Intra-Cellular Therapies. has filed a patent for salts and crystal forms of a substituted heterocycle fused gamma-carboline. The patent claims a specific compound, d2-lumateperone, in various salt forms or co-crystals, which can be used in the treatment of diseases involving certain receptor signaling pathways. GlobalData’s report on Intra-Cellular Therapies gives a 360-degree view of the company including its patenting strategy. Buy the report here.
According to GlobalData’s company profile on Intra-Cellular Therapies, Peptide pharmacophores was a key innovation area identified from patents. Intra-Cellular Therapies's grant share as of September 2023 was 34%. Grant share is based on the ratio of number of grants to total number of patents.
The patent is filed for a salt or crystal form of a substituted heterocycle fused gamma-carboline
A recently filed patent (Publication Number: US20230312573A1) describes a specific compound called d2-lumateperone and its various forms, including salts and co-crystals. The patent claims that these forms of d2-lumateperone are in solid crystalline form and can be used for the prophylaxis or treatment of diseases or abnormal conditions involving or mediated by the 5-HT2A receptor, serotonin transporter (SERT), and/or dopamine D1/D2 receptor signaling pathways.
The patent claims that d2-lumateperone can exist in different forms, including salts and co-crystals. These forms are specified as hydrochloride, mono-tosylate, or bis-tosylate salts, as well as co-crystals with isonicotinamide or lysine free base. The patent emphasizes that these forms are in solid crystalline form.
The patent also describes the methods of making these salts and co-crystals. For salts, the method involves reacting the free base form of d2-lumateperone with hydrochloric acid or toluenesulfonic acid in the presence of an organic solvent. For co-crystals, the method involves combining the free base form of d2-lumateperone with isonicotinamide or combining d2-lumateperone mono-tosylate with lysine free base, again in the presence of an organic solvent.
Furthermore, the patent mentions a method of purifying d2-lumateperone in its free or salt form. This method involves reacting d2-lumateperone with hydrochloric acid or toluenesulfonic acid, or combining the free base form of d2-lumateperone with isonicotinamide or d2-lumateperone mono-tosylate with lysine free base. The resulting salt or co-crystal can then be optionally converted back to d2-lumateperone free base or another salt form.
The patent also highlights the potential therapeutic applications of these salts and co-crystals. It claims that administering an effective amount of these forms of d2-lumateperone can be used for the prophylaxis or treatment of diseases or abnormal conditions involving or mediated by the 5-HT2A receptor, serotonin transporter (SERT), and/or dopamine D1/D2 receptor signaling pathways.
In addition, the patent mentions the possibility of formulating a pharmaceutical composition using these salts in combination with a pharmaceutically acceptable diluent or carrier.
Overall, this patent describes the various forms of d2-lumateperone, including salts and co-crystals, their methods of preparation, and their potential therapeutic applications in diseases or abnormal conditions involving specific receptor signaling pathways.
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