公开(公告)号：US20240360091A1

公开(公告)日：2024-10-31

申请号：US18688300

申请日：2022-09-02

申请人： Emory University ,  Neurop, Inc.

发明人： Dennis Liotta ,  Stephen Traynelis ,  Lawrence Wilson ,  Yesim Altas Tahirovic ,  David Menaldino ,  Scott Myers ,  Kamalesh Poornachary

IPC分类号： C07D295/135 ,  A61K31/495 ,  A61K31/496 ,  C07D209/34 ,  C07D215/22 ,  C07D295/096

CPC分类号： C07D295/135 ,  A61K31/495 ,  A61K31/496 ,  C07D209/34 ,  C07D215/22 ,  C07D295/096

摘要： Compounds that selectively inhibit GluN2B-containing N-methyl-D-aspartic acid receptors (NMDARs) are disclosed. In some cases, the compounds selectively target GluN2B over GluN2A, GluN2C, and/or GluN2D. Generally, the compounds possess an enhanced potency to GluN2B at a pH that is more acidic compared to the physiological pH. Pharmaceutical formulations containing one or more of the compounds are also disclosed. Additionally, methods of treating a condition, disorder or disease using the compounds or their pharmaceutical formulations thereof are disclosed. Exemplary conditions, disorders, and diseases relevant to this disclosure include stroke, subarachnoid hemorrhage, cerebral ischemia, cerebral vasospasm, hypoxia, acute CNS injury, spinal cord injury, traumatic brain injury, coronary artery bypass graft, persistent or chronic cough, substance abuse disorder, opiate withdrawal, opiate tolerance, bipolar disorder, suicidal ideation, pain, fibromyalgia, depression, postpartum depression, resting tremor, dementia, epilepsy, seizure disorder, movement disorder, and neurodegenerative disease.