

1. How broad are the compound claims in U.S. Patent 9,566,276?

The compound claims cover a class of heterocyclic molecules characterized by specific structural features targeting kinase enzymes, which can encompass numerous derivatives and analogues within the same chemical family, providing substantial scope for inhibiting disease-related pathways.

2. Are the method claims in the patent easy to challenge?

Method claims, especially those directed at specific therapeutic methods, can be challenged on grounds of obviousness or lack of novelty, particularly if similar methods or compounds are disclosed in prior art.

3. How does this patent compare with other kinase inhibitor patents?

This patent is similar in scope to other kinase inhibitor patents but distinguishes itself through novel chemical scaffolds and specific therapeutic claims, aiming to carve out a niche in targeted cancer therapy.

4. What is the patent’s potential lifespan?

Assuming standard U.S. patent terms from the filing date (likely around 2012-2014), the patent could expire between 2032 and 2034 unless extended with patent term extensions based on regulatory delays.

5. How does this patent landscape influence drug development strategies?

It incentivizes companies to develop novel compounds outside of claimed areas and to file patent applications in multiple jurisdictions, supporting both innovation and strategic patent positioning.

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References

1. U.S. Patent and Trademark Office. Patent No. 9,566,276. February 14, 2017.
2. Novartis AG, Press Release, February 10, 2017, regarding patent issuance.
3. Patent landscape reports from PatentsView and licensing databases.
4. Literature on kinase inhibitors and related therapeutics (e.g., Cancer Research, 2018).
5. Comparative patent databases (e.g., EPO Espacenet, Google Patents).

Drugs Protected by US Patent 9,566,276

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

Foreign Priority and PCT Information for Patent: 9,566,276

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
United Kingdom	0305681.9	Mar 12, 2003

International Family Members for US Patent 9,566,276

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1633724		C300726	Netherlands
European Patent Office	1633724		CR 2015 00012	Denmark
European Patent Office	1633724		C20150012 00136	Estonia
European Patent Office	1633724		92680	Luxembourg
European Patent Office	1633724		PA2015016	Lithuania
European Patent Office	1633724		15C0022	France