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GONADOTROPIN-RELEASING HORMONE ANTAGONIST DOSING REGIMENS FOR TREATING UTERINE FIBROIDS AND REDUCING MENSTRUAL BLOOD LOSS

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  • Publication Date:
    January 4, 2024
  • معلومة اضافية
    • Document Number:
      20240000785
    • Appl. No:
      18/244773
    • Application Filed:
      September 11, 2023
    • نبذة مختصرة :
      The invention provides compositions and methods for reducing the volume of menstrual blood loss in a patient, such as a human patient, for instance, that has uterine fibroids, by administration of a gonadotropin-releasing hormone (GnRH) antagonist. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof.
    • Claim:
      1. A method of reducing the volume of menstrual blood loss in a female human patient, the method comprising administering to the patient a compound, 3-[2-fluoro-5-(2,3-difluoro-6-methoxpenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno [3,4d]pyrimidine-5-carboxylic acid, or a pharmaceutically acceptable salt thereof, in an amount of about 100 mg per day or about 200 mg per day.
    • Claim:
      2. The method of claim 1, wherein the patient has uterine fibroids.
    • Claim:
      3. The method of claim 1, wherein the compound is administered to the patient in an amount of about 100 mg per day.
    • Claim:
      4. The method of claim 1, wherein the compound is administered to the patient in an amount of about 200 mg per day.
    • Claim:
      5. The method of claim 1, wherein the compound is administered to the patient in the form of a pharmaceutically acceptable salt thereof.
    • Claim:
      6. The method of claim 5, wherein the pharmaceutically acceptable salt is a choline salt.
    • Claim:
      7. The method of claim 1, wherein the compound is administered to the patient orally.
    • Claim:
      8. The method of claim 1, wherein the compound is administered to the patient once daily.
    • Claim:
      9. A method of treating uterine fibroids in a female human patient in need thereof, the method comprising administering to the patient a compound, 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno [3,4d]pyrimidine-5-carboxylic acid, or a pharmaceutically acceptable salt thereof, in an amount of about 100 mg per day or about 200 mg per day.
    • Claim:
      10. The method of claim 9, wherein the compound is administered to the patient in an amount of about 100 mg per day.
    • Claim:
      11. The method of claim 9, wherein the compound is administered to the patient in an amount of about 200 mg per day.
    • Claim:
      12. The method of claim 9, wherein the compound is administered to the patient in the form of a pharmaceutically acceptable salt thereof.
    • Claim:
      13. The method of claim 12, wherein the pharmaceutically acceptable salt is a choline salt.
    • Claim:
      14. The method of claim 9, wherein the compound is administered to the patient orally.
    • Claim:
      15. The method of claim 9, wherein the compound is administered to the patient once daily.
    • Claim:
      16. A kit comprising a compound, 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno [3,4d]pyrimidine-5-carboxylic acid, or a pharmaceutically acceptable salt thereof, wherein the compound is present in the kit in a unit dosage form comprising about 100 mg or about 200 mg of the compound, and wherein the kit further comprises a package insert that instructs a user of the kit to perform the method of claim 1.
    • Claim:
      17. The kit of claim 16, wherein the compound is present in the kit in the form of a pharmaceutically acceptable salt thereof.
    • Claim:
      18. The kit of claim 17, wherein the pharmaceutically acceptable salt is a choline salt.
    • Claim:
      19. The kit of claim 16, wherein the compound is present in the kit in a unit dosage form comprising about 100 mg of the compound.
    • Claim:
      20. The kit of claim 16, wherein the compound is present in the kit in a unit dosage form comprising about 200 mg of the compound.
    • Current International Class:
      61; 61; 61; 61
    • الرقم المعرف:
      edspap.20240000785