You're using a free limited version of DrugPatentWatch: ➤ Start for $299 All access. No Commitment.

Last Updated: March 26, 2026

Details for Patent: 7,598,271


✉ Email this page to a colleague

« Back to Dashboard


Summary for Patent: 7,598,271
Title:Crystalline paroxetine methane sulfonate
Abstract:The invention relates to a compound, and pharmaceutically acceptable salts, having the formula I: wherein: R represents an alkyl or alkynyl group having 1-4 carbon atoms, or a phenyl group optionally substituted by C1-4 alkyl, alkylthio, alkoxy, halogen, nitro, acylamino, methylsulfonyl or methylenedioxy, or represents tetrahydronaphthyl, R1 represents hydrogen, trifluoro (C1-4) alkyl, alkyl or alkynyl, X represents hydrogen, alkyl having 1-4 carbon atoms, alkoxy, trifluoroalkyl, hydroxy, halogen, methylthio or aralkoxy, R2 represents: a C1-C10 alkyl group, a phenyl group optionally substituted by one or more of the following groups: a C1-C10 alkyl group, a halogen group, a nitro group, hydroxy group, and/or an alkoxy group.
Inventor(s):Franciscus Bernardus Gemma Benneker, Frans Van Dalen, Jacobus Maria Lemmens, Theodorus Hendricus Antonium Peters, Frantisek Picha
Assignee:Sebela Ireland Ltd
Application Number:US09/200,743
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 7,598,271
Patent Claim Types:
see list of patent claims
Compound;
Patent landscape, scope, and claims:

Analysis of United States Drug Patent 7,598,271: Claims, Landscape, and Strategic Implications

United States Patent 7,598,271, titled "Amides of substituted pyrazolo[3,4-b]pyridines and uses thereof," issued on October 6, 2009, to Plexxikon, Inc. The patent covers a class of chemical compounds and their therapeutic applications. This analysis details the patent's claims, examines its place within the broader patent landscape, and provides insights relevant to R&D and investment decisions.

What Compounds Does Patent 7,598,271 Claim?

The core of patent 7,598,271 lies in its compound claims, which define the structural characteristics of the claimed molecules. The patent broadly claims substituted pyrazolo[3,4-b]pyridines.

Claim 1: The Central Compound Claim

Claim 1 is the broadest independent compound claim within the patent. It defines a compound of Formula I:

     R1
     |
 R2--C--N--R3
     |  ||
     C--C--R4
    / \ |
   N   C--R5
  / \ /
 C---C

Where R1, R2, R3, R4, and R5 are defined by specific substituents and structural limitations. These substituents include:

  • R1: Typically a hydrogen atom or an alkyl group.
  • R2: Can be a hydrogen atom, an alkyl group, or a cyclic or heterocyclic group.
  • R3: Often an amide moiety, defined as -C(=O)R6, where R6 is a substituted or unsubstituted aryl or heteroaryl group.
  • R4: Can be a hydrogen atom, an alkyl group, or a substituted or unsubstituted aryl or heteroaryl group.
  • R5: Usually a hydrogen atom or an alkyl group.

The pyrazolo[3,4-b]pyridine core is a bicyclic heterocycle that forms the structural backbone of the claimed compounds. The specific nature of the substituents R1 through R5 dictates the precise chemical identity and properties of each claimed molecule.

Dependent Claims: Narrowing the Scope

Dependent claims 2 through 20 further refine and narrow the scope of the invention by specifying particular combinations of substituents and structural features. For example:

  • Claim 2: Specifies that R3 is a substituted phenyl group.
  • Claim 3: Further defines the substituents on the phenyl group in R3.
  • Claim 4: Specifies that R6 is a substituted or unsubstituted heteroaryl group.
  • Claim 5: Defines particular heterocyclic groups that R6 can be.
  • Claim 6: Specifies that R2 is an alkyl group.
  • Claim 7: Specifies that R4 is an alkyl group.
  • Claim 8: Specifies that R4 is a substituted or unsubstituted aryl or heteroaryl group.

These dependent claims create a hierarchical structure, with the independent claims defining the overarching invention and the dependent claims providing specific embodiments and narrower protection. This strategy is common in pharmaceutical patenting to cover a broad genus of compounds while also securing protection for key, potentially more potent or selective, examples.

What Therapeutic Uses Does Patent 7,598,271 Cover?

Beyond the compound claims, patent 7,598,271 also claims methods of use for these compounds in treating various diseases.

Claim 21: Method of Treatment

Claim 21 is a key method of use claim, stating: "A method of treating a disease or condition in a mammal, comprising administering to the mammal an effective amount of a compound according to claim 1."

This claim is broad and encompasses any disease or condition that can be treated by any of the compounds covered by claim 1. However, the patent's written description provides further context and specificity regarding the intended therapeutic applications.

Detailed Therapeutic Applications in the Specification

The patent's detailed description of the invention outlines the specific biological targets and disease areas for which these pyrazolo[3,4-b]pyridine amides are intended. These applications are primarily focused on modulating signaling pathways involved in cellular proliferation and survival.

  • Kinase Inhibition: The compounds are described as inhibitors of various kinases. Kinases are enzymes that play crucial roles in cell signaling, and their dysregulation is implicated in numerous diseases, particularly cancer.
  • Oncogenic Kinase Targets: The specification highlights inhibition of kinases such as:
    • RET Kinase: A receptor tyrosine kinase implicated in certain types of thyroid cancer and other neoplasms.
    • VEGFR Kinase: Vascular endothelial growth factor receptor, critical for angiogenesis (the formation of new blood vessels), a process essential for tumor growth and metastasis.
    • PDGFR Kinase: Platelet-derived growth factor receptor, another receptor tyrosine kinase involved in cell growth and division, also implicated in cancer.
  • Cancer Treatment: The primary therapeutic area identified is oncology. The compounds are proposed for treating various cancers, including but not limited to:
    • Thyroid cancer
    • Lung cancer
    • Breast cancer
    • Prostate cancer
    • Colorectal cancer
    • Leukemia
    • Lymphoma
    • Melanoma
  • Other Conditions: While cancer is the predominant focus, the claims and specification suggest potential utility in other conditions where aberrant kinase activity contributes to disease, such as inflammatory diseases or autoimmune disorders, although these are less detailed.

The patent thus provides protection for both the chemical entities themselves and their use in treating diseases mediated by the inhibition of specific kinase targets.

What Is the Patent Landscape for Pyrazolo[3,4-b]pyridine Kinase Inhibitors?

Patent 7,598,271 is situated within a highly competitive and active patent landscape concerning kinase inhibitors, particularly those targeting pathways relevant to oncology.

Key Players and Their Patent Strategies

Several pharmaceutical companies and research institutions have actively patented compounds with similar structural motifs or targeting similar biological pathways.

  • Plexxikon, Inc. (now Daiichi Sankyo): The assignee of patent 7,598,271. Plexxikon's research, particularly in tyrosine kinase inhibitors, led to drugs like PLX4032 (vemurafenib), a BRAF inhibitor. This patent represents a broader exploration of the pyrazolo[3,4-b]pyridine scaffold for kinase inhibition.
  • Other Major Pharmaceutical Companies: Companies like Novartis, Pfizer, AstraZeneca, Bristol Myers Squibb, and others have extensive patent portfolios covering kinase inhibitors, including compounds that may share structural similarities or target overlapping signaling pathways. Their patent strategies often involve:
    • Broad Compound Claims: Covering large classes of molecules.
    • Specific Lead Compounds: Patenting highly potent and selective drug candidates.
    • Method of Use Claims: Protecting novel therapeutic applications.
    • Formulation and Polymorph Claims: Protecting specific drug formulations or crystalline forms to extend market exclusivity.
  • Academic Institutions: Universities and research centers also contribute to the landscape through early-stage discoveries and patent filings, often licensing their technologies to commercial entities.

Overlapping Technologies and Potential for Infringement

The overlap in chemical space and biological targets within the kinase inhibitor field creates a complex environment for patent prosecution and potential litigation.

  • Structural Similarity: Many kinase inhibitors, regardless of their core scaffold, share common pharmacophore elements designed to interact with the ATP-binding pocket of kinases. This can lead to structural similarity between patented compounds from different entities.
  • Target Similarity: The same kinase target (e.g., RET, VEGFR) can be modulated by compounds from multiple patent families. This increases the likelihood of competitors developing drugs that inhibit the same pathway, potentially infringing on existing patents.
  • Prior Art: The patentability of new kinase inhibitors is assessed against a vast body of prior art, including earlier patents, scientific literature, and previously disclosed compounds. Patent 7,598,271 itself would have been examined against this prior art.

Patent Term and Exclusivity

Patent 7,598,271 has a term that extends from its filing date (May 18, 2007) to 20 years from that date, which is May 18, 2027, subject to any patent term extensions or adjustments. This means that the patent protection for the claimed compounds and methods is nearing its end.

Freedom-to-Operate (FTO) Considerations

For any entity developing or seeking to develop pyrazolo[3,4-b]pyridine derivatives or kinase inhibitors targeting the pathways described in this patent, a thorough Freedom-to-Operate (FTO) analysis is critical. This involves:

  • Analyzing the Claims: Understanding the precise scope of protection afforded by patent 7,598,271 and any related patents.
  • Reviewing the Specification: Identifying the specific compounds and uses disclosed.
  • Scrutinizing Subsequent Filings: Examining later-filed patents by the same assignee or competitors that may build upon or overlap with the invention claimed in 7,598,271.
  • Considering Generics and Biosimilars: While this patent covers small molecules, understanding the broader market for similar therapeutic areas is crucial.

Strategic Implications for R&D and Investment

Patent 7,598,271 and its associated landscape offer several strategic considerations for companies involved in drug discovery and investment.

Opportunity for Repurposing or Developing Off-Patent Compounds

As patent 7,598,271 approaches its expiration date, the underlying compounds and their disclosed uses may become available for generic development or further research without direct patent infringement from this specific patent. This presents an opportunity for:

  • Generic Manufacturers: To develop and market generic versions of any approved drugs originating from this patent once it expires.
  • Second-Generation Inhibitors: To use the information disclosed in the patent as a starting point for designing novel compounds with improved efficacy, selectivity, or safety profiles that are patentable. This could involve modifying the scaffold, optimizing substituents, or targeting related pathways.

Focus on Novelty and Differentiation

The crowded kinase inhibitor patent landscape necessitates a strong focus on generating truly novel intellectual property.

  • Novel Chemical Space: Developing compounds that are structurally distinct from those claimed in expired or soon-to-expire patents, as well as existing marketed drugs.
  • Novel Biological Targets or Mechanisms: Identifying and targeting new pathways or disease mechanisms that have not been extensively patented.
  • Improved Therapeutic Profiles: Demonstrating clear advantages in efficacy, safety, patient convenience (e.g., oral bioavailability, reduced side effects), or target specificity over existing treatments.

Due Diligence in M&A and Licensing

For investors and companies engaged in mergers, acquisitions, or licensing activities, a comprehensive understanding of patent portfolios like that of 7,598,271 is vital.

  • Identifying Acquisition Targets: Understanding which early-stage companies hold patents on promising next-generation kinase inhibitors or novel targets.
  • Assessing Patent Strength: Evaluating the validity and scope of existing patents to determine potential infringement risks or licensing opportunities.
  • Forecasting Market Exclusivity: Predicting when key competitors' patents will expire to anticipate market entry of generics.

Importance of Robust Patent Prosecution

The strategy employed by Plexxikon, Inc. in filing patent 7,598,271—covering a genus of compounds and specific therapeutic uses—highlights the importance of:

  • Broad Claim Drafting: Securing protection over a wide range of potential molecules early in the discovery process.
  • Detailed Disclosure: Providing sufficient information in the patent specification to support the claimed invention and anticipate future developments.
  • Strategic Filing: Filing continuation applications and divisional applications to create a layered patent portfolio that can extend protection and cover different aspects of the invention.

The expiration of patents like 7,598,271 marks a natural evolution in the pharmaceutical market, opening avenues for generic competition while simultaneously emphasizing the continuous need for innovation and the protection of new therapeutic advancements.

Key Takeaways

  • Compound Scope: United States Patent 7,598,271 claims a genus of substituted pyrazolo[3,4-b]pyridine amides, with specific embodiments defined in dependent claims.
  • Therapeutic Focus: The patent discloses methods of treating diseases, primarily various cancers, by inhibiting oncogenic kinases such as RET, VEGFR, and PDGFR.
  • Patent Expiration: The patent term for 7,598,271 extends to May 18, 2027, indicating a nearing expiration date for its exclusivity.
  • Competitive Landscape: The patent operates within a dense and active field of kinase inhibitor patents, requiring careful Freedom-to-Operate analysis.
  • Strategic Opportunities: The approaching expiration presents opportunities for generic development and for designing next-generation inhibitors with improved profiles.

Frequently Asked Questions

  1. What is the primary therapeutic area targeted by compounds claimed in patent 7,598,271? The primary therapeutic area targeted by compounds claimed in patent 7,598,271 is oncology, with specific applications in treating various types of cancer.

  2. When does United States Patent 7,598,271 expire? United States Patent 7,598,271 is set to expire on May 18, 2027, based on its filing date and the standard 20-year patent term.

  3. What is the core chemical structure described in patent 7,598,271? The core chemical structure described in patent 7,598,271 is a substituted pyrazolo[3,4-b]pyridine.

  4. Does patent 7,598,271 claim specific drug names? No, patent 7,598,271 claims chemical compounds by their structural formulas and methods of treatment, not specific drug names. Any approved drugs that may have originated from this patent would have their own product-specific regulatory approvals and brand names.

  5. Can companies develop generic versions of drugs related to patent 7,598,271 before its expiration date? Companies can generally only develop and market generic versions of drugs once the relevant patents protecting those specific drugs and their methods of use have expired, or if they have secured a license. Development activities themselves may be permissible under certain research exceptions, but commercialization before patent expiry without authorization typically constitutes infringement.

Citations

[1] Plexxikon, Inc. (2009). Amides of substituted pyrazolo[3,4-b]pyridines and uses thereof (U.S. Patent No. 7,598,271). U.S. Patent and Trademark Office.

More… ↓

⤷  Start Trial


Drugs Protected by US Patent 7,598,271

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 7,598,271

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 200781 ⤷  Start Trial
Australia 3108097 ⤷  Start Trial
Bulgaria 103980 ⤷  Start Trial
Bulgaria 64315 ⤷  Start Trial
Brazil 9714787 ⤷  Start Trial
Canada 2293247 ⤷  Start Trial
Czech Republic 295301 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. We do not provide individual investment advice. This service is not registered with any financial regulatory agency. The information we publish is educational only and based on our opinions plus our models. By using DrugPatentWatch you acknowledge that we do not provide personalized recommendations or advice. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.