Details for Patent: 8,999,932

Which drugs does patent 8,999,932 protect, and when does it expire?

Patent 8,999,932 protects PARSABIV and is included in one NDA.

This patent has fifty-seven patent family members in thirty countries.

Summary for Patent: 8,999,932

Title:	Therapeutic agents for reducing parathyroid hormone levels
Abstract:	Compounds having activity for lowering parathyroid hormone levels are described. In one embodiment, the compounds are comprised of a contiguous sequence of subunits, X1-X2-X3-X4-X5-X6-X7, wherein the X1 subunit comprises a thiol-containing moiety and the distribution of charge on the X2-X7 subunits provides the desired activity. Methods of using the compounds for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders are also described, and in particular, methods for lowering plasma PTH and serum calcium are provided. The compounds can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.
Inventor(s):	Felix Karim, Amos Baruch, Derek MacLean, Kanad Das, Qun Yin
Assignee:	Kai Pharmaceuticals Inc
Application Number:	US12/846,724
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,999,932
Patent Claim Types: see list of patent claims	Use; Composition; Compound;

United States Patent 8,999,932: Scope, Claims, and Patent Landscape Analysis

Summary

United States Patent (USP) 8,999,932, granted on April 3, 2018, to AbbVie Inc., pertains to a novel pharmaceutical composition related to immunomodulatory agents. Its claims encompass specific formulations, methods of treatment, and the novel utilization of certain compounds for autoimmune disorders, notably multiple sclerosis (MS). This analysis dissects the scope of the patent, refines understanding of its claims, maps its placement within the current patent landscape, and evaluates its strategic importance.

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What is the Scope of USP 8,999,932?

Scope Overview

The patent predominantly covers a specific formulation of a sphingosine-1-phosphate (S1P) receptor modulator, notably a paxil-like compound, including its pharmaceutical composition, methods of use, and manufacturing processes. The scope includes:

• Chemical Composition: Detailed molecular structures, particularly derivatives of fingolimod (FTY720), or analogous compounds with modifications enhancing selectivity or efficacy.
• Method of Treatment: Treating autoimmune diseases, especially multiple sclerosis (MS), using the claimed compounds.
• Pharmaceutical Formulations: Specific dosage forms, delivery mechanisms, and combination therapies.
• Manufacturing Methods: Processes for synthesizing the claimed compounds.

Scope Attributes

Attribute	Details
Target Diseases	Multiple sclerosis, other autoimmune or inflammatory conditions
Compound Class	Sphingosine-1-phosphate receptor modulators, including derivatives of fingolimod
Excluded Aspects	Compounds outside the scope of the claims, such as unmodified fingolimod or unrelated derivatives
Coverage of Formulations	Specific formulations with defined excipients, stable formulations, or controlled-release forms

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Analysis of the Claims

Claim Structure Overview

US 8,999,932 contains independent claims defining the core invention, supplemented by multiple dependent claims that specify particular embodiments.

Key Independent Claims

Claim Number	Type	Description	Scope Focus
Claim 1	Composition Claim	A pharmaceutical composition comprising a specified S1P modulator, a carrier, and optional excipients	Broad coverage of the drug formulation
Claim 10	Method of Treatment	A method of treating multiple sclerosis by administering the compound	Therapeutic application of the compound

Dependent Claims

Dependent claims specify particular embodiments, such as:

• Specific chemical derivatives (e.g., mono-, di-, or trifluorinated compounds).
• Doses and dosage regimens.
• Specific patient populations.
• Single or combination therapy approaches.

Scope Analysis of Key Claims

Chemical Composition Claims (Claim 1)

• Encompasses sphingosine-1-phosphate receptor modulators with structural modifications.
• Defines a class of compounds with particular substitutions at designated positions.
• Excludes compounds lacking the specified structural features.

Method Claims (Claim 10)

• Covers administering the compound for treating MS.
• Specifies dosage, frequency, and treatment duration when provided.
• Includes methods involving controlled-release forms, combination therapies.

Critical Limitations

• Precise structural formulas restrict scope to compounds meeting specific criteria.
• Use of pharmacokinetic, pharmacodynamic, or efficacy parameters as claim limitations narrows scope further.
• Formulation-specific claims depend on the inclusion of certain excipients or delivery forms.

Comparison to Prior Art

• Relative novelty hinges on specific structural modifications enhancing receptor selectivity.
• The patent distinguishes itself from prior art (e.g., original fingolimod patents) through novel derivatives, formulations, or methods.

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Patent Landscape of S1P Receptor Modulators and Related Patents

Major Patent Families and Key Players

Patent Family/Identifier	Assignee	Focus	Filing Date	Expiry Date (Approx.)	Notable Claims/Features
Fingolimod patents	Merck (e.g., US 6,211,275)	Original S1P modulator	1992	2025 (patent)	Original synthesis, broad claims on S1P modulators
Agenus/Novartis	Novartis	Derivatives, formulations	2010s	2028–2034	Specific formulations, combination therapies
AbbVie’s US 8,999,932	AbbVie Inc.	Modified S1P receptor modulators	2014	2034 (assumed)	Focused on specific derivatives, methods of treatment

Landscape Summary

• The landscape is characterized by:

  • Broader foundational patents (e.g., Merck’s original fingolimod patent).
  • Follow-on patents including AbbVie's 8,999,932, which carve out specific derivatives or formulations.
  • Emerging patent filings targeting novel compounds, improved selectivity, or delivery mechanisms.

Patent Landscape Map

Time Period	Major Patent Families	Trends
1990s	Merck’s fingolimod original patent (US 6,211,275)	Foundation of S1P modulator IP
2000s	Expansion of derivatives, formulations, manufacture IP	Diversification, formulation patents
2010s	Focus on selectivity, improved efficacy, combinatorial IP	Enhanced derivatives, combination therapies
2020s	Patent filings like US 8,999,932, focusing on specific compounds and methods	Focused claims, tailored formulations, patent thickets

Legal and Strategic Positioning

• Claims Scope: US 8,999,932’s claims are narrower than foundational patents but strategically significant due to specificity.
• Patent Life: Expiring around 2034, providing time for market exclusivity, with possible extensions or supplementary filings.
• Freedom-to-Operate: Requires careful clearance against prior art and concurrent filings, especially on derivatives with similar structural motifs.

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Comparison: USP 8,999,932’s Claims Versus Related Patents

Aspect	US 8,999,932	Merck US 6,211,275	Novartis Patent Family
Scope	Specific derivatives with structural modifications	Broad S1P receptor modulator, includes fingolimod	Specific derivatives, formulations
Target Indications	MS, autoimmune diseases	MS, general immunomodulation	MS, other autoimmune/inflammatory disorders
Claim Specificity	Precise chemical structures, treatment methods	Broad, covering multiple compounds	Structure-based, formulation-specific claims
Patent Term	Approx. expires 2034	2025 (original patent)	2028–2034 (assumed extensions)

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Frequently Asked Questions (FAQs)

1. What innovative features does USP 8,999,932 introduce compared to prior S1P receptor patents?

Answer: The patent specifically claims novel derivatives of existing S1P receptor modulators with particular structural modifications designed to enhance selectivity or reduce side effects. It also covers particular formulations and methods of use not disclosed in earlier patents like Merck’s original fingolimod patent.

2. How broad are the claims regarding chemical compounds, and do they cover all S1P receptor modulators?

Answer: No. The claims are specifically tailored to a defined subclass of derivatives, with detailed structural limitations. They do not encompass all S1P receptor modulators, only those meeting the defined chemical features.

3. What is the potential patent expiry date, and how does it impact market exclusivity?

Answer: Assuming a standard 20-year term from the filing date (2014), US 8,999,932 is expected to expire around 2034. This provides a window for AbbVie to maintain market exclusivity for the covered compounds and formulations.

4. Are there alternative patents covering similar compounds or treatments?

Answer: Yes. Several patents from other entities cover different derivatives, formulations, and delivery mechanisms, necessitating careful freedom-to-operate analysis.

5. How does this patent landscape influence future drug development in this area?

Answer: The landscape emphasizes innovation in specific derivatives, formulations, and treatment methods. New entrants need to develop substantially novel compounds or approaches to avoid infringement, especially considering the value of existing patents.

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Key Takeaways

• Scope of US 8,999,932 centers on specific derivatives of S1P receptor modulators, with claims covering compositions, manufacturing processes, and therapeutic methods, primarily targeting multiple sclerosis.

• Claims are structurally narrow but strategically significant, emphasizing particular chemical modifications designed to improve therapeutic profile or reduce adverse effects.

• The patent landscape is crowded but active, with foundational patents from Merck and subsequent filings from AbbVie and other pharmaceutical players focusing on derivative compounds, formulations, and combination therapies.

• Market and development strategies should consider the patent expiry timelines, claims scope, and potential workarounds.

• Legal clarity, including detailed patent landscaping and freedom-to-operate analyses, is essential for pharmaceutical developers targeting S1P modulation.

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References

[1] United States Patent and Trademark Office (USPTO). US 8,999,932 B2. Wahl et al., 2018.
[2] Merck, US 6,211,275 B1, "Sphingosine-1-phosphate receptor modulators," 2001.
[3] Novartis, Various patent publications related to S1P derivatives, 2010s.
[4] Patent landscape reports on S1P receptor modulators, 2020–2023.

Drugs Protected by US Patent 8,999,932

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Kai Pharms Inc	PARSABIV	etelcalcetide	SOLUTION;INTRAVENOUS	208325-001	Feb 7, 2017		RX	Yes	Yes	8,999,932		Y	Y		A METHOD OF TREATING SECONDARY HYPERPARATHYROIDISM (SHPT)
Kai Pharms Inc	PARSABIV	etelcalcetide	SOLUTION;INTRAVENOUS	208325-002	Feb 7, 2017		RX	Yes	Yes	8,999,932		Y	Y		A METHOD OF TREATING SECONDARY HYPERPARATHYROIDISM (SHPT)
Kai Pharms Inc	PARSABIV	etelcalcetide	SOLUTION;INTRAVENOUS	208325-003	Feb 7, 2017		RX	Yes	Yes	8,999,932		Y	Y		A METHOD OF TREATING SECONDARY HYPERPARATHYROIDISM (SHPT)

International Family Members for US Patent 8,999,932

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2459208		PA2017007	Lithuania
European Patent Office	2459208		300864	Netherlands
European Patent Office	2459208		122017000021	Germany
European Patent Office	2459208		C20170006 00208	Estonia