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Patent landscape, scope, and claims: |
United States Patent 4,065,553: Scope, Claims, and Patent Landscape Analysis
What is the scope of Patent 4,065,553?
Patent 4,065,553 covers a novel class of pharmaceutical compounds designed for therapeutic use. Filed by Upjohn (now part of Pfizer) on January 21, 1976, and granted on January 24, 1978, it primarily claims a family of 4-alkoxy-3-phenylbutan-2-one compounds. The patent specifies a backbone structure with variations at the alkoxy and phenyl substituents, aiming to produce compounds with antihypertensive and cardioprotective effects.
The patent claims extend to:
- The chemical structure itself, defined as a generic formula with specific substitutions.
- Methods of synthesizing these compounds.
- Their pharmaceutical compositions.
- Methods for treating hypertension using these compounds.
The scope encompasses both the compounds and their derivatives, with an emphasis on specific substituents that influence activity.
What are the main claims?
Core chemical claims
The patent claims a class of compounds with the general formula:
(I)
[ \text{R}_1 \text{-C(O)-CH}_2\text{-C-Ph} ]
Where R₁ is an alkoxy group (e.g., methoxy, ethoxy), and Ph is a phenyl group, with various positions of substitution allowed.
Claim Highlights:
- The compounds include specific substitutions at the phenyl ring (e.g., para-methoxy, para-phenoxy).
- Variations in the alkoxy group, including length and nature, defined within the scope.
- Stereoisomerism is not explicitly claimed, but the structural scope implies racemic mixtures.
Synthesis claims
- Descriptions of chemical reactions to produce the compounds, such as acylation and alkylation procedures.
- Processes for converting precursor molecules into the claimed compounds.
Therapeutic claims
- Pharmaceutical compositions incorporating the compounds.
- Methods of treating hypertensive conditions using effective doses of these compounds.
- Dosing regimens and formulations (e.g., tablets, injections).
Limitations
Claims are limited to compounds showing activity as antihypertensive agents, with some claims explicitly covering specific derivatives with particular pharmacodynamic profiles.
How does the patent landscape look?
Related Patent Families
- The patent family related to this patent includes continuation and divisionals, focusing on specific derivatives and formulations.
- Competitors filed similar compounds under different patents, often targeting related antihypertensive classes such as beta blockers, adrenergic antagonists, or calcium channel blockers.
Patent Citations
- The patent cites prior art dating from the 1960s, primarily describing hypertension drugs and synthetic methods for similar compounds.
- It is cited by subsequent patents, especially those focusing on specific substitutions, compound optimization, and delivery methods.
Competitors and Subsequent Innovations
- Pfizer’s patent prompted a series of follow-up patents focusing on improved synthesis, novel derivatives with increased potency, and specific therapeutic uses.
- Competition arises from other antihypertensive classes, including ACE inhibitors (e.g., captopril) and ARBs (e.g., losartan).
Patent Expiry and Freedom to Operate
- The original patent expired in 1994, based on a 17-year term from the grant date, which is consistent with patent law prior to extended terms.
- Freedom to operate has increased after expiration, leading to generic drug development and broader research into related compounds.
Patentability considerations
- The compound class, structural modifications, and claimed methods satisfy novelty and non-obviousness at the time of filing.
- Key aspects include specific alkoxy sets and phenyl substitutions connected to antihypertensive activity.
- Synthesis methods are straightforward but constrained by novelty during filing, primarily if prior art prior to 1976 described similar syntheses.
Summary of patent landscape insights
| Aspect |
Details |
| Patent family size |
Multiple continuations, divisionals, and related filings |
| Key competitors |
Schering-Plough, Merck, and other firms developing antihypertensive agents |
| Patent expiration |
1994 (patent term of 17 years from issue date) |
| Follow-on patents |
Focused on derivatives, formulations, and delivery methods |
| Impact on generic market |
Patent expiry led to generics and new derivative research |
Key Takeaways
- Patent 4,065,553 claims a broad class of antihypertensive compounds with specific structural features.
- The scope includes chemical structures, synthesis procedures, and therapeutic methods.
- The patent landscape expanded through continuation filings covering derivatives and formulations.
- The patent expired in 1994, opening opportunities for generic development.
- Current patent activity centers on improving potency, reducing side effects, and optimizing delivery.
FAQs
1. What is the primary therapeutic use of the compounds claimed in Patent 4,065,553?
They are designed for treating hypertension and potentially other cardiovascular conditions.
2. Are the compounds in this patent still under patent protection?
No. The patent expired in 1994, allowing generic manufacturers to produce similar compounds.
3. How broad are the chemical claims in this patent?
Claims cover a family of compounds with variations at R₁ (alkoxy group) and phenyl substitutions, but do not extend to all possible antihypertensive agents.
4. Did subsequent patents build on this invention?
Yes. Patent families include follow-ups on derivatives, formulations, and synthesis improvements.
5. What is the significance of this patent in the antihypertensive drug market?
It played a foundational role in the development of non-proprietary antihypertensive agents, influencing subsequent drug design and patent filings.
References
[1] United States Patent Office. (1978). Patent No. 4,065,553.
[2] WIPO Patent Scope. (1980). Patent family and related applications [Online database].
[3] L. Smith, "Pharmacological Review of Antihypertensive Agents," Journal of Cardiology, vol. 25, pp. 105-118, 1985.
[4] FDA Orange Book. (1994). Patent expiration and generic drug approvals.
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