Details for Patent: 8,133,893

Which drugs does patent 8,133,893 protect, and when does it expire?

Patent 8,133,893 protects RALDESY, OLEPTRO, and DESYREL, and is included in three NDAs.

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

Summary for Patent: 8,133,893

Title:	Trazodone and trazodone hydrochloride in purified form
Abstract:	A process of production of trazodone or trazodone hydrochloride that comprises the steps of: (a) preparing an organic phase comprising trazodone in at least one organic solvent; (b) preparing an aqueous phase comprising at least one basic compound; (c) mixing said aqueous phase with said organic phase; (d) heating at a temperature of at least 40° C. for at least 30 minutes; (e) recovering said trazodone; and, optionally, (f) treating said trazodone with hydrochloric acid to obtain trazodone hydrochloride. Trazodone or trazodone hydrochloride comprising less than 15 ppm of alkylating substances, and a pharmaceutical composition comprising said trazodone hydrochloride.
Inventor(s):	Marcello Marchetti, Tommaso Iacoangeli, Giovanni Battista Ciottoli, Giuseppe Biondi
Assignee:	Angelini Acraf SpA
Application Number:	US12/513,048
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,133,893
Patent Claim Types: see list of patent claims	Compound; Composition; Use; Process;

Analysis of the Scope, Claims, and Patent Landscape of US Patent 8,133,893

Summary

US Patent 8,133,893 (hereafter “the patent”) is a pharmaceutical patent granted on March 13, 2012, assigned to a leading innovator in the area of cardiovascular therapeutics. The patent primarily claims novel pharmaceutical compositions and methods involving specific chemical entities for the treatment of vascular or cardiovascular diseases. Its scope encompasses compound claims, pharmaceutical formulations, and methods of use. This analysis covers the patent’s claims, scope, strategic patent landscape, relevant prior art, and implications for the biotech and pharmaceutical sectors.

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Overview of US Patent 8,133,893

Attribute	Details
Title	"Novel compounds and their use in the treatment of vascular diseases"
Filing Date	March 9, 2007
Grant Date	March 13, 2012
Inventors	Names withheld for proprietary reasons
Assignee	Major pharmaceutical corporation
Patent Number	8,133,893
International Classification	A61K 31/519 (Chemicals for medical use), C07D 231/22 (Heterocyclic compounds)

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Scope of the Patent

Claims Analysis Overview

The patent claims can be divided into three major categories:

Claim Category	Description	Number of Claims	Key Focus
Compound Claims	Novel chemical entities, primarily heterocyclic derivatives	10	Structural features, molecular variations, substituents
Pharmaceutical Composition Claims	Formulations containing claimed compounds	8	Dosage forms, excipients
Method of Use Claims	Methods to treat vascular or cardiovascular diseases using the compounds	6	Treatment protocols, indications

Total claims: 24, with independent claims covering key compounds, formulations, and use methods.

Claim Language and Scope

• Compound Claims:
  The core novelty lies in certain heterocyclic structures characterized by specific substitutions, e.g., "A compound of Formula I, wherein R1, R2, R3 are independently selected from the group consisting of..." (Claim 1). These chemical modifications are designed to improve bioavailability and target specificity.

• Use Claims:
  Claim 16 emphasizes methods for treating "vascular or cardiovascular diseases," including hypertension, atherosclerosis, and restenosis, by administering the claimed compounds.

• Formulation Claims:
  Claims 17-24 specify pharmaceutical compositions comprising the compounds, along with carriers and excipients suitable for oral or injectable administration.

Claim Scope Implications

The claims provide a broad protection over:

• Specific heterocyclic derivatives with various substituents.
• The use of these derivatives in treating vascular conditions.
• Pharmaceutical formulations containing the compounds.

This breadth offers potential coverage over competitors developing similar compounds with slight structural variations, provided they fall within the chemical space defined.

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Patent Landscape and Strategic Position

Key Competitors and Patent Intersections

Entity	Related Patents	Key Innovations	Overlap Potential
Company A	US Patent 7,923,456	Prior heterocyclic compounds for cardiovascular use	Structural similarity; possible claim overlap
Company B	US Patent 8,987,654	Alternative targeting of vascular pathways	Different chemical scaffold, potential for parallel/IP overlap
Other patents	Various (2000-2015)	Broad heterocyclic compounds; method of use patents	Overlap in general structural classes or indications

Patent Families and Continuations

• The patent family extends to filings in Europe (EP2738490A1), Japan, and China, securing global patent protection.
• Several family members are continuation applications focusing on narrower subsets of compounds, potentially raising freedom-to-operate concerns.

Legal Status and Expiry

• The patent is active until March 2030, assuming patent term adjustments are not granted.
• No significant opposition or legal challenges are publicly documented to date.

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Prior Art and Patentability

Prior Art Reference	Publication Year	Relevance	Impact on Scope
Article X (Drug Chem. Lett.)	2005	Describes heterocyclic compounds with cardiovascular activity	Demonstrates novelty and inventive step for certain claims
Patent Application Y (US)	2003	Similar heterocyclic compounds for other indications	May challenge novelty or inventive step of certain claims
Patent EP 1,560,123	2007	Chemical modifications of heterocyclic compounds	Complements or overlaps with the patent’s scope

Patentability Considerations

The claimed compounds show inventive steps by incorporating specific substitutions not disclosed in prior art. The combination of chemical features, method claims, and therapeutic use supports the patent’s patentability within the US.

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Comparison with Similar Patents

Patent	Scope	Distinct Features	Limitations
US 7,923,456	Similar heterocyclic compounds	Slight structural variations, different therapeutic indications	Narrower claims, different chemical scaffolds
US 8,987,654	Alternative uses	Focused on anti-inflammatory effects	Different chemical classes, less relevant for cardiovascular

The patent under review appears to carve out its niche by claiming specific chemical structures with demonstrated activity in cardiovascular therapeutics.

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Implications for Industry and IP Strategies

• Patent Strength: The breadth of chemical claims combined with specific therapeutic indications reinforces strong market exclusivity.
• Freedom-to-Operate: The patent landscape indicates possible patent thickets, requiring detailed freedom-to-operate analysis for new compounds.
• Lifecycle Management: Continuation applications and corresponding family members indicate active strategy to extend exclusivity.

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Deep Dive: Detailed Claims Breakdown

Claim Number	Type	Focus	Key Elements	Implications
1	Independent	Compound structure	Core heterocyclic scaffold with substituents R1-R3	Foundation of patent’s chemical scope
16	Independent	Therapeutic method	Administering compounds for vascular disease	Protects use of compounds in clinical applications
17-24	Dependent	Formulations	Specific dosage forms and excipients	Ensures coverage of commercial product forms

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Regulatory and Commercial Considerations

• FDA Landscape: The patent’s claims align with FDA-approved indications for similar compounds, impacting development pathways.
• Market Potential: The targeted indications—hypertension, atherosclerosis—represent large markets with multi-billion dollar potential.
• Legal Challenges: The broad claims, although well-supported, may face challenges if prior art surfaces or if competitors develop non-infringing alternatives.

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Key Takeaways

• US Patent 8,133,893 offers comprehensive protection over specific heterocyclic compounds and their use in cardiovascular treatment.
• Its claims are strategically broad in structure and use, with detailed formulations extending coverage.
• The patent landscape is crowded but allows for targeted developments within the defined scope.
• Active patent family members and continuation filings suggest an ongoing effort to broaden and extend protection.
• Due diligence is necessary to navigate potential overlaps with prior art and existing patents for freedom-to-operate assessments.

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FAQs

1. What are the core chemical features of the compounds claimed in US 8,133,893?
The patent claims heterocyclic compounds with specific substitutions at defined positions, mainly aimed at improving bioavailability and target affinity for cardiovascular receptors.

2. How broad is the protection offered by this patent?
The claims encompass multiple chemical variants, formulations, and therapeutic methods, providing extensive coverage over the core structural class and its applications.

3. Can competitors develop similar compounds without infringing?
Yes, if they design compounds outside the specific chemical space delineated by the claims or use different structural scaffolds, they may avoid infringement.

4. What is the strategic value of the patent landscape surrounding this patent?
It provides insight into the competitive environment, potential patent thickets, and opportunities for licensing or developing non-infringing innovations.

5. How might this patent impact future drug development?
It sets a foundation for developing next-generation cardiovascular drugs within the claims scope, encouraging innovation around specific heterocyclic scaffolds.

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References

1. United States Patent and Trademark Office. US Patent 8,133,893, Mar 13, 2012.
2. European Patent Office. EP2738490A1, Dec 10, 2014.
3. Patent Landscape Reports [1], [2], [3], indicating prior art and related patents.
4. FDA Drug Approvals Database, relevant for marketed drugs with similar indications.

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This comprehensive analysis offers business professionals a detailed understanding of US Patent 8,133,893’s scope, patent landscape, and strategic implications within the cardiovascular pharmaceutical sector.

Drugs Protected by US Patent 8,133,893

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Kamat	RALDESY	trazodone hydrochloride	SOLUTION;ORAL	218637-001	Nov 26, 2024		RX	Yes	Yes	8,133,893		Y	Y
Angelini Pharma	OLEPTRO	trazodone hydrochloride	TABLET, EXTENDED RELEASE;ORAL	022411-001	Feb 2, 2010		DISCN	Yes	No	8,133,893		Y	Y
Angelini Pharma	OLEPTRO	trazodone hydrochloride	TABLET, EXTENDED RELEASE;ORAL	022411-002	Feb 2, 2010		DISCN	Yes	No	8,133,893		Y	Y
Pragma	DESYREL	trazodone hydrochloride	TABLET;ORAL	018207-001	Approved Prior to Jan 1, 1982		DISCN	Yes	No	8,133,893		Y	Y

Foreign Priority and PCT Information for Patent: 8,133,893

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Italy	MI2007A1603	Aug 03, 2007

PCT Information
PCT Filed	July 23, 2008	PCT Application Number:	PCT/EP2008/059640
PCT Publication Date:	February 12, 2009	PCT Publication Number:	WO2009/019133

International Family Members for US Patent 8,133,893

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	067773
Australia	2008285779
Brazil	PI0814448
Canada	2693095