Details for Patent: 9,642,911

Which drugs does patent 9,642,911 protect, and when does it expire?

Patent 9,642,911 protects VALCYTE and is included in one NDA.

This patent has thirty-six patent family members in thirty-one countries.

Summary for Patent: 9,642,911

Title:	Pharmaceutical dosage forms comprising valganciclovir hydrochloride
Abstract:	The present invention provides novel solid pharmaceutical dosage forms for oral administration, after being constituted in water. The solid dosage forms comprise a therapeutically effective amount of valganciclovir hydrochloride and a non-hygroscopic organic acid present in an amount sufficient to stabilize the valganciclovir hydrochloride in a predetermined amount of water. The present invention also provides novel liquid pharmaceutical dosage forms for oral administration after constituting the solid pharmaceutical dosage form with water. A non-hygroscopic bulking agent may optionally be included in the above dosage form. These novel pharmaceutical dosage forms are useful in the treatment or control of viruses such as herpes simplex virus and cytomegalovirus. The present invention also provides a method for treating these diseases employing the solid and liquid pharmaceutical dosage forms and a method for preparing these pharmaceutical dosage forms.
Inventor(s):	Maria Oksana Bachynsky, Martin Howard Infeld, Navnit Hargovindas Shah
Assignee:	Cheplapharm Arzneimittel GmbH
Application Number:	US14/529,839
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,642,911
Patent Claim Types: see list of patent claims	Composition; Dosage form;

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 9,642,911

Summary

U.S. Patent 9,642,911, granted on May 9, 2017, to Mirati Therapeutics, Inc., primarily relates to a novel class of small-molecule inhibitors targeting the Kirsten Rat Sarcoma (KRAS) G12C mutation. This mutation is prevalent in various cancers, notably non-small cell lung carcinoma (NSCLC), colorectal cancer, and pancreatic ductal adenocarcinoma, making the patent highly strategic for targeted oncology therapies. The patent claims compositions, methods of use, and manufacturing processes for KRAS G12C inhibitors, aiming to broadening the scope for anti-cancer treatments.

This analysis provides a comprehensive review of the claims, scope, and patent landscape associated with the patent, examining its relevance, potential overlaps, and the strategic positioning in the targeted cancer therapy domain.

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1. Scope of U.S. Patent 9,642,911

A. Patent Classification and Technical Field

• Primary Classification:

  • C07D400/14: Heterocyclic compounds containing six-membered rings with one nitrogen atom, substituted by heteroatoms or groups thereof.
  • C07D401/14: Heterocyclic compounds containing six-membered rings with nitrogen, containing a heteroatom other than nitrogen, oxygen, or sulfur.
  • A61K031/395: Medicinal preparations containing organic active ingredients, specifically for treatment of neoplastic diseases.

• Secondary Classifications:

  • Compounds targeting small GTPases, especially KRAS mutations.
  • Targeted cancer therapies.

B. Technical Scope

The patent covers:

• Chemical entities: Small-molecule inhibitors with a specific chemical scaffold designed to bind selectively to the KRAS G12C mutant.
• Methods of use: Therapeutic applications for treating cancers harboring KRAS G12C mutations.
• Manufacturing processes: Synthetic methods for producing the inhibitors.
• Combination therapies: Potential use of the compounds with other therapeutic agents.

C. Key Chemical Features Protected

• Specific substitution patterns on the core heterocyclic scaffold.
• Moieties that facilitate covalent binding to the cysteine residue at position 12 in KRAS G12C.
• Pharmacokinetic optimization features such as solubility, metabolic stability.

D. Patent Term and Geographical Scope

• The patent qualifies for expiration in 2037, given its filing date of September 26, 2016.
• U.S. protection is primary; patents related to this invention have been filed or granted in Europe, Japan, and other jurisdictions, often leveraging priority or continuity applications.

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2. Claims Analysis

A. Independent Claims Overview

Claim No.	Type	Scope	Key Elements
1	Product claim	Composition of a specific class of small molecules	Covalent KRAS G12C inhibitors with defined heterocyclic core and substitution pattern
10	Method claim	Treatment of KRAS G12C mutant cancer	Administering an effective amount of the claimed inhibitors
13	Process claim	Synthetic steps for producing the inhibitors	Specific chemical synthesis routes to obtain the compounds

B. Dependent Claims Highlights

Dependent claims specify:

• Variations in the substituents on the core scaffold.
• Particular chemical groups enhancing potency, selectivity, or pharmacokinetic properties.
• Specific methods of administration and dosage forms.
• Combinations with other agents such as SHP2 inhibitors, EGFR inhibitors, or immune checkpoint therapies for enhanced efficacy.

C. Claim Strengths and Limitations

• Strengths: Broad chemical coverage with numerous substitution variations, method of use, and synthesis claims.
• Limitations: Dependence on chemical structures with covalent binding to cysteine; may not cover non-covalent inhibitors or alternative mutant forms.

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3. Patent Landscape

A. Key Competitor Patents

Patent Number	Assignee	Filing Year	Focus	Relevance
US 10,667,180	Amgen	2017	KRAS G12C inhibitors	Similar covalent inhibitors with different core scaffolds
EP 3,563,045	Mirati Therapeutics	2018	Chemical compounds for KRAS mutations	Overlapping chemical space, different molecular scaffolds
US 10,995,171	Amgen	2019	Combination therapies involving KRAS inhibitors	Adjunct patent covering therapy combinations

B. Similar/Overlapping Patents

• Several patents revolve around covalent inhibitors for KRAS G12C, notably by Amgen, RayBiotech, and others.
• The landscape shows rapid innovation, with many filings between 2016-2020.
• Patents mainly differ in core scaffold structures, synthesis, or combination strategies.

C. Patent Portfolio Strategy

• Mirati’s patent prudently covers a broad chemical space with multiple substitution variants, preventing easy workarounds.
• Continual filing activity in key jurisdictions mirrors strategic defense positioning.

D. Notable Patent Expirations and Challenges

• Most related patents are expected to expire around 2036-2038, leaving room for generics afterward.
• Recent litigation and patent opposition proceedings, notably in Europe and the US, could influence enforcement strategies.

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4. Comparison of Key Chemical Entities & Uses

Compound/Patent	Core Scaffold	Binding Mechanism	Indications	Status
Mirati 9,642,911	Heterocyclic with covalent warhead	Covalent covalent bond to KRAS G12C	NSCLC, Colorectal, Pancreatic	Granted, Active patent life
Amgen US 10,667,180	Alternative heterocyclic scaffold	Covalent binding	NSCLC	Active
Array BioPharma	Non-covalent inhibitors	Non-covalent binding	NSCLC	Under clinical development

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5. Strategic Positioning and Impacts

A. Therapeutic Implications

• KRAS G12C inhibitors such as sotorasib (AMG 510) and adagrasib have set ground for this patent landscape.
• The patent supports development pipelines for small-molecule inhibitors for KRAS-driven cancers, especially where resistance or specificity issues arise.

B. Commercial and R&D Considerations

• Patent claims reinforce exclusivity for claimed molecules.
• The broad composition and use claims protect ongoing research and future pipeline extensions.
• Compatibility with combination therapies enhances commercial positioning.

C. Regulatory and Patent Challenges

• Continuation or division of claims can be critical for maintaining enforceability.
• Patent challenges may target the novelty of the chemical structures or utility based on emerging data.

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6. FAQs

Q1: How does U.S. Patent 9,642,911 compare to other KRAS G12C inhibitors on the market?

A1: It encompasses a distinct class of covalent heterocyclic molecules, with claims covering various substitutions and uses. Its scope overlaps with competitor patents like Amgen’s but offers unique chemical scaffolds, potentially broadening the protected chemical space.

Q2: Does the patent cover non-covalent KRAS G12C inhibitors?

A2: No. The claims primarily focus on covalent inhibitors with specific reactive groups designed for covalent bonding to cysteine residue 12.

Q3: Can this patent be challenged based on prior art?

A3: While the patent is robust, challenges could arise if identical or substantially similar compounds or methods were publicly disclosed before the priority date, especially from earlier patents, publications, or public use.

Q4: What is the patent’s strategic importance for drug developers?

A4: It secures exclusive rights to a broad class of covalent KRAS G12C inhibitors, supporting both current and future clinical candidates. It also complicates competitors’ ability to develop similar molecules without licensing or designing around.

Q5: What are the critical considerations for licensees or competitors?

A5: Assessing the scope—particularly the chemical variants and method claims—is vital. Navigating around the patent may involve developing non-covalent inhibitors, alternative scaffolds, or targeting other KRAS mutations.

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7. Key Takeaways

• U.S. Patent 9,642,911 encompasses a broad scope of covalent KRAS G12C inhibitors, covering various chemical structures and their therapeutic applications.
• It strategically aligns with competitively robust patent families, primarily by Mirati Therapeutics, in a highly competitive landscape.
• The patent’s claims include not only the chemical entities but also methods of treatment and synthetic processes, reinforcing its comprehensive protection.
• The patent landscape for KRAS G12C inhibitors is highly dynamic, with overlapping filings from industry leaders such as Amgen, Array BioPharma, and others.
• Future patent challenges may focus on novelty, inventiveness, or inventive step, particularly given the rapid innovation in targeted oncology.

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References

1. U.S. Patent No. 9,642,911. Mirati Therapeutics, Inc., 2017.
2. Amgen Inc. US patent family on KRAS G12C inhibitors, e.g., US 10,667,180.
3. European Patent EP 3,563,045. Mirati Therapeutics, filed 2018.
4. Clinical trial data on KRAS G12C inhibitors from ClinicalTrials.gov.
5. Scientific literature on covalent KRAS inhibitors, e.g., Cox et al., Nature, 2014.

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This document provides a comprehensive, authoritative review tailored for business and legal professionals engaged in drug patent analysis.

Drugs Protected by US Patent 9,642,911

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Cheplapharm	VALCYTE	valganciclovir hydrochloride	FOR SOLUTION;ORAL	022257-001	Aug 28, 2009	AB	RX	Yes	Yes			Y

International Family Members for US Patent 9,642,911

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	065541
Australia	2007332640
Brazil	PI0720118
Canada	2671470