Patent for Aquaporin Inhibitor and Meglumine Pharmaceutical Composition

According to GlobalData’s company profile on Simcere Pharmaceutical Group, Cancer treatment biomarkers was a key innovation area identified from patents. Simcere Pharmaceutical Group‘s grant share as of September 2023 was 38%. Grant share is based on the ratio of number of grants to total number of patents.

A recently filed patent (Publication Number: US20230293556A1) describes a pharmaceutical composition that includes a compound called 2-((3,5-bis(trifluoromethyl)phenyl)carbamoyl)-4-chlorophenyl dihydrogen phosphate, along with meglumine. The weight ratio of the compound to meglumine in the composition can range from 1:0.2 to 1:4, with preferred ratios between 1:0.4 and 1:2. The composition can be in the form of an injectable pharmaceutical composition, particularly a lyophilized (freeze-dried) form. It may also contain a lyophilization excipient, such as sucrose, lactose, mannitol, glucose, or trehalose. The weight ratio of the compound to the lyophilization excipient can range from 1:1 to 1:10, with preferred ratios between 1:2.5 and 1:7.5. Additionally, the composition may include a pH adjusting agent, such as hydrochloric acid or citric acid, to achieve a pH between 7.5 and 9.5, preferably around 8.5. The patent also describes a method for preparing the pharmaceutical composition, which involves dissolving meglumine in water, adding the compound, and optionally adding other components like lyophilization excipients and pH adjusting agents. The resulting mixture can be sterile filtered and lyophilized. The lyophilization process involves preserving the product at various temperatures, starting from -50°C and gradually raising it to 20-30°C.

The patent also claims that the pharmaceutical composition has a stability of at least 6 months at room temperature, with less than 1% of a specific compound called N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxybenzamide present in the composition. Furthermore, the composition is said to contain approximately 3% water by weight. The method for preparing the composition involves cooling the water to 15-25°C, dissolving meglumine, adding the compound, and optionally adding other components. The resulting mixture can be sterile filtered and lyophilized using a specific temperature preservation process. The lyophilization process includes preserving the product at -50°C for 2-6 hours, then raising the temperature to -20 to -10°C and preserving for 20-40 hours, and finally raising the temperature to 20-30°C and preserving for 10-30 hours. The temperature is specifically raised to 25°C in the final preservation step.

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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