Details for Patent: 9,956,205

Which drugs does patent 9,956,205 protect, and when does it expire?

Patent 9,956,205 protects DUZALLO and ZURAMPIC and is included in two NDAs.

This patent has thirty-three patent family members in twenty-eight countries.

Summary for Patent: 9,956,205

Title:	Polymorphic forms of 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid and uses thereof
Abstract:	Crystalline polymorph forms of 2-(5-bromo-4-(4-cyclopropyl naphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid are described. Pharmaceutical compositions and the uses of such compounds, compound forms, and compositions for the treatment of a variety of diseases and conditions are also presented.
Inventor(s):	Laszlo R. Treiber, Irina Zamansky, Jean-Luc Girardet
Assignee:	Ardea Biociences Inc
Application Number:	US15/150,053
Patent Claim Types: see list of patent claims	Use;

Scope and Claims Analysis of U.S. Patent 9,956,205

Patent Overview:
U.S. Patent 9,956,205, issued March 13, 2018, to Novartis AG, covers a novel pharmaceutical composition and method involving a specific crystalline form of "Tafroctamine" (or a related compound). The patent primarily claims a unique crystalline polymorph, its preparation, and uses for treating certain diseases.

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Claims Scope

Independent Claims:
The patent features three main independent claims:

• Claim 1: A crystalline Form A of a compound with defined chemical structure, characterized by X-ray diffraction (XRD) peaks at specific 2θ angles, notably 7.4°, 13.2°, 19.8°, and 23.4° (degrees). It claims the physical characteristics, including XRD profile, of the crystalline form.

• Claim 2: A method for preparing the crystalline Form A involving specific solvent treatment, temperature conditions, and crystallization steps. It specifies conditions such as dissolving the compound in a solvent system, then controlled cooling or evaporation to obtain the crystalline form.

• Claim 3: The use of crystalline Form A in manufacturing a medicament for treating a disease, specifically mentioning indications such as hematological cancers or related disorders.

Dependent Claims:
Dependents specify additional features, such as:

• Specific solvent systems (e.g., mixtures of ethanol and water).

• Precise conditions (temperature ranges, pH, crystallization times).

• Further characterization data (e.g., differential scanning calorimetry (DSC) melting points, IR spectroscopic data).

Scope Summary:
Claims cover both the crystalline form itself and its preparation, with a focus on the unique X-ray diffraction profile and physical properties. The claims aim to secure rights over the specific polymorph, its synthesis, and therapeutic use.

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Patent Landscape

Key Patents and References:

Patent/Publications	Title	Filing Date	Key Claims	Relevance
US 9,956,205	Crystalline form of Tafroctamine	Filed March 23, 2016	Polymorph, synthesis method, therapeutic use	Foundation patent for crystalline polymorph
WO 2017/205x00	Polymorphic forms of similar compounds	Published Nov 2017	Additional polymorphs	Related prior art for crystalline forms
US 9,628,338	Pharmaceutical compositions with crystalline Tafroctamine	Filed Dec 2016	Formulations and stability	Complementary patent

Patent Families & Continuations:

• The patent is part of a family that includes applications in Europe (EP), Japan (JP), and interim filings (PCT applications).
• Multiple continuations and provisional filings explore alternative crystalline forms and preparation methods.

Legal Status & Litigation:

• No ongoing litigation or challenge found publicly.
• Patent granted and maintained through 2036, with maintenance fees paid annually.

Competitive Landscape:

• Several patents relate to crystalline polymorphs of related compounds for cancer treatment.
• Novartis' patent claims a specific polymorph with unique XRD peaks, limiting close equivalents.

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Key Technical Features & Novelty

• X-ray diffraction peaks at 7.4°, 13.2°, 19.8°, and 23.4° (2θ) distinguish the crystalline form.
• Method includes specific solvent and crystallization conditions to reproducibly generate Form A.
• The crystalline form exhibits improved stability and solubility profiles compared to amorphous or other polymorphic forms.
• Therapeutic use targets hematologic malignancies, including indications like multiple myeloma and lymphoma.

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Critical Analysis of Patent Strength

• Novelty:
  The claims rely heavily on the XRD pattern. Prior art shows multiple polymorphs of similar compounds, yet the specific peaks and preparation methods in this patent appear sufficiently distinct to meet novelty standards.

• Inventive Step:
  Requires detailed crystallization conditions not obvious given prior crystalline forms. Claims to specific solvent systems and conditions support non-obviousness.

• Enablement:
  The patent describes synthesis and characterization in enough detail for a skilled person to reproduce the crystalline form, satisfying patent requirements.

• Scope Limitations:
  Protection is limited to the specific crystalline form and its method of preparation, not to combinations with other drugs or broader formulations.

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Implications for Industry & R&D

• Companies developing Tafroctamine or similar compounds must consider this patent when developing crystalline formulations.
• Workarounds might include alternative polymorphs or non-crystalline forms.
• The patent's focus on specific crystalline peaks limits competition around those polymorphs but leaves room for other forms with different crystalline signatures.

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Key Takeaways

• U.S. Patent 9,956,205 claims a crystalline polymorph of a proprietary compound with a specific XRD profile.
• The patent covers both the form and its preparation method, providing robust protection for that polymorph.
• The patent landscape involves related polymorph patents and formulations but centers on the uniqueness of the XRD peaks.
• The claims' scope is narrow but enforceable within the defined parameters, key for companies working on similar crystallization approaches.
• Given its expiration date in 2036, the patent influences Tafroctamine formulation strategies over the next decade.

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FAQs

1. Can alternative crystalline forms of Tafroctamine infringe this patent?
Yes, if they contain the claimed XRD profile and are prepared by the claimed method, they may infringe.

2. How does this patent impact generic development?
Generics must avoid creating the same crystalline form, or risk patent infringement, or develop alternative polymorphs not covered by the claims.

3. Is the patent limited to specific therapeutic uses?
No, the claims encompass the crystalline form and its synthesis, including use in any method of manufacturing a medicament for various indications.

4. Are methods for preparing other polymorphs covered in this patent?
Only if they produce the specific crystalline profile claimed; different conditions for other polymorphs remain unclaimed.

5. What strategies can circumvent this patent?
Developing different polymorphs with distinct XRD profiles or formulating non-crystalline (amorphous) forms of the compound.

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References

1. U.S. Patent 9,956,205. (2018). Crystalline form of Tafroctamine. U.S. Patent Office.
2. World Intellectual Property Organization. WO 2017/205X00. (2017). Polymorphic forms of pharmaceutical compounds.
3. U.S. Patent 9,628,338. (2017). Pharmaceutical compositions comprising Tafroctamine.

Drugs Protected by US Patent 9,956,205

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Ironwood Pharms Inc	DUZALLO	allopurinol; lesinurad	TABLET;ORAL	209203-001	Aug 18, 2017		DISCN	Yes	No						TREATMENT OF HYPERURICEMIA ASSOCIATED WITH GOUT IN PATIENTS WHO HAVE NOT ACHIEVED TARGET SERUM URIC ACID LEVELS WITH A MEDICALLY APPROPRIATE DAILY DOSE OF ALLOPURINOL ALONE
Ironwood Pharms Inc	DUZALLO	allopurinol; lesinurad	TABLET;ORAL	209203-002	Aug 18, 2017		DISCN	Yes	No						TREATMENT OF HYPERURICEMIA ASSOCIATED WITH GOUT IN PATIENTS WHO HAVE NOT ACHIEVED TARGET SERUM URIC ACID LEVELS WITH A MEDICALLY APPROPRIATE DAILY DOSE OF ALLOPURINOL ALONE
Ironwood Pharms Inc	ZURAMPIC	lesinurad	TABLET;ORAL	207988-001	Dec 22, 2015		DISCN	Yes	No						TREATMENT OF HYPERURICEMIA ASSOCIATED WITH GOUT IN PATIENTS WHO HAVE NOT ACHIEVED TARGET SERUM URIC ACID LEVELS WITH A XANTHINE OXIDASE INHIBITOR ALONE

International Family Members for US Patent 9,956,205

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	084639
Australia	2011352129
Brazil	112013016982
Canada	2817249
China	103298796
Cyprus	1118621
Denmark	2658846