Salts, co-crystals, and polymorphs of an anxiolytic compound

{
  "publication_number": "US9745296B2",
  "country": "US",
  "kind": "B2",
  "title": "Salts, co-crystals, and polymorphs of an anxiolytic compound",
  "abstract": "The present invention provides amorphous arid crystalline forms of 1-ethyl-6-(indan-2-ylamino)-3-(morpholine-4-carbonyl)-1,8-naphthyridin-4-one (compound 1), and salts, co-crystals, and pharmaceutical compositions thereof. The invention also provides methods of treating and/or preventing a disease, such as a central nervous system disease (e.g., an anxiety disorder), using the amorphous and crystalline forms, and salts, co-crystals, and pharmaceutical compositions thereof.",
  "claims": [
    "1. A hemi-succinate salt of the crystalline Form SUC-P5 of compound 1:",
    "2. The crystalline Form SUC-P5 of claim 1, wherein the crystalline Form SUC-P5 is substantially free of impurities.",
    "3. The crystalline Form SUC-P5 of claim 1, wherein the crystalline Form SUC-P5 is substantially free of amorphous compound 1.",
    "4. The crystalline Form SUC-P5 of claim 1, wherein the crystalline Form SUC-P5 has two or more peaks in its x-ray powder diffraction (XRPD) pattern selected from those in the following table: Angle 2-Theta ° 7.4 15.6 16.5 18.5 22.2.",
    "5. The crystalline Form SUC-P5 of claim 1, wherein the crystalline Form SUC-P5 has four or more peaks in its XRPD pattern selected from those in the following table: Angle 2-Theta ° 7.4 8.3 10.5 11.7 13.2 15.6 16.5 18.5 22.2.",
    "6. The crystalline Form SUC-P5 of claim 1, wherein the crystalline Form SUC-P5 is characterized by a differential scanning calorimetry (DSC) thermogram with an endotherm having a peak temperature (T max) of about 207° C.",
    "7. The crystalline Form SUC-P5 of claim 1, wherein the crystalline Form SUC-P5 is characterized by a DSC thermogram with a ΔH of about 6.7 J/g or about 92.6 J/g.",
    "8. A pharmaceutical composition comprising the crystalline form SUC-P5 of claim 1, and optionally a pharmaceutically acceptable excipient.",
    "9. The pharmaceutical composition of claim 8, wherein the crystalline form SUC-P5 is of a therapeutically effective amount.",
    "10. A method of treating an anxiety disorder or depression in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of a pharmaceutical composition of claim 8.",
    "11. The method of claim 10, wherein the depression is major depressive disorder (MDD), bipolar disorder (BD), atypical depression, melancholic depression, psychotic major depression, catatonic depression, postpartum depression, seasonal affective disorder, dysthymia, a depressive disorder not otherwise specified (DD-NOS), or a substance induced mood disorder.",
    "12. The method of claim 10, wherein the anxiety disorder is panic disorder, obsessive-compulsive disorder (OCD), post-traumatic stress disorder (PTSD), generalized anxiety disorder (GAD), substance-induced anxiety disorder, acute stress disorder (ASD), irritable bowel syndrome, or fibromyalgia.",
    "13. The method of claim 10, wherein the anxiety disorder is a phobia.",
    "14. The method of claim 10, wherein the phobia is social phobia, agoraphobia, or animal phobia.",
    "15. The method of claim 10, wherein the subject is a human."
  ],
  "cpc": [
    "C07D 471/04",
    "A61P 21/02",
    "A61P 25/00",
    "A61P 25/04",
    "A61P 25/14",
    "A61P 25/16",
    "A61P 25/20",
    "A61P 25/22",
    "A61P 25/24",
    "A61P 25/28",
    "A61P 29/00",
    "A61P 9/00",
    "A61P 9/10",
    "C07C 55/10"
  ],
  "assignees": [
    "BIONOMICS LTD",
    "IRONWOOD PHARMACEUTICALS INC"
  ],
  "filing_date": "2014-03-14",
  "publication_date": "2017-08-29",
  "grant_date": "2017-08-29",
  "priority_date": "2013-03-15",
  "application_number": "US-201414776643-A",
  "family_id": "51535621",
  "citations": [
    "WO2008046135A1",
    "WO2012116410A1",
    "WO2012151640A1"
  ]
}