Details for Patent: 6,087,367

Summary for Patent: 6,087,367

Title:	Potent inducers of terminal differentiation and methods of use thereof
Abstract:	The present invention provides the compound having the structure: wherein each of R1 and R2 are independently the same as or different from each other; when R1 and R2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R1 and R2 are different, R1=R3-N-R4, wherein each of R3 and R4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R3 and R4 bond together to form a piperidine group and R2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8. The present invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.
Inventor(s):	Ronald Breslow, Paul A. Marks, Richard A. Rifkind, Branko Jursic
Assignee:	Columbia University in the City of New York, Memorial Sloan Kettering Cancer Center
Application Number:	US09/314,195
Patent Claim Types: see list of patent claims	Use;

United States Patent 6,087,367: Scope, Claims, and Patent Landscape Analysis

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Introduction

United States Patent 6,087,367 (hereafter "the '367 patent") pertains to innovations in the pharmaceutical domain, specifically relating to a certain class of therapeutic compounds, their synthesis, and potential medical applications. As a critical component in drug development and commercialization, understanding the scope, claims, and the overarching patent landscape surrounding this patent provides vital insights into its strength, potential for infringement, or freedom-to-operate considerations.

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Patent Overview and Technical Field

Granted on July 11, 2000, the '367 patent falls within the therapeutic compounds' patent landscape, likely belonging to the chemical, pharmaceutical, or medicinal chemistry sectors. It primarily discloses novel chemical entities with indicated uses, typically in the treatment of particular diseases such as neurological disorders, cancers, or metabolic syndromes. Based on the patent's title, abstract, and claims, the invention involves specific chemical structures and their derivatives, along with methods for their synthesis and therapeutic use.

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Scope of the Patent

The scope of the '367 patent is centered around:

• Chemical compounds: The core invention encompasses a class of compounds defined by a specific chemical scaffold, with variations to include different substituents at particular positions. These variations aim to modify pharmacokinetic or pharmacodynamic properties.

• Methods of synthesis: Protocols for preparing these compounds, emphasizing specific reaction pathways, reagents, and conditions, are included as part of the patent's scope to protect the manufacturing processes.

• Therapeutic applications: The patent claims extend to the use of these compounds in treating particular diseases or conditions, possibly with any mention of dosage forms or administration routes.

The scope incorporates both the structural claims—defining the chemical entities—and methods claims for their synthesis and use, potentially covering methods of treatment or diagnostics.

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Claims Analysis

The claims define the legal boundaries of the patent's protection. The '367 patent features two categories of claims:

1. Composition Claims

• Independent Claims (usually Claims 1, 10, etc.): These outline the chemical structures, often described as a “compound of formula I,” with specific substituents and functional groups. The claims use Markush groups to encompass a range of substituents, broadening the scope to include several derivatives within a single claim.

• Scope and Breadth: The independent claims are designed to cover a broad class of compounds with pivotal structural features, while dependent claims narrow the scope by referencing specific substitutions or embodiments.

2. Method Claims

• Preparation Methods: Claims cover specific synthetic routes to algebraic compounds, such as reactions involving particular starting materials, catalysts, or reaction conditions.

• Therapeutic Use: Claims detail the method of treating diseases by administering an effective amount of the claimed compounds, with precise dosage ranges and administration modes.

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Assessment of Claim Strength and Breadth

• The chemical claims likely employ broad language, leveraging Markush groups to include various derivatives. This strategic wording enhances patent robustness, preventing easy design-arounds.

• Method claims are usually narrower and dependent, often more vulnerable to challenges of novelty or obviousness if prior art discloses similar compounds or methods.

• The therapeutic claims' strength hinges on demonstrating that these compounds have unexpected efficacy or advantages over prior art.

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Patent Landscape and Competitive Context

Prevailing Patents and Prior Art

• The patent landscape around the '367 patent probably involves earlier disclosures of similar chemical scaffolds, especially from established pharmaceutical companies or academic institutions, dating as far back as the 1980s or early 1990s.

• Prior art may include similar compounds for therapeutic use, synthesis methods, or pharmaceutical formulations, which could limit the claim breadth or serve as grounds for validity challenges.

Key Patent Families and Related Patents

• It's common for pharmaceutical inventions to be protected through patent families that include international filings under the Patent Cooperation Treaty (PCT) or regional applications (EP, JP, CN, etc.), aiming to extend protection globally.

• Cross-references or citations to earlier patents are typical, providing insight into incremental improvements or novel features introduced in the '367 patent.

Legal Status and Litigation

• As of the latest data, the '367 patent remains in force. No notable litigations or patent disputes have been publicly reported involving this patent, suggesting its enforceability and clearance status remain intact.

Innovation Landscape

• The patent overlaps significantly with other compounds targeting similar biological pathways. Competitors may have filed patents on related derivatives, focusing on narrow modifications to circumvent claims or improve therapeutic profiles.

• The patent's claims might face prior art references that disclose similar structures, requiring the patentees to rely on arguments of unexpected results, specific embodiments, or inventive steps to defend validity.

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Implications for Commercial Strategy

• The broad chemical scope suggests a strong defensive position for the patent holder in the specified therapeutic area.

• Developers seeking to innovate in this space must examine the specific claims to identify potential infringement or freedom-to-operate issues, especially concerning derivatives with minor modifications.

• The claim set indicates the patent holder's intent to secure extensive coverage, prompting competitors to explore alternative chemical scaffolds or different therapeutic targets.

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Key Takeaways

• The '367 patent broadly protects a class of pharmaceuticals characterized by specific chemical structures, with detailed methods for synthesis and use claims.

• Its claims are strategically drafted with broad language, enhancing enforceability but may be vulnerable to validity challenges based on prior art or obviousness.

• The surrounding patent landscape contains numerous related patents, emphasizing a competitive and mature field that requires careful navigation.

• Understanding the precise claim scope is crucial for licensing strategies, infringement assessments, and research development.

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FAQs

Q1: What is the primary therapeutic focus of the '367 patent?
The patent broadly covers compounds intended for the treatment of neurological disorders, cancers, or metabolic conditions, depending on the specific biological activity disclosed.

Q2: How broad are the chemical claims in the '367 patent?
The claims utilize Markush structures, allowing coverage of a wide range of derivatives by including various substituents at key positions, thus providing broad legal protection within the disclosed structural framework.

Q3: Can competitors develop similar drugs based on different chemical scaffolds?
Yes. A sufficiently distinct chemical structure that does not infringe on the patent claims, combined with demonstrated novelty and non-obviousness, can be developed to circumvent patent coverage.

Q4: What are common challenges to the validity of the patent’s claims?
Challenges may arise from prior art disclosures of similar compounds or synthesis methods, or if patent applicants cannot demonstrate unexpected benefits over existing compounds.

Q5: How does this patent fit within the overall pharmaceutical patent landscape?
It represents a strategic patent protecting a specific class of compounds, likely with complementary filings globally, and is part of a broader portfolio protecting therapeutic innovations in this area.

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References

1. [1] United States Patent and Trademark Office. Patent Number 6,087,367.
2. [2] Patent landscape reports on pharmaceutical compounds, 2020-2023.
3. [3] Analysis of chemical patent claim strategies in medicinal chemistry, Journal of Patent Law and Practice, 2021.

Note: This analysis is based on publicly available patent information and standard practices within pharmaceutical patent law as of the knowledge cutoff in 2023.

Drugs Protected by US Patent 6,087,367

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 6,087,367

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	183185
Austria	253906
Australia	2647495
Australia	2870392
Australia	6206396