Nektar Therapeutics has been granted a patent for multi-arm polymer conjugates of Toll-Like Receptor (TLR) agonists, specifically TLR 7/8 agonists. The patent also covers related compositions, methods of making and using such conjugates, and a method of administering the conjugates to cancer patients. The conjugates consist of a TLR 7/8 agonist covalently attached to a water-soluble, non-peptidic polymer. GlobalData’s report on Nektar Therapeutics gives a 360-degree view of the company including its patenting strategy. Buy the report here.

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According to GlobalData’s company profile on Nektar Therapeutics, Nanoparticle drug conjugates was a key innovation area identified from patents. Nektar Therapeutics's grant share as of September 2023 was 54%. Grant share is based on the ratio of number of grants to total number of patents.

Conjugate of tlr 7/8 agonist with water-soluble polymer

Source: United States Patent and Trademark Office (USPTO). Credit: Nektar Therapeutics

A recently granted patent (Publication Number: US11744898B2) discloses a conjugate that combines a Toll-like receptor 7/8 (TLR 7/8) agonist with a multi-arm, water-soluble, non-peptidic polymer. The conjugate is formed by covalently attaching the TLR 7/8 agonist to the polymer through a linkage-containing spacer moiety. The polymer has a specific formula described as Formula III in the patent.

The patent claims specify various aspects of the conjugate. Claim 2 provides options for the structure of the linkage-containing spacer moiety, including different combinations of carbon and nitrogen atoms. Claim 3 states that the value of "n," which represents the number of repeating units in the polymer, can range from 100 to 250. Claim 4 mentions that the R1 and R2 groups in the TLR 7/8 agonist can be hydrogen. Claim 5 describes a specific configuration where R1 is —CH2—O—CH2—CH3 and R2 is hydroxyl.

The patent also includes a list of specific compounds that fall under the category of the disclosed conjugate. Claim 6 states that the conjugate can be selected from the group consisting of Compounds 1-10 and 12-15.

Furthermore, the patent discusses the use of the conjugate in pharmaceutical compositions. Claim 7 specifies that the composition comprises the conjugate and a pharmaceutically acceptable excipient, which is a substance used as a carrier or diluent in pharmaceutical formulations.

Lastly, claim 8 provides information about the weight average molecular weight of the poly(ethylene glycol) polymer used in the conjugate. The value of "n" corresponds to a weight average molecular weight ranging from about 2,000 Daltons to about 150,000 Daltons, about 5,000 Daltons to about 40,000 Daltons, or about 5,000 Daltons to about 25,000 Daltons.

Overall, this granted patent introduces a conjugate that combines a TLR 7/8 agonist with a specific multi-arm, water-soluble, non-peptidic polymer. The patent covers various aspects of the conjugate, including its structure, specific compounds, and potential use in pharmaceutical compositions.

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GlobalData, the leading provider of industry intelligence, provided the underlying data, research, and analysis used to produce this article.

GlobalData Patent Analytics tracks bibliographic data, legal events data, point in time patent ownerships, and backward and forward citations from global patenting offices. Textual analysis and official patent classifications are used to group patents into key thematic areas and link them to specific companies