Last Updated: August 9, 2026

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
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 Analysis

Summary

United 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:

      R4
       |
       N
      / \
     C---C
    / \ / \
   N---C---N
   |   |   |
   R1  R2  R3

Where:

  • R1 is selected from the group consisting of alkyl, haloalkyl, cycloalkyl, heteroalkyl, heteroarylamino, and --(CH2)p-heteroaryl;
  • R2 is selected from the group consisting of H, alkyl, haloalkyl, cycloalkyl, heteroalkyl, amino, alkylamino, dialkylamino, and --(CH2)p-heteroaryl;
  • R3 is selected from the group consisting of H, alkyl, haloalkyl, cycloalkyl, heteroalkyl, amino, alkylamino, dialkylamino, --(CH2)p-heteroaryl, and --CO-R7;
  • R4 is selected from the group consisting of H, alkyl, haloalkyl, cycloalkyl, heteroalkyl, amino, alkylamino, dialkylamino, and --(CH2)p-heteroaryl;

(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:

  • Claim 1: Covers the general structure of substituted pyrazolo[1,5-a]pyrimidines as described above, including pharmaceutically acceptable salts. This is a broad genus claim.
  • Dependent Claims (e.g., Claims 2-20): These claims narrow the scope of Claim 1 by specifying particular ranges or specific choices for the substituents R1, R2, R3, and R4. For example, they may define specific alkyl chain lengths, particular heteroaryl groups, or specific linkages. These claims define more specific species within the genus.
  • Method of Use Claims (e.g., Claims 21-28): These claims cover methods of treating diseases characterized by abnormal cell proliferation, particularly myeloproliferative neoplasms (MPNs). This includes treating myelofibrosis (MF), post-polycythemia vera myelofibrosis (Post-PV MF), and post-essential thrombocythemia myelofibrosis (Post-ET MF). The methods involve administering a therapeutically effective amount of a compound as defined in the preceding claims.
  • Formulation Claims (e.g., Claims 29-30): These claims cover pharmaceutical compositions containing the claimed compounds and a pharmaceutically acceptable carrier.

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:

  • Myelofibrosis (MF): A serious bone marrow disorder characterized by the replacement of normal hematopoietic tissue with fibrotic tissue, leading to ineffective blood cell production.
  • Polycythemia Vera (PV): A blood cancer in which the bone marrow makes too many red blood cells, leading to thickened blood and potential clotting.
  • Essential Thrombocythemia (ET): A blood cancer characterized by an overproduction of platelets.
  • Post-polycythemia vera myelofibrosis (Post-PV MF): Myelofibrosis that develops in a patient who previously had polycythemia vera.
  • Post-essential thrombocythemia myelofibrosis (Post-ET MF): Myelofibrosis that develops in a patient who previously had essential thrombocythemia.

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:

  • Incyte Corporation: The assignee of Patent 9,914,802. Incyte is a leader in MPN therapeutics. Their JAK inhibitor, ruxolitinib (Jakafi/Jakavi), is a well-established treatment for myelofibrosis and polycythemia vera. Patent 9,914,802 is likely part of their broader IP portfolio covering ruxolitinib and related next-generation compounds. Ruxolitinib is chemically known as (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile. While Patent 9,914,802 covers pyrazolo[1,5-a]pyrimidines, Incyte has other patents covering the pyrrolo[2,3-d]pyrimidine core of ruxolitinib.
  • Gilead Sciences, Inc.: Holds patents related to filgotinib, a JAK1 selective inhibitor that has been explored for inflammatory conditions, and it is also exploring indications in hematology. Gilead also acquired patents from other entities that might encompass MPN-related JAK inhibitors.
  • Pfizer Inc.: Has developed tofacitinib (Xeljanz), a JAK inhibitor initially approved for rheumatoid arthritis. Pfizer continues to research JAK inhibitors for various hematological and inflammatory diseases.
  • Novartis AG: Has developed pacritinib (Vonjo), a JAK2 and FLT3 inhibitor approved for specific types of myelofibrosis with severe thrombocytopenia. Novartis also has a broad patent portfolio in kinase inhibitors.
  • AbbVie Inc.: Through its acquisition of Allergan, and its own R&D, AbbVie is active in JAK inhibitor research and development, with patents covering various JAK inhibitors and their applications.
  • Constellation Pharmaceuticals (acquired by MorphoSys): Developed pelabresib, a BET inhibitor that can modulate JAK signaling. While not a direct JAK inhibitor, it impacts similar pathways and highlights the interconnectedness of drug development in this space.

Patent Strategy:

Companies in this space typically employ a multi-pronged patent strategy:

  1. Composition of Matter Claims: Protecting novel chemical entities with desirable JAK inhibitory activity. Patent 9,914,802 is an example of this.
  2. Method of Use Claims: Protecting specific therapeutic applications for their compounds, including specific diseases (like MF and PV) and patient populations.
  3. Formulation Claims: Protecting specific drug formulations that improve delivery, efficacy, or patient compliance.
  4. Process Claims: Protecting novel and efficient methods for synthesizing their drug candidates.
  5. Polymorph Claims: Protecting specific crystalline forms of the active pharmaceutical ingredient that may offer improved stability or bioavailability.

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?

  • Filing Date: October 14, 2016
  • Grant Date (Issue Date): May 15, 2018

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

  • United States Patent 9,914,802 protects substituted pyrazolo[1,5-a]pyrimidine compounds and their use in treating myeloproliferative neoplasms (MPNs), including myelofibrosis (MF) and polycythemia vera (PV).
  • The core innovation lies in compounds that inhibit Janus kinases (JAKs), particularly JAK1 and JAK2, addressing a key pathogenic mechanism in MPNs.
  • The patent's claims encompass a broad genus of chemical structures with specific limitations in dependent claims, alongside methods of treating MPNs.
  • The IP landscape for JAK inhibitors in MPNs is highly competitive, with Incyte Corporation (assignee of this patent) being a major player, alongside other pharmaceutical giants.
  • The patent's effective term extends to October 14, 2036, potentially longer with patent term extensions.

Frequently Asked Questions

  1. What specific mutations in JAKs are targeted by these compounds? The patent does not exclusively list specific JAK mutations but describes the compounds as JAK inhibitors, which are effective in treating MPNs often driven by mutations like JAK2 V617F and other JAK-activating alterations.

  2. Does this patent cover ruxolitinib (Jakafi/Jakavi)? United States Patent 9,914,802 covers a different chemical scaffold (pyrazolo[1,5-a]pyrimidines) than ruxolitinib, which is a pyrrolo[2,3-d]pyrimidine. However, Incyte, the assignee of both, has multiple patents protecting their JAK inhibitor portfolio.

  3. What is the typical selectivity profile of compounds described in this patent? The patent emphasizes inhibition of JAK1 and JAK2, suggesting a dual inhibitory profile. The precise selectivity over other JAK family members (JAK3, TYK2) and other kinases would be detailed in specific compound testing data within the patent.

  4. Can generic manufacturers produce these compounds before the patent expires? Generic manufacturing before the patent's expiration date (October 14, 2036, potentially extended) would constitute patent infringement unless a license is obtained or the patent is invalidated.

  5. Are there any known post-grant challenges or litigation related to Patent 9,914,802? As of the current analysis, publicly available records do not indicate significant post-grant challenges or litigation specifically targeting United States Patent 9,914,802. However, the broader landscape of JAK inhibitor patents is subject to ongoing legal scrutiny.

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.

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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

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