发明名称 Novel 1,3,8-triazaspiroÝ4.5¨decanones with high affinity for opioid receptor subtypes
摘要 The present invention relates to use of small organic compounds acting as opioid receptor ligands for the treatment of vasomotor disturbances. In particular the present invention relates to the triazaspiro compounds of general formula (Ia) or (Ib) wherein R<1> is selected among phenyl, arylalkyl or thienyl; R<2> is selected among aminophenyl, C1-6-monoalkylaminophenyl, C1-6-dialkylaminophenyl, cyanophenyl, C2-6-alkylphenyl, naphthyl, tetrahydronaphthyl, furanyl, indanyl, benzothienyl or benzofuranyl; R<3> is hydrogen, C1-6-alkyl, phenyl, benzyl, or acetyl; R<4> is hydrogen or (CH2)m-(CHR<9>)-(CH2)p-AR<11>; R<5> is hydrogen or C1-4-alkyl; z is CHR<10> wherein R<10> is hydrogen, C1-6-alkyl, phenyl or arylalkyl - or z is C2-8-alkylene, C2-8-alkenylene or C2-8-alkynylene; n is 1 or 2; or a pharmaceutically acceptable salt thereof for the treatment of migraine, non insulin dependent diabetes mellitus (type II diabetes), sepsis, inflammation, incontinence and/or vasomotor disturbances, in particular the peripheral vasomotor effects known as hot flushes or hot flashes.
申请公布号 AU3809999(A) 申请公布日期 1999.12.06
申请号 AU19990038099 申请日期 1999.05.14
申请人 NOVO-NORDISK A/S 发明人 BRETT WATSON;ROLF HOHLWEG;CHRISTIAN THOMSEN
分类号 C07D487/10;A61K31/438;A61K31/445;A61P3/10;A61P13/00;A61P25/00;A61P25/06;A61P25/30;A61P29/00;A61P31/04;A61P43/00;C07D471/10 主分类号 C07D487/10
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