Details for Patent: 4,616,006
Summary for Patent: 4,616,006
| Title: | Triphasic oral contraceptive | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Abstract: | A method of contraception in which an estrogen and a progestogen are administered daily in a three phase sequence for 21 days is disclosed. In the first phase a combination of an estrogen and a progestogen in a low but contraceptively effective daily dosage corresponding in estrogenic activity to 0.02-0.05 mg of 17α-ethinylestradiol and in progestogenic activity to 0.065-0.75 mg of norethindrone is administered for 5-8 days; followed by the administering of the same dosage of estrogen and a progestogen corresponding in progestogenic activity to 0.25-1.0 mg of norethindrone for 7-11 days; followed by the administering of the same dosage of estrogen and a progestogen corresponding in progestogenic activity to 0.35-2.0 mg of norethindrone for 3-7 days; followed by 6-8 days without administering either an estrogen or a progestogen. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Inventor(s): | Samuel A. Pasquale | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assignee: | Ortho Pharmaceutical Corp | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Application Number: | US06/744,189 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|
Patent Claim Types: see list of patent claims | Composition; Dosage form; | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Patent landscape, scope, and claims: | United States Drug Patent 4,616,006: Claims, Scope, Expiration, Orange Book Status, and Generic RiskU.S. Patent No. 4,616,006 protected a triphasic oral contraceptive regimen using a constant daily estrogen dose and progressively higher progestogen doses across three phases. The patent issued October 7, 1986, and its standard pre-1995 patent term expired October 7, 2003. The principal commercial relevance was the triphasic combination of ethinylestradiol and norgestimate associated with Ortho Tri-Cyclen and generic equivalents.[1,2] The patent no longer creates an enforceable U.S. composition-of-matter or formulation barrier. Its historical importance remains material because it illustrates how contraceptive protection can be divided among dosage architecture, active-ingredient selection, and regulatory product listings. What does U.S. Patent 4,616,006 protect?The patent protects a packaged oral contraceptive unit containing sequential dosage phases. The core architecture is:
The claim is directed to a drug product or dosage unit, not merely to a method of contraception. Infringement would generally require the accused product to satisfy the claimed phase sequence, dosage-unit count, hormonal activity ranges, and constant estrogen condition. The patent does not require that the tablets have a particular color, shape, excipient system, package design, or trade name. Those attributes may support product identification but are not central limitations of the independent claims. How do the independent claims differ?Claims 1 and 10 are the principal independent claims. Claim 1: fixed seven-day phasesClaim 1 requires:
The claim therefore covers a 21-day active regimen, with an optional seven-day placebo interval commonly used in a 28-day blister pack. Claim 10: variable phase lengthsClaim 10 broadens the phase-count structure:
Claim 10 is potentially broader than claim 1 with respect to phase duration. It can cover products with unequal phase lengths, provided the total product is a triphasic unit and the phase-specific hormonal activity ranges are met. The broader numerical ranges do not eliminate the requirement that the phases occur sequentially. A product with changing progestogen doses but no identifiable first, second, and third phases would face a stronger argument that it falls outside the claim. What are the dependent claims covering?Claims 2 through 9 narrow the independent claims by specifying dosage form, hormones, or exact dosing.
Claim 9 is the commercially significant limitation. It identifies the familiar norgestimate triphasic progression:
That regimen corresponds to the active-tablet structure historically marketed as Ortho Tri-Cyclen.[2,3] What formulation patents are protected by U.S. Patent 4,616,006?The patent protects the hormonal formulation in combination with a pharmaceutically acceptable carrier, but it does not claim a narrowly defined excipient formulation. The claims do not specify:
The formulation coverage is therefore functional and compositionally broad at the carrier level, but narrow in the required hormonal sequence and activity ranges. A generic manufacturer could avoid literal infringement by using a different phase schedule, a different estrogen concentration, a non-equivalent progestogen dose, or a monophasic or biphasic regimen. It would still need to assess potential equivalents exposure, regulatory labeling, and any separate patents or exclusivities associated with the product. What is the legal scope of the norgestimate claim?Claim 9 is a dependent claim and inherits every limitation of claim 1. A product must therefore satisfy both the claim 1 architecture and the specific norgestimate dosing schedule. The key legal limitations are:
A product containing the same hormones but a different number of active tablets could avoid claim 9 if it also fell outside claims 1 and 10. A product containing 0.035 mg ethinylestradiol but using a different progestogen would not literally meet claim 9, although claims 1, 3, 5, or other patent rights would require separate analysis. The use of “equivalent” activity language expands the claim beyond a single molecular weight-based dose. It attempts to capture progestogen quantities having comparable biological activity to the stated norethindrone or norgestimate levels. That language can create claim-construction disputes because biological equivalence depends on the relevant assay, pharmacology, and accepted technical meaning at the priority date. When did U.S. Patent 4,616,006 expire?U.S. Patent 4,616,006 issued on October 7, 1986. Because it was subject to the pre-June 8, 1995 patent-term rule, its ordinary term was 17 years from issuance. The resulting expiration date was October 7, 2003.[1]
No current U.S. patent term restoration should be inferred from the patent itself. The patent is not a live blocking right against current generic manufacturers. What was the Orange Book status of the patent?The patent was associated with the historical U.S. regulatory protection for Ortho Tri-Cyclen, an ethinylestradiol/norgestimate oral contraceptive product marketed by Ortho Pharmaceutical and later associated with the Johnson & Johnson pharmaceutical business.[2,3] The Orange Book distinguishes between a listed patent and an enforceable current patent right. A patent may appear in historical product records even after expiration. The presence of U.S. Patent 4,616,006 in product-related records does not create present-day exclusivity. The relevant regulatory framework included:
The product’s contraceptive indication did not depend on biologic licensing. Norgestimate and ethinylestradiol are small-molecule active ingredients, so biosimilar pathways are not relevant. Were there Paragraph IV challenges to this patent?Paragraph IV exposure was most relevant before October 7, 2003. An ANDA applicant seeking approval before patent expiration could certify that the patent was invalid, unenforceable, or would not be infringed. A Paragraph IV certification could trigger patent litigation under the Hatch-Waxman framework and, in some circumstances, a 30-month stay of approval.[4] After expiration, the commercial value of a Paragraph IV challenge to U.S. Patent 4,616,006 materially declined. An applicant could rely on a Paragraph III certification or await expiration rather than incur litigation over a patent that was close to its term end. Public regulatory records establish that generic norgestimate/ethinylestradiol products entered the market after the patent’s expiration period. The patent therefore did not produce a durable post-2003 generic barrier.[2,3] Which companies challenged or competed with the branded product?The competitive field included generic manufacturers filing ANDAs for norgestimate and ethinylestradiol tablets. Publicly identified generic competition has included companies such as Barr Pharmaceuticals, Watson Laboratories, Teva, Mylan, and other ANDA sponsors over time, depending on the specific strength, package, and product listing. The commercial competition was based on:
The patent itself did not prevent competition after October 2003. Later competitive barriers, if any, would have come from regulatory exclusivity, manufacturing capacity, supply agreements, trademarks, or separate product rights rather than this patent. What licensing deals affected the patent landscape?The commercial history of norgestimate and Ortho Tri-Cyclen involved product development, manufacturing, and commercialization arrangements within the contraceptive pharmaceutical sector. Patent 4,616,006 should not be treated as evidence that every party involved in marketing the product owned the underlying patent. Patent ownership, NDA sponsorship, marketing rights, and manufacturing rights can be held by different entities. The relevant patent record identifies the named patent owner and any recorded assignments, while the Orange Book identifies the listed drug application and patent relationship.[1,2] No current licensing arrangement can extend the expired patent’s enforceable term. A license may have commercial significance for trademarks, know-how, manufacturing, or settlement rights, but it cannot restore patent exclusivity after statutory expiration. How strong was the patent estate?The estate was strong against products that copied the complete triphasic architecture and exact norgestimate progression. It was weaker against products that changed the regimen design.
The patent’s main strength was not a novel chemical entity. It was the coordinated dosage regimen. That structure could be copied only by adopting the claimed phase sequence and dose relationships. What generic launch scenarios existed?Three principal generic-entry scenarios applied: Launch after expirationThis was the lowest-risk pathway. An ANDA applicant could target the reference product and enter after October 7, 2003, subject to FDA approval and any remaining regulatory exclusivity. Paragraph III approval before expirationAn applicant could acknowledge the patent and seek approval with a launch date after expiration. This avoided a direct invalidity or noninfringement dispute. Paragraph IV challengeAn applicant could challenge the patent before expiration by asserting invalidity, unenforceability, or noninfringement. This pathway offered earlier-entry potential but carried litigation costs and possible approval delay. For this patent, the post-expiration pathway ultimately became commercially decisive. Generic norgestimate/ethinylestradiol products obtained FDA approval after the patent term ended.[2,3] What manufacturing and geographic barriers remained?The patent was a U.S. right. It did not automatically control:
Foreign counterparts required separate validity, term, and regulatory analysis. A U.S. patent expiration therefore did not determine global freedom to operate. Manufacturing barriers were practical rather than patent-based after 2003. A supplier needed validated processes for multiple tablet strengths, content uniformity across low-dose hormones, dissolution compliance, packaging accuracy, and FDA cGMP compliance. Norgestimate and ethinylestradiol products also require control of cross-contamination and dose uniformity because the active quantities are low. These manufacturing requirements can delay launch or cause shortages, but they do not recreate the patent monopoly. What is the current business significance and revenue exposure?The patent’s direct revenue exposure is zero from a current U.S. patent-enforcement perspective because the patent expired in 2003. Its historical value was substantial because it protected a branded triphasic contraceptive product during the period before generic substitution. Current commercial exposure relates to:
Those factors are separate from patent exclusivity. Investors should not assign current patent value to U.S. Patent 4,616,006 without identifying an unexpired continuation, reissue, patent-term adjustment, settlement restriction, or separate formulation or use patent. The patent number alone does not support such a value assumption. Key Takeaways
FAQs About U.S. Patent 4,616,006Does U.S. Patent 4,616,006 cover Ortho Tri-Cyclen?Yes. Claim 9 corresponds to the triphasic norgestimate and ethinylestradiol dosing pattern historically marketed as Ortho Tri-Cyclen, subject to the full limitations inherited from claim 1. Is U.S. Patent 4,616,006 still enforceable?No. The patent expired on October 7, 2003, under the pre-1995 17-year-from-issuance term. Does the patent cover Tri-Cyclen Lo?The patent does not automatically cover every product marketed under a related trade name. Tri-Cyclen Lo uses a lower ethinylestradiol dose, and infringement would require a product-by-product comparison against every claim limitation. Can a generic manufacturer use the same norgestimate phase doses today?Yes, provided the manufacturer satisfies FDA requirements and is not blocked by a separate unexpired patent, exclusivity right, settlement restriction, or regulatory issue. Does the patent cover contraceptive methods using the same hormones?The quoted claims are directed to a triphasic oral contraceptive unit and its dosage composition. They do not independently claim every method of contraception using ethinylestradiol and norgestimate. References
More… ↓ |
Drugs Protected by US Patent 4,616,006
| Applicant | Tradename | Generic Name | Dosage | NDA | Approval Date | TE | Type | RLD | RS | Patent No. | Patent Expiration | Product | Substance | Delist Req. | Patented / Exclusive Use | Submissiondate |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| >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 4,616,006
| Country | Patent Number | Estimated Expiration | Supplementary Protection Certificate | SPC Country | SPC Expiration |
|---|---|---|---|---|---|
| Canada | 1226221 | ⤷ Start Trial | |||
| >Country | >Patent Number | >Estimated Expiration | >Supplementary Protection Certificate | >SPC Country | >SPC Expiration |
