United States Patent 4,100,274: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 4,100,274, titled "Polypeptide," is a significant patent that deals with novel luliberin analogues, their manufacture, and their applications. This patent, granted for its innovative compounds and processes, has implications in the fields of reproductive biology and veterinary medicine.
Background of Luliberin
Luliberin, also known as Gonadotropin-Releasing Hormone (GnRH), is a natural hormone secreted by the hypothalamus that acts on the pituitary gland to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH). These hormones are crucial for controlling reproductive processes, including ovulation and follicle maturation[1].
Scope of the Patent
The patent covers a range of novel luliberin analogues that possess luliberin agonist activity. These analogues are designed to mimic the actions of natural luliberin but with enhanced potency.
Key Compounds
The patent specifies a preferred group of compounds where:
- A is D-Tyr(Me), D-Ser(Bu t), or D-Phe
- B is Leu or MeLeu
- E is Azgly
- F is an amino radical[1].
These compounds are noted for their ability to release LH more potently than natural luliberin.
Claims of the Patent
The patent includes several claims that outline the composition, manufacture, and use of these luliberin analogues.
Composition Claims
The patent claims cover the specific chemical structures of the luliberin analogues, including their pharmaceutically acceptable acid-addition salts such as hydrochloride, phosphate, citrate, or acetate[1].
Manufacturing Claims
The patent describes the methods for manufacturing these compounds, which involve known chemical synthesis techniques. The process includes steps such as the use of ethyl chloroformate, catalytic reduction, and the use of dicyclohexylcarbodi-imide for peptide bond formation[1].
Use Claims
The patent claims the use of these compounds in controlling and improving reproduction in animals, particularly in large domestic animals during anoestrus and in artificial breeding situations. It also suggests potential use in treating infertility in humans[1].
Patent Landscape
Regulatory Considerations
The patent term and regulatory aspects are crucial. Patents like this one may be subject to term extensions under 35 U.S.C. 156(e)(1) if they undergo regulatory reviews by the FDA or the Department of Agriculture. This can extend the patent term up to five years[4].
Patent Scope Metrics
The scope of a patent can be measured using metrics such as independent claim length and independent claim count. These metrics help in assessing the breadth and clarity of the patent claims. Narrower claims are often associated with a higher probability of grant and a shorter examination process[3].
Applications and Uses
Veterinary Medicine
The luliberin analogues are particularly useful in the breeding of large domestic animals, allowing for more precise control over the time of ovulation. This is especially beneficial during anoestrus, a period when animals are not in their normal breeding cycle[1].
Human Infertility
The compounds may also be used to ameliorate infertility states in men and women by enhancing the release of LH and FSH, which are essential for reproductive processes[1].
Dosage and Administration
The patent specifies the dosage ranges for these compounds. For example, the daily oral dose can range from 50 μg/kg to 20 mg/kg, and the daily parenteral dose can range from 0.2 μg/kg to 100 μg/kg. In humans, these doses translate to a total daily dose of 3.5 mg to 1.4 g administered orally and 14 μg to 7 mg administered parenterally[1].
Manufacturing Process
Step-by-Step Synthesis
The patent details a multi-step synthesis process involving the use of various reagents and solvents. For instance, the process includes the use of N-Benzyloxycarbonyl-L-proline, ethyl chloroformate, and dicyclohexylcarbodi-imide. The steps involve cooling, stirring, and catalytic reduction to form the desired peptide bonds[1].
Conclusion
United States Patent 4,100,274 is a significant contribution to the field of reproductive biology and veterinary medicine. The novel luliberin analogues described in this patent offer enhanced potency and precise control over reproductive processes, making them valuable in both animal breeding and human infertility treatments.
Key Takeaways
- Novel Luliberin Analogues: The patent covers compounds that mimic luliberin with enhanced potency.
- Manufacturing Process: Detailed steps for synthesizing these compounds are provided.
- Applications: Useful in veterinary medicine for breeding and in human infertility treatments.
- Regulatory Considerations: Subject to patent term extensions under specific regulatory reviews.
- Dosage and Administration: Specific dosage ranges are outlined for oral and parenteral administration.
FAQs
What is the primary use of the luliberin analogues described in US Patent 4,100,274?
The primary use is in controlling and improving reproduction in animals, particularly in large domestic animals during anoestrus, and in treating infertility in humans.
How are the luliberin analogues manufactured?
The manufacturing process involves several chemical synthesis steps, including the use of ethyl chloroformate, catalytic reduction, and dicyclohexylcarbodi-imide.
What are the dosage ranges for these compounds?
The daily oral dose can range from 50 μg/kg to 20 mg/kg, and the daily parenteral dose can range from 0.2 μg/kg to 100 μg/kg.
Can the patent term of US Patent 4,100,274 be extended?
Yes, the patent term can be extended under 35 U.S.C. 156(e)(1) if the product undergoes regulatory reviews by the FDA or the Department of Agriculture.
What metrics can be used to measure the scope of a patent like US Patent 4,100,274?
Metrics such as independent claim length and independent claim count can be used to assess the breadth and clarity of the patent claims.
Sources
- US4100274A - Polypeptide - Google Patents
- Tripeptide - Patent US-3781272-A - PubChem
- Patent Claims and Patent Scope - Search eLibrary :: SSRN
- Extension Under 35 U.S.C. 156(e)(1) - OG Date: 29 July 2003
