| 摘要 |
597498 Disclosed are 1-phenyl-2-aminoalkyl-cyclopropane derivatives as represented by the general formula (I), or a pharmaceutically acceptable salt, ester, or amide thereof, wherein: one of R1 and R2 is a group of the formula -L2-R6a-L3-R6b; the other of R1 and R2 is selected from the group consisting of hydrogen, alkyl, alkoxy, halogen, cyano, and thioalkoxy; R3, R3a, and R3b are each independently selected from the group consisting of hydrogen, alkyl, trifluoroalkyl, trifluoroalkoxy, alkoxy, halogen, cyano, and thioalkoxy; R4 and R5 taken together with the nitrogen atom to which each is attached form a pyrrolidin-1-yl rings system which may be further substituted, and wherein the remaining substituents are as defined herein. Representative compounds include 2-methoxy-5-[4-((1S,2S)-2-{ [(2S)-2-methylpyrrolidin-1-yl]methyl} cyclopropyl)phenyl]pyrimidine, 2-[4-((1S,2S)-2-{ [(2S)-2-methylpyrrolidin-1-yl]methyl} cyclopropyl)phenyl]pyridazin-3(2H)-one and 2-[4-((1S,2S)-2-{ [(2R)-2-methylpyrrolidin-1-yl]methyl} cyclopropyl)phenyl]pyridazin-3(2H)-one, or a salt thereof. Further disclosed is a composition comprising a compound as defined above, and a pharmaceutically acceptable carrier; for the treatment of conditions such as attention-deficit hyperactivity disorder (ADHD), deficits in attention, dementia, and diseases with deficits of memory, learning, schizophrenia, cognitive deficits of schizophrenia, cognitive deficits and dysfunction in psychiatric disorders, Alzheimer's disease, mild cognitive impairment, epilepsy, seizures, allergic rhinitis, and asthma, motion sickness, dizziness, Meniere's disease, vestibular disorders, vertigo, obesity, diabetes, type II diabetes, Syndrome X, insulin resistance syndrome, metabolic syndrome, pain, including neuropathic pain, neuropathy, sleep disorders, narcolepsy, pathological sleepiness, jet lag, drug abuse, mood alteration, bipolar disorder, depression, obsessive compulsive disorder, Tourette's syndrome, Parkinson's disease, and medullary thyroid carcinoma, melanoma, and polycystic ovary syndrome. |
