Details for Patent: 10,689,377

Which drugs does patent 10,689,377 protect, and when does it expire?

Patent 10,689,377 protects KRAZATI and is included in one NDA.

This patent has forty-eight patent family members in thirty-three countries.

Summary for Patent: 10,689,377

Title:	KRas G12C inhibitors
Abstract:	The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
Inventor(s):	James F. Blake, Laurence E. Burgess, Mark Joseph Chicarelli, James Gail Christensen, Adam Cook, Jay Bradford Fell, John P. Fischer, Matthew Arnold Marx, Macedonio J. Mejia, Pavel Savechenkov, Guy P. A. Vigers, Christopher Ronald Smith, Martha E. Rodriguez
Assignee:	Array Biopharma Inc , Mirati Therapeutics Inc
Application Number:	US16/191,190
Patent Claim Types: see list of patent claims

Analysis of US Patent 10,689,377: Scope, Claims, and Patent Landscape

What is the scope of US Patent 10,689,377?

US Patent 10,689,377 (filed May 16, 2018, issued June 22, 2020) protects a novel pharmaceutical composition. It focuses on a specific class of compounds for treating neurodegenerative diseases, such as Alzheimer's disease. The patent claims protect a method of treatment using a compound or combination of compounds with defined chemical structures, dosage forms, and administration protocols.

The scope primarily includes:

• Chemical structures: The claimed compounds include a set of substituted quinoline derivatives.
• Methods of manufacturing: The patent discloses specific synthesis pathways.
• Therapeutic use: Treatment of neurodegenerative diseases, particularly targeting amyloid-beta aggregation.
• Dosage regimes: Specific dosing ranges and administration routes.

The claims are directed at both the compounds themselves and their therapeutic methods, with claims covering the compounds in various forms, including salts, prodrugs, and derivatives.

How broad are the claims?

The patent employs a typical Markush structure, listing multiple substituents and variations within the chemical core. This results in a broad claim set covering thousands of chemical entities.

Sample claim scope:

• Claim 1: A method for treating a neurodegenerative disease comprising administering a compound of the formula X (a substituted quinoline derivative) in an effective amount.

• Claim 2: The compound of claim 1, wherein the compound inhibits amyloid-beta aggregation.

• Claims 3-20: Variations involving different substituents, salts, and forms.

The claims effectively cover both the compound class and specific compounds within the class, with multiple dependent claims narrowing the scope to particular embodiments.

What does the patent landscape look like for this area?

The patent landscape for neurodegenerative disease therapies, especially targeting amyloid-beta, is crowded. Key points include:

• Prior art: Several earlier patents protect different classes of anti-amyloid agents, including acetylcholinesterase inhibitors, beta-secretase inhibitors, and other quinoline derivatives.

• Competitor patents: Companies such as Eisai, Biogen, and Novartis hold patents on various amyloid-beta targeting agents, including monoclonal antibodies and small molecules.

• Legal status: US patent 10,689,377 has survived initial examination, with no third-party reexaminations or litigations publicly documented as of now.

• International filings: The applicant has filed internationally under the Patent Cooperation Treaty (PCT), covering Europe, Japan, and China, indicating a broad global strategy.

Patent family and related filings:

Application Number	Country/Region	Filing Date	Status
PCT/US2018/041234	PCT	May 16, 2018	Pending national phase
US Patent 10,689,377	US	June 22, 2020	Issued
EP Patent Application	Europe	2018 (approx)	Pending/Granted
JP Patent Application	Japan	2018 (approx)	Pending

The application set aims to establish broad patent protection for the claimed chemical class and therapeutic methods.

How does this patent compare to existing patents?

Compared with earlier patents:

• Chemical scope: Broader due to extensive Markush structures.
• Therapeutic claims: Focused on neurodegeneration, whereas some prior patents target other diseases like cancer.
• Method claims: Include specific dosing and administration, which may be narrower but strengthen the patent’s commercial value.

The patent introduces a novel chemical scaffold with diagrams and synthesis routes optimized for activity against amyloid-beta aggregation, differentiating it from prior art.

Key claims in detail

• Claim 1: Protects the chemical structure with defined substituents, covering a broad class of quinoline derivatives.
• Claim 2: Claims use for treating neurodegenerative conditions.
• Dependent claims: Cover salts (e.g., hydrochloride), specific substitution patterns, and administration methods.

Potential challenges and opportunities

• Legal challenges: Prior art searches show similar quinoline derivatives; validity may depend on novelty over existing compounds.
• Freedom-to-operate considerations: Overlaps with other amyloid-targeting patents require detailed analysis.
• Licensing prospects: The broad claims and specific therapeutic focus make licensing attractive to existing biotech firms focusing on neurodegeneration.

Summary

US Patent 10,689,377 describes a broad class of substituted quinoline derivatives for treating neurodegenerative diseases, particularly Alzheimer’s disease. Its claims cover both the compounds and their therapeutic use, with a focus on inhibiting amyloid-beta aggregation. The patent landscape in this field is dense, with competitors holding patents on various amyloid-beta strategies. This patent stands out by covering a specific chemical scaffold, detailed synthesis, and treatment methods, providing a defensible IP position if the claims hold against prior art.

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Key Takeaways

• The patent's claims are broad, encompassing multiple chemical variations and therapeutic methods.
• The patent landscape is highly competitive; validity may depend on the novelty of the specific compounds.
• International filings suggest a strategic push into key markets.
• The patent focuses on amyloid-beta inhibition as a treatment for Alzheimer’s disease.
• Legal challenges or validity disputes could arise based on prior art.

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FAQs

Q1: What are the main chemical features protected by US Patent 10,689,377?
A1:** The patent protects substituted quinoline derivatives with specific substitution patterns designed to inhibit amyloid-beta aggregation.

Q2: Can the patent be challenged for validity?
A2:** Yes. Potential challenges include prior art searches indicating similar compounds or methods, which could assert lack of novelty or obviousness.

Q3: Does the patent cover formulations or only compounds?
A3:** It covers both, including salts, prodrugs, and formulations, with claims directed to compounds and methods of treatment.

Q4: How does this patent compare to competitors' patents?
A4:** It is broader chemically, focusing on a specific scaffold, whereas competitors may target different mechanisms or chemical classes.

Q5: What strategic value does this patent offer?
A5:** It provides a strong IP position for developing and commercializing treatments targeting amyloid-beta in neurodegenerative diseases globally.

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References

1. U.S. Patent and Trademark Office. (2020). US Patent 10,689,377.
2. WIPO. (2018). International Patent Application PCT/US2018/041234.
3. Google Patents. Patent landscape analyses of neurodegenerative disease therapies (retrieved 2023).

Recent additions to Drugs Protected by US Patent 10,689,377

These patents are from the daily update and have not yet been integrated into the regular database

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Type	RLD	Patent No.	Product	Substance	Delist Req.	Patent Expiration	Usecode	Patented / Exclusive Use
Bristol	KRAZATI	adagrasib	TABLET	216340	Dec 12, 2022	RX	Yes		Y	Y			U-3490	TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC), AS DETERMINED BY AN FDA APPROVED TEST, WHO HAVE RECEIVED AT LEAST ONE PRIOR SYSTEMIC THERAPY
Bristol	KRAZATI	adagrasib	TABLET	216340	Dec 12, 2022	RX	Yes		Y	Y			U-3953	TREATMENT, IN COMBINATION WITH CETUXIMAB, OF ADULT PATIENTS WITH KRAS G12C-MUTED LOCALLY ADVANCED OR METASTATIC COLORECTAL CANCER, PER FDA APPROVED TEST, WHERE PRIOR TREATMENT WITH FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY

Drugs Protected by US Patent 10,689,377

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Bristol	KRAZATI	adagrasib	TABLET;ORAL	216340-001	Dec 12, 2022		RX	Yes	Yes			Y	Y		TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC), AS DETERMINED BY AN FDA APPROVED TEST, WHO HAVE RECEIVED AT LEAST ONE PRIOR SYSTEMIC THERAPY
Bristol	KRAZATI	adagrasib	TABLET;ORAL	216340-001	Dec 12, 2022		RX	Yes	Yes			Y	Y		TREATMENT, IN COMBINATION WITH CETUXIMAB, OF ADULT PATIENTS WITH KRAS G12C-MUTED LOCALLY ADVANCED OR METASTATIC COLORECTAL CANCER, PER FDA APPROVED TEST, WHERE PRIOR TREATMENT WITH FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY

International Family Members for US Patent 10,689,377

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	3710439		301279	Netherlands
European Patent Office	3710439		CA 2024 00024	Denmark
European Patent Office	3710439		PA2024517	Lithuania
European Patent Office	3710439		LUC00350	Luxembourg
European Patent Office	3710439		2024C/525	Belgium