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Last Updated: December 22, 2024

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 wherein X is an acyl group derived from straight or branched chain aliphatic or alicyclic carboxylic acids having from 1 to 7 carbon atoms, R.sup.1 is D- or L-Pro, D- or L- .DELTA. .sup.3 -Pro, D-Phe, D-Phe(4-H1), D-Ser, D-Thr, D-Ala, D-Nal (1) or D-Nal (2), R.sup.2 is D-Phe or D-Phe(4-H1) R.sup.3 is D-Trp, D-Phe, D-Pal, D-Nal(1) or D-Nal (2), R.sup.6 is D-Cit, D-Hci, D-Cit(Q) or D-Hci(Q) and R.sup.10 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): Schally; Andrew V. (Metarie, LA), Bajusz; Sandor (New Orleans, LA)
Assignee:
Application Number:07/074,126
Patent Claim Types:
see list of patent claims
Compound; Composition; Use;
Patent landscape, scope, and claims:

Detailed Analysis of the Scope and Claims of United States Patent 4,800,191

Introduction

United States Patent 4,800,191, titled "LHRH antagonists," was granted on January 24, 1989. This patent is significant in the field of medical science, particularly in the development of peptides with high antagonist potency against Luteinizing Hormone-Releasing Hormone (LHRH). Here, we will delve into the scope, claims, and the broader patent landscape surrounding this invention.

Background

LHRH antagonists are crucial in treating various medical conditions, including genital or sexual disorders and certain types of cancer. The invention described in US Patent 4,800,191 focuses on peptides that possess improved water solubility while maintaining high antagonist potency.

Scope of the Patent

The patent covers a specific class of LHRH antagonists characterized by their chemical structure and properties. Here are the key aspects of the scope:

Chemical Structure

The peptides described in the patent have a specific structure, including various acyl groups, protecting groups, and amino acid residues. For example, the patent specifies that:

  • (X_1) is an acyl group derived from straight and branched chain aliphatic or alicyclic carboxylic acids having from 1 to 7 carbon atoms, t-Boc, or hydrogen.
  • (X_4), (X_5), and (X_8) are hydrogen or protecting groups for the Ser hydroxyl group, Tyr phenolic hydroxyl group, and Arg guanidino group, respectively[4].

Pharmacological Properties

The peptides are designed to have high antagonist potency against LHRH, which is essential for their therapeutic applications. The improved water solubility of these peptides enhances their bioavailability and efficacy.

Claims of the Patent

The patent includes several claims that define the scope of the invention:

Independent Claims

The independent claims outline the core aspects of the invention, such as the specific chemical structures and the peptides' pharmacological properties. For instance:

  • Claim 1 describes the general structure of the LHRH antagonists, including the specific amino acid sequences and protecting groups[4].

Dependent Claims

Dependent claims further specify the invention by detailing variations within the scope of the independent claims. These claims may include different combinations of amino acid residues or protecting groups.

Patent Landscape

To understand the significance and position of US Patent 4,800,191 within the broader patent landscape, we need to consider several factors:

Classification

The patent is classified under various International Patent Classification (IPC) categories, including A61P15/00 (drugs for genital or sexual disorders; contraceptives) and A61K38/00 (medicinal preparations containing peptides)[4].

Prior Art and Related Patents

The patent builds upon existing knowledge in the field of peptide chemistry and LHRH antagonists. Prior art and related patents would include other inventions related to LHRH antagonists, peptide synthesis, and therapeutic applications.

Citations and Impact

The patent's impact can be gauged by the number of forward citations it receives. Forward citations indicate how often the patent is referenced by subsequent patents, which can be a measure of its influence and importance in the field.

Examination Process and Patent Scope

The examination process for this patent would have involved a thorough review of the claims to ensure they meet the criteria for patentability, including novelty, non-obviousness, and utility. The scope of the patent claims would have been narrowed or broadened during this process to align with existing prior art and to ensure clarity and specificity[3].

Economic and Legal Implications

The economic implications of this patent include the potential for exclusive rights to manufacture and market these LHRH antagonists, which could impact the pricing and availability of these drugs. Legally, the patent holder would have the right to enforce the patent against any infringers, which could involve litigation and licensing agreements.

Current Status

As of the current date, the patent has expired, as it was granted in 1989 and patents typically have a term of 20 years from the filing date. This means that the invention is now in the public domain, and anyone can manufacture and use the described LHRH antagonists without infringing on the original patent.

Key Takeaways

  • Specific Chemical Structure: The patent describes LHRH antagonists with specific chemical structures and improved water solubility.
  • Therapeutic Applications: These peptides are designed for treating genital or sexual disorders and other medical conditions.
  • Patent Classification: Classified under IPC categories related to medicinal preparations and peptide chemistry.
  • Examination Process: The patent claims would have been scrutinized to ensure they meet patentability criteria.
  • Economic and Legal Implications: The patent provided exclusive rights but has now expired, placing the invention in the public domain.

FAQs

What is the main focus of US Patent 4,800,191?

The main focus of US Patent 4,800,191 is on LHRH antagonists with improved water solubility and high antagonist potency.

What are the key chemical features of the peptides described in the patent?

The peptides have specific acyl groups, protecting groups, and amino acid residues that contribute to their improved water solubility and antagonist potency.

Under which IPC categories is the patent classified?

The patent is classified under A61P15/00, A61K38/00, and other related IPC categories.

What is the current status of the patent?

The patent has expired, as it was granted in 1989 and the typical patent term is 20 years from the filing date.

What are the economic implications of this patent?

The patent provided exclusive rights to the patent holder, which could impact the pricing and availability of the drugs. Now that the patent has expired, the invention is in the public domain.

Sources

  1. US Patent 4,800,191 - LHRH antagonists.
  2. Patent and patent application Claims data - USPTO.
  3. Patent Claims and Patent Scope - SSRN.
  4. LHRH antagonists - US4800191A - Google Patents.
  5. LU-90425-A9 - Unified Patents.

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

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