发明名称 SUBSTITUTED 1,2,3,4-TETRAHYDRO-2-DIBENZOFURANAMINES
摘要 1. A compound of the Formula I wherein: R<1> and R<2> are independently hydrogen, C1-C4 alkyl, benzyl, or &alpha;-methyl-4-nitrobenzyl; X is nitro, halo, -OH, -NH2, -CN, -NHC(O)R<3>, -C(O)R<6>, -NHSO2R<7>, or -SO2NHR<10>; R<3> is C1-C6-alkyl, C2-C6-alkenyl, C3-C8-cycloalkyl, phenyl, substituted phenyl, naphthyl, phenyl(C1-C4-alkylene), thienylmethyl, or a heterocycle; R<6> is hydroxy, amino, C1-C6 alkoxy, benzyloxy, phenoxy, or -NHR<8>; R<7> is C1-C6-alkyl, phenyl or phenyl monosubstituted with halo or C1-C4-alkyl; R<8> is C1-C6-alkyl, C2-C6-alkenyl, C3-C8-cycloalkyl, phenyl, substituted phenyl, naphthyl, or a heterocycle; and R<10> is C1-C6-alkyl, phenyl or phenyl monosubstituted with halo or C1-C4-alkyl; m is 1; and pharmaceutically acceptable salts thereof. 2. A compound of Claim 1 where X is -NHC(O)R<3>. 3. A compound of Claim 2 where R<3> is selected from the group consisting of phenyl, substituted phenyl or a heterocycle. 4. A compound of Claim 1 where X is -C(O)R<6>. 5. A compound of Claim 4 where R<6> is -NHR<8>. 6. A method of increasing activation of the 5-HTiF receptor in a mammal comprising administering to a mammal in need of said activation an effective amount of a compound of Claim 1. 7. A method of Claim 6 where the mammal is a human. 8. A pharmaceutical formulation comprising an effective amount of a compound of Formula wherein: R<1> and R<2> are independently hydrogen, C1-C4-alkyl, benzyl, or &alpha;-methyl-4-nitrobenzyl; X is nitro, halo, -OH, -NH2, -CN, -NHC(O)R<3>, -C(O)R<6>, -NHSO2R<7>, or -SO2NHR<10>; R<3> is C1-C6-alkyl, C2-C6-alkenyl, C3-C8-cycloalkyl, phenyl, substituted phenyl, naphthyl, phenyl(C1-C4-alkylene), thienylmethyl, or a heterocycle; R<6> is hydroxy, amino, C1-C6-alkoxy, benzyloxy, phenoxy, or -NHR<8>; R<7> is C1-C6-alkyl, phenyl or phenyl monosubstituted with halo or C1-C4-alkyl; R<8> is C1-C6-alkyl, C2-C6-alkenyl, C3-C8-cycloalkyl, phenyl, substituted phenyl, naphthyl, or a heterocycle; and R<10> is C1-C6-alkyl, phenyl or phenyl monosubstituted with halo or C1-C4-alkyl; m is 1; and pharmaceutically acceptable salts thereof, in combination with a suitable pharmaceutical carrier, diluent, or excipient.
申请公布号 EA001912(B1) 申请公布日期 2001.10.22
申请号 EA19990000241 申请日期 1997.08.25
申请人 ELI LILLY AND COMPANY 发明人 FLAUGH, MICHAEL, E.;KIEFER, JUNIOR, ANTON, D.
分类号 A61K31/343;A61P25/06;A61P43/00;C07D307/91;C07D307/93;C07D405/12;C07D409/12 主分类号 A61K31/343
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