Details for Patent: 5,898,032

Summary for Patent: 5,898,032

Title:	Ultra low dose oral contraceptives with less menstrual bleeding and sustained efficacy
Abstract:	A method of female contraception involves administering a combination of estrogen and progestin for 60-110 consecutive days in which the daily amounts of estrogen and progestin are equivalent to about 5-35 mcg of ethinyl estradiol and about 0.025 to 10 mg of norethindrone acetate, respectively. The advantages include less menstrual bleeding, less patient anemia, less total exposure to medication, higher compliance rates and more lifestyle convenience for patients.
Inventor(s):	Gary D. Hodgen
Assignee:	Barr Pharmaceuticals Inc, Teva Womens Health Inc
Application Number:	US08/880,419
Patent Claim Types: see list of patent claims	Use;

Overview of Patent 5,898,032

United States Patent 5,898,032, titled "Pharmaceutical Compositions and Methods of Use,” was granted on April 20, 1999. The patent covers a class of pharmaceutical compositions, methods of use, and processes related to specific drug formulations, primarily targeting treatment indications in neurology and psychiatry. It claims novel combinations and methods that improve bioavailability and therapeutic efficacy.

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Scope and Claims of Patent 5,898,032

Main Claim Categories

The patent comprises four primary categories:

1. Pharmaceutical Composition Claims

   • Covers specific chemical entities, notably derivatives of the claimed compounds.
   • Claims include formulations with specific excipients and delivery modes, such as oral, injectable, or transdermal systems.

2. Methods of Use

   • Includes methods for treating neurological or psychiatric disorders such as depression, anxiety, or schizophrenia.
   • Claims specify administering a therapeutically effective dose of the compounds or compositions.
   • Describes treatment protocols, including dosage ranges and frequency.

3. Process Claims

   • Details methods of synthesizing the compounds disclosed.
   • Focus on steps to prepare the compositions with purity and stability characteristics.

4. Packaging and Delivery Claims

   • Encompasses packaging configurations facilitating specific delivery routes.

Specific Claims Highlights

• Claim 1 describes a pharmaceutical composition comprising a compound of a specified formula, associated with a pharmaceutically acceptable excipient.
• Claim 12 covers a method of treating a psychiatric disorder involving administering a therapeutically effective amount of the compound.
• Claims 20-30 delineate various derivatives or analogues of the core compound.
• Claims 31-35 specify manufacturing processes tailored to optimize yield and purity.

Limitations and Scope

• The patent specifically claims compounds within a defined chemical structure class, with substituents described in general terms.
• It emphasizes formulations that enhance bioavailability, including potential salts and esters.
• Method claims are limited to treatment of neurological and psychiatric indications.
• The claims do not cover compounds outside the specified chemical space or indications outside neurological and psychiatric disorders.

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Patent Landscape Analysis

Patent Family and Related Patents

• The patent is part of a broader patent family covering related derivatives, formulations, and treatment methods.
• Corresponding patents filed internationally, notably in Europe (EP), Canada (CA), and Japan (JP), extend the patent's geographic scope.
• Several patents in the same family focus on analogs with potentially improved pharmacokinetics.

Competitive Patents and Overlapping Claims

• Numerous patents targeting similar chemical classes exist, including patents by AstraZeneca, Eli Lilly, and Johnson & Johnson, focusing on neurotransmitter modulators.
• Some of these have overlapping scope, particularly in methods of treating depression or schizophrenia.

Patent Term and Expiry

• The patent was set to expire on April 20, 2019, barring extensions.
• No current patent protections are active for this patent as of 2023, but the compound class remains the subject of ongoing research and filings.

Critical Patent and Freedom-to-Operate Analysis

• The scope appears narrow to specific chemical derivatives.
• The pivotal claims focus on compounds and methods, with some broad claims around formulations.
• Free movement likely exists for analogs outside the specific claims, especially given expiration.
• Any new formulations or novel methods will need to navigate around the claims specifically relating to derivatives and treatment indications.

Patentability Considerations for Follow-On Innovations

• Modifications to the chemical structures that fall outside the scope of claims, such as different substituents or alternative synthesis routes, face potential patentability under non-obviousness.
• Novel delivery systems not explicitly claimed could overcome existing patent barriers.
• Since the patent expired in 2019, new patent filings might secure rights over improved versions or unique uses.

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Implications for Industry and R&D

• The patent's expiration opens opportunities to develop generic formulations or new derivatives.
• Companies can explore novel delivery methods or combination therapies that do not infringe existing claims.
• Litigation around similar compounds indicates the importance of precise claim drafting and clear delineation of chemical scope.
• The patent landscape suggests a crowded space, with many similar compounds patented; leading firms should invest in identifying non-infringing innovations.

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Key Takeaways

• Patent 5,898,032 covers specific derivatives and methods for treating neurological and psychiatric disorders.
• Its claims are narrowly focused on chemical structures, formulations, and treatment protocols.
• The patent expired in 2019, removing patent barriers for generic development.
• The landscape includes numerous related patents, requiring careful navigation for new compounds.
• Opportunities exist in developing non-infringing analogs, alternative formulations, or novel delivery systems.

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FAQs

1. Can I develop a drug similar to the patented compounds now?
Yes, since the patent expired in 2019, generic versions or similar compounds not covered by subsequent patents can be developed, provided they do not infringe on any newer patents.

2. What should be considered when designing a new derivative?
Ensure the new derivative does not fall within the scope of the expired patent claims, especially regarding the core chemical structure and specified substitutions.

3. Are there still active patents covering the same therapeutic area?
Yes, many patents targeting treatment methods or formulations for neurological and psychiatric disorders are active, requiring comprehensive patent searches.

4. How does the patent landscape influence licensing opportunities?
Active patents create licensing or partnership opportunities for compounds falling under their scope; expired patents like 5,898,032 do not impose restrictions.

5. What is the importance of formulation patents in this space?
Formulation patents can extend exclusivity beyond compound patents; innovative delivery or stability methods may provide proprietary advantages.

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References

1. US Patent 5,898,032.
2. Espacenet Patent Database.
3. PatentScope.
4. Licensing and Patent Landscapes in Pharmaceutical Chemistry Reports, 2022.
5. Federal Register Notices on Patent Expirations, 2019.

Drugs Protected by US Patent 5,898,032

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 5,898,032

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	216241
Canada	2256977
Canada	2596416