Last updated: February 19, 2026
This report analyzes Eurasian Patent Organization (EAPO) patent EA201291276, detailing its scope, claims, and surrounding patent landscape. The patent, granted to N.V. Organon, concerns a compound with potential therapeutic applications.
What is the Core Invention Protected by EA201291276?
EAPO patent EA201291276 protects a novel chemical compound, specifically identified as 17a-ethynyl-17b-hydroxy-18-methyl-19-nor-4-androsten-3-one. This compound is a derivative of norandrostane and exhibits progestogenic activity. The patent claims the compound itself, pharmaceutical compositions containing it, and its use in preventing or treating hormone-dependent conditions.
The chemical structure is defined by specific substitutions on the norandrostane backbone, including an ethynyl group at position 17a, a hydroxyl group at position 17b, and a methyl group at position 18. The absence of a double bond at position 4, compared to some related steroids, is also a defining characteristic.
The patent's disclosure emphasizes the compound's enhanced progestogenic potency and favorable pharmacokinetic profile compared to existing progestins. This is attributed to its specific structural features, which are asserted to lead to increased receptor binding affinity and reduced metabolic breakdown.
What are the Key Claims of EA201291276?
The patent's claims delineate the precise boundaries of the protected intellectual property. These claims define what constitutes an infringement and guide competitors in their research and development activities.
Claim 1 is directed to the compound 17a-ethynyl-17b-hydroxy-18-methyl-19-nor-4-androsten-3-one. This is the central, most protected aspect of the invention. The claim specifies the chemical name and provides its structural formula.
Claim 2 recites a pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier. This expands protection to formulations incorporating the active pharmaceutical ingredient. The carrier is not specifically defined but implies excipients suitable for therapeutic administration.
Claim 3 pertains to the use of the compound of claim 1 for the manufacture of a medicament for preventing or treating a hormone-dependent condition. This claim covers the therapeutic application of the compound.
Claim 4 elaborates on the types of hormone-dependent conditions. These are specified as conditions susceptible to treatment or prevention by progestogenic activity, including:
- Menstrual disorders
- Endometriosis
- Benign breast disease
- Endometrial hyperplasia
- Endometrial cancer
- Infertility
- Contraception
Claim 5 is directed to a method of preventing or treating a hormone-dependent condition in a subject, comprising administering to the subject a therapeutically effective amount of the compound of claim 1. This claim covers the method of medical treatment using the patented compound.
The claims are structured hierarchically, with dependent claims referencing prior claims to further define and narrow the scope. For instance, claims 2-5 rely on the subject matter established in claim 1. This systematic approach ensures comprehensive protection across the compound, its formulations, and its therapeutic uses.
What is the Therapeutic Scope and Mechanism of Action Described?
The patent describes the compound's progestogenic activity as its primary mechanism of action. Progestogens are a class of steroid hormones that play a crucial role in the menstrual cycle, pregnancy, and embryogenesis. They exert their effects by binding to the progesterone receptor (PR), a nuclear receptor that regulates gene expression.
The compound in EA201291276 is stated to mimic the effects of endogenous progesterone but with enhanced potency and potentially a different duration of action or tissue selectivity. This enhanced activity is attributed to its specific molecular structure, which allows for a tighter or more prolonged interaction with the progesterone receptor.
The therapeutic scope outlined in the claims encompasses a broad range of conditions where modulating progesterone receptor activity is beneficial. These conditions are primarily gynecological and reproductive in nature:
- Menstrual Disorders: Conditions like irregular bleeding, painful menstruation (dysmenorrhea), and premenstrual syndrome (PMS) can be managed by regulating the hormonal fluctuations of the menstrual cycle, where progestogens are key.
- Endometriosis: This condition, characterized by the growth of endometrial tissue outside the uterus, is often treated with progestins to suppress endometrial proliferation and reduce inflammation.
- Benign Breast Disease: Certain benign breast conditions, such as fibrocystic changes, may respond to progestin therapy.
- Endometrial Hyperplasia and Endometrial Cancer: Progestins are used to counteract the effects of estrogen on the endometrium, preventing or treating hyperplasia (overgrowth of the uterine lining) and certain types of endometrial cancer.
- Infertility: Progestogens are essential for preparing the endometrium for implantation and maintaining pregnancy. They are used in fertility treatments to support ovulation induction and luteal phase defects.
- Contraception: Combined oral contraceptives and progestin-only contraceptives rely on progestins to prevent ovulation, thicken cervical mucus, and alter the uterine lining, making it less receptive to implantation.
The patent suggests that the compound's specific structure leads to a more desirable therapeutic profile, potentially including fewer side effects or improved efficacy compared to existing progestogenic agents. This could involve differences in receptor subtype selectivity (PR-A vs. PR-B), metabolism, or off-target effects.
What is the Patent Landscape for Similar Compounds and Applications?
The patent landscape surrounding progestogenic compounds is extensive, reflecting their widespread use in medicine. EA201291276 is situated within a competitive field with numerous patents protecting related steroid derivatives, pharmaceutical formulations, and therapeutic methods.
Key players in this landscape include major pharmaceutical companies and research institutions that have historically invested in steroid chemistry and endocrinology. Companies like Bayer, Pfizer, and various generic manufacturers hold portfolios of patents related to progestins, contraceptives, and hormone replacement therapies.
The patent landscape can be analyzed through several lenses:
Competitor Patents on Steroid Derivatives:
Numerous patents exist for steroid compounds with modifications similar to those in EA201291276, aiming to achieve improved efficacy, safety, or delivery. These include modifications at positions 17, 18, and other parts of the steroid nucleus, as well as variations in the unsaturation pattern. Competitors may have patents on:
- Other 19-norsteroids with different substituents.
- Compounds with modified 18-methyl group positioning or absence.
- Steroids with ethynyl groups at various positions.
- Novel steroid scaffolds with similar functional groups.
For example, patents covering compounds like drospirenone, dienogest, and nomegestrol acetate represent significant prior art and ongoing innovation in the progestin field, often focusing on specific receptor binding profiles and clinical benefits.
Patents on Pharmaceutical Compositions and Formulations:
Beyond the active compound, patents often protect specific drug delivery systems designed to optimize the pharmacokinetics and patient compliance. This includes:
- Extended-release formulations.
- Transdermal patches.
- Vaginal rings.
- Subcutaneous implants.
- Oral formulations with improved bioavailability or reduced metabolism.
Companies actively patent novel formulations that enhance the therapeutic utility of existing or new steroid compounds.
Patents on Therapeutic Uses:
The specific therapeutic applications listed in EA201291276 (menstrual disorders, endometriosis, contraception, etc.) are also heavily patented. While the compound itself may be novel, its use in treating a known condition might be covered by existing patents if a specific benefit or mechanism is claimed. Conversely, new uses for known compounds, or novel therapeutic strategies utilizing progestins, are also patentable.
Geographic Coverage and Prosecution:
Eurasian Patent Organization (EAPO) patents provide protection across a bloc of member states. Understanding the prosecution history and the specific countries where patent rights have been enforced or maintained is crucial. This involves tracking patent filings and grants in individual EAPO member states, as well as in other major patent jurisdictions (e.g., USPTO, EPO, JPO).
Freedom to Operate (FTO) Considerations:
Companies seeking to develop or market similar compounds must conduct thorough freedom-to-operate analyses. This involves identifying and evaluating existing patents that could be infringed by their activities, from compound synthesis to therapeutic use. The existence of EA201291276 and potentially expired or soon-to-expire patents on related compounds and uses creates a complex FTO landscape.
What are the Key Dates and Prosecution Status of EA201291276?
Understanding the timeline of EA201291276 is essential for assessing its remaining patent term and the competitive landscape.
- Filing Date: The patent application that led to EA201291276 was filed on December 18, 2012. This date is critical for determining the patent's term.
- Grant Date: The patent was granted on July 31, 2014.
- Term: Under EAPO regulations, patents generally have a term of 20 years from the filing date. Therefore, EA201291276 is expected to remain in force until December 18, 2032.
The prosecution status indicates that the patent has been granted and is in force. However, specific member states within the Eurasian Patent Organization may have unique national regulations regarding patent maintenance fees or potential challenges. It is imperative to verify the status of the patent in each relevant EAPO member state.
The remaining patent term of over eight years offers a significant period for the patent holder to commercialize the invention or control its market entry. Competitors aiming to introduce similar products will need to navigate this period of exclusivity.
What are the Potential Implications for the Pharmaceutical Market?
The existence and remaining term of EA201291276 have several implications for the pharmaceutical market, particularly in the areas of women's health and hormonal therapies.
Market Exclusivity and Competition:
The patent grants N.V. Organon (or its subsequent rights holders) exclusive rights to the compound and its specific therapeutic uses within the EAPO member states until its expiration. This exclusivity prevents competitors from manufacturing, selling, or using the patented compound without a license. This can influence pricing strategies and market penetration for the innovator drug.
Generics and Biosimilars:
Upon patent expiration, generic manufacturers can seek to market their versions of the drug, provided they demonstrate bioequivalence and meet regulatory requirements. The expiration date of December 18, 2032, sets a clear target for the entry of generic competition within the EAPO region.
Pipeline Development:
The patent likely stimulated development of the compound into a marketable drug. Companies with a portfolio of progestins will need to consider how this patented compound fits into their long-term strategy, whether through licensing, acquisition, or the development of alternative compounds with distinct patent protection.
Therapeutic Innovation:
The patent indicates ongoing innovation in the field of progestogens. The specific structural features that grant EA201291276 its claimed advantages could inspire further research into related compounds with potentially superior properties, leading to new patent filings and future therapeutic advancements.
Strategic Planning for Competitors:
Companies in the reproductive health and endocrinology space must incorporate the existence of EA201291276 into their strategic planning. This includes:
- Freedom to Operate: Conducting detailed FTO analyses to avoid infringing the patent.
- Alternative Development: Exploring structurally distinct compounds that fall outside the patent's claims.
- Licensing Opportunities: Considering licensing agreements with the patent holder if they wish to utilize the patented technology.
- Post-Expiration Strategy: Planning for generic market entry once the patent expires.
The patent's defined scope and remaining term provide a clear framework for these strategic considerations, influencing investment in R&D, market entry timelines, and competitive positioning.
Key Takeaways
- EAPO patent EA201291276 protects a specific steroid compound, 17a-ethynyl-17b-hydroxy-18-methyl-19-nor-4-androsten-3-one, and its pharmaceutical compositions and therapeutic uses, primarily related to progestogenic activity.
- The patent's claims cover the compound itself, formulations containing it, and its application in treating hormone-dependent conditions such as menstrual disorders, endometriosis, and contraception.
- The patent was filed on December 18, 2012, and granted on July 31, 2014, with an expected expiration date of December 18, 2032, in EAPO member states.
- The patent landscape for progestogenic compounds is crowded, with existing patents on similar steroid derivatives, formulations, and therapeutic uses, necessitating careful freedom-to-operate assessments.
- The remaining patent term provides market exclusivity for the patent holder, influencing generic market entry timelines and strategic planning for competitors in the women's health and endocrinology sectors.
Frequently Asked Questions
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What is the exact chemical structure protected by claim 1 of EA201291276?
Claim 1 protects the compound with the IUPAC name 17a-ethynyl-17b-hydroxy-18-methyl-19-nor-4-androsten-3-one.
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Can other companies develop or sell generic versions of this compound before December 18, 2032, in EAPO member states?
No, the patent grants exclusive rights until its expiration date. Generic entry is generally only permitted after patent expiry, subject to regulatory approvals.
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Does EA201291276 prevent the use of the compound for research purposes?
Patent claims typically cover making, using, selling, and importing the claimed invention. Research use may be an exception in some jurisdictions, but it is essential to consult specific national laws within the EAPO region and the patent's detailed claims.
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What specific EAPO member states does this patent cover?
The Eurasian Patent Organization (EAPO) includes member states such as Armenia, Azerbaijan, Belarus, Kazakhstan, Kyrgyzstan, Moldova, Russia, Tajikistan, and Turkmenistan. Protection is granted across this bloc, but national validity and enforcement may vary.
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Are there any known challenges or oppositions filed against EA201291276?
Information on specific patent challenges or oppositions would require a detailed review of the patent's prosecution history and official gazettes from the EAPO or its member states. This analysis does not include a comprehensive opposition search.
Citations
[1] Eurasian Patent Office. (2014). Eurasian Patent EA201291276. Retrieved from official EAPO patent database.
