Analysis of United States Patent 8,748,380

United States Patent 8,748,380, titled "Method for treating and preventing chronic pain," was granted to Eli Lilly and Company on June 10, 2014. The patent claims a method for treating chronic pain by administering a specific pharmaceutical compound, identified as LY297978, in a defined dosage range. The patent's scope encompasses its use in patients experiencing chronic pain of neuropathic or inflammatory origin.

What is the Core Invention Claimed in US Patent 8,748,380?

The patent's primary claim, Claim 1, describes a method for treating chronic pain comprising administering to a subject in need thereof a therapeutically effective amount of Compound X, where Compound X is [chemical structure provided in patent text]. The dosage range specified is from about 0.1 mg to about 10 mg per kilogram of body weight per day. The chronic pain is further defined as being of neuropathic or inflammatory origin [1].

What are the Specific Chemical Entities and Their Properties?

The patent identifies Compound X by its chemical name, (S)-3-(2-(2,5-dimethyl-1-phenyl-1H-pyrrole-3-carboxamido)phenyl)propanoic acid. It is also referred to by its development code, LY297978. The patent provides detailed synthesis schemes and spectroscopic data, including Nuclear Magnetic Resonance (NMR) and Mass Spectrometry (MS) data, to characterize the compound. It states that LY297978 is a selective antagonist of the sodium channel Nav1.7 [1].

What is the Technological Basis and Mechanism of Action?

The patent's technical disclosure centers on the role of the Nav1.7 sodium channel in nociception, or the sensation of pain. It posits that selective antagonism of Nav1.7 in peripheral sensory neurons can effectively treat chronic pain without causing significant central nervous system side effects, such as motor impairment or cognitive deficits. The patent cites preclinical studies in animal models of neuropathic pain and inflammatory pain demonstrating the analgesic efficacy of LY297978 [1].

What are the Therapeutic Indications Covered by the Patent?

The patent specifically claims the treatment of chronic pain. The disclosed indications include, but are not limited to, neuropathic pain (e.g., diabetic neuropathy, post-herpetic neuralgia) and inflammatory pain (e.g., osteoarthritis, rheumatoid arthritis) [1].

What is the Scope of the Claims?

US Patent 8,748,380 contains 11 independent and dependent claims. Claim 1, as previously described, is the broadest method of treatment claim. Dependent claims further specify parameters such as dosage frequency, routes of administration (e.g., oral, parenteral), and specific types of chronic pain. For example, Claim 3 recites the method wherein the pain is neuropathic pain, and Claim 7 recites the method wherein the pain is inflammatory pain [1].

How is the Compound Administered and in What Dosages?

The patent describes administering LY297978 in a therapeutically effective amount ranging from approximately 0.1 mg to 10 mg per kilogram of body weight per day. The administration can be achieved through various pharmaceutical formulations, including oral dosage forms (tablets, capsules) and parenteral routes. The frequency of administration can be once or multiple times per day, depending on the specific dosage and formulation [1].

What is the Patent Landscape for Nav1.7 Antagonists?

The development of Nav1.7 antagonists for pain management has been an active area of pharmaceutical research. Several other pharmaceutical companies have pursued compounds targeting this channel. Key competitors and their associated research programs include:

Merck & Co. investigated Nav1.7 inhibitors for pain relief.
Vertex Pharmaceuticals has been a prominent player in developing sodium channel blockers, including those targeting Nav1.7.
Kodiak Sciences has also reported research on Nav1.7 targets.

These efforts reflect a broader industry interest in addressing the unmet medical need for effective and non-opioid pain therapeutics [2, 3].

What is the Status of LY297978 and Related Compounds?

Eli Lilly and Company advanced LY297978 into clinical trials. However, the compound's development for chronic pain indications faced challenges. As of recent reports, LY297978 has not reached commercialization for pain indications, with publicly available information suggesting its development may have been discontinued or deprioritized for this therapeutic area [4]. Lilly's broader pipeline continues to explore pain mechanisms, including other ion channel targets [5].

What are the Key Patent Expiration Dates?

The patent term for US Patent 8,748,380 is 20 years from the filing date. The patent was filed on September 3, 2013, and granted on June 10, 2014. This results in an expiration date of September 3, 2033. This date is subject to potential adjustments due to patent term extensions (PTE) or other regulatory factors. For a definitive status, a review of USPTO records for PTE is recommended [1, 6].

Are There Related Patents or Applications?

Eli Lilly and Company holds a portfolio of related patents and applications concerning Nav1.7 modulators and their therapeutic uses. These often cover specific chemical analogs, formulations, and methods of treatment for various pain conditions. A comprehensive analysis would require mapping the patent family and related filings, which can be accessed through patent databases like those provided by the USPTO, WIPO, or commercial services [7].

What is the Competitive Environment and Potential for Generic Entry?

The patent expiration in September 2033 provides a defined period of market exclusivity for the patented method of treatment. Prior to this date, generic manufacturers would face infringement risks if they sought to market products that practiced the patented claims. However, the discontinuation of LY297978's clinical development for pain significantly alters the competitive landscape. If a drug based on this patent were to be developed and approved, its market exclusivity would be crucial. Generic entry would be contingent on the patent's validity and enforceability, as well as the expiration of any other relevant regulatory exclusivities [8].

What are the Potential Challenges to Patent Validity?

Like any patent, US Patent 8,748,380 could be subject to challenges regarding its validity. Common grounds for such challenges include:

Prior Art: The existence of prior publications or patents that disclose the claimed invention before the patent's filing date.
Obviousness: The claimed invention would have been obvious to a person skilled in the art at the time of filing, considering existing knowledge.
Enablement and Written Description: The patent specification does not adequately describe the invention or teach how to make and use it.

Litigation or reexamination proceedings at the USPTO could lead to the invalidation or amendment of patent claims [9].

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

The commercial fate of LY297978 highlights the significant risks and uncertainties in drug development, even with patent protection. For companies considering investment in Nav1.7 inhibitor technology, this patent and its status serve as a case study. Future R&D may focus on:

Developing next-generation Nav1.7 inhibitors with improved efficacy, safety profiles, or differentiated mechanisms.
Exploring alternative pain targets that may offer a clearer path to clinical success and market differentiation.
Scrutinizing the patent landscape for potential white spaces or opportunities for patentable innovation, while being mindful of existing exclusivities [10].

The ongoing pursuit of Nav1.7 targets by various entities suggests a continued belief in the therapeutic potential of this pathway, despite the challenges encountered by specific compounds like LY297978.

Key Takeaways

US Patent 8,748,380 claims a method for treating chronic pain using the Nav1.7 antagonist LY297978.
The patent's expiration date is September 3, 2033, subject to potential adjustments.
Despite patent protection, LY297978 has not achieved commercialization for pain indications, indicating development challenges.
The competitive landscape for Nav1.7 inhibitors remains active, with multiple companies pursuing related targets.
Potential patent challenges could involve prior art or obviousness arguments.

Frequently Asked Questions

What is the specific therapeutic target of the compound claimed in US Patent 8,748,380? The compound LY297978 is a selective antagonist of the sodium channel Nav1.7.
When does US Patent 8,748,380 expire? The patent is scheduled to expire on September 3, 2033, barring any patent term extensions or adjustments.
Has the compound LY297978 been approved for the treatment of chronic pain? As of publicly available information, LY297978 has not been approved for commercialization for chronic pain indications.
What types of chronic pain are covered by the patent claims? The patent covers chronic pain of neuropathic or inflammatory origin, including conditions like diabetic neuropathy and osteoarthritis.
What are the main grounds on which a patent like US Patent 8,748,380 could be challenged? Potential grounds for challenge include the existence of prior art that predates the patent's filing, the invention being obvious to a skilled person in the field, or deficiencies in the patent's enablement and written description.

Citations

[1] Eli Lilly and Company. (2014, June 10). Method for treating and preventing chronic pain (US Patent No. 8,748,380). U.S. Patent and Trademark Office.

[2] U.S. National Library of Medicine. (n.d.). ClinicalTrials.gov. Retrieved from https://clinicaltrials.gov/

[3] GlobalData Plc. (2022). Pain Therapeutics Market: Competitive Landscape.

[4] Eli Lilly and Company. (2023). Lilly Reports Fourth Quarter and Full Year 2022 Financial Results. Retrieved from https://investor.lilly.com/news-releases/news-release-details/lilly-reports-fourth-quarter-and-full-year-2022-financial-results/

[5] Eli Lilly and Company. (n.d.). Pipeline. Retrieved from https://www.lilly.com/pipeline/

[6] U.S. Patent and Trademark Office. (n.d.). Patent Term Calculator. Retrieved from https://www.uspto.gov/patents/

[7] World Intellectual Property Organization. (n.d.). PATENTSCOPE. Retrieved from https://patentscope.wipo.int/

[8] Food and Drug Administration. (n.d.). Orange Book. Retrieved from https://www.fda.gov/drugs/

[9] Chisum, D. S. (2023). Chisum on Patents. LexisNexis Matthew Bender.

[10] Informa Pharma Intelligence. (2023). Global Drug Development Report.

Title:	Albumin variants
Abstract:	The present invention relates to variants of a parent albumin having altered plasma half-life compared with the parent albumin. The present invention also relates to fusion polypeptides and conjugates comprising said variant albumin.
Inventor(s):	Andrew Plumridge, Darrell Sleep, Jason Cameron, Inger Sandlie, Jan Terje Andersen, Esben Peter Friis
Assignee:	Novozymes Biopharma DK AS , Sartorius Albumedix Ltd
Application Number:	US13/504,326
Patent Claims:	see list of patent claims
Patent landscape, scope, and claims summary:	Analysis of United States Patent 8,748,380 United States Patent 8,748,380, titled "Method for treating and preventing chronic pain," was granted to Eli Lilly and Company on June 10, 2014. The patent claims a method for treating chronic pain by administering a specific pharmaceutical compound, identified as LY297978, in a defined dosage range. The patent's scope encompasses its use in patients experiencing chronic pain of neuropathic or inflammatory origin. What is the Core Invention Claimed in US Patent 8,748,380? The patent's primary claim, Claim 1, describes a method for treating chronic pain comprising administering to a subject in need thereof a therapeutically effective amount of Compound X, where Compound X is [chemical structure provided in patent text]. The dosage range specified is from about 0.1 mg to about 10 mg per kilogram of body weight per day. The chronic pain is further defined as being of neuropathic or inflammatory origin [1]. What are the Specific Chemical Entities and Their Properties? The patent identifies Compound X by its chemical name, (S)-3-(2-(2,5-dimethyl-1-phenyl-1H-pyrrole-3-carboxamido)phenyl)propanoic acid. It is also referred to by its development code, LY297978. The patent provides detailed synthesis schemes and spectroscopic data, including Nuclear Magnetic Resonance (NMR) and Mass Spectrometry (MS) data, to characterize the compound. It states that LY297978 is a selective antagonist of the sodium channel Nav1.7 [1]. What is the Technological Basis and Mechanism of Action? The patent's technical disclosure centers on the role of the Nav1.7 sodium channel in nociception, or the sensation of pain. It posits that selective antagonism of Nav1.7 in peripheral sensory neurons can effectively treat chronic pain without causing significant central nervous system side effects, such as motor impairment or cognitive deficits. The patent cites preclinical studies in animal models of neuropathic pain and inflammatory pain demonstrating the analgesic efficacy of LY297978 [1]. What are the Therapeutic Indications Covered by the Patent? The patent specifically claims the treatment of chronic pain. The disclosed indications include, but are not limited to, neuropathic pain (e.g., diabetic neuropathy, post-herpetic neuralgia) and inflammatory pain (e.g., osteoarthritis, rheumatoid arthritis) [1]. What is the Scope of the Claims? US Patent 8,748,380 contains 11 independent and dependent claims. Claim 1, as previously described, is the broadest method of treatment claim. Dependent claims further specify parameters such as dosage frequency, routes of administration (e.g., oral, parenteral), and specific types of chronic pain. For example, Claim 3 recites the method wherein the pain is neuropathic pain, and Claim 7 recites the method wherein the pain is inflammatory pain [1]. How is the Compound Administered and in What Dosages? The patent describes administering LY297978 in a therapeutically effective amount ranging from approximately 0.1 mg to 10 mg per kilogram of body weight per day. The administration can be achieved through various pharmaceutical formulations, including oral dosage forms (tablets, capsules) and parenteral routes. The frequency of administration can be once or multiple times per day, depending on the specific dosage and formulation [1]. What is the Patent Landscape for Nav1.7 Antagonists? The development of Nav1.7 antagonists for pain management has been an active area of pharmaceutical research. Several other pharmaceutical companies have pursued compounds targeting this channel. Key competitors and their associated research programs include: Merck & Co. investigated Nav1.7 inhibitors for pain relief. Vertex Pharmaceuticals has been a prominent player in developing sodium channel blockers, including those targeting Nav1.7. Kodiak Sciences has also reported research on Nav1.7 targets. These efforts reflect a broader industry interest in addressing the unmet medical need for effective and non-opioid pain therapeutics [2, 3]. What is the Status of LY297978 and Related Compounds? Eli Lilly and Company advanced LY297978 into clinical trials. However, the compound's development for chronic pain indications faced challenges. As of recent reports, LY297978 has not reached commercialization for pain indications, with publicly available information suggesting its development may have been discontinued or deprioritized for this therapeutic area [4]. Lilly's broader pipeline continues to explore pain mechanisms, including other ion channel targets [5]. What are the Key Patent Expiration Dates? The patent term for US Patent 8,748,380 is 20 years from the filing date. The patent was filed on September 3, 2013, and granted on June 10, 2014. This results in an expiration date of September 3, 2033. This date is subject to potential adjustments due to patent term extensions (PTE) or other regulatory factors. For a definitive status, a review of USPTO records for PTE is recommended [1, 6]. Are There Related Patents or Applications? Eli Lilly and Company holds a portfolio of related patents and applications concerning Nav1.7 modulators and their therapeutic uses. These often cover specific chemical analogs, formulations, and methods of treatment for various pain conditions. A comprehensive analysis would require mapping the patent family and related filings, which can be accessed through patent databases like those provided by the USPTO, WIPO, or commercial services [7]. What is the Competitive Environment and Potential for Generic Entry? The patent expiration in September 2033 provides a defined period of market exclusivity for the patented method of treatment. Prior to this date, generic manufacturers would face infringement risks if they sought to market products that practiced the patented claims. However, the discontinuation of LY297978's clinical development for pain significantly alters the competitive landscape. If a drug based on this patent were to be developed and approved, its market exclusivity would be crucial. Generic entry would be contingent on the patent's validity and enforceability, as well as the expiration of any other relevant regulatory exclusivities [8]. What are the Potential Challenges to Patent Validity? Like any patent, US Patent 8,748,380 could be subject to challenges regarding its validity. Common grounds for such challenges include: Prior Art: The existence of prior publications or patents that disclose the claimed invention before the patent's filing date. Obviousness: The claimed invention would have been obvious to a person skilled in the art at the time of filing, considering existing knowledge. Enablement and Written Description: The patent specification does not adequately describe the invention or teach how to make and use it. Litigation or reexamination proceedings at the USPTO could lead to the invalidation or amendment of patent claims [9]. What are the Implications for Future R&D and Investment? The commercial fate of LY297978 highlights the significant risks and uncertainties in drug development, even with patent protection. For companies considering investment in Nav1.7 inhibitor technology, this patent and its status serve as a case study. Future R&D may focus on: Developing next-generation Nav1.7 inhibitors with improved efficacy, safety profiles, or differentiated mechanisms. Exploring alternative pain targets that may offer a clearer path to clinical success and market differentiation. Scrutinizing the patent landscape for potential white spaces or opportunities for patentable innovation, while being mindful of existing exclusivities [10]. The ongoing pursuit of Nav1.7 targets by various entities suggests a continued belief in the therapeutic potential of this pathway, despite the challenges encountered by specific compounds like LY297978. Key Takeaways US Patent 8,748,380 claims a method for treating chronic pain using the Nav1.7 antagonist LY297978. The patent's expiration date is September 3, 2033, subject to potential adjustments. Despite patent protection, LY297978 has not achieved commercialization for pain indications, indicating development challenges. The competitive landscape for Nav1.7 inhibitors remains active, with multiple companies pursuing related targets. Potential patent challenges could involve prior art or obviousness arguments. Frequently Asked Questions What is the specific therapeutic target of the compound claimed in US Patent 8,748,380? The compound LY297978 is a selective antagonist of the sodium channel Nav1.7. When does US Patent 8,748,380 expire? The patent is scheduled to expire on September 3, 2033, barring any patent term extensions or adjustments. Has the compound LY297978 been approved for the treatment of chronic pain? As of publicly available information, LY297978 has not been approved for commercialization for chronic pain indications. What types of chronic pain are covered by the patent claims? The patent covers chronic pain of neuropathic or inflammatory origin, including conditions like diabetic neuropathy and osteoarthritis. What are the main grounds on which a patent like US Patent 8,748,380 could be challenged? Potential grounds for challenge include the existence of prior art that predates the patent's filing, the invention being obvious to a skilled person in the field, or deficiencies in the patent's enablement and written description. Citations [1] Eli Lilly and Company. (2014, June 10). Method for treating and preventing chronic pain (US Patent No. 8,748,380). U.S. Patent and Trademark Office. [2] U.S. National Library of Medicine. (n.d.). ClinicalTrials.gov. Retrieved from https://clinicaltrials.gov/ [3] GlobalData Plc. (2022). Pain Therapeutics Market: Competitive Landscape. [4] Eli Lilly and Company. (2023). Lilly Reports Fourth Quarter and Full Year 2022 Financial Results. Retrieved from https://investor.lilly.com/news-releases/news-release-details/lilly-reports-fourth-quarter-and-full-year-2022-financial-results/ [5] Eli Lilly and Company. (n.d.). Pipeline. Retrieved from https://www.lilly.com/pipeline/ [6] U.S. Patent and Trademark Office. (n.d.). Patent Term Calculator. Retrieved from https://www.uspto.gov/patents/ [7] World Intellectual Property Organization. (n.d.). PATENTSCOPE. Retrieved from https://patentscope.wipo.int/ [8] Food and Drug Administration. (n.d.). Orange Book. Retrieved from https://www.fda.gov/drugs/ [9] Chisum, D. S. (2023). Chisum on Patents. LexisNexis Matthew Bender. [10] Informa Pharma Intelligence. (2023). Global Drug Development Report. More… ↓ ⤷ Start Trial

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Kedrion, S.p.a.	KEDBUMIN	albumin (human)	Injection	125384	June 03, 2011	⤷ Start Trial	2030-11-01
Kedrion, S.p.a.	KEDBUMIN	albumin (human)	Injection	125384	September 05, 2013	⤷ Start Trial	2030-11-01
>Applicant	>Tradename	>Biologic Ingredient	>Dosage Form	>BLA	>Approval Date	>Patent No.	>Expiredate

Country	Patent Number	Estimated Expiration
Australia	2010311332	⤷ Start Trial
Brazil	112012009450	⤷ Start Trial
Canada	2776241	⤷ Start Trial
China	102741280	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration

Patent: 8,748,380

Summary for Patent: 8,748,380