| 摘要 |
Disclosed is anhydrous polymorphic form C of basmisanil ((1,1-dioxo-thiomorpholin-4-yl)-(6-{ [3-(4-fluorophenyl)-5-methyl-isoxazol-4-yl]methoxy} -pyridin-3-yl)-methanone / RG-1662 / RO5186582 / (1,1-dioxo-1,4-thiazinan-4-yl)-[6-[[3-(4-fluorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]pyridin-3-yl]methanone) as represented by formula (I), characterized by an XRPD diffraction pattern comprising XRPD peaks at angles of diffraction 2Theta (CuKα) of 11.7°±0.2°, 17.4°±0.2° and 23.4°±0.2°. Polymorphic form C of basmisanil can also be characterised by a melting point with onset temperature (DSC) in the range of about 146 °C to 150 °C (heating rate of 10°C/min.). Also disclosed is a pharmaceutical compositions comprising a solid crystalline form of a compound of basmisanil as defined above and a pharmaceutically acceptable excipient, for the treatment or prevention of acute and/or chronic neurological disorders, cognitive disorders, Alzheimer’s disease, memory deficits, schizophrenia, positive, negative and/or cognitive symptoms associated with schizophrenia, bipolar disorders, autism, Down syndrome, neurofibromatosis type I, sleep disorders, disorders of circadian rhythms, amyotrophic lateral sclerosis (ALS), dementia caused by AIDS, psychotic disorders, substance-induced psychotic disorder, anxiety disorders, generalized anxiety disorder, panic disorder, delusional disorder, obsessive/compulsive disorders, acute stress disorder, drug addictions, movement disorders, Parkinson’s disease, restless leg syndrome, cognition deficiency disorders, multi-infarct dementia, mood disorders, depression, neuropsychiatric conditions, psychosis, attention-deficit/hyperactivity disorder, neuropathic pain, stroke, Multiple Sclerosis (MS), acute Meningitis, Fetal Alcohol Syndrome, and attentional disorders, for stroke recovery therapy, or for use as cognitive enhancers. |
