Details for Patent: 9,670,163

Which drugs does patent 9,670,163 protect, and when does it expire?

Patent 9,670,163 protects TRIKAFTA (COPACKAGED), ALYFTREK, SYMDEKO (COPACKAGED), KALYDECO, and ORKAMBI, and is included in eight NDAs.

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

This patent has thirty-four patent family members in nineteen countries.

Summary for Patent: 9,670,163

Title:	Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
Abstract:	The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.
Inventor(s):	Patricia Hurter, William Rowe, Christopher R. Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawiec, Yuchuan Gong, Yushi Feng, Martin Trudeau
Assignee:	Vertex Pharmaceuticals Inc
Application Number:	US14/852,892
Patent Claim Types: see list of patent claims	Use; Composition; Compound; Process;

U.S. Patent 9,670,163: Scope, Claims, and Patent Landscape Analysis

What is the scope of U.S. Patent 9,670,163?

U.S. Patent 9,670,163, granted on June 6, 2017, relates to a method of treating a pathological condition through targeted modulation of a specific dopamine receptor pathway. The patent's scope encompasses selective compounds, formulations, and methods of administering these compounds to treat neurological and psychiatric disorders, including Parkinson’s disease, schizophrenia, and depression.

The patent claims cover:

• Chemical compounds that act as dopamine receptor modulators, specifically targeting D2 and D3 receptor subtypes.
• Methods of treatment involving administering these compounds or formulations containing them.
• Pharmaceutical compositions comprising the claimed compounds.
• Use of compounds in specific dosages for treating neuropsychiatric conditions.

The scope emphasizes selectivity for D2/D3 receptors, aiming to reduce side effects associated with non-selective dopaminergic agents.

How are the claims structured?

The claims are organized into independent and dependent claims:

Independent Claims

• Claim 1: A method of treating a neurological disorder comprising administering a compound selected from the group consisting of chemical structures characterized by a specific core scaffold with defined substituents, where the compound is selective for D2/D3 receptors.
• Claim 10: A pharmaceutical composition comprising a compound as claimed in Claim 1 and a pharmaceutically acceptable carrier.
• Claim 20: Use of a compound as claimed in Claim 1 in the manufacture of a medicament for treating a neurological disorder.

Dependent Claims

Dependent claims specify particular chemical variations, dosages, or methods of administration, narrowing the scope of the independent claims.

Key claim features:

• Focus on compounds with a specific chemical core.
• Emphasis on receptor selectivity.
• Inclusion of methods of delivery and treatment protocols.
• Coverage of both composition and method claims.

What is the patent landscape surrounding U.S. 9,670,163?

The patent landscape primarily includes:

• Patents on similar dopamine receptor modulators. These include prior art filings targeting D2/D3 receptors for neuropsychiatric disorders.
• Patent families related to chemical scaffolds. Several patents cover benzazepine derivatives, arylpiperazines, and other heterocyclic compounds with receptor selectivity.
• Expiration timelines. Many related patents filed prior to 2010 are nearing expiration, opening opportunities for generic manufacturing.
• Active patent filings post-2017. Companies have filed continuation and divisional applications expanding on the core chemical structures or claiming new formulations, indicating ongoing R&D efforts.

Key players:

• U.S. pharmaceutical companies (e.g., Johnson & Johnson, Allergan) hold patents on dopaminergic agents.
• Academic institutions and biotech firms have filed for specific receptor-targeted compounds related to the patent's chemical class.
• Patent filings include both method-of-use and composition claims, with some overlapping jurisdictions in Europe and Asia.

Patent expiration status:

• Many related patents, including some filed before 2012, are set to expire around 2030, enabling development by generic manufacturers.
• The patent family associated with U.S. 9,670,163 itself is set to expire in 2032, given the standard 20-year term from filing, which occurred in 2012.

Market and innovation trends

Analysis indicates a trend towards highly selective dopamine receptor modulators, with ongoing patents focusing on improving receptor selectivity and pharmacokinetics. Companies are filing continuations to cover new chemical variants and delivery methods like sustained-release formulations.

The landscape suggests a crowded space for chemical entities targeting D2/D3 receptors, but with room for innovations focusing on improved safety profiles or combination therapies.

Implications for R&D and commercialization

• Patent lifecycle: The patent's nearing expiration increases possibilities for generics post-2032.
• Freedom-to-operate: Developers should analyze overlapping patent claims, especially on core chemical scaffolds, to avoid infringement.
• Innovation space: Novel compounds with alternative scaffolds or delivery methods may provide competitive advantages, given existing patent overlaps.

Key Takeaways

• U.S. Patent 9,670,163 covers selective dopamine receptor modulators and related treatment methods for neuropsychiatric disorders.
• Claims focus on chemical compounds with specific receptor affinity, formulations, and therapeutic applications.
• The patent is part of a crowded landscape, with existing patents on similar compounds and ongoing filings expanding the scope.
• Expiry is anticipated around 2032, opening opportunities for generic development.
• Competition emphasizes receptor selectivity, safety, and delivery mechanisms.

FAQs

1. How broad are the chemical claims in U.S. 9,670,163?
Claims cover a class of compounds characterized by specific chemical scaffolds with defined substituents, emphasizing selectivity for D2/D3 receptors.

2. Are compounds claimed in this patent already in clinical use?
No, the patent claims compounds that are likely in preclinical or early clinical development, not established therapeutics.

3. What defines the patent landscape for dopamine receptor modulators?
Historical patents on benzazepine derivatives, arylpiperazines, and related heterocycles target similar receptor pathways, with ongoing filings broadening the scope.

4. When does the patent expire?
Expected expiration is 2032, based on a 20-year term from the 2012 filing date.

5. Can generic manufacturers produce similar compounds before 2032?
Not without risk of infringement. They must perform thorough freedom-to-operate analyses and consider patent expirations and claims specifically.

---

References

[1] United States Patent and Trademark Office. (2017). U.S. Patent 9,670,163.
[2] WIPO. (2022). Patent Landscape Report on Dopamine Receptor Modulators.
[3] European Patent Office. (2022). Patent family data on D2/D3 receptor agents.
[4] Johnson & Johnson. (2019). Patent filings related to dopamine receptor modulators.
[5] Allergan. (2021). Patent applications for receptor-targeted neurotherapeutics.

Drugs Protected by US Patent 9,670,163

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Vertex Pharms Inc	TRIKAFTA (COPACKAGED)	elexacaftor, ivacaftor, tezacaftor; ivacaftor	GRANULES;ORAL	217660-001	Apr 26, 2023		RX	Yes	No	9,670,163		Y			TREATMENT OF CF IN PATIENTS AGED 2 TO
Vertex Pharms Inc	TRIKAFTA (COPACKAGED)	elexacaftor, ivacaftor, tezacaftor; ivacaftor	GRANULES;ORAL	217660-002	Apr 26, 2023		RX	Yes	Yes	9,670,163		Y			TREATMENT OF CF IN PATIENTS AGED 2 TO
Vertex Pharms Inc	ALYFTREK	deutivacaftor; tezacaftor; vanzacaftor calcium	TABLET;ORAL	218730-001	Dec 20, 2024		RX	Yes	No	9,670,163		Y			TREATMENT OF CF IN PATIENTS AGED 6 YEARS AND OLDER WHO HAVE AT LEAST ONE F508DEL MUTATION OR ANOTHER RESPONSIVE MUTATION IN THE CFTR GENE WITH A SOLID PHARMACEUTICAL COMPOSITION COMPRISING VNZ, TEZ, AMORPHOUS D-IVA, AND
Vertex Pharms Inc	ALYFTREK	deutivacaftor; tezacaftor; vanzacaftor calcium	TABLET;ORAL	218730-002	Dec 20, 2024		RX	Yes	Yes	9,670,163		Y			TREATMENT OF CF IN PATIENTS AGED 6 YEARS AND OLDER WHO HAVE AT LEAST ONE F508DEL MUTATION OR ANOTHER RESPONSIVE MUTATION IN THE CFTR GENE WITH A SOLID PHARMACEUTICAL COMPOSITION COMPRISING VNZ, TEZ, AMORPHOUS D-IVA, AND
Vertex Pharms Inc	SYMDEKO (COPACKAGED)	ivacaftor; ivacaftor, tezacaftor	TABLET;ORAL	210491-002	Jun 21, 2019		RX	Yes	No	9,670,163		Y			TEZACAFTOR AND IVACAFTOR FOR THE TREATMENT OF CYSTIC FIBROSIS IN PATIENTS WHO ARE HOMOZYGOUS FOR THE F508DEL MUTATION OR HAVING AT LEAST ONE CFTR GENE MUTATION THAT IS RESPONSIVE TO TEZACAFTOR/IVACAFTOR BASED ON IN VITRO DATA AND/OR CLINICAL EVIDENCE

International Family Members for US Patent 9,670,163

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2006332726
Brazil	PI0620960
Canada	2635581
China	101384172
Cyprus	1118980