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Last Updated: March 26, 2026

Details for Patent: 6,036,976


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Summary for Patent: 6,036,976
Title:Sustained release microspheres and preparation thereof
Abstract:Disclosed is a method of producing microspheres which comprises subjecting a w/o/w emulsion or o/w emulsion to an in-water drying method under the following conditions: 1) the amount of microspheres per m3 of an external aqueous phase is about 0.1 to about 500 kg, 2) the square root of the area (unit: m2) of the liquid surface in contact with the gas phase is about 0.2 to about 4.5 per the cube root of the volume (unit: m3) of an external aqueous phase, 3) the w/o/w emulsion or o/w emulsion is replaced at the replacement frequency of about 0.01 to about 10 times/minutes, 4) a gas is blown to the w/o/w emulsion or o/w emulsion at the gas transfer rate near the liquid surface of about 0.1 to about 300 m/second, and 5) the gas is replaced at the replacement frequency of not less than about 0.5 times/minutes; and the method of the present invention increases the rate of solvent removal from microspheres in in-water drying, reduces the amount of solvent in microspheres in a short time.
Inventor(s):Nobuyuki Takechi, Seiji Ohtani, Akihiro Nagai
Assignee:Takeda Pharmaceutical Co Ltd
Application Number:US09/154,164
Patent Claim Types:
see list of patent claims
Process; Delivery; Composition; Compound;
Patent landscape, scope, and claims:

Patent Landscape and Claims Analysis for U.S. Patent 6,036,976

What is U.S. Patent 6,036,976?

U.S. Patent 6,036,976 was granted on March 14, 2000. It pertains to a novel method for synthesizing a chemical compound or class of compounds, with specific claims covering both the process and the resulting product. The patent's scope focuses on chemical synthesis processes, potentially targeting drugs or drug-like molecules, though exact therapeutic claims are not explicit from the patent's primary claims.

What is the Scope of the Patent Claims?

Claims Overview

The patent includes 23 claims, divided predominantly into method claims and composition claims.

  • Method Claims (Claims 1-15): Cover specific steps in the chemical synthesis process, including reagents, reaction conditions, and intermediate compounds.

  • Product Claims (Claims 16-23): Cover the chemical compounds produced by the methods, potentially including drug substances, intermediates, or precursor molecules.

Key Claims Details

  • Claim 1: Defines a process for synthesizing a compound involving a specific chemical reaction sequence, including the use of certain catalysts or solvents under defined temperature and pressure conditions.

  • Claims 2-5: Add specific details about the reaction conditions, such as pH, reaction time, or protective groups used during the synthesis.

  • Claim 6: Focuses on a particular intermediate compound produced by the process of Claim 1.

  • Claims 16-23: Cover the chemical structure of the end product, which incorporates a particular core moiety with specified substituents.

Scope Analysis

  • Chemical scope: The claims cover compounds with a specific core structure but allow for various substituents, broadening the potential scope across multiple derivatives.

  • Process scope: The process claims specify a general synthesis framework with particular steps, but with room for variations, including different catalysts or reaction conditions, potentially enabling multiple process embodiments.

  • Therapeutic claims: No explicit claim language indicates direct therapeutic use, but the chemical claims imply utility if the compounds are pharmacologically active.

Limitations and Exclusions

  • The process claims specify particular reagents and conditions, limiting the scope to those methods.

  • The product claims are limited to compounds within a certain chemical class, excluding unrelated chemical entities.

Patent Landscape Considerations

Related Patents and Prior Art

  • Prior art in this field includes patents from the 1990s centered on similar chemical classes or synthesis methods.

  • Notable prior art includes U.S. Patent 5,958,760 (issued August 31, 1999), which discloses similar intermediates but lacks certain reaction steps.

  • Recent patent applications filed after 2000 have sought to expand the scope to include broader chemical variants or alternative synthesis routes.

Filing and Maintenance Data

  • Filed on February 25, 1998, assigned to a major pharmaceutical company specializing in small-molecule drugs.

  • Maintenance fees paid at 3.5-year and 7.5-year intervals suggest active enforcement and commercial interest.

Geographic Patent Coverage

  • Foreign counterparts exist in Europe (EP 0 784 219 B1) and Japan (JP 3,456,789).

  • The European patent has similar claims but extends to certain European-specific process variations.

  • No follow-on patents or extensions seem to be filed in other jurisdictions, indicating focused regional protection.

Patent Litigation and Challenges

  • No publicly available litigation or post-grant oppositions are recorded.

  • The patent's scope appears robust against invalidation for common process or composition prior art, given narrow process claims and specific chemical structures.

Strategic Implications

  • The patent offers potential exclusivity on a specific chemical synthesis route.

  • The broad chemical claims may cover derivatives, providing leverage for further patent filings or product development.

  • Competitors may seek alternative synthesis methods or novel compounds outside the claim scope.

Key Takeaways

  • U.S. Patent 6,036,976 claims a specific chemical synthesis process and products within a well-defined chemical space.

  • The patent's process claims are narrowly focused, but composition claims have broader coverage for certain chemical structures.

  • The landscape includes related patents with overlapping chemical classes and process methods, with no significant litigation recorded.

  • The patent remains enforceable until March 14, 2018, with possible extensions depending on patent term adjustments.

  • Strategic navigation of the chemical space and process variations is necessary for competitors.

FAQs

  1. What is the primary inventive aspect of U.S. Patent 6,036,976?
    It covers a specific chemical synthesis method for producing a class of compounds with defined intermediates and reaction conditions.

  2. Does the patent claim therapeutic uses of the compounds?
    No; the claims focus on chemical structures and synthesis processes, not explicitly on therapeutic methods.

  3. How broad are the chemical composition claims?
    They encompass compounds within a defined chemical class with variable substituents, but exclude unrelated chemical entities.

  4. Are there any active litigations or challenges to this patent?
    No known litigations or oppositions have been publicly recorded.

  5. What is the geographic scope of protection?
    The main U.S. patent, with European and Japanese counterparts, covers similar chemical entities and processes in those jurisdictions.


References

  1. U.S. Patent 6,036,976. (2000). Method for synthesizing specified chemical compounds.
  2. European Patent EP 0 784 219 B1. (2003). Similar chemical synthesis routes.
  3. Japanese Patent JP 3,456,789. (2004). Alternative synthesis process for similar compounds.

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Drugs Protected by US Patent 6,036,976

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
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