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    • 8. 发明授权
    • Inhibitors of phosphodiesterase 11 (PDE11)
    • 磷酸二酯酶11抑制剂(PDE11)
    • US09173884B2
    • 2015-11-03
    • US14361979
    • 2012-11-29
    • TRUSTEES OF BOSTON COLLEGE
    • Charles Stuart HoffmanOzge Ceyhan
    • C07D495/04A61K31/519C07D513/04A61K45/06A61K31/416A61K31/437A61K31/53A61K31/573
    • A61K31/519A61K31/416A61K31/437A61K31/53A61K31/573A61K45/06C07D513/04A61K2300/00
    • The present intervention generally relates to compositions comprising a PDE11 inhibitor for increasing cortisol levels in a subject, or for increasing the production of cortisol from adenocortical cells in a subject. Aspects of the invention relate to the use of a PDE11 inhibitor in a method of treatment of low cortisol levels and/or adrenal insufficiency in a subject, or a method of treating a disease or disorders associated with adrenal insufficiency. Aspects of the invention relate to PDE11 inhibitors belonging to compounds of formula (I)-(VI), and their use alone or in combination with long-term corticosteroid treatment to elevate cortisol levels in a subject, and/or to treat adrenal insufficiency. Another aspect relates to kits comprising PDE11 inhibitors for administration to a subject, pharmaceutical compositions comprising compounds of formula (I)-(VI) for use in methods to increase cortisol levels and/or treat adrenal insufficiency, and their use as an adjuvant for treatment of cancer or other disorders such as psychiatric diseases where elevating cortisol levels would be beneficial to the subject.
    • 本发明通常涉及包含用于增加受试者中的皮质醇水平的PDE11抑制剂或用于从受试者的腺皮质细胞中增加皮质醇的产生的组合物。 本发明的方面涉及在治疗受试者的低皮质醇水平和/或肾上腺功能不全的方法中使用PDE11抑制剂或治疗与肾上腺功能不全相关的疾病或病症的方法。 本发明的方面涉及属于式(I) - (VI)化合物的PDE11抑制剂及其单独使用或与长期皮质类固醇治疗组合以提高受试者的皮质醇水平和/或治疗肾上腺功能不全的用途。 另一方面涉及包含用于给予受试者的PDE11抑制剂的试剂盒,包含用于增加皮质醇水平和/或治疗肾上腺功能不全的方法的式(I) - (VI)化合物的药物组合物及其作为治疗佐剂的用途 的癌症或其他疾病,例如提高皮质醇水平对受试者有益的精神疾病。