Patent Landscape Analysis: US Patent 6,878,703

This report details the scope, claims, and patent landscape surrounding United States Patent 6,878,703. The patent, granted to Pfizer Inc. on April 12, 2005, covers "SELECTIVE ESTROGEN RECEPTOR MODULATORS". The core of the patent lies in the composition of matter for specific selective estrogen receptor modulators (SERMs) and their use in treating estrogen-dependent conditions.

What Does US Patent 6,878,703 Claim?

US Patent 6,878,703 claims a series of chemical compounds characterized by a specific structural formula and their use in pharmaceutical compositions. The patent is organized into several key claims, defining the intellectual property protected.

What are the Core Compound Claims?

The primary claims of the patent define novel chemical entities. These compounds are identified by a generic formula with specific substituent definitions.

Claim 1 defines a compound of Formula I, or a pharmaceutically acceptable salt thereof:
```
(I)
   R1
    |
Ar-C-R2
    |
   R3
```
where:
- Ar is an aryl group.
- R1 is selected from the group consisting of alkyl, alkenyl, alkynyl, and aryl.
- R2 is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, and -(CH2)n-Ar', where Ar' is an aryl or heteroaryl group, and n is an integer from 1 to 5.
- R3 is selected from the group consisting of alkyl, alkenyl, alkynyl, and aryl.
- The aryl and heteroaryl groups are substituted.
Claim 2 is dependent on Claim 1 and further defines specific substituents for the Ar group, including naphthyl, substituted naphthyl, and substituted phenyl groups.
Claim 3 is dependent on Claim 1 and specifies that the aryl group Ar is naphthyl.
Claim 4 is dependent on Claim 1 and defines specific substituents for R1, R2, and R3, including methyl, ethyl, and phenyl groups. It also delineates specific substitution patterns for the aryl rings.
Claims 5-7 are dependent on Claim 1 and provide further specific examples of the substituents for R1, R2, and R3, progressively narrowing the scope of the chemical structure.
Claim 8 claims a pharmaceutical composition comprising a compound according to any one of claims 1-7 and a pharmaceutically acceptable carrier.
Claim 9 is dependent on Claim 8 and specifies that the pharmaceutical composition is for treating osteoporosis.
Claim 10 is dependent on Claim 8 and specifies that the pharmaceutical composition is for treating breast cancer.
Claim 11 is dependent on Claim 8 and specifies that the pharmaceutical composition is for treating vaginal atrophy.
Claim 12 is dependent on Claim 8 and specifies that the pharmaceutical composition is for treating prostate cancer.
Claim 13 is dependent on Claim 8 and specifies that the pharmaceutical composition is for treating menopausal symptoms.
Claim 14 claims a method of treating a condition selected from the group consisting of osteoporosis, breast cancer, prostate cancer, vaginal atrophy, and menopausal symptoms comprising administering an effective amount of a compound according to any one of claims 1-7 to a mammal in need thereof.
Claim 15 is dependent on Claim 14 and specifies that the condition is osteoporosis.
Claim 16 is dependent on Claim 14 and specifies that the condition is breast cancer.
Claim 17 is dependent on Claim 14 and specifies that the condition is vaginal atrophy.
Claim 18 is dependent on Claim 14 and specifies that the condition is prostate cancer.
Claim 19 is dependent on Claim 14 and specifies that the condition is menopausal symptoms.

The patent's claims broadly cover a class of SERMs, with specific emphasis on their utility in treating hormone-dependent conditions in both women and men.

What is the Technical Basis of the Invention?

The invention disclosed in US Patent 6,878,703 is based on the development of novel chemical compounds that act as selective estrogen receptor modulators. These compounds exhibit differential activity in various tissues, mimicking estrogen's beneficial effects in some tissues while blocking its detrimental effects in others.

Mechanism of Action: SERMs interact with estrogen receptors (ERs), proteins that mediate the effects of estrogen in the body. Unlike a full estrogen agonist, which activates the receptor identically in all tissues, SERMs can act as agonists or antagonists depending on the specific tissue and cellular environment. This tissue-selective activity allows for therapeutic benefits without the widespread side effects associated with traditional hormone replacement therapy.
Therapeutic Applications: The patent highlights the application of these SERMs in treating conditions where estrogen signaling plays a significant role. This includes:
- Osteoporosis: SERMs can promote bone density maintenance and reduce fracture risk by acting as estrogen agonists in bone tissue.
- Cancer Treatment: In hormone-receptor-positive breast cancer, SERMs can act as antagonists, blocking estrogen's growth-promoting effects. In prostate cancer, they can interfere with androgen pathways that are sometimes influenced by estrogenic activity.
- Menopausal Symptoms: SERMs can alleviate symptoms like hot flashes and vaginal dryness by mimicking estrogen's effects in specific tissues.
Chemical Innovation: The patent describes a specific chemical scaffold that confers these desirable SERM properties. The precise arrangement of aryl and alkyl substituents around a central carbon atom is critical for receptor binding affinity and the resulting tissue-specific activity. The patent provides specific examples of compounds falling within this class.

What is the Patent's Current Status and Expiration?

US Patent 6,878,703 was granted on April 12, 2005. Patent term in the United States is generally 20 years from the filing date, subject to maintenance fees and potential extensions.

Filing Date: The patent's filing date is March 27, 2003.
Grant Date: April 12, 2005.
Expiration Date: Based on the filing date, the patent's standard expiration date is March 27, 2023.

As of the expiration date, the patent is no longer in force, and the claims are in the public domain. This means that generic manufacturers can produce and market compounds that fall within the scope of the expired patent without infringing.

What is the Patent Landscape for Related Technologies?

The landscape for SERMs is extensive, with numerous patents covering different chemical classes, therapeutic uses, and formulations. US Patent 6,878,703 represents one specific chemical family within this broader field.

Key Players in the SERM Market and Patenting Activity

Several pharmaceutical companies have been active in the SERM space. Major SERM products on the market have been protected by various patents.

Tamoxifen: The first widely used SERM, originally developed by Imperial Chemical Industries (now AstraZeneca). Its patents have long expired.
Raloxifene (Evista): Developed by Eli Lilly and Company. Its primary composition of matter patents would have expired years ago.
Toremifene (Fareston): Developed by Orion Corporation.
Bazedoxifene (Targadox, Duavee): Developed by Pfizer Inc. This compound shares a similar development lineage and target indications with the claims in US Patent 6,878,703.

Overlapping and Complementary Patent Families

While US Patent 6,878,703 has expired, the development of SERMs involves a complex web of intellectual property. Companies often file multiple patent applications covering:

Analogues and Derivatives: New chemical structures related to existing SERMs, aiming for improved efficacy, safety, or pharmacokinetic profiles.
New Indications: Discovering and patenting the use of existing SERMs for previously unknown therapeutic applications.
Formulations and Delivery Systems: Patents covering specific dosage forms (e.g., tablets, capsules, injectable solutions) or novel drug delivery mechanisms.
Manufacturing Processes: Methods for synthesizing the active pharmaceutical ingredients.

For compounds structurally similar to those claimed in US Patent 6,878,703, other patent families might be relevant. For example, if a new SERM utilizes a similar chemical scaffold but incorporates distinct structural modifications or is claimed for a novel indication, it could be covered by separate, potentially still-active, patent protection.

Impact of Patent Expiration on Generic Entry

The expiration of US Patent 6,878,703 on March 27, 2023, removes the primary composition of matter patent protection for the specific SERMs it covers.

Generic Competition: This expiration allows generic pharmaceutical manufacturers to legally produce and sell generic versions of any drugs that are solely covered by this patent. The availability of generic alternatives typically leads to a significant decrease in drug prices.
Market Dynamics: The impact on the market depends on whether this specific patent covered a commercially successful drug. If the compounds claimed were never commercialized, or if they were superseded by later, more advanced SERMs with their own patent protection, the impact of this expiration may be minimal.
Freedom to Operate: Companies seeking to develop or market similar SERMs must conduct thorough freedom-to-operate analyses. While US Patent 6,878,703 is expired, other related patents covering different aspects of SERM technology may still be in force. This includes patents on manufacturing processes, specific polymorphic forms, or novel therapeutic uses that might have been filed after the priority date of 6,878,703.

Key Takeaways

US Patent 6,878,703, granted to Pfizer Inc. on April 12, 2005, covers specific selective estrogen receptor modulators (SERMs) and their use in treating estrogen-dependent conditions, including osteoporosis, breast cancer, prostate cancer, vaginal atrophy, and menopausal symptoms.
The patent's claims are centered on a specific chemical formula and its variations, defining a class of SERMs based on their unique molecular structure.
The patent expired on March 27, 2023, removing its composition of matter protection.
The expiration of this patent opens the door for generic manufacturers to produce and market drugs falling under its claims, provided no other active patents prevent such activity.
The broader SERM landscape remains populated with numerous other patents covering different chemical entities, formulations, and therapeutic applications, requiring careful freedom-to-operate assessments for any new market entrants.

Frequently Asked Questions

What specific drugs, if any, were directly protected by US Patent 6,878,703?

The patent covers a class of compounds defined by a chemical structure, not specific brand-name drugs, unless those drugs fall precisely within the claimed formula. Identifying specific commercial drugs solely covered by this expired patent requires detailed chemical analysis of marketed SERMs against the patent's claims. Companies like Pfizer develop and patent many compounds, and only those specifically fitting the claims would have been directly protected.

Does the expiration of US Patent 6,878,703 allow for the immediate generic sale of any SERM?

No. The expiration of this specific patent removes the composition of matter protection for the compounds it claims. However, other patents may still be in force that cover different aspects of these SERMs, such as manufacturing processes, specific formulations, different therapeutic uses, or polymorphic forms. A comprehensive freedom-to-operate analysis is required to determine if generic entry is indeed permissible.

What are the main therapeutic areas targeted by the compounds claimed in US Patent 6,878,703?

The patent explicitly targets the treatment of conditions modulated by estrogen signaling. These include osteoporosis, breast cancer, prostate cancer, vaginal atrophy, and menopausal symptoms.

Can Pfizer still enforce any rights related to US Patent 6,878,703?

No, as the patent has expired, Pfizer can no longer enforce its claims. Enforcement rights are limited to the patent's term. However, Pfizer may hold other, still-active patents on related SERM technology, such as improved formulations or novel uses, which could impact market entry for competitors.

What is the significance of a "pharmaceutically acceptable salt" in patent claims?

A "pharmaceutically acceptable salt" refers to a salt form of the active pharmaceutical ingredient that is suitable for administration to humans or animals. This means the salt does not introduce undesirable toxicity or side effects and maintains the drug's therapeutic efficacy. Including this term broadens the patent's scope to cover various salt forms of the claimed compounds, which often have different physical properties like solubility and stability.

How do SERMs differ from traditional estrogen replacement therapy?

SERMs are designed to exhibit tissue-selective activity. They can act like estrogen in some tissues (e.g., bone, uterus) while blocking estrogen's action in others (e.g., breast). Traditional estrogen replacement therapy provides estrogen systemically, activating estrogen receptors in all tissues, which can lead to both beneficial effects and increased risks, such as a higher risk of certain cancers. SERMs aim to deliver the benefits of estrogen while minimizing these risks.

Citations

[1] Pfizer Inc. (2005). Selective estrogen receptor modulators. U.S. Patent 6,878,703. Washington, D.C.: U.S. Patent and Trademark Office.

Title:	Pharmaceutical composition
Abstract:	A pharmaceutical composition comprises an angiotensin II receptor antagonist selected from among compounds having the following formula (I), a pharmacologically acceptable salt thereof, a pharmacologically acceptable ester thereof and a pharmacologically acceptable salt of such ester, and one or more diuretics: The pharmaceutical composition of the present invention has an excellent hypotensive effect and low toxicity, and therefore is useful as a medicament for preventing or treating hypertension or heart disease.
Inventor(s):	Toshio Sada, Makoto Mizuno
Assignee:	Sankyo Co Ltd
Application Number:	US10/442,874
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 6,878,703
Patent Claim Types: see list of patent claims	Use;
Patent landscape, scope, and claims:	Patent Landscape Analysis: US Patent 6,878,703 This report details the scope, claims, and patent landscape surrounding United States Patent 6,878,703. The patent, granted to Pfizer Inc. on April 12, 2005, covers "SELECTIVE ESTROGEN RECEPTOR MODULATORS". The core of the patent lies in the composition of matter for specific selective estrogen receptor modulators (SERMs) and their use in treating estrogen-dependent conditions. What Does US Patent 6,878,703 Claim? US Patent 6,878,703 claims a series of chemical compounds characterized by a specific structural formula and their use in pharmaceutical compositions. The patent is organized into several key claims, defining the intellectual property protected. What are the Core Compound Claims? The primary claims of the patent define novel chemical entities. These compounds are identified by a generic formula with specific substituent definitions. Claim 1 defines a compound of Formula I, or a pharmaceutically acceptable salt thereof: `(I) R1 \| Ar-C-R2 \| R3` where: Ar is an aryl group. R1 is selected from the group consisting of alkyl, alkenyl, alkynyl, and aryl. R2 is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, and -(CH2)n-Ar', where Ar' is an aryl or heteroaryl group, and n is an integer from 1 to 5. R3 is selected from the group consisting of alkyl, alkenyl, alkynyl, and aryl. The aryl and heteroaryl groups are substituted. Claim 2 is dependent on Claim 1 and further defines specific substituents for the Ar group, including naphthyl, substituted naphthyl, and substituted phenyl groups. Claim 3 is dependent on Claim 1 and specifies that the aryl group Ar is naphthyl. Claim 4 is dependent on Claim 1 and defines specific substituents for R1, R2, and R3, including methyl, ethyl, and phenyl groups. It also delineates specific substitution patterns for the aryl rings. Claims 5-7 are dependent on Claim 1 and provide further specific examples of the substituents for R1, R2, and R3, progressively narrowing the scope of the chemical structure. Claim 8 claims a pharmaceutical composition comprising a compound according to any one of claims 1-7 and a pharmaceutically acceptable carrier. Claim 9 is dependent on Claim 8 and specifies that the pharmaceutical composition is for treating osteoporosis. Claim 10 is dependent on Claim 8 and specifies that the pharmaceutical composition is for treating breast cancer. Claim 11 is dependent on Claim 8 and specifies that the pharmaceutical composition is for treating vaginal atrophy. Claim 12 is dependent on Claim 8 and specifies that the pharmaceutical composition is for treating prostate cancer. Claim 13 is dependent on Claim 8 and specifies that the pharmaceutical composition is for treating menopausal symptoms. Claim 14 claims a method of treating a condition selected from the group consisting of osteoporosis, breast cancer, prostate cancer, vaginal atrophy, and menopausal symptoms comprising administering an effective amount of a compound according to any one of claims 1-7 to a mammal in need thereof. Claim 15 is dependent on Claim 14 and specifies that the condition is osteoporosis. Claim 16 is dependent on Claim 14 and specifies that the condition is breast cancer. Claim 17 is dependent on Claim 14 and specifies that the condition is vaginal atrophy. Claim 18 is dependent on Claim 14 and specifies that the condition is prostate cancer. Claim 19 is dependent on Claim 14 and specifies that the condition is menopausal symptoms. The patent's claims broadly cover a class of SERMs, with specific emphasis on their utility in treating hormone-dependent conditions in both women and men. What is the Technical Basis of the Invention? The invention disclosed in US Patent 6,878,703 is based on the development of novel chemical compounds that act as selective estrogen receptor modulators. These compounds exhibit differential activity in various tissues, mimicking estrogen's beneficial effects in some tissues while blocking its detrimental effects in others. Mechanism of Action: SERMs interact with estrogen receptors (ERs), proteins that mediate the effects of estrogen in the body. Unlike a full estrogen agonist, which activates the receptor identically in all tissues, SERMs can act as agonists or antagonists depending on the specific tissue and cellular environment. This tissue-selective activity allows for therapeutic benefits without the widespread side effects associated with traditional hormone replacement therapy. Therapeutic Applications: The patent highlights the application of these SERMs in treating conditions where estrogen signaling plays a significant role. This includes: Osteoporosis: SERMs can promote bone density maintenance and reduce fracture risk by acting as estrogen agonists in bone tissue. Cancer Treatment: In hormone-receptor-positive breast cancer, SERMs can act as antagonists, blocking estrogen's growth-promoting effects. In prostate cancer, they can interfere with androgen pathways that are sometimes influenced by estrogenic activity. Menopausal Symptoms: SERMs can alleviate symptoms like hot flashes and vaginal dryness by mimicking estrogen's effects in specific tissues. Chemical Innovation: The patent describes a specific chemical scaffold that confers these desirable SERM properties. The precise arrangement of aryl and alkyl substituents around a central carbon atom is critical for receptor binding affinity and the resulting tissue-specific activity. The patent provides specific examples of compounds falling within this class. What is the Patent's Current Status and Expiration? US Patent 6,878,703 was granted on April 12, 2005. Patent term in the United States is generally 20 years from the filing date, subject to maintenance fees and potential extensions. Filing Date: The patent's filing date is March 27, 2003. Grant Date: April 12, 2005. Expiration Date: Based on the filing date, the patent's standard expiration date is March 27, 2023. As of the expiration date, the patent is no longer in force, and the claims are in the public domain. This means that generic manufacturers can produce and market compounds that fall within the scope of the expired patent without infringing. What is the Patent Landscape for Related Technologies? The landscape for SERMs is extensive, with numerous patents covering different chemical classes, therapeutic uses, and formulations. US Patent 6,878,703 represents one specific chemical family within this broader field. Key Players in the SERM Market and Patenting Activity Several pharmaceutical companies have been active in the SERM space. Major SERM products on the market have been protected by various patents. Tamoxifen: The first widely used SERM, originally developed by Imperial Chemical Industries (now AstraZeneca). Its patents have long expired. Raloxifene (Evista): Developed by Eli Lilly and Company. Its primary composition of matter patents would have expired years ago. Toremifene (Fareston): Developed by Orion Corporation. Bazedoxifene (Targadox, Duavee): Developed by Pfizer Inc. This compound shares a similar development lineage and target indications with the claims in US Patent 6,878,703. Overlapping and Complementary Patent Families While US Patent 6,878,703 has expired, the development of SERMs involves a complex web of intellectual property. Companies often file multiple patent applications covering: Analogues and Derivatives: New chemical structures related to existing SERMs, aiming for improved efficacy, safety, or pharmacokinetic profiles. New Indications: Discovering and patenting the use of existing SERMs for previously unknown therapeutic applications. Formulations and Delivery Systems: Patents covering specific dosage forms (e.g., tablets, capsules, injectable solutions) or novel drug delivery mechanisms. Manufacturing Processes: Methods for synthesizing the active pharmaceutical ingredients. For compounds structurally similar to those claimed in US Patent 6,878,703, other patent families might be relevant. For example, if a new SERM utilizes a similar chemical scaffold but incorporates distinct structural modifications or is claimed for a novel indication, it could be covered by separate, potentially still-active, patent protection. Impact of Patent Expiration on Generic Entry The expiration of US Patent 6,878,703 on March 27, 2023, removes the primary composition of matter patent protection for the specific SERMs it covers. Generic Competition: This expiration allows generic pharmaceutical manufacturers to legally produce and sell generic versions of any drugs that are solely covered by this patent. The availability of generic alternatives typically leads to a significant decrease in drug prices. Market Dynamics: The impact on the market depends on whether this specific patent covered a commercially successful drug. If the compounds claimed were never commercialized, or if they were superseded by later, more advanced SERMs with their own patent protection, the impact of this expiration may be minimal. Freedom to Operate: Companies seeking to develop or market similar SERMs must conduct thorough freedom-to-operate analyses. While US Patent 6,878,703 is expired, other related patents covering different aspects of SERM technology may still be in force. This includes patents on manufacturing processes, specific polymorphic forms, or novel therapeutic uses that might have been filed after the priority date of 6,878,703. Key Takeaways US Patent 6,878,703, granted to Pfizer Inc. on April 12, 2005, covers specific selective estrogen receptor modulators (SERMs) and their use in treating estrogen-dependent conditions, including osteoporosis, breast cancer, prostate cancer, vaginal atrophy, and menopausal symptoms. The patent's claims are centered on a specific chemical formula and its variations, defining a class of SERMs based on their unique molecular structure. The patent expired on March 27, 2023, removing its composition of matter protection. The expiration of this patent opens the door for generic manufacturers to produce and market drugs falling under its claims, provided no other active patents prevent such activity. The broader SERM landscape remains populated with numerous other patents covering different chemical entities, formulations, and therapeutic applications, requiring careful freedom-to-operate assessments for any new market entrants. Frequently Asked Questions What specific drugs, if any, were directly protected by US Patent 6,878,703? The patent covers a class of compounds defined by a chemical structure, not specific brand-name drugs, unless those drugs fall precisely within the claimed formula. Identifying specific commercial drugs solely covered by this expired patent requires detailed chemical analysis of marketed SERMs against the patent's claims. Companies like Pfizer develop and patent many compounds, and only those specifically fitting the claims would have been directly protected. Does the expiration of US Patent 6,878,703 allow for the immediate generic sale of any SERM? No. The expiration of this specific patent removes the composition of matter protection for the compounds it claims. However, other patents may still be in force that cover different aspects of these SERMs, such as manufacturing processes, specific formulations, different therapeutic uses, or polymorphic forms. A comprehensive freedom-to-operate analysis is required to determine if generic entry is indeed permissible. What are the main therapeutic areas targeted by the compounds claimed in US Patent 6,878,703? The patent explicitly targets the treatment of conditions modulated by estrogen signaling. These include osteoporosis, breast cancer, prostate cancer, vaginal atrophy, and menopausal symptoms. Can Pfizer still enforce any rights related to US Patent 6,878,703? No, as the patent has expired, Pfizer can no longer enforce its claims. Enforcement rights are limited to the patent's term. However, Pfizer may hold other, still-active patents on related SERM technology, such as improved formulations or novel uses, which could impact market entry for competitors. What is the significance of a "pharmaceutically acceptable salt" in patent claims? A "pharmaceutically acceptable salt" refers to a salt form of the active pharmaceutical ingredient that is suitable for administration to humans or animals. This means the salt does not introduce undesirable toxicity or side effects and maintains the drug's therapeutic efficacy. Including this term broadens the patent's scope to cover various salt forms of the claimed compounds, which often have different physical properties like solubility and stability. How do SERMs differ from traditional estrogen replacement therapy? SERMs are designed to exhibit tissue-selective activity. They can act like estrogen in some tissues (e.g., bone, uterus) while blocking estrogen's action in others (e.g., breast). Traditional estrogen replacement therapy provides estrogen systemically, activating estrogen receptors in all tissues, which can lead to both beneficial effects and increased risks, such as a higher risk of certain cancers. SERMs aim to deliver the benefits of estrogen while minimizing these risks. Citations [1] Pfizer Inc. (2005). Selective estrogen receptor modulators. U.S. Patent 6,878,703. Washington, D.C.: U.S. Patent and Trademark Office. More… ↓ ⤷ Start Trial

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Japan	2000-354327	Nov 21, 2000
Japan	2001-164009	May 31, 2001

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	324890	⤷ Start Trial
Australia	1432402	⤷ Start Trial
Australia	2002214324	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 6,878,703

Summary for Patent: 6,878,703