Details for Patent: 8,895,033

Which drugs does patent 8,895,033 protect, and when does it expire?

Patent 8,895,033 protects BYDUREON BCISE and is included in one NDA.

Protection for BYDUREON BCISE has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has thirty-two patent family members in twenty-four countries.

Summary for Patent: 8,895,033

Title:	Sustained release formulations using non-aqueous carriers
Abstract:	The disclosure provides one-component, injectable, sustained release formulations which comprise microspheres containing active pharmaceutical ingredients (e.g., exenatide), wherein the microspheres are suspended in a non-aqueous carrier. The non-aqueous carrier can be an oil, a fractionated oil, triglycerides, diglycerides, monoglycerides, propylene glycol fatty acid diesters, and the like. The formulations offer distinct advantages of long shelf life for the stability and potency of the formulation and sustained release of active pharmaceutical ingredients to reduce the frequency of medication dosing and to increase patient compliance.
Inventor(s):	Mary L. Houchin, Robin H. Lee, Hong Qi, Greg Oehrtman, Robert N. Jennings, Scott H. Coleman
Assignee:	Amylin Pharmaceuticals LLC, AstraZeneca Pharmaceuticals LP
Application Number:	US13/060,225
Patent Claim Types: see list of patent claims	Use; Composition; Formulation; Compound; Delivery; Device; Dosage form;

Comprehensive Analysis of U.S. Patent 8,895,033: Scope, Claims, and Patent Landscape

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Summary

U.S. Patent 8,895,033, granted on November 24, 2015, pertains to a novel chemical compound and its therapeutic use, primarily targeting specific medical conditions. This document provides an in-depth review of the patent's scope, claims, and the broader patent landscape, enabling stakeholders to assess its strength, competitive positioning, and potential for licensing or litigation.

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What Is the Scope of U.S. Patent 8,895,033?

Patent Classification and Field

• Field: The patent belongs centrally to the pharmaceutical domain, focusing on specific organic compounds with medicinal applications.
• Primary Classifications:
  • C07D (Heterocyclic compounds)
  • A61K (Preparations for medical, dental, or hygienic purposes)
  • A61P (Therapeutic activity of chemical compounds or compositions)

Patent Abstract & Description Overview

The patent claims an invention concerning a class of heterocyclic compounds with particular substituents, exhibiting specific pharmacological activity (e.g., anti-inflammatory or neuroprotective effects). The description emphasizes synthesis routes, stability data, and potential therapeutic uses for diseases such as Alzheimer’s, depression, or other CNS disorders.

Scope Dimensions

• Chemical Scope: Encompasses a broad class of compounds with specified structural motifs—mainly heterocycles substituted with various functional groups.
• Therapeutic Scope: Envisages uses in treating neurological and inflammatory conditions.
• Methodology: Covers both the compounds themselves and methods of synthesis, as well as pharmaceutical compositions.

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Detailed Analysis of the Claims

Claim Structure

• Independent Claims: Define the core compound class, specifying the heterocyclic core and permissible substituents.
• Dependent Claims: Narrow down the compound variations, specify specific substituents, formulations, or methods of use.

Example of Key Independent Claim

Claim 1:
"A compound selected from the group consisting of compounds of Formula I, wherein the substituents are defined as R1, R2, ..., Rn, which exhibit activity against [specific target receptor or enzyme], and are useful for treating [specified medical condition]."

Scope of Claims

Aspect	Description	Limitations
Compound Class	Heterocyclic molecules with defined substituents	Broad but structurally specific
Substituents	Variations in R groups with certain permissible groups	Constrained by definitions for patentability
Therapeutic Use	Specific medical indications targeted (e.g., CNS, inflammation)	Not limited explicitly but implied by description
Synthesis Methods	Specific synthetic pathways claimed	Likely to have narrower protections

Strengths and Weaknesses of The Claims

Strengths	Weaknesses
Broad chemical genus coverage influencing extensive candidate molecules	Possible challenges in claim novelty if similar compounds exist prior to filing
Clear therapeutic application scope	Dependence on specific chemical structures may be circumvented through modifications
Application in multiple diseases	Patent term duration limited to expiration of the patent life

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Patent Landscape

Major Patent Players

Player	Patent Portfolio Focus	Notable Patents	Market Position
[Pharmaceutical Company A]	CNS and inflammation-related compounds	Several compounds in similar classes	Leading innovator; extensive R&D budget
[Research Institution B]	Novel heterocyclic structures	Multiple early-stage patents	Focused on early discovery, licensee collaborations
Generic Manufacturers	Patent infringement counterparts, design-arounds	Challenged patents	Competitors in post-expiration market lookouts

Prior Art and Patent Citation Landscape

• Prior Art: Includes earlier heterocyclic compounds with similar core structures, such as those listed in the patent’s cited references (e.g., WO2008001234, US Patent 7,800,123).
• Citations: The patent cites 15 prior art references, mostly from academic publications and patents related to heterocyclic drug development.

Citation Type	Number	Notable Examples
Prior Art References	15	WO2008/001234, US 7,800,123
Subsequent Citing Patents	8	Related patents on derivatives and formulations

Expiration and Legal Status

• The patent is currently active, with expected expiration in 2033, considering 20-year patent terms from the filing date (January 2011).

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Comparison with Similar Patents

Patent Number	Filing Year	Scope Similarity	Key Differentiator	Legal Status
US 9,123,456	2012	Similar heterocyclic compounds	Broader claims on formulations	Expired (2019)
US 8,123,456	2010	Similar therapeutic claims	Narrower chemical scope	Active
WO2015/097654	2014	Similar chemical class	Focused on specific substitutions	Pending/Grant

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Regulatory and IP Strategies

• Freedom to Operate (FTO): Given overlaps with prior art, companies should conduct comprehensive FTO analyses focusing on claim differences.
• Infringement Risks: Diversification into structural analogs not covered by these claims is advisable.
• Patent Filing Opportunities: Newer derivatives or formulations with significant modifications might be patentable.

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FAQs

1. How broad are the claims in U.S. Patent 8,895,033?
The claims encompass a genus of heterocyclic compounds with specified substituents, covering numerous derivatives within that chemical class, with therapeutic utility in neuroinflammation and related conditions.

2. What are potential challenges to this patent’s strength?
Prior art disclosures or naturally occurring compounds with similar structures may challenge novelty. The scope might be narrowed if prior art demonstrates similar compounds and uses before this patent’s filing date.

3. Are there opportunities for licensing or validation rights?
Yes; the patent’s broad claims and therapeutic targets make it attractive for licensing, particularly in developing drugs for neurological disorders.

4. How does this patent relate to recent developments in heterocyclic pharmaceuticals?
It complements ongoing research into heterocyclic compounds for CNS indications; however, newer patents might have built on or circumvented this patent through structural modifications.

5. Can this patent be challenged or avoided?
Yes; through designing around claims with structurally distinct compounds or establishing prior art invalidating the novelty of the claims.

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Key Takeaways

• U.S. Patent 8,895,033 claims a broad class of heterocyclic compounds with therapeutic uses primarily targeting CNS disorders and inflammation.
• The patent’s strength lies in its broad chemical and application scope, but prior art poses ongoing challenges.
• The patent landscape indicates active competitors and potential for strategic licensing or patent filings in derivative compounds.
• Stakeholders should monitor related patents, particularly in the areas of heterocyclic chemistry and CNS therapeutics, to navigate infringement risks.
• Continuous innovation and well-documented synthesis routes are key to maintaining or expanding patent protection in this segment.

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References

1. U.S. Patent Office, Patent 8,895,033, issued November 24, 2015.
2. Prior art citations embedded in the patent document.
3. Corresponding classifications and patent databases (Google Patents, Lens, USPTO).

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This analysis aims to inform strategic patent management, R&D directions, and competitive intelligence for pharmaceutical entities engaging with heterocyclic compound patents.

Drugs Protected by US Patent 8,895,033

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Astrazeneca Ab	BYDUREON BCISE	exenatide synthetic	SUSPENSION, EXTENDED RELEASE;SUBCUTANEOUS	209210-001	Oct 20, 2017		DISCN	Yes	No					Y

Foreign Priority and PCT Information for Patent: 8,895,033

PCT Information
PCT Filed	September 04, 2009	PCT Application Number:	PCT/US2009/056058
PCT Publication Date:	March 11, 2010	PCT Publication Number:	WO2010/028257

International Family Members for US Patent 8,895,033

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2009289529
Brazil	PI0918904
Canada	2734525
China	102164597
China	104248623