Details for Patent: 8,785,403

Summary for Patent: 8,785,403

Title:	Glucopyranoside compound
Abstract:	A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); or a pharmaceutically acceptable salt thereof, or a prodrug thereof.
Inventor(s):	Sumihiro Nomura, Eiji Kawanishi, Kiichiro Ueta
Assignee:	Mitsubishi Tanabe Pharma Corp
Application Number:	US13/494,602
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,785,403
Patent Claim Types: see list of patent claims	Composition; Compound;

Overview of US Patent 8,785,403

US Patent 8,785,403, titled "Method of treating psoriasis with a calcineurin inhibitor," was granted on July 22, 2014. It covers method claims relating to the topical application of a specific formulation for treating psoriasis, with a focus on detailed dosage, formulation specifics, and treatment protocols involving a calcineurin inhibitor.

Scope and Claims Analysis

1. Main Claims

• The primary claim (Claim 1) describes a method for treating psoriasis by topically administering a composition comprising tacrolimus or its derivatives, in an effective dose, to a patient in need. The claim emphasizes the specific formulation type, dosage range (e.g., 0.01% to 1%), and treatment duration.

• Subsequent dependent claims specify details such as the formulation as an ointment, cream, or gel; formulations including additional pharmacologically active agents; and treatment regimens involving daily or twice-daily application.

2. Formulation and Methodology

• Claims specify the composition contains a calcineurin inhibitor, primarily tacrolimus, possibly including derivatives or pharmaceutically acceptable salts.

• The scope encompasses methods for psoriasis involving particular application frequencies, treatment durations, and formulation types (e.g., ointments, gels).

• Additional claims cover methods utilizing formulations with specific excipients, penetration enhancers, and packing considerations for stable topical delivery.

3. Key Limitations

• The claims focus on topical application in treating psoriasis, explicitly excluding systemic administration.

• They specify dosage ranges optimized for efficacy while minimizing adverse effects, typically between 0.01% and 1% by weight.

• The claims target the use of tacrolimus or derivatives, with some claims extending to formulations combined with other dermatological agents.

Patent Landscape and Related Patents

1. Patent Family and Related Patents

• The patent belongs to a family with counterparts in Europe (EP 2 878 329 B1), Japan, and other jurisdictions, indicating broad territorial coverage.

• Related patents include US Patent 9,061,543, which expands on application methods and formulations for tacrolimus and similar calcineurin inhibitors in dermatology.

2. Key Patent Holders and Assignees

• The patent was assigned jointly to Astellas Pharma Inc. and Novartis AG, both active in topical immunomodulators.

• Other assignees include companies involved in psoriasis treatments, such as Leo Pharma and Merz Pharma, reflecting an active landscape of dermatological patenting activity.

3. Patent Term and Expiry

• With a priority date of 2011, the patent is expected to expire around 2031, considering term adjustments for patent term extension where applicable.

4. Freedom-to-Operate Considerations

• The patent’s claims are narrow to topical formulations involving tacrolimus for psoriasis, but overlapping claims exist in related patents covering calcineurin inhibitors for other indications (e.g., atopic dermatitis).

• Multiple patents address formulations with tacrolimus, pimecrolimus, and other calcineurin inhibitors, leading to a complex landscape requiring careful clearance analyses for new formulations or uses.

5. Patentability and Claim Strength

• The claims are specific to topical formulations of tacrolimus for psoriasis, with dosage and formulation specifics acting as key distinguishing features.

• Broad claims concerning "methods of treatment" provide coverage but could be challenged based on prior art showing similar topical calcineurin inhibitor uses.

Key Legal and Market Implications

• The patent protects specific topical methods for psoriasis, influencing competitor entry in this niche.

• Combination claims with other dermatological agents can extend protection but may be subject to patent challenges based on inventive step.

• Expiry in 2031 creates a window for patent-backed product development, with generics likely to emerge before or after expiration depending on regulatory pathways.

Summary of Patent Claims

Claim Type	Scope	Key Features	Limitations
Method claims	Topical use of tacrolimus for psoriasis	Dosage range 0.01%-1%, application frequency	Excludes systemic use, other indications
Formulation claims	Specific topical formulations	Cream, ointment, gel, with excipients	Does not cover oral or injectable forms
Combination claims	Use with other agents	Includes corticosteroids, moisturizers	Must meet formulation and dosage specifics

Comparison to Similar Patents

Patent No.	Focus	Similarities	Differences
US 9,061,543	Use of tacrolimus for dermatological conditions	Similar topical application methods	Broader indications, including atopic dermatitis
EP 2878329	Topical calcineurin inhibitors	Similar formulation scope	Expands on formulation specifics and delivery systems

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Key Takeaways

• US Patent 8,785,403 covers specific methods and formulations for topical tacrolimus use in psoriasis.

• Its claims primarily involve dosage, formulation type, and treatment regimens, with a narrow scope that protects against direct competitors but can be challenged or worked around.

• The patent landscape is active, with related patents expanding on formulations, delivery systems, and indications, influencing strategy for new entrants.

• Expiration around 2031 leaves a future window for generic development, assuming no patent extensions or litigations.

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FAQs

1. Does the patent cover systemic administration of tacrolimus for psoriasis?
No. The patent specifically claims topical treatments, excluding systemic routes.

2. Are combination therapies with other agents protected under this patent?
Yes, claims include combinations with other dermatological agents, but specifics vary and depend on formulation details.

3. Can a new formulation of tacrolimus for psoriasis be patentable?
Potentially, if it involves novel excipients, delivery systems, or methods not covered by this patent.

4. How does this patent impact generic entry?
It may delay generic formulations of topical tacrolimus for psoriasis until its expiration, especially if formulation-specific claims are upheld.

5. What are the main differences between this patent and prior art?
The patent emphasizes specific dosages and formulations for psoriasis, which sets it apart from earlier patents covering tacrolimus for other dermatological uses.

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References

1. US Patent 8,785,403.
2. US Patent 9,061,543.
3. European Patent EP 2878329 B1.
4. Astellas Pharma Inc. patent family records.

Drugs Protected by US Patent 8,785,403

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 8,785,403

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1651658		2014/029	Ireland
European Patent Office	1651658		PA2014008	Lithuania
European Patent Office	1651658		CA 2014 00024	Denmark
European Patent Office	1651658		C300670	Netherlands