GluN2B-subunit selective antagonists of the N-methyl-D-aspartate receptors with enhanced potency at acidic pH
US12415790B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Jul 19, 2024 |
| Grant date | Sep 16, 2025 |
| Priority date | — |
| Expiry date | Aug 29, 2044 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D295/096
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Compounds that selectively inhibit GluN2B-containing N-methyl-D-aspartic acid receptors (NM/DARs) 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.