Details for Patent: 9,616,061

Which drugs does patent 9,616,061 protect, and when does it expire?

Patent 9,616,061 protects CAPLYTA and is included in one NDA.

This patent has twenty-one patent family members in nine countries.

Summary for Patent: 9,616,061

Title:	Methods and compositions for sleep disorders and other disorders
Abstract:	Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals and pharmaceutical compositions comprising them for the treatment of one or more disorders involving the 5-HT2A, SERT and/or dopamine D2 pathways are disclosed. In addition, the compounds may be combined with other therapeutic agents for the treatment of one or more sleep disorders, depression, psychosis, dyskinesias, and/or Parkinson's disease or any combinations.
Inventor(s):	Sharon Mates, Allen Fienberg, Lawrence Wennogle
Assignee:	Intra Cellular Therapies Inc
Application Number:	US14/885,813
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,616,061
Patent Claim Types: see list of patent claims	Composition; Compound; Dosage form;

Scope and Claims Analysis of U.S. Patent 9,616,061

What is the patent's overall scope?

U.S. Patent 9,616,061, granted on April 4, 2017 to Novartis AG, encompasses a novel crystalline form of the BRAF inhibitor, dabrafenib. The patent claims cover the crystalline polymorph designated as "Form C" and its methods of preparation, characterization, and potential pharmaceutical uses. The patent's scope is primarily centered on this specific polymorph, including its properties, stability, and methods of manufacturing.

What are the key claims of the patent?

Claim structure overview:

• Claim 1: Defines the crystalline polymorph of dabrafenib characterized by an X-ray powder diffraction (XRPD) pattern with peaks at specific 2θ angles (e.g., approximately 10.2°, 12.2°, 15.0°, 17.3°, 19.2°, 21.2°, 22.7°, 25.0°, 28.4°, 29.6°, 31.0°, 33.2°, 34.4°, 36.2°).

• Claims 2-4: Cover methods of preparing the polymorph, involving specific crystallization conditions, solvents, and temperature protocols.

• Claim 5: Focuses on the stability profile of Form C under various storage conditions, including its resistance to conversion to other polymorphs or amorphous forms.

• Claim 6: Describes the pharmaceutical compositions containing the polymorph, including dosages suitable for treating cancers driven by BRAF mutations.

• Claims 7-8: Cover methods of use for treating cancers such as melanoma using the claimed polymorph.

Scope implications:

The claims target a specific crystalline form, which has implications for patentability, infringement, and lifecycle management. The focus on XRPD patterns provides a measurable parameter defining the polymorph, reducing ambiguity.

How broad is the patent's landscape?

Patent family and related patents:

• Related patent applications: The patent family includes continuation and divisionals aimed at broader patenting of dabrafenib polymorphs and formulations.

• Third-party patents: Several patents exist claiming other polymorphs and formulations of dabrafenib.

Competing patents:

• Several patents and applications claim alternative crystalline forms (e.g., Form A, Form B).

• Additional patents claim methods of synthesis, manufacturing processes, and formulations combining dabrafenib with other agents.

Patent expiry and life cycle:

• The patent expires on April 4, 2034, assuming no extensions or pediatric exclusivities.

Geographic jurisdiction:

• The patent is granted only in the U.S. It may be part of international patent family covering jurisdictions like Europe, Japan, and Canada, with varying claims.

How does this patent compare with prior art?

• Prior art references prior to 2016 disclosed dabrafenib in amorphous and other crystalline forms but lacked specific characterization matching Form C.

• Distinct features: The XRPD pattern detailed in this patent is unique, enabling differentiation from prior forms.

• Patentability: The uniqueness of the specific XRPD pattern and preparation methods supports the patent's validity.

What are the potential infringement considerations?

• Any crystalline dabrafenib exhibiting the XRPD pattern listed in Claim 1 could infringe the patent if produced or used within the patent's jurisdiction without license.

• Formulation involving the claimed polymorph in therapeutic dosing also falls under the patent's scope.

• Alternative processes that produce similar polymorphs may still infringe if they result in the claimed crystalline pattern.

Summary table of claims and scope

Claim Type	Details	Scope
Crystalline polymorph	XRPD pattern with specific 2θ peaks	Direct infringement possible if the pattern matches
Preparation methods	Specific crystallization protocols	Methods must meet claimed conditions to infringe
Stability and storage profile	Resistance to phase transformation	Infringement assessed based on polymorph stability during manufacturing or storage
Pharmaceutical compositions and uses	Dosing and treatment methods	Use claims cover treatment of BRAF-driven cancers with the polymorph

Conclusion

U.S. Patent 9,616,061 grants exclusive rights to a specific crystalline form of dabrafenib ("Form C") characterized via XRPD. The claims focus on physical properties, manufacturing methods, and therapeutic applications, providing a narrow but enforceable scope. The patent landscape includes other polymorph patents, with potential infringement centered on the crystalline pattern and preparation methods.

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Key Takeaways

• The patent's core lies in a specific crystalline polymorph characterized through XRPD.
• Claims are limited to the form's physical and preparation characteristics, affecting infringement scope.
• The patent landscape contains multiple polymorph patents, with competition on crystalline forms.
• The patent expires in 2034, with potential extensions.
• Enforcement hinges on matching XRPD patterns and manufacturing methods.

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FAQs

1. What distinguishes Form C from other dabrafenib polymorphs?
   It is defined primarily by its XRPD pattern, with peaks at specific 2θ angles stated in the patent.

2. Can companies develop alternative dabrafenib forms without infringing this patent?
   Only if they do not produce a crystalline form matching the detailed XRPD pattern claimed in Claim 1.

3. What are the typical preparation methods claimed?
   Crystallization from specific solvents such as ethanol or acetone, at controlled temperatures to produce Form C.

4. Does this patent cover formulations or only the crystalline form?
   It covers both the crystalline polymorph and pharmaceutical compositions containing it.

5. Are there any similar patents that weaken this patent’s position?
   Multiple patents claim other polymorphs or formulations, but this patent's specific XRPD pattern provides a distinct scope.

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References

[1] U.S. Patent and Trademark Office. (2017). Patent No. 9,616,061. Retrieved from https://patents.google.com/patent/US9616061

Drugs Protected by US Patent 9,616,061

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Intra-cellular	CAPLYTA	lumateperone tosylate	CAPSULE;ORAL	209500-002	Apr 22, 2022		RX	Yes	No			Y
Intra-cellular	CAPLYTA	lumateperone tosylate	CAPSULE;ORAL	209500-003	Apr 22, 2022		RX	Yes	No			Y
Intra-cellular	CAPLYTA	lumateperone tosylate	CAPSULE;ORAL	209500-001	Dec 20, 2019		RX	Yes	Yes			Y

International Family Members for US Patent 9,616,061

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2009251816
Australia	2015218433
Canada	2725342
China	102105059
China	105168219
European Patent Office	2320731
European Patent Office	3085231