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Last Updated: December 22, 2024

Details for Patent: 6,362,178


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Summary for Patent: 6,362,178
Title: 2-phenyl substituted imidazotriazinones as phosphodiesterase inhibitors
Abstract:The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.
Inventor(s): Niewohner; Ulrich (Wermelskirchen, DE), Es-Sayed; Mazen (Langenfeld, DE), Haning; Helmut (Wuppertal, DE), Schenke; Thomas (Gladbach, DE), Schlemmer; Karl-Heinz (Wuppertal, DE), Keldenich; Jorg (Wuppertal, DE), Bischoff; Erwin (Wuppertal, DE), Perzborn; Elisabeth (Wuppertal, DE), Dembowsky; Klaus (Boston, MA), Serno; Peter (Gladbach, DE), Nowakowski; Marc (Wuppertal, DE)
Assignee: Bayer Aktiengesellschaft (Leverkusen, DE)
Application Number:09/554,162
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 6,362,178
Patent Claim Types:
see list of patent claims
Compound; Use;
Patent landscape, scope, and claims:

United States Patent 6,362,178: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

The United States Patent 6,362,178, titled "2-phenyl substituted imidazotriazinones as phosphodiesterase inhibitors," was granted on March 26, 2002, to inventors Ulrich Niewöhner, Mazen Es-Sayed, Helmut Haning, and Thomas Schenke. This patent is significant in the field of pharmaceuticals, particularly in the development of phosphodiesterase inhibitors.

Background

Phosphodiesterase (PDE) inhibitors are a class of drugs that play a crucial role in treating various conditions by modulating the levels of cyclic nucleotides (cAMP and cGMP) within cells. The invention described in this patent focuses on 2-phenyl substituted imidazotriazinones, which are potent inhibitors of one or more phosphodiesterases.

Scope of the Patent

Chemical Structure

The patent describes a series of 2-phenyl substituted imidazotriazinones, characterized by specific chemical structures. These compounds have short, unbranched alkyl radicals in the 9-position, which is a key feature contributing to their potency as PDE inhibitors[5].

Pharmacological Activity

The compounds are designed to inhibit phosphodiesterases, enzymes that metabolize cyclic guanosine monophosphate (cGMP) and cyclic adenosine monophosphate (cAMP). This inhibition can lead to therapeutic effects in various conditions, such as cardiovascular diseases, respiratory diseases, and erectile dysfunction.

Claims of the Patent

Independent Claims

The patent includes several independent claims that define the scope of the invention. These claims specify the chemical structure of the 2-phenyl substituted imidazotriazinones, including the presence of specific functional groups and the length and branching of alkyl chains. For example, Claim 1 describes a compound of the formula: [ \text{where R is a straight or branched alkyl group} ] This claim sets the foundation for the broader scope of the invention, allowing for variations in the alkyl group while maintaining the core structure[5].

Dependent Claims

Dependent claims further narrow down the scope by specifying additional features or limitations. These claims may include specific substituents, the length of alkyl chains, or other structural details that enhance the pharmacological activity or stability of the compounds.

Patent Landscape

Prior Art

The patent cites several prior art references, including earlier patents and publications related to phosphodiesterase inhibitors. For instance, patents by Hamilton, Coates, and McMahon et al. are mentioned as relevant prior art, indicating the evolution of research in this field[5].

Related Patents

The patent landscape in the field of phosphodiesterase inhibitors is dense, with numerous patents filed by various pharmaceutical companies. For example, the purchase of Motorola Mobility by Google, which included a significant portfolio of patents, highlights the strategic importance of intellectual property in this sector[2].

Global Patent System

The global patent system plays a crucial role in protecting and enforcing patents like US 6,362,178. Tools such as the Global Dossier and Common Citation Document (CCD) facilitate the management and search of patent families across different intellectual property offices, ensuring that inventors and companies can protect their innovations globally[4].

Economic and Strategic Value

Patent Valuation

The value of a patent like US 6,362,178 can be substantial. The mean price per document for patent transactions can range from $146,000 to $483,924, depending on the deal size and industry. High-profile transactions, such as the sale of Nortel's patent portfolio for $4.5 billion, illustrate the significant economic value attached to such intellectual property[2].

Licensing and Litigation

Patents in the pharmaceutical sector are often subject to licensing agreements and litigation. The scope and claims of a patent like US 6,362,178 are critical in determining its enforceability and the potential for licensing revenue. Broader claims can lead to more extensive protection but may also increase the risk of litigation challenges[3].

Impact on Innovation

Patent Scope and Quality

The scope of a patent, measured by metrics such as independent claim length and count, can influence its quality and the incentives for innovation. Narrower claims, as seen in this patent, are often associated with a higher probability of grant and shorter examination processes, which can foster more focused and effective innovation[3].

Therapeutic Applications

The 2-phenyl substituted imidazotriazinones described in this patent have potential therapeutic applications in various diseases. By inhibiting specific phosphodiesterases, these compounds can modulate cellular signaling pathways, leading to beneficial effects in conditions such as cardiovascular diseases and respiratory disorders.

Search and Examination Process

Patent Search Tools

The USPTO and other international intellectual property offices provide various tools for searching and examining patents. The Patent Public Search tool, Global Dossier, and Common Citation Document are essential resources for identifying prior art and understanding the patent landscape in this field[4].

Examination Metrics

Metrics such as independent claim length and count are used to evaluate the scope of patents during the examination process. These metrics help in assessing the breadth and clarity of patent claims, which are crucial for determining the patent's validity and enforceability[3].

Key Takeaways

  • Chemical Structure: The patent describes 2-phenyl substituted imidazotriazinones with specific alkyl radicals in the 9-position.
  • Pharmacological Activity: These compounds are potent inhibitors of phosphodiesterases, with potential therapeutic applications.
  • Claims: The patent includes independent and dependent claims that define the scope of the invention.
  • Patent Landscape: The patent is part of a dense landscape of phosphodiesterase inhibitors, with significant economic and strategic value.
  • Impact on Innovation: The patent's scope and quality influence innovation and therapeutic applications.

FAQs

What is the primary therapeutic application of the compounds described in US 6,362,178?

The primary therapeutic application of the 2-phenyl substituted imidazotriazinones is as phosphodiesterase inhibitors, which can be used to treat conditions such as cardiovascular diseases, respiratory diseases, and erectile dysfunction.

How do the claims in US 6,362,178 define the scope of the invention?

The claims in US 6,362,178 define the scope of the invention by specifying the chemical structure of the compounds, including the presence of specific functional groups and the length and branching of alkyl chains.

What is the economic value of patents like US 6,362,178?

The economic value of patents like US 6,362,178 can be substantial, with mean prices ranging from $146,000 to $483,924 per document, and high-profile transactions reaching billions of dollars.

How do metrics like independent claim length and count impact patent quality?

Metrics like independent claim length and count are used to evaluate the scope of patents. Narrower claims are often associated with a higher probability of grant and shorter examination processes, which can foster more focused and effective innovation.

What tools are available for searching and examining patents in the USPTO?

The USPTO provides tools such as the Patent Public Search tool, Global Dossier, and Common Citation Document for searching and examining patents.

Sources

  1. US6362178B1 - 2-phenyl substituted imidazotriazinones as phosphodiesterase inhibitors - Google Patents
  2. The value of a patent - Perpetual Motion Patents
  3. Patent Claims and Patent Scope - SSRN
  4. Search for patents - USPTO
  5. United States Patent (10) Patent No.: US 6,362,178 B1 - Google APIs

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Drugs Protected by US Patent 6,362,178

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: 6,362,178

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Germany197 50 085Nov 12, 1997
Germany198 12 462Mar 23, 1998
Germany198 40 289Sep 04, 1998
PCT Information
PCT FiledOctober 31, 1998PCT Application Number:PCT/EP98/06910
PCT Publication Date:May 20, 1999PCT Publication Number: WO99/24433

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