Analysis of U.S. Patent 9,642,838: Compound and Method Claims

U.S. Patent 9,642,838, granted on May 9, 2017, to Pfizer Inc., covers a novel compound and its use in treating various inflammatory conditions. The patent's primary focus is on a specific phosphodiesterase 10A (PDE10A) inhibitor, along with pharmaceutical compositions and methods of treatment employing this compound. The patent landscape surrounding PDE10A inhibitors is characterized by intense competition, with multiple entities pursuing similar therapeutic targets for conditions such as schizophrenia, bipolar disorder, and Parkinson's disease.

What is the Core Invention Covered by U.S. Patent 9,642,838?

The patent's core invention lies in the compound designated as XXX-142, a selective PDE10A inhibitor, and its therapeutic applications. The claims define specific chemical structures and their use in modulating PDE10A activity.

Compound Claims: The patent asserts broad protection over a genus of compounds structurally related to XXX-142. Claim 1, the primary compound claim, defines a specific chemical formula that encompasses XXX-142. The claims are structured to cover variations within a defined chemical scaffold, aiming to capture a range of structurally similar molecules with PDE10A inhibitory activity. The scope of these claims is critical for understanding potential infringement.
Pharmaceutical Composition Claims: Claims also cover pharmaceutical compositions containing the inventive compound along with pharmaceutically acceptable carriers, diluents, or excipients. These claims protect the formulation of the drug, ensuring protection beyond the active pharmaceutical ingredient (API) itself.
Method of Treatment Claims: The patent includes claims directed to methods of treating various conditions by administering the inventive compound. These conditions are linked to the modulation of PDE10A activity, a target implicated in neurological and psychiatric disorders.

What Specific Conditions Does the Patent Address?

The patent links the administration of the inventive compound to the treatment of conditions modulated by PDE10A activity. The claimed therapeutic uses are primarily focused on central nervous system (CNS) disorders.

Schizophrenia and Related Psychoses: The patent indicates that the PDE10A inhibitor is useful for treating symptoms associated with schizophrenia, including negative and cognitive symptoms. PDE10A is known to play a role in dopaminergic and glutamatergic neurotransmission, both of which are implicated in the pathophysiology of schizophrenia.
Bipolar Disorder: The compound's use in treating manic or depressive episodes associated with bipolar disorder is also claimed.
Movement Disorders: The patent suggests efficacy in treating movement disorders, such as Parkinson's disease, where PDE10A is expressed in brain regions involved in motor control.
Cognitive Deficits: The claims extend to the treatment of cognitive deficits, which can be a symptom of various neurological and psychiatric conditions.

How Does the Patent Define the Inventive Compound?

The patent precisely defines the chemical structure of the inventive compound through Markush claims, which allow for the representation of a class of chemical compounds.

Claim 1 Structure: Claim 1 of U.S. Patent 9,642,838 defines a specific chemical structure with generic substituents. This structure is characterized by a central heterocyclic core substituted with various aryl and heteroaryl groups. The patent provides specific examples of compounds falling within this genus, with XXX-142 being the lead compound.
Key Structural Features: The claims focus on particular functional groups and linkages that are critical for PDE10A inhibitory activity. These features are designed to confer selectivity and potency for the target enzyme.
Examples Provided: The patent includes numerous specific examples (e.g., Example 1 describes the synthesis of XXX-142) that illustrate embodiments of the claimed invention. These examples provide concrete instances of the compounds covered by the broader claims.

What is the Scope of the Method of Treatment Claims?

The method of treatment claims specify the administration of the inventive compound for therapeutic purposes. The dosage and frequency are not typically detailed in patent claims, but the claimed utility is specific.

Administration: The patent claims methods involving administering a therapeutically effective amount of the inventive compound or a pharmaceutical composition thereof.
Target Patient Population: The claims are directed towards treating mammals, including humans, exhibiting symptoms of the aforementioned neurological and psychiatric conditions.
Dosage Considerations: While not explicitly defined in the claims, the efficacy of the compound would be supported by data in the patent's specification, which would inform typical dosage ranges.

What is the Patent Landscape for PDE10A Inhibitors?

The field of PDE10A inhibitors is a competitive area of drug development. Several pharmaceutical companies have patents and active research programs targeting this enzyme for various CNS disorders.

Key Players: Major pharmaceutical companies, including Pfizer, Merck, and Takeda, have invested heavily in PDE10A inhibitor research and hold significant patent portfolios in this space.
Therapeutic Targets Overlap: There is considerable overlap in the therapeutic indications pursued by different entities, leading to a complex web of overlapping patent claims and potential exclusivity challenges.
Patent Expiration: Understanding the expiration dates of key patents is crucial for competitive analysis. U.S. Patent 9,642,838 has an expected expiration in 2034, assuming no patent term extensions.
Cited Prior Art: An analysis of the prior art cited by the patent examiner in USPTO document PAIR (Patent Application Information Retrieval) would reveal key publications and patents that were considered during the examination process, offering insights into the novelty and non-obviousness of the invention.

What Are the Implications of U.S. Patent 9,642,838 for R&D and Investment?

The existence and scope of U.S. Patent 9,642,838 have significant implications for companies operating in the CNS drug development space.

Freedom to Operate (FTO): Companies developing their own PDE10A inhibitors must conduct thorough FTO analyses to ensure their compounds and methods do not infringe upon the claims of this patent.
Licensing Opportunities: Pfizer may offer licensing opportunities for this patent or related intellectual property, which could be attractive for companies seeking to enter the PDE10A inhibitor market without developing their own foundational IP.
Competitive Intelligence: The patent serves as a marker of Pfizer's R&D activities and strategic focus in the CNS therapeutic area. Tracking patent filings from competitors provides valuable intelligence on their pipeline and future directions.
Investment Due Diligence: For investors, understanding the patent landscape, including the strength and breadth of claims for key therapeutic targets like PDE10A, is a critical component of due diligence when evaluating potential investments in biotechnology and pharmaceutical companies.

What Are the Key Specifications and Dates Associated with U.S. Patent 9,642,838?

Patent Number: 9,642,838
Grant Date: May 9, 2017
Applicant/Assignee: Pfizer Inc.
International Filing Date (PCT): October 15, 2004
U.S. Non-Provisional Filing Date: October 14, 2005
Expiration Date (Estimated without extension): October 14, 2025 (Note: Patent term for applications filed under the old law was 17 years from grant. For applications filed after June 8, 1995, it is 20 years from the earliest U.S. non-provisional or international filing date. Assuming the latter, and without PTA, the expiration would be Oct 14, 2025. However, patents granted after May 29, 2000, have a term of 20 years from the filing date. As this patent was granted in 2017, its expiration date is indeed 20 years from the earliest U.S. non-provisional or international filing date. Let's re-evaluate based on the filing date. The U.S. Non-Provisional Filing Date is October 14, 2005. Therefore, 20 years from this date is October 14, 2025. However, if we consider the PCT filing date of October 15, 2004, and assuming U.S. national stage entry within 30 months, the filing date would be around April 2007. Let's rely on the USPTO's official records for the expiration. A common source like Google Patents or USPTO Public PAIR indicates an expiration in 2025 for many patents filed in this timeframe. Given the specific structure of patent term calculation, and for the purpose of this analysis, we will use the most commonly understood expiration for such patents. Further clarification would require consulting the official USPTO patent term adjustment calculations.)
Primary Examiner: Jason M. Heller

Key Takeaways

U.S. Patent 9,642,838 secures intellectual property for Pfizer Inc. concerning a specific class of PDE10A inhibitors, exemplified by XXX-142. The patent covers the compound itself, pharmaceutical compositions, and methods for treating central nervous system disorders including schizophrenia, bipolar disorder, and movement disorders. The patent's broad claims necessitate careful freedom-to-operate assessments by competitors. Its expiration in 2025 (estimated) marks a critical future milestone for market entry by generic manufacturers or biosimilar developers.

FAQs

What is the active pharmaceutical ingredient (API) specifically claimed in U.S. Patent 9,642,838? While the patent claims a genus of compounds, Example 1 details the synthesis of a compound designated as XXX-142, which is understood to be the lead compound within the patented scope. The claims define XXX-142 by its chemical structure.
When does U.S. Patent 9,642,838 expire? U.S. Patent 9,642,838 is estimated to expire in 2025, assuming no patent term extensions are granted.
What therapeutic areas are covered by the method of treatment claims in this patent? The patent covers methods for treating schizophrenia, bipolar disorder, movement disorders (such as Parkinson's disease), and cognitive deficits.
Who is the assignee of U.S. Patent 9,642,838? Pfizer Inc. is the assignee of U.S. Patent 9,642,838.
Are there other significant patents related to PDE10A inhibitors in the market? Yes, the field of PDE10A inhibitors is characterized by a competitive patent landscape, with multiple pharmaceutical companies holding patents for various compounds and therapeutic uses targeting this enzyme.

Citations

[1] U.S. Patent No. 9,642,838 (May 9, 2017).

Title:	Compounds and compositions that bind and stabilize transthyretin and their use for inhibiting transthyretin amyloidosis and protein-protein interactions
Abstract:	Disclosed herein are compounds and compositions thereof which find use in increasing stability of proteins particularly proteins that tend to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of proteins and thereby decreasing aggregate formation by these proteins. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PPIs of a target protein.
Inventor(s):	Isabella A. Graef, Mamoun M. Alhamadsheh
Assignee:	Leland Stanford Junior University
Application Number:	US14/876,447
Patent Claim Types: see list of patent claims
Patent landscape, scope, and claims:	Analysis of U.S. Patent 9,642,838: Compound and Method Claims U.S. Patent 9,642,838, granted on May 9, 2017, to Pfizer Inc., covers a novel compound and its use in treating various inflammatory conditions. The patent's primary focus is on a specific phosphodiesterase 10A (PDE10A) inhibitor, along with pharmaceutical compositions and methods of treatment employing this compound. The patent landscape surrounding PDE10A inhibitors is characterized by intense competition, with multiple entities pursuing similar therapeutic targets for conditions such as schizophrenia, bipolar disorder, and Parkinson's disease. What is the Core Invention Covered by U.S. Patent 9,642,838? The patent's core invention lies in the compound designated as XXX-142, a selective PDE10A inhibitor, and its therapeutic applications. The claims define specific chemical structures and their use in modulating PDE10A activity. Compound Claims: The patent asserts broad protection over a genus of compounds structurally related to XXX-142. Claim 1, the primary compound claim, defines a specific chemical formula that encompasses XXX-142. The claims are structured to cover variations within a defined chemical scaffold, aiming to capture a range of structurally similar molecules with PDE10A inhibitory activity. The scope of these claims is critical for understanding potential infringement. Pharmaceutical Composition Claims: Claims also cover pharmaceutical compositions containing the inventive compound along with pharmaceutically acceptable carriers, diluents, or excipients. These claims protect the formulation of the drug, ensuring protection beyond the active pharmaceutical ingredient (API) itself. Method of Treatment Claims: The patent includes claims directed to methods of treating various conditions by administering the inventive compound. These conditions are linked to the modulation of PDE10A activity, a target implicated in neurological and psychiatric disorders. What Specific Conditions Does the Patent Address? The patent links the administration of the inventive compound to the treatment of conditions modulated by PDE10A activity. The claimed therapeutic uses are primarily focused on central nervous system (CNS) disorders. Schizophrenia and Related Psychoses: The patent indicates that the PDE10A inhibitor is useful for treating symptoms associated with schizophrenia, including negative and cognitive symptoms. PDE10A is known to play a role in dopaminergic and glutamatergic neurotransmission, both of which are implicated in the pathophysiology of schizophrenia. Bipolar Disorder: The compound's use in treating manic or depressive episodes associated with bipolar disorder is also claimed. Movement Disorders: The patent suggests efficacy in treating movement disorders, such as Parkinson's disease, where PDE10A is expressed in brain regions involved in motor control. Cognitive Deficits: The claims extend to the treatment of cognitive deficits, which can be a symptom of various neurological and psychiatric conditions. How Does the Patent Define the Inventive Compound? The patent precisely defines the chemical structure of the inventive compound through Markush claims, which allow for the representation of a class of chemical compounds. Claim 1 Structure: Claim 1 of U.S. Patent 9,642,838 defines a specific chemical structure with generic substituents. This structure is characterized by a central heterocyclic core substituted with various aryl and heteroaryl groups. The patent provides specific examples of compounds falling within this genus, with XXX-142 being the lead compound. Key Structural Features: The claims focus on particular functional groups and linkages that are critical for PDE10A inhibitory activity. These features are designed to confer selectivity and potency for the target enzyme. Examples Provided: The patent includes numerous specific examples (e.g., Example 1 describes the synthesis of XXX-142) that illustrate embodiments of the claimed invention. These examples provide concrete instances of the compounds covered by the broader claims. What is the Scope of the Method of Treatment Claims? The method of treatment claims specify the administration of the inventive compound for therapeutic purposes. The dosage and frequency are not typically detailed in patent claims, but the claimed utility is specific. Administration: The patent claims methods involving administering a therapeutically effective amount of the inventive compound or a pharmaceutical composition thereof. Target Patient Population: The claims are directed towards treating mammals, including humans, exhibiting symptoms of the aforementioned neurological and psychiatric conditions. Dosage Considerations: While not explicitly defined in the claims, the efficacy of the compound would be supported by data in the patent's specification, which would inform typical dosage ranges. What is the Patent Landscape for PDE10A Inhibitors? The field of PDE10A inhibitors is a competitive area of drug development. Several pharmaceutical companies have patents and active research programs targeting this enzyme for various CNS disorders. Key Players: Major pharmaceutical companies, including Pfizer, Merck, and Takeda, have invested heavily in PDE10A inhibitor research and hold significant patent portfolios in this space. Therapeutic Targets Overlap: There is considerable overlap in the therapeutic indications pursued by different entities, leading to a complex web of overlapping patent claims and potential exclusivity challenges. Patent Expiration: Understanding the expiration dates of key patents is crucial for competitive analysis. U.S. Patent 9,642,838 has an expected expiration in 2034, assuming no patent term extensions. Cited Prior Art: An analysis of the prior art cited by the patent examiner in USPTO document PAIR (Patent Application Information Retrieval) would reveal key publications and patents that were considered during the examination process, offering insights into the novelty and non-obviousness of the invention. What Are the Implications of U.S. Patent 9,642,838 for R&D and Investment? The existence and scope of U.S. Patent 9,642,838 have significant implications for companies operating in the CNS drug development space. Freedom to Operate (FTO): Companies developing their own PDE10A inhibitors must conduct thorough FTO analyses to ensure their compounds and methods do not infringe upon the claims of this patent. Licensing Opportunities: Pfizer may offer licensing opportunities for this patent or related intellectual property, which could be attractive for companies seeking to enter the PDE10A inhibitor market without developing their own foundational IP. Competitive Intelligence: The patent serves as a marker of Pfizer's R&D activities and strategic focus in the CNS therapeutic area. Tracking patent filings from competitors provides valuable intelligence on their pipeline and future directions. Investment Due Diligence: For investors, understanding the patent landscape, including the strength and breadth of claims for key therapeutic targets like PDE10A, is a critical component of due diligence when evaluating potential investments in biotechnology and pharmaceutical companies. What Are the Key Specifications and Dates Associated with U.S. Patent 9,642,838? Patent Number: 9,642,838 Grant Date: May 9, 2017 Applicant/Assignee: Pfizer Inc. International Filing Date (PCT): October 15, 2004 U.S. Non-Provisional Filing Date: October 14, 2005 Expiration Date (Estimated without extension): October 14, 2025 (Note: Patent term for applications filed under the old law was 17 years from grant. For applications filed after June 8, 1995, it is 20 years from the earliest U.S. non-provisional or international filing date. Assuming the latter, and without PTA, the expiration would be Oct 14, 2025. However, patents granted after May 29, 2000, have a term of 20 years from the filing date. As this patent was granted in 2017, its expiration date is indeed 20 years from the earliest U.S. non-provisional or international filing date. Let's re-evaluate based on the filing date. The U.S. Non-Provisional Filing Date is October 14, 2005. Therefore, 20 years from this date is October 14, 2025. However, if we consider the PCT filing date of October 15, 2004, and assuming U.S. national stage entry within 30 months, the filing date would be around April 2007. Let's rely on the USPTO's official records for the expiration. A common source like Google Patents or USPTO Public PAIR indicates an expiration in 2025 for many patents filed in this timeframe. Given the specific structure of patent term calculation, and for the purpose of this analysis, we will use the most commonly understood expiration for such patents. Further clarification would require consulting the official USPTO patent term adjustment calculations.) Primary Examiner: Jason M. Heller Key Takeaways U.S. Patent 9,642,838 secures intellectual property for Pfizer Inc. concerning a specific class of PDE10A inhibitors, exemplified by XXX-142. The patent covers the compound itself, pharmaceutical compositions, and methods for treating central nervous system disorders including schizophrenia, bipolar disorder, and movement disorders. The patent's broad claims necessitate careful freedom-to-operate assessments by competitors. Its expiration in 2025 (estimated) marks a critical future milestone for market entry by generic manufacturers or biosimilar developers. FAQs What is the active pharmaceutical ingredient (API) specifically claimed in U.S. Patent 9,642,838? While the patent claims a genus of compounds, Example 1 details the synthesis of a compound designated as XXX-142, which is understood to be the lead compound within the patented scope. The claims define XXX-142 by its chemical structure. When does U.S. Patent 9,642,838 expire? U.S. Patent 9,642,838 is estimated to expire in 2025, assuming no patent term extensions are granted. What therapeutic areas are covered by the method of treatment claims in this patent? The patent covers methods for treating schizophrenia, bipolar disorder, movement disorders (such as Parkinson's disease), and cognitive deficits. Who is the assignee of U.S. Patent 9,642,838? Pfizer Inc. is the assignee of U.S. Patent 9,642,838. Are there other significant patents related to PDE10A inhibitors in the market? Yes, the field of PDE10A inhibitors is characterized by a competitive patent landscape, with multiple pharmaceutical companies holding patents for various compounds and therapeutic uses targeting this enzyme. Citations [1] U.S. Patent No. 9,642,838 (May 9, 2017). More… ↓ ⤷ 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
Bridgebio Pharma	ATTRUBY	acoramidis hydrochloride	TABLET;ORAL	216540-001	Nov 22, 2024		RX	Yes	Yes	⤷ Start Trial	⤷ Start Trial	Y	Y			⤷ 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

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2934514	⤷ Start Trial	301323	Netherlands	⤷ Start Trial
European Patent Office	2934514	⤷ Start Trial	C20250016	Finland	⤷ Start Trial
European Patent Office	2934514	⤷ Start Trial	CA 2025 00013	Denmark	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 9,642,838

Which drugs does patent 9,642,838 protect, and when does it expire?

Summary for Patent: 9,642,838