Gilead Sciences has been granted a patent for a crystalline form of Compound I, which is used in the production of 4-amino-2-butoxy-8-(3-(pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one. The patent also covers methods of making this compound. GlobalData’s report on Gilead Sciences 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 Gilead Sciences, Peptide pharmacophores was a key innovation area identified from patents. Gilead Sciences's grant share as of September 2023 was 44%. Grant share is based on the ratio of number of grants to total number of patents.

Crystalline form of compound i

Source: United States Patent and Trademark Office (USPTO). Credit: Gilead Sciences Inc

A recently granted patent (Publication Number: US11773098B2) describes a crystalline form of Compound I, along with its characterization and methods of preparation. The patent claims that the crystalline form of Compound I has a specific XRPD pattern, which is determined using CuKa1 radiation. The XRPD pattern is characterized by peaks at specific degrees 2?, such as 5.5, 9.4, 10.8, 11.9, 12.9, 14.4, 16.0, 19.0, 21.9, and 23.9 degrees (±0.2 degrees 2?). The patent further specifies that the crystalline form can have different numbers of peaks in the XRPD pattern, ranging from four to seven or more.

Additionally, the patent claims that the crystalline form of Compound I can exhibit a differential scanning calorimetry (DSC) endotherm at about 142°C or about 274°C. The DSC endotherm refers to the measurement of heat absorption during a heating process, which can provide information about the thermal properties of the crystalline form.

Furthermore, the patent describes a pharmaceutical composition comprising the crystalline form of Compound I. The composition can also include at least one additional therapeutic agent selected from a wide range of options. These additional therapeutic agents include HBV combination drugs, HBV DNA polymerase inhibitors, immunomodulators, toll-like receptor modulators, interferon alpha receptor ligands, hyaluronidase inhibitors, recombinant IL-7, hepatitis B surface antigen (HBsAg) inhibitors, compounds targeting hepatitis B core antigen (HBcAg), cyclophilin inhibitors, HBV therapeutic vaccines, HBV prophylactic vaccines, HBV viral entry inhibitors, and many more.

In summary, the granted patent discloses a specific crystalline form of Compound I, characterized by its XRPD pattern and DSC endotherm. The patent also covers methods of preparing the crystalline form and its use in pharmaceutical compositions, which can further include various additional therapeutic agents for the treatment of hepatitis B virus (HBV) infection.

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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