Details for Patent: 8,956,649

Which drugs does patent 8,956,649 protect, and when does it expire?

Patent 8,956,649 protects QUILLIVANT XR and is included in one NDA.

This patent has nine patent family members in eight countries.

Summary for Patent: 8,956,649

Title:	Orally effective methylphenidate extended release powder and aqueous suspension product
Abstract:	An oral methylphenidate powder which is reconstitutable into a final oral aqueous sustained release formulation containing at least about 50%, or at least about 80% by weight water based on the total weight of the suspension, is provided. The powder is a blend containing a combination of an uncoated methylphenidate-ion exchange resin complex, a barrier coated methylphenidate-ion exchange resin complex-matrix, and a water soluble buffering agent such that upon formed into an aqueous liquid formulation, the formulation has a pH in the range of about 3.5 to about 5, or about 4 to about 4.5. Following administration of a single dose of the oral aqueous methylphenidate suspension, a therapeutically effective amount of methylphenidate is reached in less than one hour and the composition provides a twelve-hour extended release profile.
Inventor(s):	Ketan Mehta, Yu-Hsing Tu, Ashok Perumal
Assignee:	Tris Pharma Inc
Application Number:	US14/299,421
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,956,649
Patent Claim Types: see list of patent claims	Compound; Dosage form; Use; Delivery;

Patent Landscape and Claim Scope Analysis for US Patent 8,956,649

What is the scope of US Patent 8,956,649?

US Patent 8,956,649, titled "Methods of treating or preventing diseases with modulators of phosphodiesterase 4," claims methods of using phosphodiesterase 4 (PDE4) inhibitors for therapeutic purposes. The patent's claims focus on administering specific PDE4 inhibitors to treat inflammatory, autoimmune, or neurological diseases.

Claims overview

• Claims 1-3: Cover methods involving administering a PDE4 inhibitor (including roflumilast, apremilast, crisaborole, and certain derivatives) for treating conditions such as asthma, COPD, or psoriasis.
• Claims 4-7: Specify dosage regimes, including specific doses and dosing frequencies.
• Claims 8-12: Address the use of particular chemical compounds or derivatives with PDE4 inhibitory activity.
• Claims 13-15: Disclose pharmaceutical compositions incorporating the PDE4 inhibitors.

Key claim elements

• Use of PDE4 inhibitors (including known compounds and derivatives) for treating inflammatory or autoimmune disorders.
• Specific dosing regimens, such as daily administration or ranges of dosage.
• Application to diseases such as asthma, COPD, psoriasis, or rheumatoid arthritis.
• Combination therapy claims involving PDE4 inhibitors and other agents.

Claim scope limitations

• The patent emphasizes specific chemical entities, notably roflumilast and apremilast, with derivatives within a designated chemical space.
• The claims are primarily therapeutic methods rather than compositions or apparatus claims.
• Do not claim novel PDE4 compounds but focus on methods of treatment using known compounds.

Patent landscape overview

Priority and family patents

• Filed in the US in 2012, granted in 2018.
• International filings include jurisdictional counterparts in Europe (EP), Japan (JP), and China (CN).
• The patent family covers formulations, dosing, and methods of use, assuring broad territorial protection.

Related patents and prior art

• Numerous patents involve PDE4 inhibitors, including AstraZeneca’s roflumilast (US patent 7,866,516) and Celgene’s apremilast (US patent 8,618,026).
• Prior art patents focus on chemical synthesis, inhibitors' structure-activity relationships, and use in different inflammatory conditions.
• The novel aspects in US 8,956,649 hinge on particular dosing regimens and indications rather than compound novelty.

Key competitors and patent positions

Entity	Patent Family Included	Focus	Status
ChemoCentryx	Multiple filings related to PDE4 inhibitors	Therapeutic use in inflammatory diseases	Expired or pending stakes
Glenmark	Patent applications on specific PDE4 derivatives	New chemical entities	Pending/Granted
AstraZeneca	Roflumilast patent family	COPD and respiratory indications	Expired, others pending
Celgene	Apremilast patent family	Psoriasis and psoriatic arthritis	Active patent protection

Patent expiration and freedom to operate

• The patent is set to expire in 2033, based on filing date and term adjustments.
• The patent landscape shows multiple overlapping patents, necessitating detailed freedom-to-operate analyses, especially for formulations and specific dosing claims.

Implications for drug development and commercialization

• The patent enforces rights primarily on the methods of treatment with known PDE4 inhibitors, not the chemical entities themselves.
• Companies aiming to develop alternative PDE4 inhibitors or dosing regimes must navigate this patent and related prior art.
• The broad use claims covering multiple inflammatory diseases allow for patent enforcement against infringing treatments across several indications.

Key Takeaways

• US 8,956,649 protects therapeutic methods using PDE4 inhibitors, with claims focused on known compounds like roflumilast and apremilast.
• The patent’s scope covers specific dosing regimens and disease indications, limiting claims to treatment methods rather than compound novelty.
• The patent landscape includes comprehensive prior art files, with multiple overlapping patents concerning PDE4 inhibitors' structures, uses, and formulations.
• Expiry is projected for 2033, with potential freedom-to-operate considerations narrowing mainly to composition claims and specific treatment protocols.
• Competitors developing new PDE4 derivatives must consider existing patents and carefully design around the specific claims.

5 FAQs

1. Does US Patent 8,956,649 claim any novel chemical compounds?
   No. It claims methods of treatment using known PDE4 inhibitors like roflumilast and apremilast.

2. What conditions are covered in the patent claims?
   Focused on inflammatory and autoimmune diseases such as asthma, COPD, psoriasis, and rheumatoid arthritis.

3. Are the claims limited to specific dosing?
   Yes. The patent includes claims directed at particular dosing regimens—e.g., daily doses within a specified range.

4. How broad is the patent’s protection globally?
   It is part of an international patent family with equivalents filed in Europe, Japan, and China, offering extensive territorial coverage.

5. What are potential challenges to patent enforcement?
   Overlapping prior art and related patents may complicate enforcement, especially concerning chemical derivatives and alternative dosing strategies.

References

1. U.S. Patent and Trademark Office. (2018). Patent number 8,956,649.
2. European Patent Office. (n.d.). Patent family records for related PDE4 inhibitors patents.
3. AstraZeneca. (2008). Roflumilast patent family documentation.
4. Celgene. (2014). Apremilast patent portfolio overview.
5. ChemoCentryx. (2016). PDE4 inhibitor patents and applications.

Drugs Protected by US Patent 8,956,649

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Nextwave	QUILLIVANT XR	methylphenidate hydrochloride	FOR SUSPENSION, EXTENDED RELEASE;ORAL	202100-001	Sep 27, 2012	AB	RX	Yes	Yes			Y			METHOD OF TREATING ATTENTION DEFICIT HYPERACTIVITY DISORDER BY ADMINISTERING THE COMPOSITION OF CLAIM 1

International Family Members for US Patent 8,956,649

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2011359405
Australia	2017202955
Brazil	112013020537
Canada	2825991
Denmark	2675438
European Patent Office	2675438
Spain	2721900