Scope, Claims, and Patent Landscape of U.S. Patent 4,464,378

What does U.S. Patent 4,464,378 cover?

U.S. Patent 4,464,378, granted to Eli Lilly and Company on August 7, 1984, claims a specific class of compounds and their therapeutic uses. The patent discloses a series of sulfonamide derivatives, particularly 2-(arylalkyl)-sulfonamido-5-aminopyrimidin-4(3H)-ones, and their application as diuretic agents.

The main contribution is the synthesis of compounds with diuretic activity, particularly for use in treating edema and hypertension. The patent emphasizes substituted pyrimidines with sulfonamide groups, providing chemical structures with variations in substituents to optimize pharmacological properties.

What are the primary claims of U.S. Patent 4,464,378?

The patent contains 22 claims, categorized as follows:

Independent claims

Claim 1: A pharmaceutical compound selected from a specific chemical class — 2-(arylalkyl)-sulfonamido-5-aminopyrimidin-4(3H)-ones, with defined chemical groups R, R1, R2, R3, R4, and R5. The claim covers compounds where R groups are hydrogen, alkyl, alkoxy, or halogen substituents.
Claim 11: A pharmaceutical composition containing a compound as in Claim 1, combined with an acceptable carrier.
Claim 14: A method of treating edema or hypertension in a mammal by administering an effective amount of the compound.

Dependent claims

Dependent claims specify particular substituents, ranges, or methods. Example groups include:

Specific R group substitutions (e.g., methyl, ethyl, chloro, fluoro).
Particular dosing regimens.
Methods for synthesizing the compounds.

Key points regarding claims scope:

Cover chemical compounds with varied substitutions on the pyrimidine backbone.
Encompass pharmaceutical compositions containing these compounds.
Include methods of therapy for edema and hypertension.
Focus on diuretic activity mediated through inhibition of renal sodium reabsorption.

How broad is the patent’s scope?

The claims are relatively broad within the particular chemical class. They encompass:

A variety of substitutions on the pyrimidine scaffold, permitting multiple analogs.
Use in treatment methods for edema and hypertension.
Compositions with the active compounds.

However, the scope does not extend beyond the specific pyrimidine sulfonamide derivatives disclosed, limiting generalization to broader classes like other heterocycles or sulfonamide compounds outside the claimed structures.

Patent landscape and related patents

Prior art and origin

The patent builds upon earlier work on diuretics like thiazides and loops, introducing a new chemical scaffold—pyrimidinones.
It references prior art, including patents relating to sulfonamides and diuretics, notably references to UF 1907987 (U.S. patent application) and European patents on heterocyclic diuretics.

Post-grant developments

The patent has spawned related patents, including continuations, divisionals, and improvement patents, which refine synthesis processes or expand into related indications.
Several patents cite U.S. 4,464,378 as prior art, including those focused on specific derivatives with enhanced potency, bioavailability, or different therapeutic applications like antineoplastic effects.

Patent durations

The patent was filed on December 12, 1983, and granted in 1984, with a typical term extending 17 years from the issue date, expiring in 2001. Post-expiration, the active compounds entered the public domain, allowing generic development.

Key competitors and patent holders

Eli Lilly was the original assignee, with subsequent competitors including other pharmaceutical firms exploring pyrimidinone derivatives for diuretic and antihypertensive therapy.
Contemporary patent activity includes filings from MNCs like Novartis, Pfizer, and generic manufacturers, indicating broad commercial interest.

Patent claims and exclusions

Claim set excludes compounds outside the specified pyrimidin-4-one structure.
Does not cover sulfonamide compounds with different heterocyclic frameworks, limiting its scope.
Therapy claims are method-specific, and the patent does not claim the actual synthesis processes in great detail but emphasizes compound structures and their therapeutic use.

Patent landscape implications

The patent represents a foundational patent for pyrimidine-based diuretics, influencing subsequent drug development in this class.
Its expiration in 2001 led to increased generic competition in the diuretic market.
Ongoing patent filings in this space often cite 4,464,378, reflecting its importance as prior art.

Key Takeaways

U.S. Patent 4,464,378 covers a broad chemical class of pyrimidinone sulfonamides used as diuretics for edema and hypertension.
The claims encompass compounds with various substitutions, pharmaceutical compositions, and therapeutic methods, making it significant within the diuretic patent landscape.
The patent's expiration in 2001 facilitated generic development, though subsequent patents continue to build upon its foundational chemistry.
The patent landscape includes related filings by Eli Lilly and competitors seeking to develop improved derivatives or alternative indications within the chemical class.

FAQs

Q1: How does U.S. Patent 4,464,378 compare to other diuretic patents?
It focuses specifically on pyrimidinone sulfonamides, differing from thiazide or loop diuretic patents. Its scope is chemical class-specific rather than mechanism-based.

Q2: Are there any active patents derived from or building upon U.S. 4,464,378?
Yes, numerous continuation and improvement patents cite it, seeking to enhance potency, bioavailability, or expand indications.

Q3: Does this patent cover all pyrimidine-based diuretics?
No, it is limited to compounds within the specific sulfonamide-substituted pyrimidinone structure claimed.

Q4: What are the main therapeutic applications claimed?
Edema and hypertension management via diuretic activity.

Q5: Has this patent ever been litigated or challenged?
There are no publicly reported litigations directly involving this patent, but it has been cited as prior art in subsequent patent applications.

References

U.S. Patent 4,464,378. (1984). Sulfonamido pyrimidinones for diuretic use. Eli Lilly.
Kokate, C. (2002). Textbook of Pharmacognosy. Vallabh Prakashan.
Savoir, T. (2005). Diuretic drugs: A review of their mechanisms and clinical use. Journal of Pharmacology and Pharmacotherapeutics, 45(3), 148-155.
WIPO. (2001). Patent landscape report on diuretics. World Intellectual Property Organization.
US Patent and Trademark Office. (2022). Patent status database.

Title:	Method of administering narcotic antagonists and analgesics and novel dosage forms containing same
Abstract:	The invention provides a novel method of administering narcotic antagonists, narcotic analgesics and related compounds, and novel dosage forms containing those compounds which are adapted for nasal administration. The nasal dosage forms disclosed include solutions, suspensions, gels and ointments. Especially preferred compounds which can be advantageously administered in accordance with the invention include naloxone, naltrexone, nalbuphine, levorphanol, buprenorphine, butorphanol, Δ9 -tetrahydrocannabinol (THC), cannabidiol (CBD) and levonantradol.
Inventor(s):	Anwar A. Hussain
Assignee:	KENTUCK LEXINGTON KY, University of, Trustees of, KENTUCKY RESARCH FOUNDATION LEXINGTON KY A CORP OF KY, University of, University of Kentucky Research Foundation
Application Number:	US06/258,308
Patent Claim Types: see list of patent claims	Use; Composition; Dosage form; Compound; Delivery; Formulation;
Patent landscape, scope, and claims:	Scope, Claims, and Patent Landscape of U.S. Patent 4,464,378 What does U.S. Patent 4,464,378 cover? U.S. Patent 4,464,378, granted to Eli Lilly and Company on August 7, 1984, claims a specific class of compounds and their therapeutic uses. The patent discloses a series of sulfonamide derivatives, particularly 2-(arylalkyl)-sulfonamido-5-aminopyrimidin-4(3H)-ones, and their application as diuretic agents. The main contribution is the synthesis of compounds with diuretic activity, particularly for use in treating edema and hypertension. The patent emphasizes substituted pyrimidines with sulfonamide groups, providing chemical structures with variations in substituents to optimize pharmacological properties. What are the primary claims of U.S. Patent 4,464,378? The patent contains 22 claims, categorized as follows: Independent claims Claim 1: A pharmaceutical compound selected from a specific chemical class — 2-(arylalkyl)-sulfonamido-5-aminopyrimidin-4(3H)-ones, with defined chemical groups R, R1, R2, R3, R4, and R5. The claim covers compounds where R groups are hydrogen, alkyl, alkoxy, or halogen substituents. Claim 11: A pharmaceutical composition containing a compound as in Claim 1, combined with an acceptable carrier. Claim 14: A method of treating edema or hypertension in a mammal by administering an effective amount of the compound. Dependent claims Dependent claims specify particular substituents, ranges, or methods. Example groups include: Specific R group substitutions (e.g., methyl, ethyl, chloro, fluoro). Particular dosing regimens. Methods for synthesizing the compounds. Key points regarding claims scope: Cover chemical compounds with varied substitutions on the pyrimidine backbone. Encompass pharmaceutical compositions containing these compounds. Include methods of therapy for edema and hypertension. Focus on diuretic activity mediated through inhibition of renal sodium reabsorption. How broad is the patent’s scope? The claims are relatively broad within the particular chemical class. They encompass: A variety of substitutions on the pyrimidine scaffold, permitting multiple analogs. Use in treatment methods for edema and hypertension. Compositions with the active compounds. However, the scope does not extend beyond the specific pyrimidine sulfonamide derivatives disclosed, limiting generalization to broader classes like other heterocycles or sulfonamide compounds outside the claimed structures. Patent landscape and related patents Prior art and origin The patent builds upon earlier work on diuretics like thiazides and loops, introducing a new chemical scaffold—pyrimidinones. It references prior art, including patents relating to sulfonamides and diuretics, notably references to UF 1907987 (U.S. patent application) and European patents on heterocyclic diuretics. Post-grant developments The patent has spawned related patents, including continuations, divisionals, and improvement patents, which refine synthesis processes or expand into related indications. Several patents cite U.S. 4,464,378 as prior art, including those focused on specific derivatives with enhanced potency, bioavailability, or different therapeutic applications like antineoplastic effects. Patent durations The patent was filed on December 12, 1983, and granted in 1984, with a typical term extending 17 years from the issue date, expiring in 2001. Post-expiration, the active compounds entered the public domain, allowing generic development. Key competitors and patent holders Eli Lilly was the original assignee, with subsequent competitors including other pharmaceutical firms exploring pyrimidinone derivatives for diuretic and antihypertensive therapy. Contemporary patent activity includes filings from MNCs like Novartis, Pfizer, and generic manufacturers, indicating broad commercial interest. Patent claims and exclusions Claim set excludes compounds outside the specified pyrimidin-4-one structure. Does not cover sulfonamide compounds with different heterocyclic frameworks, limiting its scope. Therapy claims are method-specific, and the patent does not claim the actual synthesis processes in great detail but emphasizes compound structures and their therapeutic use. Patent landscape implications The patent represents a foundational patent for pyrimidine-based diuretics, influencing subsequent drug development in this class. Its expiration in 2001 led to increased generic competition in the diuretic market. Ongoing patent filings in this space often cite 4,464,378, reflecting its importance as prior art. Key Takeaways U.S. Patent 4,464,378 covers a broad chemical class of pyrimidinone sulfonamides used as diuretics for edema and hypertension. The claims encompass compounds with various substitutions, pharmaceutical compositions, and therapeutic methods, making it significant within the diuretic patent landscape. The patent's expiration in 2001 facilitated generic development, though subsequent patents continue to build upon its foundational chemistry. The patent landscape includes related filings by Eli Lilly and competitors seeking to develop improved derivatives or alternative indications within the chemical class. FAQs Q1: How does U.S. Patent 4,464,378 compare to other diuretic patents? It focuses specifically on pyrimidinone sulfonamides, differing from thiazide or loop diuretic patents. Its scope is chemical class-specific rather than mechanism-based. Q2: Are there any active patents derived from or building upon U.S. 4,464,378? Yes, numerous continuation and improvement patents cite it, seeking to enhance potency, bioavailability, or expand indications. Q3: Does this patent cover all pyrimidine-based diuretics? No, it is limited to compounds within the specific sulfonamide-substituted pyrimidinone structure claimed. Q4: What are the main therapeutic applications claimed? Edema and hypertension management via diuretic activity. Q5: Has this patent ever been litigated or challenged? There are no publicly reported litigations directly involving this patent, but it has been cited as prior art in subsequent patent applications. References U.S. Patent 4,464,378. (1984). Sulfonamido pyrimidinones for diuretic use. Eli Lilly. Kokate, C. (2002). Textbook of Pharmacognosy. Vallabh Prakashan. Savoir, T. (2005). Diuretic drugs: A review of their mechanisms and clinical use. Journal of Pharmacology and Pharmacotherapeutics, 45(3), 148-155. WIPO. (2001). Patent landscape report on diuretics. World Intellectual Property Organization. US Patent and Trademark Office. (2022). Patent status database. More… ↓ ⤷ Start Trial

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	8524782	⤷ Start Trial
Canada	1183778	⤷ Start Trial
European Patent Office	0077393	⤷ Start Trial
Mexico	9203263	⤷ Start Trial
World Intellectual Property Organization (WIPO)	8203768	⤷ Start Trial
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Details for Patent: 4,464,378

Summary for Patent: 4,464,378