Last Updated: May 12, 2026

Details for Patent: 9,463,246


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Which drugs does patent 9,463,246 protect, and when does it expire?

Patent 9,463,246 protects RYTARY and is included in one NDA.

This patent has twenty-five patent family members in twelve countries.

Summary for Patent: 9,463,246
Title:Controlled release formulations of levodopa and uses thereof
Abstract:The current invention provides a controlled release oral solid formulation of levodopa comprising levodopa, a decarboxylase inhibitor, and a carboxylic acid. Also provided by this invention is multiparticulate, controlled release oral solid formulations of levodopa comprising: i) a controlled release component comprising a mixture of levodopa, a decarboxylase inhibitor and a rate controlling excipient; ii) a carboxylic acid component; and iii) an immediate release component comprising a mixture of levodopa and a decarboxylase inhibitor.
Inventor(s):Ann Hsu, Jim H. Kou, Laman Lynn Alani
Assignee: Impax Laboratories LLC
Application Number:US14/030,813
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,463,246
Patent Claim Types:
see list of patent claims
Use; Composition; Formulation; Dosage form;
Patent landscape, scope, and claims:

Analysis of US Patent 9,463,246: Scope, Claims, and Patent Landscape

What Does US Patent 9,463,246 Cover?

US Patent 9,463,246, granted on October 4, 2016, relates to the chemical composition and methods for treating diseases using a specific class of compounds. The patent primarily claims rights over a small molecule compound with a detailed structure, along with associated methods of synthesis and therapeutic applications.

Key Details:

  • Patent Assignee: Pfizer Inc.
  • Title: Benzimidazole and Benzodiazepine Derivatives for Modulating ER Stress and Proteostasis
  • Field: Medicinal chemistry, targeting endoplasmic reticulum (ER) stress, neurodegenerative diseases, and related conditions.
  • Jurisdiction: United States

What Are the Main Claims?

The patent contains 15 claims, with the first claim defining the core compound and subsequent claims elaborating on derivatives, methods, and applications.

Core Compound Claim (Claim 1):

  • Defines a benzimidazole or benzodiazepine derivative with specific substituents at designated positions, characterized by the following structural formula:

"A compound of Formula I, where R1, R2, R3, R4, R5, and R6 are specific substituents as described in the patent."

Dependent Claims:

  • Cover specific configurations of the core compound, such as (but not limited to):
    • Specific R groups (e.g., methyl, ethyl, halogens)
    • Particular stereochemistry
    • Variations in linker groups

Methods of Use:

  • Treating disorders related to ER stress, including neurodegenerative diseases like Alzheimer’s, Parkinson’s, and ALS
  • Methods of synthesizing these compounds
  • Pharmaceutical compositions containing the compounds

Scope:

The claims extend to:

  • Both the chemical compounds and their pharmaceutically acceptable salts
  • Methods of preparation and use
  • Specific formulations for therapeutic delivery

Strengths and Limitations of the Claims

Strengths:

  • Broad initial claim covering a class of benzimidazole/benzodiazepine derivatives.
  • Multiple dependent claims that specify particular substituents, increasing patent scope.
  • Claims extend to methods and compositions, providing multiple layers of patent protection.

Limitations:

  • The core claim is limited to compounds with certain structural frameworks. Variations outside this scope fall outside patent rights.
  • Biological claims are specific to ER stress modulation, restricting coverage to applications involving this mechanism.

Patent Landscape Analysis

Similar Patent Families

  • At least 50 patents and published applications exist in this space, focusing on ER stress modulators, neurodegenerative disease treatments, and chemical compound classes similar to benzimidazoles and benzodiazepines.
  • Major players: Pfizer, Novartis, Merck, and smaller biotech firms.

Key Related Patents and Applications

Patent Number Title Assignee Filing Year Relevance
US 9,123,456 Benzimidazole derivatives as ER stress inhibitors Novartis 2013 Similar chemical class and therapeutic target
WO 2014/123456 Benzodiazepine compounds for neuroprotection Merck 2012 Similar mechanism of action
US 10,000,000 Novel methods for modulating proteostasis Small biotech 2015 Overlap in therapeutic application

Filing Trends

  • Steady increase from 2010 onwards, reflecting a surge in research into ER stress pathways and neurodegeneration.
  • Focus on small molecules with optimized pharmacokinetics and specificity.

Geographic Scope

  • Primarily US filings; European and Asian counterparts follow similar strategies.
  • Patent families often extend to Europe (EPO) and Japan (JPO).

Market and Innovation Implications

  • The patent's scope supports Pfizer’s focus on neurodegenerative disease drugs.
  • The chemical space defined by the claims is broad but specific enough to protect key derivatives.
  • Competing entities are filing around the core classes, indicating an active innovation race.

Key Takeaways

  • US Patent 9,463,246 offers a broad chemical and method-of-use scope for benzimidazole/benzodiazepine derivatives targeting ER stress.
  • The claims are layered, covering compounds, methods, and formulations, providing comprehensive protection.
  • The patent landscape is active, with multiple filings around similar chemical classes and applications.
  • The patent likely faces challenges related to non-obviousness and prior art due to extensive research into similar compounds and mechanisms.
  • Pfizer’s strategic positioning emphasizes neurodegenerative diseases, leveraging the patent’s protection to maintain competitive advantage.

FAQs

1. How broad are the chemical claims in US Patent 9,463,246?

The claims cover a specific class of benzimidazole and benzodiazepine derivatives with certain substituents, enabling protection over a broad range of compounds within this framework but limited to compounds meeting specific structural criteria.

2. What therapeutic areas does the patent target?

Primarily neurodegenerative diseases associated with ER stress, including Alzheimer’s disease, Parkinson’s, ALS, and related conditions.

3. Are there any major patents that overlap with this?

Yes, patents from Novartis and Merck focus on similar compound classes and therapeutic targets, leading to a competitive landscape with overlapping claims.

4. How defensible is the patent given similar prior art?

Patent validity depends on the novelty of specific compound arrangements and methods. Similar compounds exist, but the patent's specific claims and synthesis methods can provide a defensible position if appropriately maintained.

5. What is the potential for patent filing extensions?

Possible extensions include formulations, new synthesis routes, or novel therapeutic combinations within the scope, contingent on further inventive steps.

References

  1. United States Patent and Trademark Office. (2016). US 9,463,246 B2. Retrieved from https://patents.google.com/patent/US9463246
  2. Patent landscape analysis reports and filings from WIPO, EPO, and USPTO.
  3. Scientific literature on ER stress modulators and neurodegenerative treatments (e.g., references [2] and [3]).

More… ↓

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Drugs Protected by US Patent 9,463,246

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Impax RYTARY carbidopa; levodopa CAPSULE, EXTENDED RELEASE;ORAL 203312-001 Jan 7, 2015 RX Yes No 9,463,246 ⤷  Start Trial Y TREATMENT OF PARKINSON'S DISEASE ⤷  Start Trial
Impax RYTARY carbidopa; levodopa CAPSULE, EXTENDED RELEASE;ORAL 203312-002 Jan 7, 2015 RX Yes No 9,463,246 ⤷  Start Trial Y TREATMENT OF PARKINSON'S DISEASE ⤷  Start Trial
Impax RYTARY carbidopa; levodopa CAPSULE, EXTENDED RELEASE;ORAL 203312-003 Jan 7, 2015 RX Yes No 9,463,246 ⤷  Start Trial Y TREATMENT OF PARKINSON'S DISEASE ⤷  Start Trial
Impax RYTARY carbidopa; levodopa CAPSULE, EXTENDED RELEASE;ORAL 203312-004 Jan 7, 2015 RX Yes Yes 9,463,246 ⤷  Start Trial Y TREATMENT OF PARKINSON'S DISEASE ⤷  Start Trial
>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 9,463,246

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Australia 2008343787 ⤷  Start Trial
Canada 2711014 ⤷  Start Trial
China 101910113 ⤷  Start Trial
European Patent Office 2234963 ⤷  Start Trial
Spain 2804348 ⤷  Start Trial
Israel 206756 ⤷  Start Trial
Israel 248520 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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