发明名称 SELECTIVE iGLuR5 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF MIGRAINE
摘要 1. The use 3S,4aR,6S,8aR-6-(((4-carboxy) phenyl) methyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid as a selective iGluR5 receptor antagonist for the manufacture of a medicament for treating migraine. 2. The use of a compound of formula I wherein R<1> and R<2> are each independently H, C1-C20 alkyl or a pharmaceutically acceptable salt thereof as the selective iGluR5 receptor antagonist for the manufacture of a medicament for treating migraine. 3. The use according to claim 2, characterized in that the compound of formula I is selected from 4aR,6S,8aR-6-(((2S)-2-(Ethoxycarbonyl)-4,4-difluoropyrrolidinyl)methyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylate, or 3S,4aR,6S,8Ar-6-(((2S)-2-(Carboxylic acid)-4,4difluoropyrrolidinyl) methyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic Acid. 4. A compound of formula wherein R<1> and R<2> are each independently H, C1-C20 alkyl or a pharmaceutically acceptable salt thereof. 5. The compound according to claim 4, characterized in that R<1> and R<2> are each independently H, C1-C6 alkyl. 6. A compound which is 3S,4aR,6S,8aR Ethyl 6-(((2S)-2-(Ethoxycarbonyl)-4,4 difluoropyrrolidinyl) methyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylate, or a pharmaceutically acceptable salt thereof. 7. A compound which is 3S,4aR,6S,8aR-6-(((2S)-2(Carboxylic acid)-4,4-difluoropyrrolidinyl) methyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid, or a pharmaceutically acceptable salt thereof. 8. A pharmaceutical composition which comprises a compound according to any one of claims 4-7 in combination with one or more pharmaceutically acceptable carriers, diluents, or excipients. 9. A pharmaceutical composition for the treatment of migraine which comprises a compound according to any one of claims 4-7 in combination with a pharmaceutically acceptable carrier, diluent, or excipient. 10. A compound which is 3S,4aR,6S,8aR-Ethyl 6-(((2S)-2-(Ethoxycarbonyl)-4,4-difluoropyrrolidinyl) methyl)-1,2,3,4,4a,5,6,7,8,8a-decahydrosioquionline-3-carboxylate mandelate.
申请公布号 EA004290(B1) 申请公布日期 2004.02.26
申请号 EA20020000132 申请日期 2000.06.27
申请人 ELI LILLY AND COMPANY 发明人 BLEAKMAN, DAVID;CHAPPELL, AMY, SUZON;FILLA, SANDRA, ANN;JOHNSON, KIRK, WILLIS;ORNSTAIN, PAUL, LESLIE
分类号 A61K45/00;A61K31/00;A61K31/472;A61K31/4725;A61K31/5377;A61P21/02;A61P25/00;A61P25/04;A61P25/06;A61P25/14;A61P25/16;A61P25/18;A61P25/22;A61P25/24;A61P25/28;A61P25/30;A61P27/02;A61P43/00;C07D401/06;(IPC1-7):A61K31/00;A61K31/537;C07D413/06 主分类号 A61K45/00
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