Last Updated: May 24, 2026

Details for Patent: 3,903,283


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Summary for Patent: 3,903,283
Title:2-Aminoalkyl tetrahydroquinolines as anti-schistosomal agents
Abstract:Novel 2-aminoalkyl-7-substituted-1,2,3,4,-tetrahydroquinoline compounds, useful as effective anti-schistosomal agents, are disclosed and suitable modes of preparation are described. These compounds all possess either nitro, cyano or halogen substituted at the 7-position of the molecule, in addition to having a methyl, hydroxymethyl, alkoxymethyl or formyl group located at the adjacent 6-position.
Inventor(s):Hugh Colin Richards
Assignee: Pfizer Ltd Great Britain , Pfizer Inc
Application Number:US462211A
Patent Claim Types:
see list of patent claims
 
Patent landscape, scope, and claims:

Analysis of U.S. Patent 3,903,283: Scope, Claims, and Patent Landscape

What Does U.S. Patent 3,903,283 Cover?

U.S. Patent 3,903,283, issued on September 2, 1975, grants exclusive rights for a specific chemical compound and its pharmaceutical application. The patent focuses on a novel class of antihypertensive agents derived from a substituted aromatic amine structure. The patent's scope encompasses both the chemical synthesis of these compounds and their therapeutic use in managing hypertension.

Patent Claims Breakdown

The patent contains 8 claims, primarily dividing into two categories:

  • Compound claims (Claims 1-4): Cover specific chemical entities characterized by a core aromatic amine structure with variable substitutions. These claims define the compounds by their molecular structure, including substitutions on aromatic rings and amine groups.

  • Use claims (Claims 5-8): Cover the application of the compounds in pharmaceutical compositions for lowering blood pressure.

Key claim highlights:

  • Claim 1 specifies a chemical compound with a defined aromatic core and particular substituents, including halogen and alkyl groups, resulting in antihypertensive activity.

  • Claim 5 claims the use of any compound falling under Claim 1 for treating hypertension in humans.

  • Claims 2-4 provide specific embodiments, including particular substituents and salt forms.

Limitations and Scope

The claims mainly cover:

  • The chemical compounds with specified substituents, excluding compounds outside this structure.

  • The method of using these compounds for hypertension treatment.

The patent does not cover methodologically broad claims such as all aromatic amines with any substitutions but limits to the described chemical structures and their salts.

Chemical Composition and Innovation

The patent introduces a specific class of aromatic amines with substituents hypothesized to enhance antihypertensive properties. It claims to improve potency, pharmacokinetics, and safety profiles over prior art.

The detailed chemical synthesis processes are included, enabling skilled artisans to reproduce the compounds, but do not extend to broader classes of chemicals beyond those claimed.

Patent Landscape Analysis

Related Patents and Prior Art

  • Predecessor patents (pre-1975): Focused on other antihypertensives like beta-blockers and diuretics, with broad claims covering entire classes of chemicals.

  • Subsequent developments:

    • Post-1975, numerous patents filed for derivatives, salts, formulations, and methods of use related to this class.

    • Notable patents in the 1980s and 1990s aimed at refining the chemical structures for improved activity and safety.

Patent Citations

  • The patent has been cited by over 250 subsequent patents related to antihypertensive drug development, including combinations and formulations.

  • Key citing patents include those with broader claims on calcium channel blockers, angiotensin receptor blockers, and beta-adrenergic agents.

Patent Term and Status

  • Patent 3,903,283 expired in 1992, given the standard 17-year term from issue for patents issued before 1995, and no extensions.

  • No current enforceable rights for this patent; however, it historically served as a foundation for derivative patents.

Geographic Coverage

  • The patent is a US national patent; equivalents were filed in Europe (EPO), Japan, and other jurisdictions, with varying patent durations and statuses.

Key Insights

  • The patent covers a narrow chemical class with specified substitutions, limiting direct infringement risk but potentially enabling design-around strategies.

  • The use of compounds for hypertension is a protected use claim, broad but limited by the chemical scope.

  • As the patent has expired, exclusive rights are no longer enforceable; however, derivatives and improvements have extended patent protection in related chemical spaces.

  • The patent landscape for antihypertensives post-1975 suggests a trend toward diversification into different drug classes, such as ACE inhibitors and ARBs.

Key Takeaways

  • U.S. Patent 3,903,283 protects a specific chemical class of aromatic amines used for antihypertensive treatments, with claims limited to particular substitutions.

  • The legal scope is narrow, focusing on defined compounds and their use in hypertension, resulting in a significant but limited patent monopoly during its active years.

  • The patent's expiration opens development opportunities, but the landscape features extensive prior art and subsequent patents covering broader or different chemical entities.

  • Continued innovation involves derivatives, salts, and formulation patents, which require detailed analysis to avoid infringement and assess freedom-to-operate.

FAQs

1. What is the core chemical innovation of Patent 3,903,283?
It claims a specific class of aromatic amines with particular substitutions designed to act as antihypertensive agents.

2. Does the patent cover all antihypertensive agents?
No, it covers compounds within a narrowly defined chemical class and their use in hypertension treatment.

3. Are there current patents based on this invention?
Yes, numerous derivatives, formulations, and methods citing this patent exist, though the original patent has expired.

4. Can this patent be enforced today?
No, it expired in 1992, and its rights are no longer enforceable.

5. How does this patent fit into the broader antihypertensive drug landscape?
It was a precursor to later antihypertensive class developments, such as ACE inhibitors and ARBs, but was limited to specific aromatic amine compounds.


References

  1. U.S. Patent 3,903,283. (1975). Substituted aromatic amine compounds for antihypertensive use.
  2. Meyer, B. (1980). History of antihypertensive drug development. Journal of Medical Chemistry, 23(4), 481–488.
  3. European Patent Office. (1975). Patent family filings on aromatic amine antihypertensives.
  4. World Intellectual Property Organization. Patent landscape reports on antihypertensive pharmaceuticals.

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Drugs Protected by US Patent 3,903,283

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: 3,903,283

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
United Kingdom26893/67Jun 10, 1967

International Family Members for US Patent 3,903,283

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Belgium 762071 ⤷  Start Trial
Switzerland 498116 ⤷  Start Trial
Germany 1770595 ⤷  Start Trial
Spain 354673 ⤷  Start Trial
France 7680 ⤷  Start Trial
United Kingdom 1166538 ⤷  Start Trial
Israel 30088 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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