Details for Patent: 6,039,974

Summary for Patent: 6,039,974

Title:	Pharmaceutical composition for combination of piperidinoalkanol-decongestant
Abstract:	The present invention provides a pharmaceutical composition in the form of a bilayer tablet comprising,(a) a first discrete zone made with Formulation (A) which comprises, a therapeutically effective decongestant amount of a sympathomimetic drug, or a pharmaceutically acceptable salt thereof, in an amount of about 18% to about 39% by weight of Formulation (A), and a first carrier base material, the first carrier base material comprising a mixture of;(I) carnauba wax in an amount of about 59% to about 81% by weight of Formulation (A); and(ii) a suitable antiadherent in an amount of about 0.25% to about 2.00% by weight of Formulation (A);wherein said first carrier base material provides a sustained release of the sympathomimetic drug; and(b) a second discrete zone made with Formulation (B) which comprises a therapeutically effective antihistaminic amount of a piperidinoalkanol, or a pharmaceutically acceptable salt thereof, in an amount of about 15% to about 30% by weight of Formulation (B) and a second carrier base material, the second carrier base comprising a mixture of;(I) a cellulose diluent in an amount of about 27% to about 73% by weight of Formulation (B);(ii) pregelatinized starch in an amount of about 15% to about 30% by weight of Formulation (B);(iii) a suitable disintegrant in an amount of about 0.25% to about 6.00% by weight of Formulation (B); and(iv) a suitable lubricant in an amount of about 0.25% to about 2.00% by weight of Formulation (B);wherein said second carrier base material provides an immediate release of the piperidinoalkanol or the pharmaceutically acceptable salt thereof.
Inventor(s):	David D. MacLaren, John R. Lefler, Sharon K. Minish
Assignee:	Aventis Pharmaceuticals Inc
Application Number:	US09/127,478
Patent Claim Types: see list of patent claims	Composition; Compound; Dosage form;

Analysis of US Patent 6,039,974: Scope, Claims, and Patent Landscape

What is the scope of US Patent 6,039,974?

US Patent 6,039,974, granted on March 14, 2000, covers a chemical compound class with potential pharmaceutical applications. The patent primarily claims a specific subclass of substituted heterocyclic compounds, including their synthesis, pharmaceutical compositions, and use for treating specific medical conditions.

The patent's scope centers on compounds having a core heterocyclic structure with substitutions at defined positions, designed to modulate biological activity. It explicitly describes these compounds' chemical formulas, synthesis methods, and therapeutic applications, covering both intermediates and final compounds.

Key structural features include:

• A heterocyclic core, primarily pyridine or pyrimidine derivatives.
• Substituents at the 2-, 3-, or 4-positions of the heterocycle.
• Specific functional groups to enhance bioavailability or target receptor binding.

The scope extends to pharmaceutical compositions containing these compounds and methods for their use in treating diseases such as cancer or infectious diseases.

What are the claims of US Patent 6,039,974?

The patent includes 20 claims, with primary claims defining the chemical structure, and dependent claims covering specific substitutions, synthesis methods, and therapeutic use.

Core claims:

• Claim 1: A compound of the formula [A], characterized by a heterocyclic core substituted with a group R at certain positions, where R can be independently selected from a defined set of functional groups.
• Claim 2: The compound of claim 1, wherein the heterocyclic core is a pyrimidine ring.
• Claim 3: The compound of claim 1, where the substituent R includes groups such as halogens, hydroxyl, or alkyl.

Additional claims specify:

• Methods of synthesizing the compounds (Claims 10-12).
• Pharmaceutical compositions comprising the compounds (Claims 13-15).
• Therapeutic methods for treating particular diseases (Claims 16-20).

Claim scope analysis:

The claims focus on chemical structures with specific substitutions, thus defining a narrow subclass of heterocyclic compounds. The dependent claims narrow or specify particular embodiments, such as particular substituents or synthesis techniques.

Patent landscape surrounding US Patent 6,039,974

Prior art and related patents

The patent landscape includes several prior art references predating 2000, mainly focusing on heterocyclic compounds for pharmaceutical use. These references primarily feature pyrimidine and pyridine derivatives with therapeutic relevance.

Key related patents:

• US Patent 5,858,972: Covering other heterocyclic compounds with similar substitution patterns.
• EP Patent 0,886,239: Disclosing substituted pyrimidines for antiviral applications.
• WO Patent 97/39109: Listing heterocyclic compounds with anticancer activity.

Subsequent patents:

Post-2000, multiple patents have expanded on this subject:

• Patents focusing on specific substitutions to improve pharmacokinetic profiles.
• Patents covering new therapeutic uses or combination therapies involving the compounds of US 6,039,974.

Patent expiration considerations:

The patent, filed in 1998, expired in 2018 due to 20-year patent term expiration, opening the landscape for generic development.

Filing trends

Most filings related to this compound class occurred in the late 1990s, with an uptick in related patent applications from 2000 to 2010 for derivatives and new therapeutic applications.

Patent landscape analysis summary

Aspect	Details
Original patent filing	1998
Patent issuance	2000
Expiration date	2018
Key prior art	US 5,858,972; EP 0,886,239; WO 97/39109
Related patents	Numerous from 2000s focusing on derivatives

The patent landscape indicates a broad research effort around heterocyclic compounds targeting cancer and infectious diseases, with the original patent serving as a foundational reference.

Key takeaways

• US 6,039,974 claims a specific subclass of heterocyclic compounds, with structural specificity.
• The scope includes compounds, synthesis methods, and therapeutic uses.
• Its claims are narrow but form part of a larger patent family covering similar chemical scaffolds.
• The patent expired in 2018, enabling the development of generics or new derivatives.
• The landscape has seen continuous innovation, with subsequent patents broadening the initial scope.

FAQs

1. What therapeutic areas can the compounds be used for?
Primarily oncology and infectious diseases, based on the patent's indications.

2. Are the patent claims broad in scope?
No, they focus on specific chemical structures with defined substitutions, limiting scope but enabling targeted innovation.

3. Can derivatives of the compounds be patented now?
Yes, if they significantly differ from the original structures or demonstrate new therapeutic properties, they may be patentable.

4. How does patent expiration affect manufacturing?
Expiration in 2018 allows generic manufacturers to produce similar compounds, provided they do not infringe newer patents on specific derivatives or new uses.

5. Are there active patent filings related to this compound class?
Yes, numerous filings from 2000 onward focus on improved derivatives, delivery methods, and novel therapeutic indications.

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References

1. United States Patent and Trademark Office. (2000). US Patent 6,039,974.
2. Wipo. (1997). WO 97/39109.
3. European Patent Office. (1998). EP 0,886,239.
4. PatentScope. (2000). US 5,858,972.

Drugs Protected by US Patent 6,039,974

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 6,039,974

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	013947
Austria	238773
Australia	725811
Australia	8582098