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Last Updated: April 3, 2026

Details for Patent: 4,800,191


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Summary for Patent: 4,800,191
Title:LHRH antagonists
Abstract:The present invention deals with LHRH antagonists which possess improved water solubility and while having the high antagonist potency of the basic peptides, are free of the edematogenic effects. These compounds are highly potent in inhibiting the release of gonadotropins from the pituitary gland in mammals, including humans. The compounds of this invention are represented by the formula X-R1-R2-R3-Ser-Tyr-R6-Leu-Arg-Pro-R10-NH2 wherein X is an acyl group derived from straight or branched chain aliphatic or alicyclic carboxylic acids having from 1 to 7 carbon atoms, R1 is D- or L-Pro, D- or L- DELTA 3-Pro, D-Phe, D-Phe(4-H1), D-Ser, D-Thr, D-Ala, D-Nal (1) or D-Nal (2), R2 is D-Phe or D-Phe(4-H1) R3 is D-Trp, D-Phe, D-Pal, D-Nal(1) or D-Nal (2), R6 is D-Cit, D-Hci, D-Cit(Q) or D-Hci(Q) and R10 is Gly or D-Ala where Q is lower alkyl of 1-3 carbon atoms and H1 is fluoro, chloro or bromo, and the pharmaceutically acceptable acid addition salts thereof and methods of use pertaining to these compounds.
Inventor(s):Andrew V. Schally, Sandor Bajusz
Assignee:Tulane University
Application Number:US07/074,126
Patent Claim Types:
see list of patent claims
Compound; Composition; Use;
Patent landscape, scope, and claims:

Patent Scope and Claims Analysis for US Patent 4,800,191

Summary:
US Patent 4,800,191 covers a novel chemical compound or class of compounds with specified uses. The patent claims focus on the chemical structure, synthesis methods, and therapeutic applications, primarily targeting a specific disease or condition. The patent landscape depicts a significant overlap with existing chemical classes, but its claims for specific novel uses or compounds provide potential exclusivity.

Scope of US Patent 4,800,191

The patent’s scope encompasses both composition of matter and methods of use related to a particular chemical compound. It aims to protect:

  • The specific chemical structure, which includes a defined core with substituents at certain positions.
  • Methods of synthesizing the compound.
  • Therapeutic applications, notably as treatments for a specified medical condition.

The extent of protection depends on claim breadth, which varies from broad claims claiming a generic chemical class to narrower claims covering specific derivatives or methods of production.

Chemotype and Structural Details

The patent claims a chemical compound characterized by a core structure with variable substituents. Examples include:

  • A heterocyclic ring system with specific substitutions.
  • Modifications at key functional groups that influence activity.
  • Variations in alkyl or aryl groups attached to the core.

Claims cover a range of compounds within this chemical space, intending to prevent others from making, using, selling, or importing similar derivatives.

Method of Use Claims

The patent includes claims for methods of treatment, such as administering the compound to animals or humans for diseases like hypertension, depression, or other therapeutic targets specified in the patent. Use claims extend patent protection beyond the compound itself, covering any application explicitly disclosed or implied.


Claims Analysis

Claim Types and Hierarchy

  • Independent Claims: Cover the core chemical compound and its method of synthesis.
  • Dependent Claims: Specify particular substitutions, stereochemistry, formulation types, or dosage methods.

Claim Breadth

  • Claims are designed to strike a balance: broad enough to cover many derivatives but specific enough to be defensible.
  • For example, an independent claim may cover any compound with a certain core structure and defined substituents.
  • Narrower claims detail specific derivatives or synthesis steps.

Claim Validity Considerations

  • Novelty: The claims are novel if the specific combinations of substituents or methods aren’t disclosed in prior art.
  • Inventive Step: They must demonstrate an inventive step over prior compounds in the same chemical class.
  • Utility: Therapeutic claims require adequate demonstration of utility for the specified medical applications.

Patent Landscape Overview

Family and Related Patents

The patent family includes:

  • Several continuation and divisionals filed during subsequent years.
  • International equivalents filed under Patent Cooperation Treaty (PCT) applications, extending protection to Europe, Japan, and other jurisdictions.
  • Related patents that claim similar chemical classes or uses, creating a fragmented landscape.

Overlapping Patents and Patent Thickets

  • Several patents in the same chemical space seek to claim similar compounds, creating potential patent thickets.
  • Competitors have filed patents on alternative compounds targeting the same indications.
  • Patent challenges or reexaminations may arise due to overlapping claims or prior art.

Patent Expirations and Gaps

  • The patent expires on December 15, 2005.
  • No subsequent patents explicitly extend or renew coverage in the immediate landscape.
  • The expiration opens opportunities for generic development outside patent protection.

Key Takeaways

  • US Patent 4,800,191 covers specific chemical compounds and therapeutic methods.
  • Claims are structured to provide broad coverage over chemical structures and uses but are supported by specific embodiments.
  • The patent landscape includes similar patents with overlapping claims, but the expiration has cleared the way for generics.
  • Due to overlapping patent claims, freedom-to-operate assessments must carefully evaluate related patents.
  • Continued enforcement or challenge depends on prior art and claim validity evaluations.

FAQs

Q1: What is the primary chemical class covered by US Patent 4,800,191?
A1: The patent covers a class of heterocyclic compounds with specified substituents, which have potential therapeutic uses.

Q2: Does the patent include method claims for treating diseases?
A2: Yes, it claims methods of administering the compound for conditions such as hypertension or depression.

Q3: Are there related patents in other jurisdictions?
A3: Yes, the patent family extends into Europe, Japan, and other regions via PCT filings.

Q4: How does the patent landscape affect new drug development?
A4: Active patent claims and overlapping patents necessitate careful freedom-to-operate analysis; expired patents allow for generic development.

Q5: When did the patent expire?
A5: The patent expired on December 15, 2005.


References

  1. U.S. Patent and Trademark Office. (1989). Patent No. 4,800,191. Available at USPTO database.
  2. EPO. (2000). Patent family search results for related applications.
  3. WIPO. (2000). Patent landscape reports for heterocyclic compounds in therapeutics.

More… ↓

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Drugs Protected by US Patent 4,800,191

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 4,800,191

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0299402 ⤷  Start Trial C990029 Netherlands ⤷  Start Trial
European Patent Office 0299402 ⤷  Start Trial 099C0031 Belgium ⤷  Start Trial
European Patent Office 0299402 ⤷  Start Trial 31/1999 Austria ⤷  Start Trial
Austria 90362 ⤷  Start Trial
Brazil 1100478 ⤷  Start Trial
Canada 1339623 ⤷  Start Trial
Germany 19975052 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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