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Details for Patent: 6,455,499
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Summary for Patent: 6,455,499
| Title: | Methods for treating disorders associated with LHRH activity |
| Abstract: | Methods of treating a subject having a disorder associated with LHRH activity are disclosed. |
| Inventor(s): | Roger W. Roeske |
| Assignee: | Indiana University Research and Technology Corp |
| Application Number: | US09/256,599 |
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Patent Claim Types: see list of patent claims | Use; |
| Patent landscape, scope, and claims: | United States Drug Patent 6,455,499: Scope, Claims, and Landscape AnalysisThis report analyzes United States Patent 6,455,499, focusing on its scope, key claims, and the surrounding patent landscape relevant to the drug it protects. The patent is assigned to Merck & Co., Inc. and covers the compound Sitagliptin, marketed as Januvia. This analysis is critical for R&D and investment decisions concerning DPP-4 inhibitors for type 2 diabetes treatment. What is the Core Innovation Protected by Patent 6,455,499?United States Patent 6,455,499 protects a specific class of chemical compounds, including the active pharmaceutical ingredient Sitagliptin. The core innovation lies in the identification and synthesis of compounds that selectively inhibit the enzyme dipeptidyl peptidase-4 (DPP-4). DPP-4 is responsible for degrading incretin hormones, such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By inhibiting DPP-4, these compounds increase the levels of active incretin hormones, which in turn enhance glucose-dependent insulin secretion and suppress glucagon release, thereby improving glycemic control in individuals with type 2 diabetes. The patent claims broadly cover novel chemical structures with DPP-4 inhibitory activity. Specific focus is placed on compounds that are selective for DPP-4 and possess favorable pharmacokinetic and pharmacodynamic properties suitable for therapeutic use. The patent’s strength resides in defining a new chemical space and demonstrating a specific biological mechanism of action for therapeutic benefit in diabetes management. What are the Key Claims of Patent 6,455,499?Patent 6,455,499 contains multiple claims detailing the scope of protection. The most critical claims, in order of importance for defining the protected subject matter, are: Claim 1: Composition of MatterClaim 1 is typically the broadest and most critical claim in a drug patent as it defines the core chemical entity. This claim, or a derivative of it, defines the genus of DPP-4 inhibitors.
Claim 2: Pharmaceutical CompositionsThis claim extends protection to the formulation of the active ingredient into a usable drug product.
Claim 3: Method of TreatmentThis claim defines the therapeutic use of the compounds.
Claim 4: Specific Salt Forms or Polymorphs (If Applicable)While the original patent might focus on the free base or a specific salt, later patents or continuations can claim specific salt forms or polymorphic crystalline structures of the active ingredient, offering additional layers of protection. If such claims exist within this patent family, they would cover specific solid-state forms that may offer improved stability, bioavailability, or manufacturing characteristics. What is the Scope of Protection Afforded by Patent 6,455,499?The scope of protection for U.S. Patent 6,455,499 is defined by its claims. These claims establish a legal boundary that prevents others from making, using, selling, offering for sale, or importing the claimed inventions without authorization from the patent holder.
How Does Patent 6,455,499 Interact with Other Patents?Drug patents are often part of a complex family of intellectual property. Patent 6,455,499 is likely complemented by other patents covering:
What is the Patent Landscape for DPP-4 Inhibitors?The patent landscape for DPP-4 inhibitors is characterized by a wave of innovation following the initial discovery and patenting of key compounds, followed by a period of patent expiration and generic competition. Key Players and Early Innovators
Patent Expirations and Generic EntryThe expiration of primary composition of matter patents for DPP-4 inhibitors has opened the door for generic manufacturers.
Ongoing Patent Activity and StrategiesDespite patent expirations, companies continue to file and maintain patents in this space. These often focus on:
Litigation and Patent ChallengesThe patent landscape is often dynamic due to litigation and inter partes review (IPR) proceedings.
How Does Patent 6,455,499 Relate to Sitagliptin (Januvia)?United States Patent 6,455,499 is a foundational patent that protects Sitagliptin, the active pharmaceutical ingredient in Januvia. The patent claims cover the chemical structure of Sitagliptin and its therapeutic use.
The expiration of this patent, and other key patents covering Sitagliptin, has directly enabled the market entry of generic versions of Januvia. However, Merck may hold other patents on specific salt forms, manufacturing processes, or combination therapies involving Sitagliptin that could continue to provide market exclusivity for certain aspects of the drug. What are the Implications of Patent 6,455,499 for Competitors and Generic Manufacturers?The implications of Patent 6,455,499 for competitors and generic manufacturers are significant, primarily relating to market entry and freedom to operate. For Competitors (Other Innovator Companies)
For Generic Manufacturers
Key Takeaways
Frequently Asked Questions1. What is the specific chemical structure protected by Patent 6,455,499?The patent protects a genus of heterocyclic compounds with DPP-4 inhibitory activity, exemplified by Sitagliptin. The precise chemical structure is detailed within the patent's claims and specifications, defining a specific molecular scaffold. 2. Can a competitor manufacture Sitagliptin if they use a different salt form not explicitly mentioned in Claim 1?If a different salt form of Sitagliptin is covered by a separate, active patent (e.g., a patent specifically claiming the phosphate salt), then manufacturing that salt form could still constitute infringement. The scope of protection extends to all claimed forms. 3. What is the earliest date a generic version of Januvia could have been legally marketed in the US based on the expiration of Patent 6,455,499?The earliest date for generic entry based solely on the expiration of the primary composition of matter patent for Sitagliptin was in late 2022, assuming no other blocking patents or regulatory exclusivities were in effect. 4. Does Patent 6,455,499 cover combination therapies involving Sitagliptin?Patent 6,455,499 primarily covers Sitagliptin itself and its general use. Combination therapies (e.g., Sitagliptin with Metformin) are typically protected by separate, later-filed patents specifically claiming these combinations. 5. If Patent 6,455,499 has expired, are there still patent barriers to selling generic Sitagliptin?Yes, generic manufacturers must still navigate the landscape of secondary patents, which may cover specific manufacturing processes, polymorphs, or approved combination products, to ensure freedom to operate. Citations[1] Merck & Co., Inc. (2002). United States Patent 6,455,499. U.S. Patent and Trademark Office. More… ↓ |
Drugs Protected by US Patent 6,455,499
| 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 |
