Share This Page
Details for Patent: 4,868,216
✉ Email this page to a colleague
Summary for Patent: 4,868,216
| Title: | Sulfamoyl-substituted phenethylamine derivatives and process of producing them |
| Abstract: | Novel sulfamoyl-substituted phenethylamine derivatives which exhibit α-adrenergic blocking action and are useful as an antihypertensive agent and an agent for the treatment of congestive heart failure. |
| Inventor(s): | Kazuo Imai, Kunihiro Niigata, Takashi Fujikura, Shinichi Hashimoto, Toichi Takenaka |
| Assignee: | Astellas Pharma Inc |
| Application Number: | US07/311,366 |
|
Patent Claim Types: see list of patent claims | Use; Composition; |
| Patent landscape, scope, and claims: | United States Patent 4,868,216 Scope, Claim Construction, and Patent Landscape for 5-(2-(2-(2-ethoxyphenoxy)ethylamino)-2-methylethyl)-2-methoxybenzenesulfonamide HydrochlorideExecutive summary: U.S. Patent 4,868,216 claims a method of producing alpha-adrenergic antagonistic action in a host by administering an alpha-adrenergic-antagonist amount of a specific pharmaceutical composition containing 5-{2-[2-(2-ethoxyphenoxy)ethylamino]-2-methylethyl}-2-methoxybenzenesulfonamide hydrochloride plus a pharmaceutically acceptable excipient. The claim is composition-based by drug identity but functional by outcome (alpha-adrenergic antagonism). The enforceable scope is driven by (1) whether accused products contain the named hydrochloride, (2) whether administration qualifies as an “alpha-adrenergic antagonistic amount,” and (3) whether the administered formulation has the claimed “pharmaceutical composition” characteristics. The surrounding landscape typically clusters around (a) drug substance and salt form, (b) pharmaceutical formulations (oral, parenteral, sustained release), (c) dosing/regimen and method-of-treatment variants, and (d) design-around alternatives such as different salts, polymorphs, prodrugs, or non-infringing analog compounds. What does U.S. Patent 4,868,216 claim and what is its practical enforceable scope?Featured snippet answer: Claim 1 covers administering a formulation containing the named benzene sulfonamide hydrochloride to produce alpha-adrenergic antagonistic action in a host, with the formulation including a pharmaceutically acceptable excipient and the administered amount being an alpha-adrenergic-antagonist amount. Claim 1 key elements (mapping to infringement questions)Claim 1 (method claim) states:
Infringement pressure points
How broad is the claim likely to be on drug form and dosing?Because the claim is drug-identity anchored (specific named hydrochloride) and outcome functional, it tends to be broad on:
It tends to be narrow on:
What is the scope of “alpha-adrenergic antagonistic amount” in U.S. Patent 4,868,216?Featured snippet answer: The claim limits infringement to administration at an amount sufficient to produce alpha-adrenergic antagonistic effects in the host. In practice, this is evaluated by whether the dosing corresponds to the pharmacologically effective alpha-blocking range for the claimed hydrochloride. Interpretation pathways used in practice
Key litigation dynamicThis limitation is likely the most contested in infringement disputes because it creates a dosing-based factual issue. Under U.S. patent litigation practice, the outcome still usually collapses back to whether the administered product and dose are expected to generate alpha-adrenergic antagonism. What pharmaceutical compositions are covered by the excipient limitation?Featured snippet answer: The claim covers the claimed active hydrochloride in combination with any pharmaceutically acceptable excipient, which usually includes standard formulation components used in oral and parenteral dosage forms. Practical coverage sweepBecause “pharmaceutically acceptable excipient” is broad, most mainstream dosage forms containing the API and standard excipients fall inside literal scope. Typical excipient classes include:
The excipient limitation is less likely to exclude sustained-release or combination formulations as long as the claimed compound remains present. Which patents likely overlap with U.S. Patent 4,868,216 in the U.S. market?Featured snippet answer: Overlap is usually structured around the same active entity: (1) substance and salt form patents, (2) formulation patents for tablets/capsules/solutions and controlled release, (3) dosing and regimen claims framed as alpha-adrenergic antagonism or related therapeutic outcomes, and (4) method-of-treatment patents for specific indications where alpha-blockade is used. Landscape categories to expect around this claimEven without listing each specific co-pending/issued patent number, the enforceability and attack surface for a method claim like this is generally concentrated in four technical buckets: 1) Compound and salt-form patents
These often create the “core” exclusivity that formulation or method claims build on. If a later party uses a different salt (or demonstrates the marketed product is a different salt form), the method claim may be avoided. 2) Formulation and dosage form patents
Those typically do not change the active ingredient identity, so they often remain within method-of-administration scope if dosing achieves alpha antagonism. 3) Method-of-use patents and label-driven claims
If the same therapeutic area is pursued by multiple patents, claim charts usually show many overlapping elements: same API, similar dosing, and functional pharmacology outcomes. 4) Enforcement-adjacent patents
Where claim 1 sits in that ecosystemClaim 1 is a method of producing a pharmacological effect via administration of the named composition. That places it as a potentially strong lever against:
It is weaker against:
What generic entry risks exist for products containing the same hydrochloride?Featured snippet answer: If a generic contains the same 5-{...}-2-methoxybenzenesulfonamide hydrochloride and is administered at a pharmacologically antagonistic dose, U.S. Patent 4,868,216 presents material litigation risk for method-of-use infringement. Generic entry risk increases if the reference product lists the same active ingredient and a comparable dosing regimen that produces alpha blockade. Risk drivers
Design-around options that plausibly reduce risk
How do formulation patents affect the infringement picture under U.S. Patent 4,868,216?Featured snippet answer: Formulation patents usually do not change the core infringement inquiry for claim 1 if the generic still contains the claimed hydrochloride at an antagonistic dose. Instead, formulation IP more often shifts litigation to other patents (composition or manufacturing patents) and to Orange Book listed exclusivities. Common outcomes
What is the Orange Book status of U.S. Patent 4,868,216?No Orange Book status can be stated from the information provided. Without the FDA reference product name, application number, listed NDA/ANDA, and patent listing details, a complete and accurate Orange Book mapping cannot be produced. When does exclusivity end for products covered by this kind of method claim?No definitive exclusivity timeline can be stated from the single claim text provided. A complete and accurate “lose exclusivity” timeline requires file dates, priority chain, patent grant date and expiration, prosecution history, terminal disclaimers, and any FDA 180-day exclusivity interactions for the specific reference product. What patent litigation issues typically arise for alpha-adrenergic antagonist method-of-administration claims?Featured snippet answer: Litigation usually centers on (1) whether the accused product uses the exact claimed hydrochloride, (2) whether the administered dosing is sufficient to produce alpha-adrenergic antagonism, and (3) whether route/dosage form limitations exist in claim construction. Typical dispute set
Key patent estate implications for licensing and freedom-to-operateFeatured snippet answer: The claim is enforceable against competing products that (i) contain the named hydrochloride and (ii) are administered at alpha-adrenergic antagonist doses. Licensing strategy typically targets chemical identity and dosage regimes, not only formulation design. Actionable estate strategy
Key Takeaways
FAQs
References
More… ↓ |
Drugs Protected by US Patent 4,868,216
| 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 |
Foreign Priority and PCT Information for Patent: 4,868,216
| Foriegn Application Priority Data | ||
| Foreign Country | Foreign Patent Number | Foreign Patent Date |
| Japan | 55-14382 | Feb 08, 1980 |
International Family Members for US Patent 4,868,216
| Country | Patent Number | Estimated Expiration | Supplementary Protection Certificate | SPC Country | SPC Expiration |
|---|---|---|---|---|---|
| European Patent Office | 0034432 | ⤷ Start Trial | SPC/GB96/017: EXPIRE | United Kingdom | ⤷ Start Trial |
| European Patent Office | 0034432 | ⤷ Start Trial | 96C0048 | Belgium | ⤷ Start Trial |
| Argentina | 227533 | ⤷ Start Trial | |||
| >Country | >Patent Number | >Estimated Expiration | >Supplementary Protection Certificate | >SPC Country | >SPC Expiration |
