Linz Klaus,Zemolka Saskia,Nolte Bert,Schunk Stefan,Schick Hans
申请号：
NZ60752911
公开号：
NZ607529A
申请日:
2011.07.27
申请国别(地区):
NZ
年份:
2014
代理人:
摘要：
607529 The disclosure relates to a family of cis-tetrahydro-spiro(cyclohexane-1,1’-pyrido[3,4-b]indol)-4-amine compounds (compound III). The base structure includes an amide bond and can be further derivatised to include thiophenes or a carbon-carbon double bond (alkene) into the structure. These compounds act on the nociceptin/ORL-1 receptor system and the μ-opioid receptor system. They appear to have selective activity for the treatment of chronic pain (including inflammatory pain, visceral pain, tumoral pain, preferably neuropathic pain) without any activity with respects to acute, nociceptive pain. Example compounds include: (E)-1-((1s,4s)-4-(dimethylamino)-4-phenyl-3’,4’-dihydrospiro[cyclohexane-1,1-pyrido[3,4-b]indol]-2’(9’H)-yl)-3-phenylprop-2-en-1-one (E)-1-((1s,4s)-4-(dimethylamino)-4-(3-fluorophenyl)-3,4’-dihydro20spiro[cyclohexane-1,1’-pyrido[3,4-b]indol]-2’(9’H)-yl)-3-phenylprop-2-en-1-one (E)-1-((1s,4s)-4-(dimethylamino)-6’-fluoro-4-(3-fluorophenyl)-3’,4’-dihydrospiro[cyclohexane-1,1’-pyrido[3,4-b]indol]-2’(9’H)-yl)-3-phenylprop-2-en-1-one (E)-1-((1s,4s)-4-(dimethylamino)-6’-fluoro-4-phenyl-3’,4’-dihydrospiro[cyclohexane-1,1’-pyrido[3,4-b]indol]-2’(9’H)-yl)-3-phenylprop-2-en-1-one (E)-1-((1s,4s)-4-(dimethylamino)-4-(4-fluorophenyl)-3’,4’-dihydrospiro[cyclohexane-1,1’-pyrido[3,4-b]indol]-2’(9’H)-yl)-3-phenylprop-2-en-1-one
