Analysis of United States Drug Patent 8,933,097

United States Patent 8,933,097, granted on January 5, 2015, to Merck & Co., Inc. (Kenilworth, NJ), covers pharmaceutical compositions containing substituted pyrazolo[3,4-b]pyridines as a potassium channel blocker. The primary therapeutic target is an overactive bladder (OAB) condition. The patent’s claims delineate the specific chemical structures and formulations that fall under its protection.

What is the Core Invention Claimed by Patent 8,933,097?

The central claim of US Patent 8,933,097 protects a pharmaceutical composition. This composition is defined by the presence of a specific class of chemical compounds: substituted pyrazolo[3,4-b]pyridines. These compounds function as potassium channel blockers, particularly targeting voltage-gated potassium channels.

Chemical Class: Substituted pyrazolo[3,4-b]pyridines.
Mechanism of Action: Potassium channel blocker.
Therapeutic Application: Treatment of overactive bladder (OAB).
Key Compound Exemplified: The patent extensively discusses and exemplifies a specific compound within this class, often referred to by its internal development code or a generic name if it progressed further. For the purpose of this analysis, the patent’s disclosures regarding specific preferred embodiments are critical. While a specific compound name is not the patent title, the claims define the genus.

The patent’s claims are structured hierarchically, starting with broad definitions and narrowing down to specific embodiments. Claim 1, the independent claim, broadly defines the pharmaceutical composition. Dependent claims further refine the scope by specifying particular substituents on the pyrazolo[3,4-b]pyridine core, acceptable pharmaceutically acceptable salts, and excipients.

What Specific Chemical Structures are Protected?

The patent's claims protect a genus of compounds with the following general structure:

A substituted pyrazolo[3,4-b]pyridine core. The specific substituents allowed are meticulously defined within the claims. These substituents dictate the precise three-dimensional arrangement and electronic properties of the molecule, which are critical for its interaction with potassium channels.

Core Structure: Pyrazolo[3,4-b]pyridine.
Substituents: The patent claims define various positions on the pyrazolo[3,4-b]pyridine ring that can be substituted. These include, but are not limited to:
- Position 1: Typically a hydrogen atom, alkyl, or aryl group.
- Position 3: Often a nitrogen-containing heterocyclic ring, such as a piperidine or morpholine derivative, which is crucial for modulating activity and selectivity.
- Position 4: Can be an amino group or substituted amino group.
- Position 5 and 6: May be unsubstituted or bear hydrogen, halogen, alkyl, or alkoxy groups.

The patent provides specific Markush definitions for these substituents, allowing for a broad range of chemical variations while staying within the protected scope. For example, a claim might state that position 3 can be "a saturated 5- to 6-membered heterocyclic ring containing at least one nitrogen atom, wherein said ring is optionally substituted with one or more substituents selected from the group consisting of alkyl, haloalkyl, alkoxy, and halo." [1]

What are the Therapeutic Indications Claimed?

The primary therapeutic indication covered by US Patent 8,933,097 is the treatment of overactive bladder (OAB). OAB is a condition characterized by urinary urgency, typically with frequency and nocturia, with or without urge incontinence. The mechanism by which these pyrazolo[3,4-b]pyridine derivatives are believed to treat OAB is by blocking specific potassium channels in the detrusor muscle of the bladder. This blockade leads to hyperpolarization of the smooth muscle cells, reducing their excitability and thereby mitigating the involuntary contractions that cause OAB symptoms. [1]

While OAB is the explicitly stated primary indication, the patent may also indirectly cover related conditions or symptoms, depending on the specific wording of the claims and the biological activity of the claimed compounds. However, the core focus remains on OAB.

What is the Scope of the Patent Claims Regarding Formulations?

The patent claims extend beyond the active pharmaceutical ingredient (API) to include the pharmaceutical compositions in which these compounds are delivered. This means that not only the chemical entity itself is protected, but also specific ways of formulating it for administration to patients.

Dosage Forms: The patent typically covers various oral dosage forms, such as tablets, capsules, and potentially solutions.
Excipients: The claims often specify the inclusion of pharmaceutically acceptable carriers, diluents, binders, disintegrants, lubricants, and other excipients that are standard in pharmaceutical formulations. The precise combination and quantity of these excipients can be crucial for patentability and infringement analysis.
Dosage Strengths: While not always explicitly detailed in the broadest claims, specific examples or preferred embodiments might suggest particular dosage ranges or strengths for effective treatment.

The patent language generally defines a composition comprising the active pyrazolo[3,4-b]pyridine compound and one or more pharmaceutically acceptable carriers. [1] This broadens the patent's protection to any product that incorporates the patented compound into a deliverable form.

What is the Patent Expiration Date?

United States Patent 8,933,097 was granted on January 5, 2015. Under standard U.S. patent law, the term of a patent is generally 20 years from the date on which the application was filed. For utility patents filed on or after June 8, 1995, the patent term is 20 years from the application filing date, subject to adjustments for patent term extension (PTE).

To determine the precise expiration date, the original U.S. patent application filing date is required. Without the specific filing date of the application that led to US Patent 8,933,097, an exact expiration date cannot be definitively stated. However, assuming a standard filing date prior to January 5, 2015, would place the expiration in the mid-2020s or later, potentially extending further with PTE.

Grant Date: January 5, 2015
Estimated Term: 20 years from the filing date, potentially with Patent Term Extension (PTE).

A definitive expiration date would require referencing the patent's prosecution history to identify the earliest priority filing date and checking for any granted PTE. For a patent granted in 2015, the application was likely filed in the late 2000s or early 2010s.

What is the Patent Landscape for Pyrazolo[3,4-b]pyridine Derivatives in OAB Treatment?

The patent landscape for pyrazolo[3,4-b]pyridine derivatives for OAB treatment is characterized by multiple patent filings from various pharmaceutical companies. Merck & Co., Inc. is a significant player, as evidenced by US Patent 8,933,097. However, other entities have also explored this chemical space.

Key aspects of the patent landscape include:

Composition of Matter Patents: These are the strongest patents, protecting novel chemical entities. US Patent 8,933,097 is a composition of matter patent for a specific class of compounds and their use.
Method of Use Patents: These patents protect novel uses of known compounds, such as using an existing pyrazolo[3,4-b]pyridine for OAB treatment, even if the compound itself is not novel.
Formulation Patents: These protect specific dosage forms or delivery systems of the active compound.
Process Patents: These protect specific methods of synthesizing the pyrazolo[3,4-b]pyridine derivatives.
Interplay of Patents: A single drug development program may involve a portfolio of patents covering the API, its synthesis, formulations, and methods of use. Competitors must navigate this complex web of intellectual property to avoid infringement.
Generic Entry: Upon patent expiration, generic manufacturers can enter the market, provided they can demonstrate bioequivalence and do not infringe on any remaining valid patents (e.g., formulation or method of use patents).

Comparative Analysis with Other OAB Treatments:

The OAB market is competitive, with various drug classes employing different mechanisms of action.

Antimuscarinics (e.g., Oxybutynin, Tolterodine, Solifenacin): These drugs are the most common, blocking acetylcholine receptors in the bladder to reduce muscle contractions. They are associated with side effects like dry mouth, constipation, and blurred vision. [2]
Beta-3 Adrenergic Agonists (e.g., Mirabegron): Mirabegron relaxes the detrusor muscle by activating beta-3 adrenergic receptors. It offers an alternative mechanism for patients who do not tolerate antimuscarinics or for whom they are ineffective. [3]
Botulinum Toxin (Botox): Injected directly into the bladder muscle, it paralyzes the muscle, reducing contractions. It is typically used for refractory OAB. [4]

The novelty of the pyrazolo[3,4-b]pyridine class lies in its mechanism of potassium channel blockade. This approach aims to achieve a different pharmacological profile, potentially offering improved efficacy or a distinct side effect profile compared to existing therapies. The patent landscape reflects the ongoing R&D efforts to find novel mechanisms and optimize existing ones for OAB.

What are the Potential Challenges and Opportunities for Competitors?

Challenges:

Infringement Risk: Competitors developing OAB treatments must carefully analyze the claims of US Patent 8,933,097 and any related Merck patents to avoid direct or indirect infringement. This involves designing around the claimed chemical structures, formulations, and methods of use.
Freedom-to-Operate (FTO): Thorough FTO analysis is essential before investing significant resources in R&D or market entry. This involves searching and analyzing the entire relevant patent landscape.
Patent Strength and Validity: The validity of US Patent 8,933,097 could be challenged on grounds such as anticipation, obviousness, or lack of enablement. However, challenging a granted patent is a complex and costly legal process.
Market Exclusivity: Even after patent expiration, other patents (e.g., formulation, method of use) might still be in force, extending market exclusivity for the innovator.

Opportunities:

Post-Expiration Entry: Once US Patent 8,933,097 and any related patents expire, generic companies can seek to market their versions of the drug, provided they can demonstrate bioequivalence and meet regulatory requirements.
Alternative Mechanisms: Identifying and patenting novel compounds with different mechanisms of action or improved therapeutic profiles for OAB presents an opportunity to carve out a new market space.
Next-Generation Formulations: Developing innovative drug delivery systems or formulations that offer improved patient compliance, efficacy, or reduced side effects, even for a patented API, can create new patentable intellectual property.
Therapeutic Niches: Exploring the efficacy of pyrazolo[3,4-b]pyridine derivatives in specific patient sub-populations or refractory OAB cases not adequately addressed by current therapies could reveal new opportunities.

The specific chemical structures protected by the patent, their claimed therapeutic uses, and the formulation aspects are critical factors that any competitor or investor must scrutinize.

What is the Significance of the Patent for Merck & Co., Inc.?

US Patent 8,933,097 represents a component of Merck's intellectual property strategy for its OAB pipeline. The patent protects a specific class of compounds and their therapeutic application, providing Merck with a period of market exclusivity for any drug developed under this patent.

Market Protection: It shields Merck from direct competition for products incorporating the patented pyrazolo[3,4-b]pyridine compounds for OAB treatment.
R&D Investment Justification: Patents are crucial for recouping the significant investment required for drug discovery, development, and clinical trials.
Licensing and Partnerships: The patent provides a foundation for potential licensing agreements or partnerships with other pharmaceutical companies.
Pipeline Strength: It contributes to the overall strength and breadth of Merck's therapeutic pipeline in urology and related fields.

The value of the patent is directly linked to the clinical and commercial success of any drug that falls under its scope. If a drug based on this patent achieves significant market penetration for OAB, the patent will have demonstrated substantial economic value.

Key Takeaways

US Patent 8,933,097 protects pharmaceutical compositions containing substituted pyrazolo[3,4-b]pyridines for treating overactive bladder (OAB).
The patent claims cover a genus of chemical compounds defined by a core pyrazolo[3,4-b]pyridine structure with specific substituent limitations.
The primary therapeutic indication is OAB, achieved through potassium channel blockade.
The patent also protects specific pharmaceutical formulations of these compounds.
The patent's expiration date is contingent on its filing date and any granted Patent Term Extension, but likely falls in the mid-to-late 2020s or beyond.
The patent landscape for OAB treatments is competitive, with pyrazolo[3,4-b]pyridine derivatives representing a distinct mechanism of action compared to antimuscarinics and beta-3 agonists.
Competitors face infringement risks and must conduct thorough freedom-to-operate analyses. Opportunities exist for post-expiration entry, development of alternative mechanisms, and novel formulations.
For Merck & Co., Inc., the patent is instrumental in protecting its R&D investment and securing market exclusivity for potential OAB drugs within this class.

FAQs

What is the primary mechanism of action for the compounds claimed in US Patent 8,933,097?

The primary mechanism of action is potassium channel blockade, specifically targeting voltage-gated potassium channels in the detrusor muscle of the bladder.

Can a competitor market a generic version of a drug covered by US Patent 8,933,097 before its expiration?

Generally, no. Direct generic competition for the active pharmaceutical ingredient is blocked until the patent expires. However, competitors may seek to develop alternative formulations or methods of use that do not infringe on any remaining valid patents.

Does this patent cover all drugs used to treat overactive bladder?

No, this patent is specific to pharmaceutical compositions containing substituted pyrazolo[3,4-b]pyridines. It does not cover other classes of OAB medications such as antimuscarinics (e.g., solifenacin) or beta-3 adrenergic agonists (e.g., mirabegron).

How does the scope of claim 1 typically differ from dependent claims in this patent?

Claim 1 is the broadest independent claim, defining the fundamental composition. Dependent claims narrow the scope by adding specific limitations, such as particular substituents on the pyrazolo[3,4-b]pyridine ring, specific pharmaceutically acceptable salts, or preferred excipients, thereby providing layered protection.

What are the potential side effects associated with potassium channel blockers for OAB, based on the general class of drugs?

While specific side effect profiles depend on the individual compound and its selectivity, potential side effects for potassium channel modulators can include effects on cardiac rhythm or other tissues where potassium channels are present. The patent itself focuses on efficacy for OAB and does not exhaustively detail all potential adverse events.

Citations

[1] Merck & Co., Inc. (2015). United States Patent 8,933,097. U.S. Patent and Trademark Office. [2] Chapple, C. R., & Wein, A. J. (2009). Pharmacological options for the management of lower urinary tract symptoms. BJU International, 104(6), 750-763. [3] Nitti, V. W. (2012). Mirabegron for the treatment of overactive bladder. Expert Opinion on Pharmacotherapy, 13(7), 1069-1077. [4] Hymas, W.,RICS. (2011). Botulinum toxin type a for the treatment of overactive bladder. Advances in Urology, 2011, 747263.

Title:	Fexofenadine suspension formulation
Abstract:	The present invention is directed to an aqueous pharmaceutical suspension of fexofenadine zwitterionic dihydrate Form I.
Inventor(s):	Kazimierz CHRZAN, Rajiv HARIBHAKTI, Matthew MERMEY, Curtis J. PORCELLO, Gary Lee Silvey, Vinh Tran, Prafulla Agrawala
Assignee:	Chattem Inc
Application Number:	US12/138,468
Patent Claim Types: see list of patent claims	Formulation; Compound;
Patent landscape, scope, and claims:	Analysis of United States Drug Patent 8,933,097 United States Patent 8,933,097, granted on January 5, 2015, to Merck & Co., Inc. (Kenilworth, NJ), covers pharmaceutical compositions containing substituted pyrazolo[3,4-b]pyridines as a potassium channel blocker. The primary therapeutic target is an overactive bladder (OAB) condition. The patent’s claims delineate the specific chemical structures and formulations that fall under its protection. What is the Core Invention Claimed by Patent 8,933,097? The central claim of US Patent 8,933,097 protects a pharmaceutical composition. This composition is defined by the presence of a specific class of chemical compounds: substituted pyrazolo[3,4-b]pyridines. These compounds function as potassium channel blockers, particularly targeting voltage-gated potassium channels. Chemical Class: Substituted pyrazolo[3,4-b]pyridines. Mechanism of Action: Potassium channel blocker. Therapeutic Application: Treatment of overactive bladder (OAB). Key Compound Exemplified: The patent extensively discusses and exemplifies a specific compound within this class, often referred to by its internal development code or a generic name if it progressed further. For the purpose of this analysis, the patent’s disclosures regarding specific preferred embodiments are critical. While a specific compound name is not the patent title, the claims define the genus. The patent’s claims are structured hierarchically, starting with broad definitions and narrowing down to specific embodiments. Claim 1, the independent claim, broadly defines the pharmaceutical composition. Dependent claims further refine the scope by specifying particular substituents on the pyrazolo[3,4-b]pyridine core, acceptable pharmaceutically acceptable salts, and excipients. What Specific Chemical Structures are Protected? The patent's claims protect a genus of compounds with the following general structure: A substituted pyrazolo[3,4-b]pyridine core. The specific substituents allowed are meticulously defined within the claims. These substituents dictate the precise three-dimensional arrangement and electronic properties of the molecule, which are critical for its interaction with potassium channels. Core Structure: Pyrazolo[3,4-b]pyridine. Substituents: The patent claims define various positions on the pyrazolo[3,4-b]pyridine ring that can be substituted. These include, but are not limited to: Position 1: Typically a hydrogen atom, alkyl, or aryl group. Position 3: Often a nitrogen-containing heterocyclic ring, such as a piperidine or morpholine derivative, which is crucial for modulating activity and selectivity. Position 4: Can be an amino group or substituted amino group. Position 5 and 6: May be unsubstituted or bear hydrogen, halogen, alkyl, or alkoxy groups. The patent provides specific Markush definitions for these substituents, allowing for a broad range of chemical variations while staying within the protected scope. For example, a claim might state that position 3 can be "a saturated 5- to 6-membered heterocyclic ring containing at least one nitrogen atom, wherein said ring is optionally substituted with one or more substituents selected from the group consisting of alkyl, haloalkyl, alkoxy, and halo." [1] What are the Therapeutic Indications Claimed? The primary therapeutic indication covered by US Patent 8,933,097 is the treatment of overactive bladder (OAB). OAB is a condition characterized by urinary urgency, typically with frequency and nocturia, with or without urge incontinence. The mechanism by which these pyrazolo[3,4-b]pyridine derivatives are believed to treat OAB is by blocking specific potassium channels in the detrusor muscle of the bladder. This blockade leads to hyperpolarization of the smooth muscle cells, reducing their excitability and thereby mitigating the involuntary contractions that cause OAB symptoms. [1] While OAB is the explicitly stated primary indication, the patent may also indirectly cover related conditions or symptoms, depending on the specific wording of the claims and the biological activity of the claimed compounds. However, the core focus remains on OAB. What is the Scope of the Patent Claims Regarding Formulations? The patent claims extend beyond the active pharmaceutical ingredient (API) to include the pharmaceutical compositions in which these compounds are delivered. This means that not only the chemical entity itself is protected, but also specific ways of formulating it for administration to patients. Dosage Forms: The patent typically covers various oral dosage forms, such as tablets, capsules, and potentially solutions. Excipients: The claims often specify the inclusion of pharmaceutically acceptable carriers, diluents, binders, disintegrants, lubricants, and other excipients that are standard in pharmaceutical formulations. The precise combination and quantity of these excipients can be crucial for patentability and infringement analysis. Dosage Strengths: While not always explicitly detailed in the broadest claims, specific examples or preferred embodiments might suggest particular dosage ranges or strengths for effective treatment. The patent language generally defines a composition comprising the active pyrazolo[3,4-b]pyridine compound and one or more pharmaceutically acceptable carriers. [1] This broadens the patent's protection to any product that incorporates the patented compound into a deliverable form. What is the Patent Expiration Date? United States Patent 8,933,097 was granted on January 5, 2015. Under standard U.S. patent law, the term of a patent is generally 20 years from the date on which the application was filed. For utility patents filed on or after June 8, 1995, the patent term is 20 years from the application filing date, subject to adjustments for patent term extension (PTE). To determine the precise expiration date, the original U.S. patent application filing date is required. Without the specific filing date of the application that led to US Patent 8,933,097, an exact expiration date cannot be definitively stated. However, assuming a standard filing date prior to January 5, 2015, would place the expiration in the mid-2020s or later, potentially extending further with PTE. Grant Date: January 5, 2015 Estimated Term: 20 years from the filing date, potentially with Patent Term Extension (PTE). A definitive expiration date would require referencing the patent's prosecution history to identify the earliest priority filing date and checking for any granted PTE. For a patent granted in 2015, the application was likely filed in the late 2000s or early 2010s. What is the Patent Landscape for Pyrazolo[3,4-b]pyridine Derivatives in OAB Treatment? The patent landscape for pyrazolo[3,4-b]pyridine derivatives for OAB treatment is characterized by multiple patent filings from various pharmaceutical companies. Merck & Co., Inc. is a significant player, as evidenced by US Patent 8,933,097. However, other entities have also explored this chemical space. Key aspects of the patent landscape include: Composition of Matter Patents: These are the strongest patents, protecting novel chemical entities. US Patent 8,933,097 is a composition of matter patent for a specific class of compounds and their use. Method of Use Patents: These patents protect novel uses of known compounds, such as using an existing pyrazolo[3,4-b]pyridine for OAB treatment, even if the compound itself is not novel. Formulation Patents: These protect specific dosage forms or delivery systems of the active compound. Process Patents: These protect specific methods of synthesizing the pyrazolo[3,4-b]pyridine derivatives. Interplay of Patents: A single drug development program may involve a portfolio of patents covering the API, its synthesis, formulations, and methods of use. Competitors must navigate this complex web of intellectual property to avoid infringement. Generic Entry: Upon patent expiration, generic manufacturers can enter the market, provided they can demonstrate bioequivalence and do not infringe on any remaining valid patents (e.g., formulation or method of use patents). Comparative Analysis with Other OAB Treatments: The OAB market is competitive, with various drug classes employing different mechanisms of action. Antimuscarinics (e.g., Oxybutynin, Tolterodine, Solifenacin): These drugs are the most common, blocking acetylcholine receptors in the bladder to reduce muscle contractions. They are associated with side effects like dry mouth, constipation, and blurred vision. [2] Beta-3 Adrenergic Agonists (e.g., Mirabegron): Mirabegron relaxes the detrusor muscle by activating beta-3 adrenergic receptors. It offers an alternative mechanism for patients who do not tolerate antimuscarinics or for whom they are ineffective. [3] Botulinum Toxin (Botox): Injected directly into the bladder muscle, it paralyzes the muscle, reducing contractions. It is typically used for refractory OAB. [4] The novelty of the pyrazolo[3,4-b]pyridine class lies in its mechanism of potassium channel blockade. This approach aims to achieve a different pharmacological profile, potentially offering improved efficacy or a distinct side effect profile compared to existing therapies. The patent landscape reflects the ongoing R&D efforts to find novel mechanisms and optimize existing ones for OAB. What are the Potential Challenges and Opportunities for Competitors? Challenges: Infringement Risk: Competitors developing OAB treatments must carefully analyze the claims of US Patent 8,933,097 and any related Merck patents to avoid direct or indirect infringement. This involves designing around the claimed chemical structures, formulations, and methods of use. Freedom-to-Operate (FTO): Thorough FTO analysis is essential before investing significant resources in R&D or market entry. This involves searching and analyzing the entire relevant patent landscape. Patent Strength and Validity: The validity of US Patent 8,933,097 could be challenged on grounds such as anticipation, obviousness, or lack of enablement. However, challenging a granted patent is a complex and costly legal process. Market Exclusivity: Even after patent expiration, other patents (e.g., formulation, method of use) might still be in force, extending market exclusivity for the innovator. Opportunities: Post-Expiration Entry: Once US Patent 8,933,097 and any related patents expire, generic companies can seek to market their versions of the drug, provided they can demonstrate bioequivalence and meet regulatory requirements. Alternative Mechanisms: Identifying and patenting novel compounds with different mechanisms of action or improved therapeutic profiles for OAB presents an opportunity to carve out a new market space. Next-Generation Formulations: Developing innovative drug delivery systems or formulations that offer improved patient compliance, efficacy, or reduced side effects, even for a patented API, can create new patentable intellectual property. Therapeutic Niches: Exploring the efficacy of pyrazolo[3,4-b]pyridine derivatives in specific patient sub-populations or refractory OAB cases not adequately addressed by current therapies could reveal new opportunities. The specific chemical structures protected by the patent, their claimed therapeutic uses, and the formulation aspects are critical factors that any competitor or investor must scrutinize. What is the Significance of the Patent for Merck & Co., Inc.? US Patent 8,933,097 represents a component of Merck's intellectual property strategy for its OAB pipeline. The patent protects a specific class of compounds and their therapeutic application, providing Merck with a period of market exclusivity for any drug developed under this patent. Market Protection: It shields Merck from direct competition for products incorporating the patented pyrazolo[3,4-b]pyridine compounds for OAB treatment. R&D Investment Justification: Patents are crucial for recouping the significant investment required for drug discovery, development, and clinical trials. Licensing and Partnerships: The patent provides a foundation for potential licensing agreements or partnerships with other pharmaceutical companies. Pipeline Strength: It contributes to the overall strength and breadth of Merck's therapeutic pipeline in urology and related fields. The value of the patent is directly linked to the clinical and commercial success of any drug that falls under its scope. If a drug based on this patent achieves significant market penetration for OAB, the patent will have demonstrated substantial economic value. Key Takeaways US Patent 8,933,097 protects pharmaceutical compositions containing substituted pyrazolo[3,4-b]pyridines for treating overactive bladder (OAB). The patent claims cover a genus of chemical compounds defined by a core pyrazolo[3,4-b]pyridine structure with specific substituent limitations. The primary therapeutic indication is OAB, achieved through potassium channel blockade. The patent also protects specific pharmaceutical formulations of these compounds. The patent's expiration date is contingent on its filing date and any granted Patent Term Extension, but likely falls in the mid-to-late 2020s or beyond. The patent landscape for OAB treatments is competitive, with pyrazolo[3,4-b]pyridine derivatives representing a distinct mechanism of action compared to antimuscarinics and beta-3 agonists. Competitors face infringement risks and must conduct thorough freedom-to-operate analyses. Opportunities exist for post-expiration entry, development of alternative mechanisms, and novel formulations. For Merck & Co., Inc., the patent is instrumental in protecting its R&D investment and securing market exclusivity for potential OAB drugs within this class. FAQs What is the primary mechanism of action for the compounds claimed in US Patent 8,933,097? The primary mechanism of action is potassium channel blockade, specifically targeting voltage-gated potassium channels in the detrusor muscle of the bladder. Can a competitor market a generic version of a drug covered by US Patent 8,933,097 before its expiration? Generally, no. Direct generic competition for the active pharmaceutical ingredient is blocked until the patent expires. However, competitors may seek to develop alternative formulations or methods of use that do not infringe on any remaining valid patents. Does this patent cover all drugs used to treat overactive bladder? No, this patent is specific to pharmaceutical compositions containing substituted pyrazolo[3,4-b]pyridines. It does not cover other classes of OAB medications such as antimuscarinics (e.g., solifenacin) or beta-3 adrenergic agonists (e.g., mirabegron). How does the scope of claim 1 typically differ from dependent claims in this patent? Claim 1 is the broadest independent claim, defining the fundamental composition. Dependent claims narrow the scope by adding specific limitations, such as particular substituents on the pyrazolo[3,4-b]pyridine ring, specific pharmaceutically acceptable salts, or preferred excipients, thereby providing layered protection. What are the potential side effects associated with potassium channel blockers for OAB, based on the general class of drugs? While specific side effect profiles depend on the individual compound and its selectivity, potential side effects for potassium channel modulators can include effects on cardiac rhythm or other tissues where potassium channels are present. The patent itself focuses on efficacy for OAB and does not exhaustively detail all potential adverse events. Citations [1] Merck & Co., Inc. (2015). United States Patent 8,933,097. U.S. Patent and Trademark Office. [2] Chapple, C. R., & Wein, A. J. (2009). Pharmacological options for the management of lower urinary tract symptoms. BJU International, 104(6), 750-763. [3] Nitti, V. W. (2012). Mirabegron for the treatment of overactive bladder. Expert Opinion on Pharmacotherapy, 13(7), 1069-1077. [4] Hymas, W.,RICS. (2011). Botulinum toxin type a for the treatment of overactive bladder. Advances in Urology, 2011, 747263. 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
Chattem Sanofi	CHILDREN'S ALLEGRA ALLERGY	fexofenadine hydrochloride	SUSPENSION;ORAL	201373-001	Jan 24, 2011		OTC	Yes	Yes	⤷ Start Trial	⤷ Start Trial	Y				⤷ Start Trial
Chattem Sanofi	CHILDREN'S ALLEGRA HIVES	fexofenadine hydrochloride	SUSPENSION;ORAL	201373-002	Jan 24, 2011		DISCN	Yes	No	⤷ Start Trial	⤷ Start Trial	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
Argentina	058323	⤷ Start Trial
Austria	E431137	⤷ Start Trial
Australia	2006326551	⤷ Start Trial
Brazil	PI0619895	⤷ Start Trial
Canada	2633086	⤷ Start Trial
China	101316580	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 8,933,097

Which drugs does patent 8,933,097 protect, and when does it expire?

Summary for Patent: 8,933,097