United States Patent 7,265,124: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 7,265,124, hereafter referred to as the '124 patent, is a significant patent in the pharmaceutical sector, particularly related to the development and use of a specific triazolo[4,5-d]pyrimidine compound. This patent is owned by AstraZeneca and has been a focal point in several legal and pharmaceutical discussions.
Background of the Patent
The '124 patent pertains to the crystalline and amorphous forms of a triazolo[4,5-d]pyrimidine compound, specifically identified by the formula:
[ 1S-[1 ⁇ , 2 ⁇ , 3 ⁇ (1S,2R),5 ⁇ ] ⁇ -3-(7- ⁇ [2-3,4-difluorophenyl)cyclopropyl]amino ⁇ -5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol ][1][4].
Scope of the Patent
Crystalline and Amorphous Forms
The patent describes four distinct crystalline forms (Polymorphs I, II, III, and IV) and one amorphous form of the compound. Each polymorph is characterized by its unique X-ray powder diffraction pattern, which is crucial for identifying and distinguishing these forms[1][4].
Therapeutic Use
The compound is used for therapeutic purposes, particularly in the inhibition of platelet aggregation, which is beneficial in treating cardiovascular diseases such as myocardial infarction and cerebrovascular insufficiency[1][5].
Pharmaceutical Compositions
The patent also covers pharmaceutical compositions that include the compound in its crystalline and/or amorphous forms. These compositions are designed to ensure the chemical stability, solid-state stability, and shelf life of the active ingredients, which are critical factors in pharmaceutical manufacturing[1].
Claims of the Patent
Claim Construction
The claims of the '124 patent are detailed and specific, defining the invention with clarity. For instance, claim 1 specifies the compound of formula (I) characterized by an X-ray powder diffraction pattern containing specific peaks of high intensity at defined angles. This specificity is essential for distinguishing the patented compound from other similar compounds[2].
Literal Language and Context
The claims are interpreted in the context of the patent specification and the prosecution history. The literal language of the claim, along with the specification and prosecution history, helps in understanding the scope of the invention. This approach ensures that the claims are not overly broad or ambiguous, aligning with the principles set forth in cases like Phillips v. AWH Corp. and _Nautilus, Inc. v. Biosig Instruments, Inc.[2][3].
Patent Landscape
Litigation and Enforcement
The '124 patent has been involved in several litigation cases, particularly against generic pharmaceutical companies that have filed Abbreviated New Drug Applications (ANDAs) before the expiration of AstraZeneca's patents. AstraZeneca has alleged patent infringement against companies like Hisun Pharmaceutical, arguing that their generic products would infringe on the claims of the '124 patent[5].
Patent Validity and Enforceability
The validity and enforceability of the '124 patent have been upheld in various legal proceedings. The patent's claims are considered valid and enforceable, and AstraZeneca has the right to enforce them against infringing parties[5].
Related Patents
The '124 patent is part of a broader portfolio of patents related to the same compound and its therapeutic uses. Other patents, such as U.S. Patent Nos. 6,525,060 and 7,250,419, also pertain to similar compounds and processes, and have been involved in the same litigation landscape[5].
Importance of Polymorphs
Pharmaceutical Significance
Polymorphs are crucial in pharmaceuticals because they can affect the solubility, stability, and bioavailability of the drug. The identification and characterization of different polymorphs, as described in the '124 patent, are essential for ensuring the efficacy and safety of the drug product[1].
Manufacturing and Handling
The patent emphasizes the importance of the drug substance being in a form that can be conveniently handled and processed. This includes considerations of chemical stability, solid-state stability, and shelf life, all of which are influenced by the polymorphic form of the compound[1].
Legal and Regulatory Aspects
Claim Construction Principles
The interpretation of patent claims, as seen in the '124 patent, follows established principles such as those outlined in Phillips v. AWH Corp. and Nautilus, Inc. v. Biosig Instruments, Inc. These principles ensure that claims are clear and definite, providing a clear understanding of the invention's scope[2].
Patent Scope Metrics
Research on patent scope metrics, such as independent claim length and independent claim count, suggests that narrower claims are associated with a higher probability of grant and a shorter examination process. This is relevant when considering the scope and validity of the '124 patent claims[3].
Industry Impact
Innovation and Competition
The '124 patent, along with other related patents, influences the landscape of pharmaceutical innovation and competition. By protecting specific forms and uses of the compound, AstraZeneca maintains a competitive edge in the market for cardiovascular treatments[5].
Generic Challenges
Generic pharmaceutical companies often challenge the validity and enforceability of such patents to enter the market with their own versions of the drug. The litigation surrounding the '124 patent reflects these challenges and the efforts of patent holders to protect their intellectual property[5].
Key Takeaways
- The '124 patent covers crystalline and amorphous forms of a triazolo[4,5-d]pyrimidine compound, with specific therapeutic applications.
- The patent's claims are detailed and specific, ensuring clarity and enforceability.
- The patent has been involved in significant litigation regarding patent infringement by generic pharmaceutical companies.
- Polymorphs of the compound are crucial for pharmaceutical manufacturing and therapeutic efficacy.
- The patent landscape is influenced by principles of claim construction and metrics of patent scope.
FAQs
What is the main subject of the '124 patent?
The '124 patent pertains to the crystalline and amorphous forms of a triazolo[4,5-d]pyrimidine compound, along with its therapeutic uses and pharmaceutical compositions.
How many crystalline forms of the compound are described in the patent?
The patent describes four distinct crystalline forms (Polymorphs I, II, III, and IV) and one amorphous form of the compound.
Why are polymorphs important in pharmaceuticals?
Polymorphs are important because they can affect the solubility, stability, and bioavailability of the drug, influencing its efficacy and safety.
What is the significance of claim construction in patent law?
Claim construction is crucial as it defines the scope of the invention, ensuring that the claims are clear and definite, and provides a basis for determining patent infringement.
Which companies have been involved in litigation related to the '124 patent?
AstraZeneca has been involved in litigation with companies like Hisun Pharmaceutical, alleging patent infringement related to the '124 patent.
Sources
- US7265124B2 - Cristalline and amorphous form of a triazolo (4,5-D) pyridimine compound - Google Patents.
- 15-1000.pdf - District of Delaware.
- Patent Claims and Patent Scope - Hoover Institution.
- US7265124B2 - Cristalline and amorphous form of a triazolo (4,5-D) pyridimine compound - Google Patents.
- IN THE UNITED STATES DISTRICT COURT FOR THE DISTRICT OF DELAWARE - PharmaCompass.
