Analysis of US Patent 9,872,865: Compound and Method Claims
US Patent 9,872,865, granted on January 23, 2018, to The Regents of the University of California, covers a specific class of compounds and methods for their use. The patent's primary focus is on novel pharmaceutical compositions and their application in treating conditions modulated by the sonic hedgehog (SHH) pathway. The claims define a genus of chemical structures and specific compositions, as well as methods of administration.
What Compounds Are Claimed by US Patent 9,872,865?
Claim 1 defines the broadest scope of the claimed compounds. It describes a compound represented by a specific Markush structure or a pharmaceutically acceptable salt thereof. This Markush structure encompasses a wide range of potential chemical entities defined by variable groups (R1, R2, R3, R4, R5, R6, R7, R8) and specific core ring systems. The patent enumerates distinct ranges and specific examples for each of these variables, creating a large theoretical chemical space.
The key structural elements defined are:
- A central bicyclic ring system.
- Variable substituents attached to specific positions of this bicyclic core. These substituents include, but are not limited to, substituted aryl, heteroaryl, alkyl, cycloalkyl, and alkoxy groups.
- Specific examples of substituents are provided, such as phenyl, pyridyl, and pyrazolyl groups, which can be further substituted with halogens, alkyls, alkoxys, and other functional groups.
The patent then provides a detailed list of specific exemplified compounds, identified by numerical designations (e.g., Compound 1, Compound 2, etc.). These exemplified compounds represent specific instantiations of the broad Markush claim, with defined R-groups and specific core structures. The patent claims include a broad genus of compounds defined by the Markush formula, as well as at least 28 specific, individually claimed compounds.
What Methods of Treatment Are Covered by the Patent?
The patent claims methods of treating conditions that involve the modulation of the SHH pathway. Specifically, the claims focus on inhibiting the activity of the SHH pathway. This pathway is implicated in various physiological processes, including cell growth, differentiation, and tissue development. Dysregulation of the SHH pathway is associated with certain types of cancer, as well as other diseases.
Claim 7 defines a method of treating a disease by administering a therapeutically effective amount of one of the claimed compounds. The patent lists specific diseases that can be treated, including:
- Various forms of cancer, such as basal cell carcinoma, medulloblastoma, prostate cancer, lung cancer, and pancreatic cancer.
- Fibrotic disorders, such as liver fibrosis, kidney fibrosis, and pulmonary fibrosis.
- Acne vulgaris.
- Certain dermatological conditions.
The patent also details specific dosages and routes of administration. The claimed methods involve administering the pharmaceutical composition orally, intravenously, topically, or by inhalation. The dosage ranges specified are generally between 0.1 mg and 1000 mg per day, depending on the route of administration and the specific compound used.
What is the Scope of the Composition Claims?
Claims 1-6 and 9-15 cover pharmaceutical compositions. These claims are structured to encompass not only the novel compounds themselves but also formulations designed for therapeutic administration.
- Claim 1: As discussed, this claim is for a compound of the Markush structure or a pharmaceutically acceptable salt thereof. This establishes the foundational intellectual property for the chemical entities.
- Claim 9: This claim defines a pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier, diluent, or excipient. This broadens the patent protection to include the practical application of the novel compounds in a usable drug form. The carrier or excipient can be any suitable material for formulating drugs, including inert substances, binders, disintegrants, lubricants, and solubilizers.
The patent provides detailed examples of these compositions, including specific formulations for oral tablets, capsules, and topical creams. These examples specify the concentration of the active pharmaceutical ingredient (API), the type and amount of excipients, and manufacturing procedures.
What is the Patent Landscape for SHH Pathway Inhibitors?
The sonic hedgehog (SHH) pathway is a significant target for drug development, particularly in oncology and dermatology. Several other entities hold patents on compounds and methods related to SHH pathway modulation. Key players in this space include:
- Genentech (Roche): Holds patents related to vismodegib (Erivedge), a first-in-class SHH pathway inhibitor approved for advanced basal cell carcinoma. Patents cover the compound, formulations, and methods of treatment.
- Pfizer: Has developed and patented sonidegib (Odomzo), another SHH pathway inhibitor approved for basal cell carcinoma. Their patent portfolio includes compounds, compositions, and therapeutic uses.
- Curis, Inc.: Has patents covering various small molecule inhibitors of the SHH pathway, including compounds that have progressed into clinical trials for different cancer indications.
- National Institutes of Health (NIH): Holds patents on compounds and methods related to SHH pathway signaling, often focusing on fundamental research and novel therapeutic targets.
The patent landscape is characterized by a mix of broad genus claims covering large families of chemical compounds and specific claims for individual molecules and their precise therapeutic applications. Companies often seek to patent multiple aspects, including the core chemical structure, specific analogs, different salt forms, polymorphic forms, pharmaceutical compositions, and methods of use in treating specific diseases.
Comparison with Other SHH Inhibitors
US Patent 9,872,865 occupies a specific niche within the broader SHH inhibitor landscape. While approved drugs like vismodegib and sonidegib have established therapeutic profiles, this patent protects a distinct chemical scaffold and associated methods. The scope of the Markush claim in US Patent 9,872,865 is broad, potentially covering a significant number of novel chemical entities not directly claimed by competitors. However, the enforceability of such broad claims often depends on enablement and prior art.
The patent's focus on treating a range of cancers and fibrotic disorders, in addition to dermatological conditions, suggests a versatile therapeutic platform. The specific substitution patterns and core structure defined in the claims differentiate these compounds from existing marketed SHH inhibitors, offering potential advantages in terms of efficacy, safety profile, or resistance mechanisms.
The patent landscape is dynamic, with ongoing patent filings and expirations. Analysis of this patent must be situated within a broader understanding of the active patent estates of competitors, including granted patents, pending applications, and potential patent term extensions.
Key Takeaways
US Patent 9,872,865 protects a genus of novel compounds and pharmaceutical compositions designed to inhibit the sonic hedgehog (SHH) pathway. The claims encompass a broad Markush structure and numerous specific exemplified compounds, along with methods for treating cancers, fibrotic disorders, and dermatological conditions. The patent's strength lies in its broad chemical scope, potentially covering numerous novel entities. Its relevance in the competitive landscape of SHH inhibitors depends on the distinctiveness of its chemical structures from existing patented and marketed agents, and its ability to address unmet medical needs.
FAQs
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What is the primary therapeutic target of the compounds claimed in US Patent 9,872,865?
The primary therapeutic target is the sonic hedgehog (SHH) pathway, with the claimed compounds functioning as inhibitors of this pathway.
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Are there any specific diseases mentioned in the patent that these compounds are intended to treat?
Yes, the patent lists various forms of cancer (including basal cell carcinoma, medulloblastoma, prostate, lung, and pancreatic cancer), fibrotic disorders (such as liver, kidney, and pulmonary fibrosis), and acne vulgaris.
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Does the patent claim only the chemical compounds, or does it also cover their formulation and use?
The patent claims both the novel chemical compounds (under a broad Markush structure and specific examples) and pharmaceutical compositions containing these compounds along with pharmaceutically acceptable carriers, diluents, or excipients. It also claims methods of treatment using these compounds.
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Who is the assignee of US Patent 9,872,865?
The assignee of US Patent 9,872,865 is The Regents of the University of California.
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What is the granted date of US Patent 9,872,865?
US Patent 9,872,865 was granted on January 23, 2018.
Citations
[1] The Regents of the University of California. (2018). US Patent 9,872,865 B2. United States Patent and Trademark Office.
