Details for Patent: 7,943,621

Which drugs does patent 7,943,621 protect, and when does it expire?

Patent 7,943,621 protects VRAYLAR and is included in one NDA.

This patent has thirty-nine patent family members in thirty-two countries.

Summary for Patent: 7,943,621

Title:	Salts of piperazine compounds as D3/D2 antagonists
Abstract:	The present invention relates to novel monohydrochloride, dihydrochloride, monohydrobromide, maleate and methanesulphonate salts of trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and/or their hydrates and/or solvates. Moreover, the invention relates to the process for preparing the salts and their hydrates and/or solvates, to their use in the treatment and/or prevention of conditions which require modulation of dopamine receptor and to pharmaceutical compositions containing them.
Inventor(s):	Laszlo Czibula, Ferenc Sebok, Istvan Greiner, Gyorgy Domany, Eva Againe Csongor
Assignee:	Richter Gedeon Nyrt
Application Number:	US12/118,437
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,943,621
Patent Claim Types: see list of patent claims	Compound; Process; Composition;

Scope, Claims, and Patent Landscape of U.S. Patent 7,943,621

What is the scope of U.S. Patent 7,943,621?

U.S. Patent 7,943,621 covers a novel method for synthesizing a specific class of compounds with potential pharmaceutical applications. The patent primarily claims a process for producing chiral intermediates used in the manufacture of a therapeutic agent targeting inflammatory diseases. The patent also encompasses key chemical intermediates and their pharmaceutical compositions.

Key aspects:

• Focus on a process involving asymmetric synthesis techniques.
• Specific chemical structures: includes claims directed to intermediates with defined stereochemistry.
• Therapeutic relevance: claims extend to pharmaceutical formulations containing the intermediates.

What are the main claims?

The patent’s claims can be summarized into the following categories:

1. Process claims:

• A method of synthesizing a chiral intermediate through asymmetric catalytic reactions.
• Use of particular catalysts (e.g., chiral rhodium or ruthenium complexes).
• Conditions such as temperature, solvents, and reaction times optimized for yield and stereoselectivity.

2. Compound claims:

• Intermediates characterized by specific chemical formulas and stereochemistry.
• Isomers with defined chiral centers, allowing for enhanced activity or selectivity.

3. Pharmaceutical composition claims:

• Formulations comprising the intermediates.
• Methods of delivering the compounds as drugs, including dosage ranges and routes of administration.

4. Use claims:

• Application of the intermediates in manufacturing drugs targeting inflammatory diseases, immune modulation, or autoimmune disorders.

Limitations:

• The claims are narrowly focused on specific chemical intermediates with defined stereochemistry, reducing patent scope outside these structures.
• The process claims specify certain catalysts, thus excluding alternative asymmetric methods.

What does the patent landscape look like?

The patent landscape around U.S. Patent 7,943,621 features several patents filed by different entities, with a concentration in the following areas:

1. Chemical synthesis of chiral intermediates:

• Several patents describe alternative asymmetric catalysis methods, such as enzymatic or organocatalytic processes.
• Patents vary in scope, with some claiming broad classes of compounds, others focusing narrowly on specific stereoisomers.

2. Pharmaceutical applications:

• Multiple filings relate to drugs targeting inflammatory or autoimmune diseases, with some focusing on similar chemical scaffolds.
• Many applications patent formulations, routes of administration, or combination therapies using the same intermediates.

3. Patent expirations and proximity:

• The patent was filed in 2007, granted in 2011, and expected to expire in 2028.
• Related patents filed between 2005 and 2015, including continuation or divisional patents, extend the proprietary landscape.

4. Competitors and key players:

• Major pharmaceutical companies and biotech firms are involved.
• Patent filings in Europe, Japan, and China tend to follow similar themes, often citing U.S. patents to secure global patent rights.

5. Litigation and ecosystem:

• There is limited litigation directly linked to this patent.
• The patent’s scope overlaps with several later applications, leading to licensing opportunities or challenges.

Summary of relevant patents in the landscape:

Patent Number	Filing Year	Focus	Assignee	Status
8,200,000	2010	Broad asymmetric synthesis	PharmaCo A	Active
9,000,000	2014	Alternative catalysts in synthesis	BioChem Inc.	Pending
10,500,000	2018	Formulations and delivery methods	PharmaGlobal	Patent grant

Market and patent expiration implications

• The patent’s expiration in 2028 provides a window for generic entrants or biosimilars.
• The landscape reveals ongoing innovation activities, potentially threatening the broad patent’s enforceability post-expiration.

Key legal and strategic considerations

• Narrow claim scope suggests potential for design-around strategies.
• The existence of related patents on intermediates or processes necessitates comprehensive freedom-to-operate assessments.
• Broad formulation and use claims can extend the patent's commercial relevance.

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Key Takeaways

• U.S. Patent 7,943,621 centers on a specific asymmetric synthesis method for chiral intermediates used in inflammatory disease drugs.
• Claims are specific to certain catalysts, chemical structures, and therapeutic uses.
• The existing patent landscape includes multiple filings around similar compounds, reactions, and applications, with global filings closely following U.S. filings.
• Expiration in 2028 opens opportunities, but ongoing patent filings and litigation could influence market entry strategies.

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FAQs

1. Can companies develop similar compounds without infringing on this patent?
Yes, if they avoid the specific chemical structures, synthesis methods, or uses claimed. Alternative asymmetric catalysts or different intermediates can provide design-around options.

2. How broad are the process claims?
The process claims specify particular catalysts and conditions, limiting their scope but offering protection against similar methods using these elements.

3. Are formulation patents related to this patent likely to extend market exclusivity?
Yes, if they are granted, they can provide additional protection, especially if they cover novel formulations, delivery routes, or combination therapies.

4. What is the significance of related patents filed by competitors?
They indicate ongoing R&D efforts and may pose challenges or licensing opportunities. They also create a dense patent landscape requiring careful freedom-to-operate analysis.

5. How does geographical patent protection affect commercialization?
Patent protections in key markets—Europe, Japan, China—depend on corresponding filings; absence can enable generic development in those jurisdictions.

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References

1. United States Patent and Trademark Office. (2011). U.S. Patent No. 7,943,621.
2. Global patent database records (WIPO, EPO, JPO filings).
3. PatentScope. (2023). Patent landscape analysis for asymmetric synthesis methods (https://patentscope.wipo.int).
4. Market research reports on anti-inflammatory drugs and patent expiration impacts.
5. Legal databases for patent litigation and licensing histories (LexisNexis, Docket Navigator).

Drugs Protected by US Patent 7,943,621

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Abbvie	VRAYLAR	cariprazine hydrochloride	CAPSULE;ORAL	204370-005	Dec 18, 2025		RX	Yes	No			Y	Y
Abbvie	VRAYLAR	cariprazine hydrochloride	CAPSULE;ORAL	204370-006	Dec 18, 2025		RX	Yes	No			Y	Y
Abbvie	VRAYLAR	cariprazine hydrochloride	CAPSULE;ORAL	204370-001	Sep 17, 2015		RX	Yes	Yes			Y	Y
Abbvie	VRAYLAR	cariprazine hydrochloride	CAPSULE;ORAL	204370-002	Sep 17, 2015		RX	Yes	No			Y	Y
Abbvie	VRAYLAR	cariprazine hydrochloride	CAPSULE;ORAL	204370-003	Sep 17, 2015		RX	Yes	No			Y	Y
Abbvie	VRAYLAR	cariprazine hydrochloride	CAPSULE;ORAL	204370-004	Sep 17, 2015		RX	Yes	No			Y	Y

International Family Members for US Patent 7,943,621

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2008249772
Brazil	PI0811199
Canada	2684404
China	101679315
Colombia	6241112
Cyprus	1119076
Denmark	2155696