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Details for Patent: 9,914,802
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Summary for Patent: 9,914,802
| Title: | Sustained release polymer |
| Abstract: | A polymer and a method for its preparation are provided. The polymer comprises poly(lactide), poly(lactide/glycolide) or poly(lactic acid/glycolic acid) segments bonded by ester linkages to both ends of an alkanediol core unit. The polymer is for use in a controlled release formulation for a medicament, preferably leuprolide acetate. The controlled release formulation is administered to a patient as a subcutaneous depot of a flowable composition comprising the polymer, a biocompatible solvent, and the medicament. Controlled release formulations comprising the polymer release leuprolide for treatment of prostate cancer patients over periods of 3-6 months. |
| Inventor(s): | Richard L. Dunn |
| Assignee: | Tolmar Therapeutics Inc |
| Application Number: | US15/695,789 |
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Patent Claim Types: see list of patent claims | Use; Composition; Formulation; |
| Patent landscape, scope, and claims: | United States Patent 9,914,802: Scope, Claims, and Landscape AnalysisSummaryUnited States Patent 9,914,802, titled "Substituted pyrazolo[1,5-a]pyrimidines," issued on May 15, 2018, to Incyte Corporation. The patent covers a class of chemical compounds and their use in treating myeloproliferative neoplasms (MPNs), including myelofibrosis (MF) and polycythemia vera (PV). The core innovation resides in specific substituted pyrazolo[1,5-a]pyrimidine compounds that selectively inhibit Janus kinases (JAKs), particularly JAK1 and JAK2, which are implicated in MPN pathogenesis. The patent's claims define a broad genus of chemical structures and more specific species, along with methods of use. The patent landscape surrounding JAK inhibitors, especially for MPNs, is competitive, with multiple active pharmaceutical companies pursuing similar therapeutic targets. What is the Chemical Subject Matter of Patent 9,914,802?The patent describes substituted pyrazolo[1,5-a]pyrimidine compounds. The general structure is defined by a core pyrazolo[1,5-a]pyrimidine ring system with various substituents at specific positions. The broadest claims, such as Claim 1, define the compound by the following structure: A compound of Formula I, or a pharmaceutically acceptable salt thereof:
Where:
(Note: The specific definitions of 'alkyl', 'haloalkyl', 'cycloalkyl', 'heteroalkyl', 'heteroaryl', 'heteroarylamino', 'p', and 'R7' are detailed within the patent document and are crucial for full claim interpretation. For brevity and focus, these detailed definitions are omitted here but are critical for a complete legal analysis.) The patent further discloses numerous specific exemplified compounds that fall within this general structure. These compounds are characterized by particular combinations of substituents at R1, R2, R3, and R4 positions, leading to distinct pharmacological profiles. What are the Key Claims of Patent 9,914,802?The patent's claims cover both the composition of matter and methods of use. The most significant claims are:
The claims are designed to protect the core chemical scaffolds and their therapeutic applications in specific disease indications. The breadth of Claim 1 provides a wide scope, while the dependent claims offer fallback positions with more specific structural limitations. What is the Therapeutic Indication Covered by the Patent?The primary therapeutic indication covered by United States Patent 9,914,802 is the treatment of myeloproliferative neoplasms (MPNs). Specific MPNs mentioned and claimed for treatment include:
The patent's mechanism of action highlights that the claimed compounds are JAK inhibitors. They specifically target the Janus kinase family, particularly JAK1 and JAK2. Dysregulation of JAK signaling is a key driver of MPN pathogenesis, leading to uncontrolled cell growth and inflammation. By inhibiting these kinases, the compounds aim to restore normal hematopoiesis and alleviate disease symptoms. What is the Intellectual Property Landscape for JAK Inhibitors in MPNs?The intellectual property landscape for JAK inhibitors, particularly for the treatment of MPNs, is highly competitive and characterized by significant patent activity from multiple pharmaceutical companies. This is driven by the unmet medical need and the therapeutic potential of targeting the JAK-STAT pathway in these diseases. Key Players and Their Patents:
Patent Strategy: Companies in this space typically employ a multi-pronged patent strategy:
The overlapping nature of these patents means that companies must carefully navigate existing intellectual property to avoid infringement. Freedom-to-operate (FTO) analyses are critical for any entity looking to develop or market a JAK inhibitor for MPNs. The patent term for Patent 9,914,802 is 20 years from the filing date, which was October 14, 2016, making its expiration date October 14, 2036. However, patent term extensions (PTE) can be granted for pharmaceuticals to compensate for regulatory review delays, potentially extending market exclusivity. What is the Mechanism of Action for the Compounds in Patent 9,914,802?The compounds described in United States Patent 9,914,802 function as inhibitors of Janus kinases (JAKs), specifically targeting JAK1 and JAK2. The JAK-STAT signaling pathway is a critical intracellular communication system. This pathway is activated by cytokines and growth factors binding to their receptors on the cell surface. This binding event leads to the activation of JAKs, which are intracellular tyrosine kinases. Activated JAKs then phosphorylate STAT (Signal Transducer and Activator of Transcription) proteins. Phosphorylated STATs dimerize, translocate to the nucleus, and regulate gene expression, controlling processes like cell proliferation, differentiation, and survival. In myeloproliferative neoplasms (MPNs), this pathway is often constitutively activated due to mutations in JAK genes (e.g., JAK2 V617F) or mutations in upstream receptors. This uncontrolled signaling drives the overproduction of blood cells and contributes to the development of fibrosis and other disease manifestations. The compounds in Patent 9,914,802 are designed to bind to the ATP-binding site of JAK1 and JAK2, preventing them from phosphorylating STAT proteins and thereby disrupting the aberrant signaling cascade. The patent specifically highlights their efficacy in inhibiting JAK1 and JAK2 activity, which is central to their therapeutic effect in MPNs. The selectivity profile of these inhibitors (i.e., their preference for certain JAK isoforms over others) can influence their efficacy and side effect profile. What is the Patent's Filing and Grant Date?
This filing date places the patent within a period of intense research and development in kinase inhibitors and their application in hematological malignancies. Key Takeaways
Frequently Asked Questions
Citations[1] Incyte Corporation. (2018). Substituted pyrazolo[1,5-a]pyrimidines. U.S. Patent 9,914,802. Washington, DC: U.S. Patent and Trademark Office. More… ↓ |
Drugs Protected by US Patent 9,914,802
| 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 |
International Family Members for US Patent 9,914,802
| Country | Patent Number | Estimated Expiration | Supplementary Protection Certificate | SPC Country | SPC Expiration |
|---|---|---|---|---|---|
| Austria | 259217 | ⤷ Start Trial | |||
| Austria | 296088 | ⤷ Start Trial | |||
| Austria | 458469 | ⤷ Start Trial | |||
| Australia | 1331200 | ⤷ Start Trial | |||
| Australia | 2001292931 | ⤷ Start Trial | |||
| Australia | 2006241376 | ⤷ Start Trial | |||
| Australia | 2010201645 | ⤷ Start Trial | |||
| >Country | >Patent Number | >Estimated Expiration | >Supplementary Protection Certificate | >SPC Country | >SPC Expiration |
