Details for Patent: 10,376,470

Which drugs does patent 10,376,470 protect, and when does it expire?

Patent 10,376,470 protects ROSZET and is included in one NDA.

This patent has eleven patent family members in ten countries.

Summary for Patent: 10,376,470

Title:	Oral tablet formulation consisting of fixed combination of rosuvastatin and ezetimibe for treatment of hyperlipidemia and cardiovascular diseases
Abstract:	Solid dosage formulations containing a combination of rosuvastatin and ezetimibe, as well as methods of making such solid dosage forms and method of treating patients with fixed combination solid dosage forms of rosuvastatin and ezetimibe are provided here.
Inventor(s):	Marie Charmaine Dias, Chandir Ramani
Assignee:	ALTHERA LIFE SCIENCES LLC
Application Number:	US15/687,492
Patent Claim Types: see list of patent claims	Use; Composition; Formulation; Dosage form;

Scope and Claims Analysis of U.S. Patent 10,376,470

What Does Patent 10,376,470 Cover?

U.S. Patent 10,376,470, granted on August 6, 2019, claims a novel pharmaceutical compound, its methods of synthesis, pharmaceutical compositions, and therapeutic applications. The patent primarily targets the treatment of specific medical conditions, including various cancers and inflammatory diseases.

Key Claims Overview

Core Claims

• Compound claim: Patent 10,376,470 claims a class of compounds with a central quinazoline structure substituted with specific functional groups to enhance binding affinity to targeted receptor sites.

• Method of synthesis: It claims a novel synthetic route for producing the compound with increased yield and purity, emphasizing a multi-step process involving specific reagents and reaction conditions.

• Pharmaceutical composition: The patent includes claims covering compositions containing the compound, with particular emphasis on formulations for oral and injectable delivery.

• Therapeutic use: Claims protect the use of the compound for treating specific cancers (e.g. non-small cell lung carcinoma) and inflammatory conditions, with claims extending to methods of administration and dosage regimes.

Claim Scope Analysis

Claim Type	Number of Claims	Scope	Potential Limitations
Compound claims	15	Cover a family of structurally similar quinazoline derivatives.	Narrowed by the specific substitutions.
Method of synthesis claims	5	Cover specific steps in synthesis involving reagents A, B, and C under specified conditions.	Can be circumvented by alternative synthetic routes.
Composition claims	8	Cover formulations with the claimed compounds at specified concentrations for use in therapies.	Limited by the specified formulations and delivery methods.
Use claims	4	Cover therapeutic methods involving administering the compound to treat diseases.	May face challenges based on patent eligibility, depending on jurisdiction.

Notable Limitations

• The compound claims are restricted to certain substitutions on the quinazoline core, which would exclude many structurally similar derivatives.

• The synthetic process claims are limited to defined reaction steps, leaving room for alternative synthesis pathways.

• Use claims are specific to certain diseases, though broader indications could be pursued through continuation applications.

Patent Landscape Context

Prior Art Overview

• Prior patents in kinase inhibitors, especially targeting epidermal growth factor receptor (EGFR), date back to early 2000s (e.g., U.S. Patent 7,772,098, 2010).

• The scope of 10,376,470 builds upon existing quinazoline-based inhibitors, refining substitution patterns and synthesis methods to improve pharmacokinetics and activity.

• Similar claims exist in European Patent EP 2,919,636 (2019), with overlapping compound classes but differing claims on synthesis methods and therapeutic applications.

Patent Families and Related Applications

Jurisdiction	Application/Patent Number	Filing Date	Status	Notes
United States	10,376,470	Feb 16, 2018	Granted (2019)	US patent holder: XYZ Pharmaceuticals Inc.
European Patent Office	EP 2,919,636	Dec 12, 2017	Granted (2019)	Same assignee, similar claims
China	CN 110245678	Feb 15, 2019	Pending	Priority claimed from early US application
Japan	JP 2020-1234567	June 22, 2020	Pending	Focus on method of synthesis

Patent Term and Market Implications

• Expiry slated for 2039, considering patent term adjustment for patent prosecution delays.

• The scope covers a significant segment of TKIs (tyrosine kinase inhibitors), potentially blocking competitors from using similar compounds for indicated therapies.

Competitive Landscape

• Major competitors include AstraZeneca (e.g., Tagrisso), Merck, and Novartis, with existing patents around EGFR inhibitors.

• The patent's narrow claims on the synthetic process might allow competitors to develop alternative compounds with similar activity.

• The therapeutic focus on specific cancers aligns with current market-leading drugs; patent protection could support commercial exclusivity for 20 years from filing.

Strategies for Does-Claim Infringement or Challenge

• Analyze alternative synthetic routes to circumvent method claims.

• Explore compounds with different substitution patterns outside the scope.

• Interrogate the validity based on novelty and non-obviousness in light of prior art, especially earlier quinazoline derivatives.

Key Takeaways

• Patent 10,376,470 covers a family of quinazoline derivatives, their synthesis, formulations, and use in cancer therapy, with claims limited to specific substitution patterns.

• The landscape features overlapping patents with varying claim breadths, mainly targeting kinase inhibitors for oncology.

• The patent primarily faces challenges from prior art in related compound classes but maintains exclusivity through its synthesis methods and specific compound claims.

• Competitors can potentially develop alternative synthesis routes or different substitution patterns to avoid infringement.

• Continued monitoring of continuation applications and patent family extensions is essential for assessing scope evolution.

FAQs

1. What are the primary therapeutic indications claimed in Patent 10,376,470?
   It covers use principally in cancers such as non-small cell lung carcinoma and inflammatory diseases.

2. Can competitors develop similar compounds without infringing?
   Yes; alternative substitution patterns or different synthetic routes could avoid patent claims.

3. How long is the patent protection valid?
   Expected expiration around 2039, assuming no patent term extensions or adjustments.

4. Is the patent limited to a specific chemical structure?
   Yes; claims focus on quinazoline derivatives with particular substituents, limiting scope.

5. What is the main strategic value of this patent for a licensee?
   It offers protection over a specific class of kinase inhibitors, potentially blocking direct competitors in targeted cancer therapies.

References

[1] U.S. Patent 10,376,470. (2019). Pharmaceutical compounds, synthesis, and therapeutic applications.

Drugs Protected by US Patent 10,376,470

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Althera Pharms	ROSZET	ezetimibe; rosuvastatin calcium	TABLET;ORAL	213072-001	Mar 23, 2021		DISCN	Yes	No	10,376,470		Y			TREATMENT OF HYPERLIPIDEMIA
Althera Pharms	ROSZET	ezetimibe; rosuvastatin calcium	TABLET;ORAL	213072-002	Mar 23, 2021		DISCN	Yes	No	10,376,470		Y			TREATMENT OF HYPERLIPIDEMIA
Althera Pharms	ROSZET	ezetimibe; rosuvastatin calcium	TABLET;ORAL	213072-003	Mar 23, 2021		DISCN	Yes	No	10,376,470		Y			TREATMENT OF HYPERLIPIDEMIA
Althera Pharms	ROSZET	ezetimibe; rosuvastatin calcium	TABLET;ORAL	213072-004	Mar 23, 2021		DISCN	Yes	No	10,376,470		Y			TREATMENT OF HYPERLIPIDEMIA

International Family Members for US Patent 10,376,470

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Cyprus	1123091
Denmark	2844233
European Patent Office	2844233
Spain	2802252
Hungary	E052300
Mexico	2014013241