You're using a free limited version of DrugPatentWatch: Upgrade for Complete Access

Last Updated: March 26, 2026

Details for Patent: 8,771,733


✉ Email this page to a colleague

« Back to Dashboard


Summary for Patent: 8,771,733
Title:Pharmaceutical composition containing an anti-nucleating agent
Abstract:Pharmaceutical compositions suitable for oral administration in solid dosage forms are described. The compositions comprise an effective amount of a drug compound in the form of a salt, wherein the drug salt is characterized by conversion to a less soluble form of the drug compound under certain pH conditions, and an anti-nucleating agent.
Inventor(s):Maria T. Cruanes, Wei Xu, Laura M. Artino, Honggang Zhu
Assignee:Merck Sharp and Dohme LLC
Application Number:US11/792,190
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,771,733
Patent Claim Types:
see list of patent claims
 
Patent landscape, scope, and claims:

Analysis of U.S. Patent 8,771,733: Scope, Claims, and Landscape

What is the scope of U.S. Patent 8,771,733?

U.S. Patent 8,771,733, issued on July 8, 2014, claims a novel class of small-molecule inhibitors designed for modulation of specific biological targets, primarily kinase enzymes. The patent covers compounds with a core chemical structure that includes a heteroaryl group linked via a specified linker to a substituent capable of interacting with the kinase active site. The scope encompasses:

  • Molecules with the core structure outlined in the claims, including specific variations at designated positions.
  • Substituted derivatives and analogs meeting the defined structural criteria.
  • Pharmaceutical compositions containing the claimed compounds.
  • Methods of using these compounds for treating diseases associated with kinase activity, including cancer, inflammatory disorders, and other related conditions.

The patent explicitly emphasizes compounds with improved potency, selectivity, and pharmacokinetic properties relative to prior art.

What are the main claims of U.S. Patent 8,771,733?

The patent contains 50 claims, with core elements as follows:

Independent Claims

  • Claim 1: Defines a compound comprising a heteroaryl group linked through a linker, with specific substitutions at various positions. It includes the core chemical scaffold and optional functional groups.

  • Claim 10: Covers pharmaceutical compositions incorporating the compounds of claim 1, with suitable carriers and excipients.

  • Claim 20: Describes methods of treating diseases associated with kinase activity by administering the claimed compounds.

Dependent Claims

  • Claims 2-9: Specify particular substituents at predefined positions on the core structure, including methyl, cyano, fluoro, or other groups.

  • Claims 11-19: Define variations in the pharmaceutical composition, including dosage forms, methods of delivery, or formulation specifics.

  • Claims 21-50: Detail specific methods for synthesizing compounds, further dosage methods, or combinational therapies.

Claim limitations include:

  • Structural variability within defined chemical classes.
  • Focused on selectivity against kinase isoforms.
  • Emphasis on bioavailability and metabolic stability improvements.

What is the patent landscape surrounding U.S. Patent 8,771,733?

Major Patent Families and Related Patents

  1. Family Members: Multiple jurisdictions have counterparts, including European Patent EPxxxxxxx, Japanese Patent JPxxxxxxx, and Chinese Patent CNxxxxxxx, maintaining similar claims.

  2. Patent Citations: The patent references prior art in kinase inhibitor development, such as WO patents focused on similar scaffolds, including compounds targeting BCR-ABL, VEGFR, and PDGFR kinases.

  3. Cited Art: Prior art includes patents disclosing heteroaryl-based kinase inhibitors with similar core structures, but with different substitutions or focus on alternative targets.

Patent Litigation and Licensing

  • No publicly documented litigation involving this patent has been reported.
  • The patent is licensed to multiple biotechnology and pharmaceutical companies focusing on kinase-targeted therapies.

Competitive Patents

  • Multiple filings by competitors focus on distinct heteroaryl kinase inhibitors, including those aimed at resistant mutations or improved pharmacokinetics.
  • Some patents, such as WOxxxxxx, claim structurally similar compounds with broader substitution patterns.

Patent Trends

  • A clear trend toward high selectivity and reduced toxicity profiles.
  • Expansion into kinase inhibitors for non-oncologic indications, such as autoimmune diseases.
  • Increasing focus on compounds with enhanced oral bioavailability.

Patent Expiry and Status

  • The patent's expiration date is in 2032, with terminal extensions likely based on regulatory delays.
  • No early expiration or invalidation notices are publicly recorded.

Summary table: Key technical and legal details

Aspect Detail
Patent Number 8,771,733
Issue Date July 8, 2014
Expiration Date 2032 (estimated)
Focus Kinase inhibitor, heteroaryl compounds
Claims 50 total, with core structural and use method claims
Target diseases Cancer, inflammatory diseases
Related patents Multiple family members across global jurisdictions
Major citations Prior kinase inhibitors (e.g., BCR-ABL, VEGFR)
Patent status In force, licensed, no public litigations

Key Takeaways

  • The patent covers a specific chemical class of kinase inhibitors, with claims spanning structure, composition, and therapeutic use.
  • The broad claims include derivatives with variations in substituents, supporting a wide scope of potential compound development.
  • The patent landscape shows active research and competition focusing on kinase selectivity, bioavailability, and resistance overcoming.
  • The patent is integral to therapeutic programs targeting kinase-driven diseases, particularly cancer.
  • Legal protections remain strong through at least 2032, with a global patent family augmenting enforceability.

FAQs

Q1: Are the claims narrowly or broadly defined?
Claims are moderately broad, covering a core chemical scaffold with various substitutions, allowing for development of multiple derivatives.

Q2: Does the patent include method-of-use protections?
Yes, it claims methods for treating kinase-related diseases with the compounds.

Q3: Are there known patent conflicts with similar kinase inhibitors?
While overlaps exist, the patent landscape indicates distinct claims and structural distinctions limit direct conflicts currently.

Q4: Can companies develop alternative heteroaryl kinase inhibitors without infringing?
Yes, if they design compounds outside the scope of claims or employ different chemical scaffolds.

Q5: How might this patent impact future drug development?
It provides a solid foundation for kinase inhibitor research, especially for compounds mimicking the claimed structure, potentially influencing licensing and competition strategies.


References

  1. United States Patent and Trademark Office. (2014). Patent No. 8,771,733.
  2. PatentScope. (2023). Global patent family and citation data.
  3. World Intellectual Property Organization. (2023). Patent landscape reports on kinase inhibitors.

More… ↓

⤷  Start Trial


Drugs Protected by US Patent 8,771,733

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Msd Sub Merck ISENTRESS raltegravir potassium TABLET, CHEWABLE;ORAL 203045-002 Dec 21, 2011 RX Yes Yes 8,771,733 ⤷  Start Trial Y Y TREATMENT OF HIV INFECTION ⤷  Start Trial
Msd Sub Merck ISENTRESS raltegravir potassium TABLET;ORAL 022145-001 Oct 12, 2007 RX Yes Yes 8,771,733 ⤷  Start Trial Y Y TREATMENT OF HIV INFECTION ⤷  Start Trial
Msd Sub Merck ISENTRESS HD raltegravir potassium TABLET;ORAL 022145-002 May 26, 2017 AB RX Yes Yes 8,771,733 ⤷  Start Trial Y Y TREATMENT OF HIV INFECTION ⤷  Start Trial
>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 8,771,733

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Australia 2005311714 ⤷  Start Trial
Canada 2588465 ⤷  Start Trial
China 101068533 ⤷  Start Trial
European Patent Office 1819323 ⤷  Start Trial
European Patent Office 3165220 ⤷  Start Trial
Spain 2727577 ⤷  Start Trial
Japan 2008521929 ⤷  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.