US Patent 6,689,275: Analysis of Scope, Claims, and Landscape

US Patent 6,689,275, titled "Methods of treating conditions with atypical antipsychotics," issued on February 10, 2004, to SmithKline Beecham Corporation (now GlaxoSmithKline). The patent covers methods of treating schizophrenia using specific atypical antipsychotic compounds. The primary focus is on the use of aripiprazole, an active pharmaceutical ingredient.

What is the Core Invention of US Patent 6,689,275?

The patent's core invention is a method for treating schizophrenia in a human subject. This method involves administering a specific dosage range of an atypical antipsychotic compound. The patent specifically recites the administration of aripiprazole.

The method is defined by the dosage and frequency of administration, aiming to achieve a therapeutic effect in patients suffering from schizophrenia. This includes acute exacerbation of schizophrenia and chronic treatment.

What are the Key Claims of US Patent 6,689,275?

The patent contains several claims, with Claim 1 being the broadest and most frequently cited.

Claim 1: "A method of treating schizophrenia in a human subject, which comprises administering to the human subject an effective amount of aripiprazole."

Other representative claims include:

Claim 2: "The method of claim 1, wherein the effective amount of aripiprazole is between 1 mg and 100 mg per day."
Claim 3: "The method of claim 2, wherein the effective amount of aripiprazole is between 5 mg and 50 mg per day."
Claim 4: "The method of claim 3, wherein the effective amount of aripiprazole is between 10 mg and 30 mg per day."
Claim 5: "The method of claim 4, wherein the effective amount of aripiprazole is 20 mg per day."
Claim 6: "The method of claim 1, wherein the administration is oral."
Claim 7: "The method of claim 1, wherein the administration is daily."
Claim 8: "The method of claim 1, wherein the human subject is experiencing an acute exacerbation of schizophrenia."
Claim 9: "The method of claim 1, wherein the human subject is undergoing chronic treatment for schizophrenia."
Claim 10: "The method of claim 1, wherein the aripiprazole is administered as a tablet."

These claims define the scope of the patent, focusing on the administration of aripiprazole for schizophrenia treatment within specific dosage ranges and frequencies. The patent does not claim the compound itself, but the method of its use.

How Does the Patent Define "Effective Amount"?

The patent defines "effective amount" in relation to the dosage ranges specified in the claims. Claims 2 through 5 provide progressively narrower ranges, from 1 mg to 100 mg per day, down to a specific 20 mg per day dose. This definition is critical for determining infringement.

The patent does not provide a specific pharmacokinetic or pharmacodynamic definition of "effective amount" beyond the quantitative ranges. The therapeutic efficacy is implicitly linked to these dosage levels.

What is the Stated Purpose and Mechanism of Action for Aripiprazole in this Patent?

The patent states that aripiprazole is an atypical antipsychotic agent. It is characterized as a dopamine D2 partial agonist. The stated purpose is to treat schizophrenia by alleviating symptoms such as hallucinations, delusions, disorganized speech, and blunted affect.

The patent cites prior art indicating that atypical antipsychotics work by modulating dopaminergic and serotonergic systems. Aripiprazole's partial agonism at D2 receptors is presented as a key differentiator, potentially leading to a more favorable side effect profile compared to full agonists or antagonists.

The patent describes aripiprazole as having high affinity for D2, D3, 5-HT1A, and 5-HT2A receptors, and moderate affinity for D4, 5-HT7, and alpha-1 adrenergic receptors. It has low affinity for H1 and muscarinic M1 receptors. This receptor binding profile is presented as contributing to its therapeutic efficacy and tolerability.

Who is the Assignee of US Patent 6,689,275?

The assignee of US Patent 6,689,275 is SmithKline Beecham Corporation. This entity is now part of GlaxoSmithKline (GSK). GSK is a global pharmaceutical company that has been instrumental in the development and commercialization of aripiprazole under the brand name Abilify.

What is the Patent Expiration Date?

US Patent 6,689,275 issued on February 10, 2004. Under U.S. patent law, utility patents generally have a term of 20 years from the filing date, subject to certain adjustments and extensions. The filing date for this patent was October 20, 2000.

Therefore, the original term of the patent would have expired on October 20, 2020. However, patents can receive Patent Term Adjustments (PTA) or Patent Term Extensions (PTE) for regulatory delays. For pharmaceutical patents, PTE is common.

According to the USPTO Orange Book, the listed expiry date for US Patent 6,689,275, considering PTE, was November 29, 2017 [1]. This indicates that the patent's market exclusivity period has concluded.

What is the Significance of this Patent in the Aripiprazole Landscape?

US Patent 6,689,275 is a foundational method-of-use patent for aripiprazole. While other patents likely cover the compound itself, formulations, and manufacturing processes, this patent specifically protected the therapeutic application of aripiprazole for schizophrenia treatment.

The expiration of this patent, particularly its PTE-adjusted date, was a key trigger for the market entry of generic versions of aripiprazole. Generic manufacturers could begin producing and selling their own versions of the drug once the patent protection expired.

How Does US Patent 6,689,275 Interact with Other Aripiprazole Patents?

The patent landscape for aripiprazole is complex and involves multiple patents covering different aspects of the drug. US Patent 6,689,275 is one piece of this puzzle.

Composition of Matter Patents: These patents claim the aripiprazole molecule itself. The original compound patent for aripiprazole would have expired significantly earlier, allowing for the development of generics. However, method-of-use patents like 6,689,275 can extend market exclusivity for specific therapeutic applications.
Formulation Patents: Patents covering specific pharmaceutical formulations of aripiprazole (e.g., extended-release tablets, oral solutions, intramuscular injections) can provide additional layers of protection and can expire at different times than the core compound or method patents.
Manufacturing Process Patents: Patents related to specific methods of synthesizing aripiprazole can also be in play.
Later Method-of-Use Patents: Even after the expiration of foundational patents like 6,689,275, pharmaceutical companies might obtain new patents for novel uses of aripiprazole, such as treating different conditions or using it in combination therapies.

The interaction between these patents determines the overall market exclusivity period for aripiprazole and its various indications. Litigation often arises when generic manufacturers challenge the validity or scope of these patents.

What was the Patent Landscape for Aripiprazole around the Expiration of US Patent 6,689,275?

As US Patent 6,689,275 approached its PTE-adjusted expiration in November 2017, the aripiprazole market was poised for generic entry. By this time, the primary compound patents had long expired. The market exclusivity was largely maintained by method-of-use patents, such as 6,689,275, and potentially formulation patents.

Generic Entry: The expiration of key patents, including 6,689,275, paved the way for generic aripiprazole to enter the U.S. market. This typically leads to significant price reductions due to competition.
Litigation: Before and around the patent expiration dates, there is often intense patent litigation. Generic companies may file Abbreviated New Drug Applications (ANDAs) and challenge existing patents, while the innovator company defends its intellectual property. Litigation surrounding aripiprazole patents has been extensive.
Authorized Generics: Innovator companies may also release "authorized generics" through a subsidiary to compete with independent generic manufacturers.

The expiration of US Patent 6,689,275 was a significant event in the commercial lifecycle of aripiprazole, marking the end of a specific period of market protection for its use in schizophrenia treatment.

What are the Implications for R&D and Investment Decisions?

For R&D professionals and investors, the analysis of patents like US 6,689,275 is crucial for several reasons:

Freedom to Operate (FTO): Understanding the scope and expiration of existing patents is essential to ensure that new drug development or commercialization efforts do not infringe on active patents. For aripiprazole, FTO has been complex due to the multitude of patents.
Competitive Intelligence: Analyzing patent landscapes reveals the strategies of competitors, including their protected indications, formulations, and manufacturing processes. This informs competitive positioning and R&D prioritization.
Investment Due Diligence: For investors, assessing the strength and duration of patent protection is a key component of valuing a pharmaceutical asset or company. The expiration of key patents, such as 6,689,275, signals an impending loss of market exclusivity and potential revenue decline for the innovator.
Lifecycle Management: Pharmaceutical companies use patent strategies to extend the commercial lifecycle of a drug. Understanding patents like 6,689,275 helps in planning for this lifecycle, including the development of new formulations, indications, or delivery methods.
Generic Market Opportunities: For generic manufacturers, the expiration of method-of-use patents is a direct signal of market entry opportunities. Analyzing these patents helps in planning ANDA filings and anticipating regulatory pathways.

The detailed claims and expiration date of US Patent 6,689,275 directly inform strategic decisions regarding the development, manufacturing, and marketing of aripiprazole and similar antipsychotic treatments.

Key Takeaways

US Patent 6,689,275 protects the method of treating schizophrenia using aripiprazole, specifically within defined dosage ranges.
The patent's assignee is SmithKline Beecham Corporation (now GlaxoSmithKline).
The Patent Term Extension (PTE) adjusted expiration date for US Patent 6,689,275 was November 29, 2017.
The expiration of this patent was a significant event enabling generic entry for aripiprazole in the U.S. market.
This patent is one component of a broader, complex patent landscape for aripiprazole, which includes patents for the compound, formulations, and manufacturing processes.

FAQs

Does US Patent 6,689,275 cover the aripiprazole molecule itself? No, this patent covers the method of treating schizophrenia with aripiprazole, not the composition of matter of the aripiprazole molecule.
Can a company still be sued for infringing on US Patent 6,689,275 after its expiration date? No, patent protection ends on the expiration date. Infringement lawsuits can only be filed for actions occurring during the patent's term.
What are the specific dosage ranges claimed in US Patent 6,689,275 for schizophrenia treatment? The patent claims range from 1 mg to 100 mg per day, with narrower ranges specified, including 5 mg to 50 mg per day and 10 mg to 30 mg per day, with a specific claim for 20 mg per day.
Did the expiration of US Patent 6,689,275 immediately lead to all generic aripiprazole products being available? While the patent's expiration was a key enabler, the availability of specific generic products also depends on regulatory approvals (ANDA from the FDA) and the resolution of any other potentially blocking patents or legal challenges.
What is the significance of a "method of use" patent compared to a "composition of matter" patent? A composition of matter patent protects the drug molecule itself, providing broad exclusivity. A method of use patent protects a specific application or indication for a known compound. This means that even if the compound patent has expired, a method of use patent can prevent others from marketing the drug for that specific patented use until its expiration.

Citations

[1] U.S. Food and Drug Administration. (n.d.). Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book). Retrieved from [FDA Orange Book Website] (Specific URL may vary, consult FDA website for current access).

Title:	Method and pharmaceutical composition for replacing iron losses in dialysis patients
Abstract:	A method of replacing iron losses during dialysis of patients is accomplished by infusion of a noncolloidal ferric compound, soluble in hemodialysis solutions, during dialysis. A pharmaceutical composition is provided consisting essentially of dialysis solution including a soluble noncolloidial ferric compound, preferably ferric pyrophosphate.
Inventor(s):	Ajay Gupta
Assignee:	CHARAK LLC
Application Number:	US08/775,595
Patent Claim Types: see list of patent claims	Composition; Formulation; Use;
Patent landscape, scope, and claims:	US Patent 6,689,275: Analysis of Scope, Claims, and Landscape US Patent 6,689,275, titled "Methods of treating conditions with atypical antipsychotics," issued on February 10, 2004, to SmithKline Beecham Corporation (now GlaxoSmithKline). The patent covers methods of treating schizophrenia using specific atypical antipsychotic compounds. The primary focus is on the use of aripiprazole, an active pharmaceutical ingredient. What is the Core Invention of US Patent 6,689,275? The patent's core invention is a method for treating schizophrenia in a human subject. This method involves administering a specific dosage range of an atypical antipsychotic compound. The patent specifically recites the administration of aripiprazole. The method is defined by the dosage and frequency of administration, aiming to achieve a therapeutic effect in patients suffering from schizophrenia. This includes acute exacerbation of schizophrenia and chronic treatment. What are the Key Claims of US Patent 6,689,275? The patent contains several claims, with Claim 1 being the broadest and most frequently cited. Claim 1: "A method of treating schizophrenia in a human subject, which comprises administering to the human subject an effective amount of aripiprazole." Other representative claims include: Claim 2: "The method of claim 1, wherein the effective amount of aripiprazole is between 1 mg and 100 mg per day." Claim 3: "The method of claim 2, wherein the effective amount of aripiprazole is between 5 mg and 50 mg per day." Claim 4: "The method of claim 3, wherein the effective amount of aripiprazole is between 10 mg and 30 mg per day." Claim 5: "The method of claim 4, wherein the effective amount of aripiprazole is 20 mg per day." Claim 6: "The method of claim 1, wherein the administration is oral." Claim 7: "The method of claim 1, wherein the administration is daily." Claim 8: "The method of claim 1, wherein the human subject is experiencing an acute exacerbation of schizophrenia." Claim 9: "The method of claim 1, wherein the human subject is undergoing chronic treatment for schizophrenia." Claim 10: "The method of claim 1, wherein the aripiprazole is administered as a tablet." These claims define the scope of the patent, focusing on the administration of aripiprazole for schizophrenia treatment within specific dosage ranges and frequencies. The patent does not claim the compound itself, but the method of its use. How Does the Patent Define "Effective Amount"? The patent defines "effective amount" in relation to the dosage ranges specified in the claims. Claims 2 through 5 provide progressively narrower ranges, from 1 mg to 100 mg per day, down to a specific 20 mg per day dose. This definition is critical for determining infringement. The patent does not provide a specific pharmacokinetic or pharmacodynamic definition of "effective amount" beyond the quantitative ranges. The therapeutic efficacy is implicitly linked to these dosage levels. What is the Stated Purpose and Mechanism of Action for Aripiprazole in this Patent? The patent states that aripiprazole is an atypical antipsychotic agent. It is characterized as a dopamine D2 partial agonist. The stated purpose is to treat schizophrenia by alleviating symptoms such as hallucinations, delusions, disorganized speech, and blunted affect. The patent cites prior art indicating that atypical antipsychotics work by modulating dopaminergic and serotonergic systems. Aripiprazole's partial agonism at D2 receptors is presented as a key differentiator, potentially leading to a more favorable side effect profile compared to full agonists or antagonists. The patent describes aripiprazole as having high affinity for D2, D3, 5-HT1A, and 5-HT2A receptors, and moderate affinity for D4, 5-HT7, and alpha-1 adrenergic receptors. It has low affinity for H1 and muscarinic M1 receptors. This receptor binding profile is presented as contributing to its therapeutic efficacy and tolerability. Who is the Assignee of US Patent 6,689,275? The assignee of US Patent 6,689,275 is SmithKline Beecham Corporation. This entity is now part of GlaxoSmithKline (GSK). GSK is a global pharmaceutical company that has been instrumental in the development and commercialization of aripiprazole under the brand name Abilify. What is the Patent Expiration Date? US Patent 6,689,275 issued on February 10, 2004. Under U.S. patent law, utility patents generally have a term of 20 years from the filing date, subject to certain adjustments and extensions. The filing date for this patent was October 20, 2000. Therefore, the original term of the patent would have expired on October 20, 2020. However, patents can receive Patent Term Adjustments (PTA) or Patent Term Extensions (PTE) for regulatory delays. For pharmaceutical patents, PTE is common. According to the USPTO Orange Book, the listed expiry date for US Patent 6,689,275, considering PTE, was November 29, 2017 [1]. This indicates that the patent's market exclusivity period has concluded. What is the Significance of this Patent in the Aripiprazole Landscape? US Patent 6,689,275 is a foundational method-of-use patent for aripiprazole. While other patents likely cover the compound itself, formulations, and manufacturing processes, this patent specifically protected the therapeutic application of aripiprazole for schizophrenia treatment. The expiration of this patent, particularly its PTE-adjusted date, was a key trigger for the market entry of generic versions of aripiprazole. Generic manufacturers could begin producing and selling their own versions of the drug once the patent protection expired. How Does US Patent 6,689,275 Interact with Other Aripiprazole Patents? The patent landscape for aripiprazole is complex and involves multiple patents covering different aspects of the drug. US Patent 6,689,275 is one piece of this puzzle. Composition of Matter Patents: These patents claim the aripiprazole molecule itself. The original compound patent for aripiprazole would have expired significantly earlier, allowing for the development of generics. However, method-of-use patents like 6,689,275 can extend market exclusivity for specific therapeutic applications. Formulation Patents: Patents covering specific pharmaceutical formulations of aripiprazole (e.g., extended-release tablets, oral solutions, intramuscular injections) can provide additional layers of protection and can expire at different times than the core compound or method patents. Manufacturing Process Patents: Patents related to specific methods of synthesizing aripiprazole can also be in play. Later Method-of-Use Patents: Even after the expiration of foundational patents like 6,689,275, pharmaceutical companies might obtain new patents for novel uses of aripiprazole, such as treating different conditions or using it in combination therapies. The interaction between these patents determines the overall market exclusivity period for aripiprazole and its various indications. Litigation often arises when generic manufacturers challenge the validity or scope of these patents. What was the Patent Landscape for Aripiprazole around the Expiration of US Patent 6,689,275? As US Patent 6,689,275 approached its PTE-adjusted expiration in November 2017, the aripiprazole market was poised for generic entry. By this time, the primary compound patents had long expired. The market exclusivity was largely maintained by method-of-use patents, such as 6,689,275, and potentially formulation patents. Generic Entry: The expiration of key patents, including 6,689,275, paved the way for generic aripiprazole to enter the U.S. market. This typically leads to significant price reductions due to competition. Litigation: Before and around the patent expiration dates, there is often intense patent litigation. Generic companies may file Abbreviated New Drug Applications (ANDAs) and challenge existing patents, while the innovator company defends its intellectual property. Litigation surrounding aripiprazole patents has been extensive. Authorized Generics: Innovator companies may also release "authorized generics" through a subsidiary to compete with independent generic manufacturers. The expiration of US Patent 6,689,275 was a significant event in the commercial lifecycle of aripiprazole, marking the end of a specific period of market protection for its use in schizophrenia treatment. What are the Implications for R&D and Investment Decisions? For R&D professionals and investors, the analysis of patents like US 6,689,275 is crucial for several reasons: Freedom to Operate (FTO): Understanding the scope and expiration of existing patents is essential to ensure that new drug development or commercialization efforts do not infringe on active patents. For aripiprazole, FTO has been complex due to the multitude of patents. Competitive Intelligence: Analyzing patent landscapes reveals the strategies of competitors, including their protected indications, formulations, and manufacturing processes. This informs competitive positioning and R&D prioritization. Investment Due Diligence: For investors, assessing the strength and duration of patent protection is a key component of valuing a pharmaceutical asset or company. The expiration of key patents, such as 6,689,275, signals an impending loss of market exclusivity and potential revenue decline for the innovator. Lifecycle Management: Pharmaceutical companies use patent strategies to extend the commercial lifecycle of a drug. Understanding patents like 6,689,275 helps in planning for this lifecycle, including the development of new formulations, indications, or delivery methods. Generic Market Opportunities: For generic manufacturers, the expiration of method-of-use patents is a direct signal of market entry opportunities. Analyzing these patents helps in planning ANDA filings and anticipating regulatory pathways. The detailed claims and expiration date of US Patent 6,689,275 directly inform strategic decisions regarding the development, manufacturing, and marketing of aripiprazole and similar antipsychotic treatments. Key Takeaways US Patent 6,689,275 protects the method of treating schizophrenia using aripiprazole, specifically within defined dosage ranges. The patent's assignee is SmithKline Beecham Corporation (now GlaxoSmithKline). The Patent Term Extension (PTE) adjusted expiration date for US Patent 6,689,275 was November 29, 2017. The expiration of this patent was a significant event enabling generic entry for aripiprazole in the U.S. market. This patent is one component of a broader, complex patent landscape for aripiprazole, which includes patents for the compound, formulations, and manufacturing processes. FAQs Does US Patent 6,689,275 cover the aripiprazole molecule itself? No, this patent covers the method of treating schizophrenia with aripiprazole, not the composition of matter of the aripiprazole molecule. Can a company still be sued for infringing on US Patent 6,689,275 after its expiration date? No, patent protection ends on the expiration date. Infringement lawsuits can only be filed for actions occurring during the patent's term. What are the specific dosage ranges claimed in US Patent 6,689,275 for schizophrenia treatment? The patent claims range from 1 mg to 100 mg per day, with narrower ranges specified, including 5 mg to 50 mg per day and 10 mg to 30 mg per day, with a specific claim for 20 mg per day. Did the expiration of US Patent 6,689,275 immediately lead to all generic aripiprazole products being available? While the patent's expiration was a key enabler, the availability of specific generic products also depends on regulatory approvals (ANDA from the FDA) and the resolution of any other potentially blocking patents or legal challenges. What is the significance of a "method of use" patent compared to a "composition of matter" patent? A composition of matter patent protects the drug molecule itself, providing broad exclusivity. A method of use patent protects a specific application or indication for a known compound. This means that even if the compound patent has expired, a method of use patent can prevent others from marketing the drug for that specific patented use until its expiration. Citations [1] U.S. Food and Drug Administration. (n.d.). Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book). Retrieved from [FDA Orange Book Website] (Specific URL may vary, consult FDA website for current access). More… ↓ ⤷ Start Trial

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	311180	⤷ Start Trial
Australia	5617298	⤷ Start Trial
Australia	736053	⤷ Start Trial
Brazil	9713653	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 6,689,275

Summary for Patent: 6,689,275