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Last Updated: December 22, 2024

Details for Patent: 7,820,660


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Summary for Patent: 7,820,660
Title:N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase
Abstract: N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: ##STR00001## are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
Inventor(s): Crescenzi; Benedetta (Rome, IT), Gardelli; Cristina (Ariccia, IT), Muraglia; Ester (Rome, IT), Nizi; Emanuela (Siena, IT), Orvieto; Federica (Rome, IT), Pace; Paola (Rome, IT), Pescatore; Giovanna (Cosenza, IT), Petrocchi; Alessia (Rome, IT), Poma; Marco (Grosseto, IT), Rowley; Michael (Axa, IT), Scarpelli; Rita (Rome, IT), Summa; Vincenzo (Velletri, IT)
Assignee: Instituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A. (Rome, IT)
Application Number:12/214,595
Patent Claim Types:
see list of patent claims
Compound;
Patent landscape, scope, and claims:

United States Patent 7,820,660: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

United States Patent 7,820,660, titled "N-Substituted 5-Hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides and Pharmaceutically Acceptable Salts Thereof," is a significant patent in the field of pharmaceuticals, particularly in the development of HIV integrase inhibitors. This patent, granted to inventors Benedetta Crescenzi, Cristina Gardelli, Emanuela Muraglia, and others, is crucial for understanding the advancements in HIV treatment.

Background and Field of the Invention

The patent is directed to N-substituted 5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides and their pharmaceutically acceptable salts. These compounds are designed to inhibit HIV integrase, an enzyme essential for the replication of the HIV virus. The invention is part of a broader effort to develop effective antiretroviral therapies[1].

Claims of the Patent

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

  • Compound Claims: The patent claims various N-substituted 5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides, including specific substituents such as halogen, hydroxyl, alkyl, and aryl groups. These compounds are optionally mono-substituted or have multiple substituents[1].
  • Pharmaceutically Acceptable Salts: The patent also claims pharmaceutically acceptable salts of these compounds, which are essential for their therapeutic use[1].
  • Saturated Heterocyclic Rings: The claims include 4- to 8-membered saturated heterocyclic rings containing heteroatoms such as nitrogen, oxygen, and sulfur. These rings can be optionally substituted with various groups[1].

Scope of the Invention

The scope of the patent is broad, covering a wide range of compounds and their salts. This breadth is intended to encompass various structural variations that could be effective as HIV integrase inhibitors. The patent specifies that the compounds can be used in the treatment of HIV infection and other diseases where HIV integrase is a target[1].

Patent Landscape

Related Patents and Publications

The patent is part of a series of related patents and publications focused on HIV integrase inhibitors. Other patents, such as US 7,169,780 and US 7,435,734, are cited as part of the same family of inventions. These patents collectively contribute to the development of antiretroviral therapies[1].

International Applications and Foreign Patents

The patent is linked to international applications and foreign patents, such as those filed under the PCT (Patent Cooperation Treaty) and in various countries like Canada and Europe. This indicates a global effort in the development and protection of these compounds[1].

Significance and Impact

The invention described in this patent is significant because it provides highly specific inhibitors of HIV integrase, which is crucial for the replication of the HIV virus. This specificity reduces the risk of side effects and improves the efficacy of the treatment.

"The particular advantage of the present invention is highly specific inhibition of HIV integrase and HIV replication"[1].

Industry Expert Insights

Industry experts emphasize the importance of such targeted therapies in managing HIV. For example, Dr. Anthony Fauci, a leading figure in HIV research, has highlighted the critical role of antiretroviral therapies in controlling the disease.

Statistics and Trends

The development of HIV integrase inhibitors has significantly improved treatment outcomes. According to the CDC, the use of antiretroviral therapy has led to a substantial decrease in HIV-related deaths and an improvement in the quality of life for people living with HIV.

Challenges and Future Directions

Despite the advancements, there are ongoing challenges in HIV treatment, such as drug resistance and the need for more effective and less toxic therapies. Continuous research and development in this area are essential to address these challenges.

Patent Examination and Quality

The USPTO has emphasized the importance of patent quality and thorough examination processes. Recommendations from the GAO, such as defining patent quality and reassessing examination times, are relevant to ensuring that patents like US 7,820,660 meet high standards of innovation and utility[4].

Litigation and Patent Disputes

Patents in the pharmaceutical sector are often subject to litigation. For instance, the case of Arbutus Biopharma Corporation v. Moderna Therapeutics highlights the complexities of patent disputes and the importance of clear patent claims and prior art analysis[5].

Conclusion

United States Patent 7,820,660 represents a critical milestone in the development of HIV integrase inhibitors. The patent's broad scope and specific claims underscore the innovative efforts in pharmaceutical research aimed at combating HIV.

Key Takeaways

  • Specific Inhibition: The patent describes compounds with highly specific inhibition of HIV integrase.
  • Broad Scope: The claims cover a wide range of N-substituted 5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides and their salts.
  • Global Effort: The patent is part of an international effort to develop antiretroviral therapies.
  • Significant Impact: The invention has improved treatment outcomes for HIV patients.
  • Ongoing Challenges: Continuous research is needed to address drug resistance and other challenges.

Frequently Asked Questions (FAQs)

Q: What is the main focus of United States Patent 7,820,660? A: The patent focuses on N-substituted 5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides and their pharmaceutically acceptable salts as inhibitors of HIV integrase.

Q: Who are the inventors of this patent? A: The inventors include Benedetta Crescenzi, Cristina Gardelli, Emanuela Muraglia, and others.

Q: What is the significance of this patent in HIV treatment? A: The patent describes highly specific inhibitors of HIV integrase, which are crucial for effective antiretroviral therapy.

Q: Are there related patents and publications? A: Yes, the patent is part of a series of related patents and publications focused on HIV integrase inhibitors.

Q: How does the USPTO ensure the quality of patents like US 7,820,660? A: The USPTO emphasizes thorough examination processes and has implemented recommendations to improve patent quality, such as defining patent quality and reassessing examination times[4].

Cited Sources

  1. United States Patent and Trademark Office. N-SUBSTITUTED HYDROXYPYRIMIDINONE CARBOXAMIDE INHIBITORS OF HIV INTEGRASE. US Patent 7,820,660 B2, October 26, 2010.
  2. USA.gov. U.S. Patent and Trademark Office (USPTO).
  3. USPTO. Patent Claims Research Dataset.
  4. GAO. Intellectual Property: Patent Office Should Define Quality, Reassess Time Allotted for Examination.
  5. CAFC. ARBUTUS BIOPHARMA CORPORATION v. MODERNATX, INC..

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Drugs Protected by US Patent 7,820,660

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 7,820,660

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 1441735 ⤷  Subscribe CA 2008 00021 Denmark ⤷  Subscribe
European Patent Office 1441735 ⤷  Subscribe 91428 Luxembourg ⤷  Subscribe
European Patent Office 1441735 ⤷  Subscribe C20080001 00016 Estonia ⤷  Subscribe
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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