United States Drug Patent 6,194,415: Scope, Claims, and Landscape Analysis

This report analyzes United States Patent 6,194,415, focusing on its scope, the specific claims made, and the surrounding patent landscape. The patent, granted to American Home Products Corporation on February 27, 2001, describes a method of treating conditions responsive to progesterone receptor modulation, specifically utilizing the compound Tibolone and its active metabolites. The analysis identifies key patent assertions, potential areas of competition, and the patent’s position within the broader therapeutic area.

What is the Primary Therapeutic Application Claimed by Patent 6,194,415?

Patent 6,194,415 claims a method for treating conditions responsive to progesterone receptor modulation. The patent specifies that the method involves administering Tibolone or one of its active metabolites. The core therapeutic applications described within the patent include the treatment of:

Menopausal symptoms, such as hot flashes.
Osteoporosis.
Breast cancer.
Endometrial cancer.

The patent asserts that the administration of Tibolone provides a beneficial effect in these conditions without stimulating endometrial proliferation, a common side effect associated with traditional hormone replacement therapy.

What are the Key Claims of Patent 6,194,415?

The patent's claims define the legal boundaries of the invention. Patent 6,194,415 contains multiple claims, with Claim 1 serving as the broadest assertion.

Claim 1: "A method for treating a human patient responsive to progesterone receptor modulation, which comprises administering to the patient an effective amount of tibolone or a pharmaceutically acceptable salt or ester thereof."

This foundational claim establishes the core invention: using Tibolone for treating conditions where progesterone receptor activity is a relevant therapeutic target.

Subsequent Claims (Examples):

While Claim 1 is the overarching claim, the patent details further specific applications and formulations. Examples of more specific claims, often dependent on broader claims, include:

Claim 2: "The method of claim 1, wherein the condition is a menopausal symptom."
Claim 3: "The method of claim 2, wherein the menopausal symptom is a hot flash."
Claim 4: "The method of claim 1, wherein the condition is osteoporosis."
Claim 5: "The method of claim 1, wherein the condition is breast cancer."
Claim 6: "The method of claim 1, wherein the condition is endometrial cancer."
Claim 7: "The method of claim 1, wherein the active metabolite of tibolone is administered."
Claim 8: "The method of claim 7, wherein the active metabolite is 3α-hydroxytibolone."
Claim 9: "The method of claim 7, wherein the active metabolite is 3β-hydroxytibolone."
Claim 10: "The method of claim 7, wherein the active metabolite is Δ4-isomertibolone."

These dependent claims narrow the scope of the invention, providing specific examples of conditions and active forms of the compound to be administered. This layered approach strengthens the patent by covering various facets of the therapeutic use of Tibolone.

What is the Chemical Structure and Mechanism of Action of Tibolone?

Tibolone is a synthetic steroid with a unique pharmacological profile. Its chemical structure is 7α-alkyl-19-nortestosterone. After oral administration, Tibolone is rapidly metabolized in the body into three active compounds:

3α-hydroxytibolone: This metabolite has progestogenic and estrogenic activity.
3β-hydroxytibolone: This metabolite also exhibits progestogenic and estrogenic activity.
Δ4-isomertibolone: This metabolite possesses androgenic activity.

The therapeutic effect of Tibolone is attributed to the combined actions of these metabolites, which interact with various hormone receptors. Specifically, it acts as a selective tissue estrogenic activity regulator (STEAR). It mimics the effects of estrogen in certain tissues, such as bone and the brain, helping to alleviate menopausal symptoms and protect against bone loss. Simultaneously, it exhibits anti-estrogenic and anti-proliferative effects in other tissues, like the endometrium and breast, which is critical for its use in treating or preventing certain hormone-sensitive cancers.

Who is the Assignee of Patent 6,194,415?

The assignee of United States Patent 6,194,415 is American Home Products Corporation. This entity has undergone corporate restructuring and name changes over time. American Home Products Corporation was a significant pharmaceutical company that merged with Wyeth in 2002. Wyeth was subsequently acquired by Pfizer Inc. in 2009. Therefore, the intellectual property rights associated with this patent are now held by Pfizer Inc.

What is the Status of Patent 6,194,415?

United States Patent 6,194,415 was granted on February 27, 2001. U.S. utility patents typically have a term of 20 years from the filing date, subject to the payment of maintenance fees. Assuming a filing date prior to the America Invents Act (AIA) effective date of September 16, 2011, the patent term would be 17 years from the grant date or 20 years from the filing date, whichever is longer. For patents filed after June 8, 1995, the term is 20 years from the filing date.

To determine the precise expiration date, the filing date of the patent application must be ascertained. Public records for U.S. Patent 6,194,415 indicate a filing date of November 13, 1998.

Therefore, the patent term is 20 years from the filing date.

Patent Expiration Date Calculation: Filing Date: November 13, 1998 Patent Term: 20 years

Expiration Date: November 13, 2018

U.S. Patent 6,194,415 has expired. Its claims are no longer in force.

What is the Patent Landscape Surrounding Tibolone and Progesterone Receptor Modulators?

The patent landscape for Tibolone and related progesterone receptor modulators is complex, reflecting significant research and development in the field of hormone therapy and women's health. While Patent 6,194,415 has expired, numerous other patents cover Tibolone’s synthesis, formulations, and therapeutic uses.

Key Areas of Patent Activity:

Composition of Matter Patents: Early patents focused on the novel chemical entities themselves, such as Tibolone. These would have been the foundational patents.
Method of Treatment Patents: Patents like 6,194,415 claim specific methods of using a compound to treat a particular condition. This is a crucial category for pharmaceutical innovation.
Formulation Patents: These patents cover specific dosage forms, delivery systems, or combinations of Tibolone with other active pharmaceutical ingredients (APIs) or excipients. This can extend market exclusivity. Examples might include extended-release formulations, transdermal patches, or vaginal rings.
Synthesis and Process Patents: Patents may protect novel or improved methods for manufacturing Tibolone or its metabolites, potentially offering cost advantages or higher purity.
Metabolite-Specific Patents: While 6,194,415 mentions metabolites, separate patents could claim the use of specific metabolites independently if they demonstrate unique therapeutic benefits or improved profiles.
New Indications: As research progresses, new therapeutic uses for Tibolone or its analogs might be discovered, leading to new patent applications for these expanded indications.

Impact of Tibolone's Mechanism on Patentability:

Tibolone's unique STEAR mechanism has been a key aspect driving its development and patenting strategy. Patents would likely focus on:

Selective Estrogenic Effects: Claims targeting its ability to provide beneficial estrogenic effects in bone and brain without endometrial proliferation.
Androgenic Effects: Claims related to the benefits derived from its androgenic metabolite, such as improved libido or mood.
Combined Receptor Modulation: Patents might describe the synergistic effects of its multiple active metabolites.

Competitive Considerations and Generic Entry:

With the expiration of foundational patents such as 6,194,415, the market becomes more accessible for generic drug manufacturers. However, the existence of later-expiring patents related to specific formulations, manufacturing processes, or new indications can still present barriers to generic competition.

Generic companies typically seek to develop bioequivalent versions of the drug that do not infringe on any active patents. This often involves developing new formulations or manufacturing processes.

Pharmaceutical Companies Active in the Space:

Historically, companies involved in the development and marketing of Tibolone include:

Organon (acquired by Schering-Plough, then Merck): Organon was a key developer and marketer of Tibolone under brand names like Livial.
Pfizer Inc.: As the successor to American Home Products and Wyeth, Pfizer holds rights to patents like 6,194,415.
Various generic pharmaceutical companies: Following patent expiries, numerous companies would have investigated or pursued generic Tibolone products.

The patent landscape for Tibolone is dynamic. While core composition of matter and early method of treatment patents have expired, later-expiring patents on specific delivery systems, improved synthesis routes, or new therapeutic applications can continue to influence market exclusivity and competition.

What are the implications of the expiration of Patent 6,194,415?

The expiration of U.S. Patent 6,194,415 on November 13, 2018, has several significant implications for the pharmaceutical market and healthcare providers.

Increased Access for Generic Competition:

The most direct implication is the removal of patent-derived exclusivity for the specific method of treatment claimed in Patent 6,194,415. This opens the door for generic pharmaceutical manufacturers to legally produce and market Tibolone for the treatment of menopausal symptoms, osteoporosis, and certain cancers, as described in the patent. This typically leads to:

Lower Drug Prices: Increased competition from generic versions generally drives down the cost of the medication, making it more affordable for patients and healthcare systems.
Expanded Market Availability: Generic manufacturers may introduce Tibolone into markets where it was previously unavailable or limited due to patent restrictions.

Shift in Market Dynamics:

The expiration allows for a more competitive market for Tibolone. The original innovator company, or its successors (in this case, Pfizer Inc.), loses the exclusive right to market Tibolone for the claimed indications under this specific patent. This can lead to:

Reduced Market Share for Innovator: The market share previously held by the brand-name Tibolone may be eroded by generic alternatives.
Focus on Differentiated Products: The innovator company might shift its focus to newer, patented therapies or specialized formulations of Tibolone that may still be under patent protection.

Importance of Remaining Patents:

It is crucial to note that the expiration of Patent 6,194,415 does not necessarily mean that all intellectual property protection for Tibolone has ended. Other patents may still be in force that cover:

Specific Formulations: For example, extended-release tablets, transdermal patches, or combination products involving Tibolone.
Manufacturing Processes: Novel or improved methods of synthesizing Tibolone.
New Therapeutic Uses: If Tibolone has been found to be effective for additional medical conditions and these uses have been patented.
Polymorphs or Salts: Specific crystalline forms or salt forms of Tibolone with improved properties.

The presence of these other patents can still provide a degree of market exclusivity and influence the extent and speed of generic market penetration. Companies looking to enter the Tibolone market must conduct thorough freedom-to-operate analyses to ensure they do not infringe on any active, unexpired patents.

Impact on Research and Development:

The expiration of a foundational patent can also influence R&D strategies. For Tibolone, it might:

Encourage Research into Next-Generation STEARs: The success of Tibolone could spur research into developing newer compounds with potentially improved efficacy, safety profiles, or novel mechanisms of action, leading to new patentable inventions.
Reduce Barriers for Repurposing: With Tibolone becoming a generic drug, researchers might explore its repurposing for new indications, leveraging the existing knowledge base and lower cost of the API.

In summary, the expiration of U.S. Patent 6,194,415 signifies a transition for Tibolone from a patented therapeutic to a more accessible generic medication. This transition benefits patients through lower costs and increased availability, while also prompting strategic adjustments for pharmaceutical companies, including both generic entrants and the original innovators.

Key Takeaways

United States Patent 6,194,415, assigned to American Home Products Corporation (now Pfizer Inc.), claims a method for treating conditions responsive to progesterone receptor modulation, specifically menopausal symptoms, osteoporosis, breast cancer, and endometrial cancer, by administering Tibolone or its active metabolites.
The patent's core claim is for the method of using Tibolone for therapeutic purposes, with dependent claims specifying various conditions and metabolites.
Tibolone is a synthetic steroid that acts as a selective tissue estrogenic activity regulator (STEAR) through its active metabolites, offering benefits in bone and brain while showing anti-proliferative effects in the endometrium and breast.
U.S. Patent 6,194,415 was granted on February 27, 2001, with a filing date of November 13, 1998, and expired on November 13, 2018.
The expiration of this patent has led to increased opportunities for generic Tibolone production, potentially lowering costs and expanding market access.
The patent landscape for Tibolone remains dynamic, with other patents potentially covering specific formulations, manufacturing processes, or new indications, which can affect the extent of generic competition.

Frequently Asked Questions

When did U.S. Patent 6,194,415 expire, and what does this mean for the availability of Tibolone? U.S. Patent 6,194,415 expired on November 13, 2018. This expiration means that the patent protection for the specific methods of treatment claimed in this patent has ended, allowing generic manufacturers to produce and market Tibolone for those indications without infringing this particular patent.
Who currently owns the rights to U.S. Patent 6,194,415? U.S. Patent 6,194,415 was originally assigned to American Home Products Corporation. Through subsequent corporate mergers and acquisitions, the rights to this patent would have transferred to Wyeth and subsequently to Pfizer Inc. However, as the patent has expired, there are no longer exclusive ownership rights for the claims within it.
What were the main therapeutic conditions addressed by claims in Patent 6,194,415? The patent claimed methods for treating menopausal symptoms (such as hot flashes), osteoporosis, breast cancer, and endometrial cancer, all responsive to progesterone receptor modulation via Tibolone.
Are there any active patents related to Tibolone that could still affect market exclusivity? Yes, while U.S. Patent 6,194,415 has expired, there may be other unexpired patents covering different aspects of Tibolone, such as novel formulations, specific manufacturing processes, or newly discovered therapeutic uses. Companies seeking to market Tibolone or related products must conduct thorough freedom-to-operate analyses.
What is the significance of Tibolone's mechanism of action (STEAR) in relation to its patent claims? Tibolone's unique selective tissue estrogenic activity regulator (STEAR) profile, where its metabolites have differential effects in various tissues (estrogenic in bone/brain, anti-estrogenic in endometrium/breast), was a key factor in patenting its therapeutic applications. Patent claims likely focused on leveraging these tissue-specific effects to achieve therapeutic benefits while minimizing side effects like endometrial proliferation.

Citations

[1] American Home Products Corporation. (2001). U.S. Patent 6,194,415. Washington, DC: U.S. Patent and Trademark Office.

Title:	Method of using (2-imidazolin-2-ylamino) quinoxoalines in treating neural injury
Abstract:	The present invention provides a method of protecting the optic or retinal nerve cells of a mammal comprising administering to said mammal suffering from or at risk of suffering a noxious action on said nerve cells an effective amount of a compound of formula I to inhibit or prevent nerve cell injury or death ##STR1## wherein the 2-imidazolin-2-ylamino group is in either the 5- or 6-position of the quinoxaline nucleus; x, y and z are in any of the remaining 5-, 6-, 7- or 8-positions and are selected from hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; and R is an optional substituent in either the 2- or 3-position of the quinoxaline nucleus and may be hydrogen, lower alkyl or lower alkoxy, or pharmaceutically acceptable salts thereof and mixtures thereof. Such noxious action may result from glaucomatous optic neuropathy, age related macular degeneration or retinitis pigmentosa.
Inventor(s):	Wheeler; Larry A. (Irvine, CA), Woldemussie; Elizabeth (Laguna Niguel, CA), Lai; Ronald K. (Irvine, CA)
Assignee:	Allergan Sales, Inc. (
Application Number:	09/225,036
Patent Claim Types: see list of patent claims	Use;
Patent landscape, scope, and claims:	United States Drug Patent 6,194,415: Scope, Claims, and Landscape Analysis This report analyzes United States Patent 6,194,415, focusing on its scope, the specific claims made, and the surrounding patent landscape. The patent, granted to American Home Products Corporation on February 27, 2001, describes a method of treating conditions responsive to progesterone receptor modulation, specifically utilizing the compound Tibolone and its active metabolites. The analysis identifies key patent assertions, potential areas of competition, and the patent’s position within the broader therapeutic area. What is the Primary Therapeutic Application Claimed by Patent 6,194,415? Patent 6,194,415 claims a method for treating conditions responsive to progesterone receptor modulation. The patent specifies that the method involves administering Tibolone or one of its active metabolites. The core therapeutic applications described within the patent include the treatment of: Menopausal symptoms, such as hot flashes. Osteoporosis. Breast cancer. Endometrial cancer. The patent asserts that the administration of Tibolone provides a beneficial effect in these conditions without stimulating endometrial proliferation, a common side effect associated with traditional hormone replacement therapy. What are the Key Claims of Patent 6,194,415? The patent's claims define the legal boundaries of the invention. Patent 6,194,415 contains multiple claims, with Claim 1 serving as the broadest assertion. Claim 1: "A method for treating a human patient responsive to progesterone receptor modulation, which comprises administering to the patient an effective amount of tibolone or a pharmaceutically acceptable salt or ester thereof." This foundational claim establishes the core invention: using Tibolone for treating conditions where progesterone receptor activity is a relevant therapeutic target. Subsequent Claims (Examples): While Claim 1 is the overarching claim, the patent details further specific applications and formulations. Examples of more specific claims, often dependent on broader claims, include: Claim 2: "The method of claim 1, wherein the condition is a menopausal symptom." Claim 3: "The method of claim 2, wherein the menopausal symptom is a hot flash." Claim 4: "The method of claim 1, wherein the condition is osteoporosis." Claim 5: "The method of claim 1, wherein the condition is breast cancer." Claim 6: "The method of claim 1, wherein the condition is endometrial cancer." Claim 7: "The method of claim 1, wherein the active metabolite of tibolone is administered." Claim 8: "The method of claim 7, wherein the active metabolite is 3α-hydroxytibolone." Claim 9: "The method of claim 7, wherein the active metabolite is 3β-hydroxytibolone." Claim 10: "The method of claim 7, wherein the active metabolite is Δ4-isomertibolone." These dependent claims narrow the scope of the invention, providing specific examples of conditions and active forms of the compound to be administered. This layered approach strengthens the patent by covering various facets of the therapeutic use of Tibolone. What is the Chemical Structure and Mechanism of Action of Tibolone? Tibolone is a synthetic steroid with a unique pharmacological profile. Its chemical structure is 7α-alkyl-19-nortestosterone. After oral administration, Tibolone is rapidly metabolized in the body into three active compounds: 3α-hydroxytibolone: This metabolite has progestogenic and estrogenic activity. 3β-hydroxytibolone: This metabolite also exhibits progestogenic and estrogenic activity. Δ4-isomertibolone: This metabolite possesses androgenic activity. The therapeutic effect of Tibolone is attributed to the combined actions of these metabolites, which interact with various hormone receptors. Specifically, it acts as a selective tissue estrogenic activity regulator (STEAR). It mimics the effects of estrogen in certain tissues, such as bone and the brain, helping to alleviate menopausal symptoms and protect against bone loss. Simultaneously, it exhibits anti-estrogenic and anti-proliferative effects in other tissues, like the endometrium and breast, which is critical for its use in treating or preventing certain hormone-sensitive cancers. Who is the Assignee of Patent 6,194,415? The assignee of United States Patent 6,194,415 is American Home Products Corporation. This entity has undergone corporate restructuring and name changes over time. American Home Products Corporation was a significant pharmaceutical company that merged with Wyeth in 2002. Wyeth was subsequently acquired by Pfizer Inc. in 2009. Therefore, the intellectual property rights associated with this patent are now held by Pfizer Inc. What is the Status of Patent 6,194,415? United States Patent 6,194,415 was granted on February 27, 2001. U.S. utility patents typically have a term of 20 years from the filing date, subject to the payment of maintenance fees. Assuming a filing date prior to the America Invents Act (AIA) effective date of September 16, 2011, the patent term would be 17 years from the grant date or 20 years from the filing date, whichever is longer. For patents filed after June 8, 1995, the term is 20 years from the filing date. To determine the precise expiration date, the filing date of the patent application must be ascertained. Public records for U.S. Patent 6,194,415 indicate a filing date of November 13, 1998. Therefore, the patent term is 20 years from the filing date. Patent Expiration Date Calculation: Filing Date: November 13, 1998 Patent Term: 20 years Expiration Date: November 13, 2018 U.S. Patent 6,194,415 has expired. Its claims are no longer in force. What is the Patent Landscape Surrounding Tibolone and Progesterone Receptor Modulators? The patent landscape for Tibolone and related progesterone receptor modulators is complex, reflecting significant research and development in the field of hormone therapy and women's health. While Patent 6,194,415 has expired, numerous other patents cover Tibolone’s synthesis, formulations, and therapeutic uses. Key Areas of Patent Activity: Composition of Matter Patents: Early patents focused on the novel chemical entities themselves, such as Tibolone. These would have been the foundational patents. Method of Treatment Patents: Patents like 6,194,415 claim specific methods of using a compound to treat a particular condition. This is a crucial category for pharmaceutical innovation. Formulation Patents: These patents cover specific dosage forms, delivery systems, or combinations of Tibolone with other active pharmaceutical ingredients (APIs) or excipients. This can extend market exclusivity. Examples might include extended-release formulations, transdermal patches, or vaginal rings. Synthesis and Process Patents: Patents may protect novel or improved methods for manufacturing Tibolone or its metabolites, potentially offering cost advantages or higher purity. Metabolite-Specific Patents: While 6,194,415 mentions metabolites, separate patents could claim the use of specific metabolites independently if they demonstrate unique therapeutic benefits or improved profiles. New Indications: As research progresses, new therapeutic uses for Tibolone or its analogs might be discovered, leading to new patent applications for these expanded indications. Impact of Tibolone's Mechanism on Patentability: Tibolone's unique STEAR mechanism has been a key aspect driving its development and patenting strategy. Patents would likely focus on: Selective Estrogenic Effects: Claims targeting its ability to provide beneficial estrogenic effects in bone and brain without endometrial proliferation. Androgenic Effects: Claims related to the benefits derived from its androgenic metabolite, such as improved libido or mood. Combined Receptor Modulation: Patents might describe the synergistic effects of its multiple active metabolites. Competitive Considerations and Generic Entry: With the expiration of foundational patents such as 6,194,415, the market becomes more accessible for generic drug manufacturers. However, the existence of later-expiring patents related to specific formulations, manufacturing processes, or new indications can still present barriers to generic competition. Generic companies typically seek to develop bioequivalent versions of the drug that do not infringe on any active patents. This often involves developing new formulations or manufacturing processes. Pharmaceutical Companies Active in the Space: Historically, companies involved in the development and marketing of Tibolone include: Organon (acquired by Schering-Plough, then Merck): Organon was a key developer and marketer of Tibolone under brand names like Livial. Pfizer Inc.: As the successor to American Home Products and Wyeth, Pfizer holds rights to patents like 6,194,415. Various generic pharmaceutical companies: Following patent expiries, numerous companies would have investigated or pursued generic Tibolone products. The patent landscape for Tibolone is dynamic. While core composition of matter and early method of treatment patents have expired, later-expiring patents on specific delivery systems, improved synthesis routes, or new therapeutic applications can continue to influence market exclusivity and competition. What are the implications of the expiration of Patent 6,194,415? The expiration of U.S. Patent 6,194,415 on November 13, 2018, has several significant implications for the pharmaceutical market and healthcare providers. Increased Access for Generic Competition: The most direct implication is the removal of patent-derived exclusivity for the specific method of treatment claimed in Patent 6,194,415. This opens the door for generic pharmaceutical manufacturers to legally produce and market Tibolone for the treatment of menopausal symptoms, osteoporosis, and certain cancers, as described in the patent. This typically leads to: Lower Drug Prices: Increased competition from generic versions generally drives down the cost of the medication, making it more affordable for patients and healthcare systems. Expanded Market Availability: Generic manufacturers may introduce Tibolone into markets where it was previously unavailable or limited due to patent restrictions. Shift in Market Dynamics: The expiration allows for a more competitive market for Tibolone. The original innovator company, or its successors (in this case, Pfizer Inc.), loses the exclusive right to market Tibolone for the claimed indications under this specific patent. This can lead to: Reduced Market Share for Innovator: The market share previously held by the brand-name Tibolone may be eroded by generic alternatives. Focus on Differentiated Products: The innovator company might shift its focus to newer, patented therapies or specialized formulations of Tibolone that may still be under patent protection. Importance of Remaining Patents: It is crucial to note that the expiration of Patent 6,194,415 does not necessarily mean that all intellectual property protection for Tibolone has ended. Other patents may still be in force that cover: Specific Formulations: For example, extended-release tablets, transdermal patches, or combination products involving Tibolone. Manufacturing Processes: Novel or improved methods of synthesizing Tibolone. New Therapeutic Uses: If Tibolone has been found to be effective for additional medical conditions and these uses have been patented. Polymorphs or Salts: Specific crystalline forms or salt forms of Tibolone with improved properties. The presence of these other patents can still provide a degree of market exclusivity and influence the extent and speed of generic market penetration. Companies looking to enter the Tibolone market must conduct thorough freedom-to-operate analyses to ensure they do not infringe on any active, unexpired patents. Impact on Research and Development: The expiration of a foundational patent can also influence R&D strategies. For Tibolone, it might: Encourage Research into Next-Generation STEARs: The success of Tibolone could spur research into developing newer compounds with potentially improved efficacy, safety profiles, or novel mechanisms of action, leading to new patentable inventions. Reduce Barriers for Repurposing: With Tibolone becoming a generic drug, researchers might explore its repurposing for new indications, leveraging the existing knowledge base and lower cost of the API. In summary, the expiration of U.S. Patent 6,194,415 signifies a transition for Tibolone from a patented therapeutic to a more accessible generic medication. This transition benefits patients through lower costs and increased availability, while also prompting strategic adjustments for pharmaceutical companies, including both generic entrants and the original innovators. Key Takeaways United States Patent 6,194,415, assigned to American Home Products Corporation (now Pfizer Inc.), claims a method for treating conditions responsive to progesterone receptor modulation, specifically menopausal symptoms, osteoporosis, breast cancer, and endometrial cancer, by administering Tibolone or its active metabolites. The patent's core claim is for the method of using Tibolone for therapeutic purposes, with dependent claims specifying various conditions and metabolites. Tibolone is a synthetic steroid that acts as a selective tissue estrogenic activity regulator (STEAR) through its active metabolites, offering benefits in bone and brain while showing anti-proliferative effects in the endometrium and breast. U.S. Patent 6,194,415 was granted on February 27, 2001, with a filing date of November 13, 1998, and expired on November 13, 2018. The expiration of this patent has led to increased opportunities for generic Tibolone production, potentially lowering costs and expanding market access. The patent landscape for Tibolone remains dynamic, with other patents potentially covering specific formulations, manufacturing processes, or new indications, which can affect the extent of generic competition. Frequently Asked Questions When did U.S. Patent 6,194,415 expire, and what does this mean for the availability of Tibolone? U.S. Patent 6,194,415 expired on November 13, 2018. This expiration means that the patent protection for the specific methods of treatment claimed in this patent has ended, allowing generic manufacturers to produce and market Tibolone for those indications without infringing this particular patent. Who currently owns the rights to U.S. Patent 6,194,415? U.S. Patent 6,194,415 was originally assigned to American Home Products Corporation. Through subsequent corporate mergers and acquisitions, the rights to this patent would have transferred to Wyeth and subsequently to Pfizer Inc. However, as the patent has expired, there are no longer exclusive ownership rights for the claims within it. What were the main therapeutic conditions addressed by claims in Patent 6,194,415? The patent claimed methods for treating menopausal symptoms (such as hot flashes), osteoporosis, breast cancer, and endometrial cancer, all responsive to progesterone receptor modulation via Tibolone. Are there any active patents related to Tibolone that could still affect market exclusivity? Yes, while U.S. Patent 6,194,415 has expired, there may be other unexpired patents covering different aspects of Tibolone, such as novel formulations, specific manufacturing processes, or newly discovered therapeutic uses. Companies seeking to market Tibolone or related products must conduct thorough freedom-to-operate analyses. What is the significance of Tibolone's mechanism of action (STEAR) in relation to its patent claims? Tibolone's unique selective tissue estrogenic activity regulator (STEAR) profile, where its metabolites have differential effects in various tissues (estrogenic in bone/brain, anti-estrogenic in endometrium/breast), was a key factor in patenting its therapeutic applications. Patent claims likely focused on leveraging these tissue-specific effects to achieve therapeutic benefits while minimizing side effects like endometrial proliferation. Citations [1] American Home Products Corporation. (2001). U.S. Patent 6,194,415. Washington, DC: U.S. Patent and Trademark Office. More… ↓ ⤷ Start Trial

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	311187	⤷ Start Trial
Austria	322267	⤷ Start Trial
Austria	447956	⤷ Start Trial
Australia	2846000	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 6,194,415

Summary for Patent: 6,194,415