US 11,998,524 B2
Forms of aticaprant
Philippe Fernandes, Beerse (BE); Mark Schmidt, Antwerp (BE); Vanina Popova, Nijlen (BE); Adam Savitz, Greenwich, CT (US); Rama Melkote, Basking Ridge, NJ (US); Wayne C. Drevets, Rancho Santa Fe, CA (US); Srihari Gopal, Belle Mead, NJ (US); Darrel Pemberton, Oud Turnhout (BE); Chakradhar Lagishetty, King of Prussia, PA (US); and Iva Kezic, Antwerp (BE)
Assigned to Janssen Pharmaceuticals, Inc., Titusville, NJ (US)
Filed by Janssen Pharmaceuticals, Inc., Titusville, NJ (US)
Filed on Mar. 6, 2023, as Appl. No. 18/178,961.
Claims priority of provisional application 63/317,475, filed on Mar. 7, 2022.
Prior Publication US 2023/0277499 A1, Sep. 7, 2023
Int. Cl. A61K 31/40 (2006.01); A61P 25/24 (2006.01)
CPC A61K 31/40 (2013.01) [A61P 25/24 (2018.01); C07B 2200/13 (2013.01)] 44 Claims
 
1. A method of treating major depressive disorder in a human patient, comprising administering an effective amount of crystalline aticaprant of Form I, II, or III to the human patient, wherein the patient had a previous inadequate response to other antidepressant therapy, wherein:
crystalline Form I is characterized by four or more x-ray diffraction pattern peaks at 2θ (±0.2) of 4.6°, 17.3°, 17.4°, 18.0°, and 24.0°,
crystalline Form II is characterized by four or more x-ray diffraction pattern peaks at 2θ (±0.2) of 3.1°, 19.0°, 24.0°, 24.3°, and 26.2°,
crystalline Form III is characterized by four or more x-ray diffraction pattern peaks at 2θ (±0.2) of 4.1°, 9.0°, 17.6°, 18.0°, and 21.4°,
wherein aticaprant has the following structure:

OG Complex Work Unit Chemistry