KALLEL EDWARD ADAM,ARUMUGAM VIJAYALAKSMI,HILGRAF NICOLE,GROOTENHUIS PETER DIEDERIK JAN,MILLER MARK THOMAS,HADIDA-RUAH SARA SABINA,BINCH HAYLEY MARIE,DENINNO MICHAEL PAUL,FANNING LEV TYLER DEWEY,JOSHI
申请号：
NZ61501412
公开号：
NZ615014A
申请日:
2012.03.13
申请国别(地区):
NZ
年份:
2016
代理人:
摘要：
Disclosed are 1&rsquo-benzoyl-spiro[morpholine-2,4&rsquo-piperidine] derivatives and analogues as represented by the general formula (I) wherein the substituents are as defined herein. Representative compounds include 1&rsquo-(4-(3-hydroxypentan-3-yl)-3-methylbenzoyl)-4-(pyrimidin-2-yl)-6-ethyl-spiro[morpholine-2,4&rsquo-piperidine], 1&rsquo-(4-isopropoxy-3-methylbenzoyl)-4-(benzyl)-6-hydroxyethyl-spiro[morpholine-2,4&rsquo-piperidine], 1&rsquo-(4-(cyclopropyl(hydroxy)methyl)-benzoyl)-4-(2,2,2-trifluoroethyl)-6-phenyl-spiro[morpholine-2,4&rsquo-piperidine], 1&rsquo-(4-(isopropoxy)-3-methylbenzoyl)-4-(2-butyn-1-yl)-6-(2-fluoroethyl)-spiro[morpholine-2,4&rsquo-piperidine]. Also disclosed is a pharmaceutical composition comprising a compound as defined above and a pharmaceutically acceptable carrier, for inhibiting a voltage gated sodium ion channel, and for treating or lessening the severity of a condition selected from acute, chronic, neuropathic, or inflammatory pain, arthritis, migraine, cluster headaches, trigeminal neuralgia, herpatic neuralgia, general neuralgias, epilepsy or epilepsy conditions, neurodegenerative disorders, psychiatric disorders, anxiety, depression, dipolar disorder, myotonia, arrhythmia, movement disorders, neuroendocrine disorders, ataxia, multiple sclerosis, irritable bowel syndrome, incontinence, visceral pain, osteoarthritis pain, postherpetic neuralgia, diabetic neuropathy, radicular pain, sciatica, back pain, head or neck pain, severe or intractable pain, nociceptive pain, breakthrough pain, postsurgical pain, cancer pain, stroke, cerebral ischemia, traumatic brain injury, amyotrophic lateral sclerosis, stress- or exercise induced angina, palpitations, hypertension, migraine, and abnormal gastro-intestinal motility.
