Ayala Pharmaceuticals has been granted a patent for novel pharmaceutically acceptable salts of conjugates that combine chemotherapeutic drugs, specifically cytidine analogs, with amino acids like aspartic and glutamic acid. These compounds aim to enhance drug uptake in target cells and minimize side effects in cancer treatment. GlobalData’s report on Ayala Pharmaceuticals 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 Ayala Pharmaceuticals, Personalized cancer vaccines was a key innovation area identified from patents. Ayala Pharmaceuticals's grant share as of July 2024 was 15%. Grant share is based on the ratio of number of grants to total number of patents.
Pharmaceutical salts of chemotherapeutic drug-amino acid conjugates
The granted patent US12071450B2 outlines a novel process for synthesizing a compound represented by formula (1). The method involves two primary steps: first, the coupling of a compound of formula (i) with a drug, specifically cytarabine or its protected derivative (designated as D or D-(P3)n), using a coupling reagent to produce an intermediate of formula (ii). In the second step, the process entails the removal of protecting groups (P1, P2, and potentially P3) through the application of a strong acid (Y) or a deprotecting agent followed by a strong acid, resulting in the formation of the final salt represented by formula (1).
Further details in the claims specify that the hydroxyl protecting group P3 can be located on the 2', 3', and/or 5'-OH moieties of cytarabine. The process may also utilize a base during the coupling step, with examples including 4-DMAP, imidazole, pyridine, and N-methylmorpholine, either individually or in combination. Additionally, the strong acid Y used in the deprotection step can be a pharmaceutically acceptable organic or inorganic acid, with specific examples including HCl, HBr, boric acid, and various sulfonic and phosphoric acids. This patent presents a detailed methodology for the preparation of a specific compound, which may have implications in pharmaceutical applications.
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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
