发明名称 5-Amino-4-Hydroxy-7-(1H-Indolmethyl)-8-Methylnonamide Derivatives as Renin Inhibitors for the Treatment of Hypertension
摘要 The application relates to novel alkanamides of the general formula (I) where X is -CH<SUB>2</SUB>- or >CH-OH; (A) R<SUP>1 </SUP>is e.g. an optionally substituted heterocyclyl radical or an optionally substituted polycyclic, unsaturated hydrocarbon radical where X is hydroxymethylene; R<SUP>2 </SUP>is C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl or C<SUB>3</SUB>-C<SUB>6</SUB>-cydoalkyl; R<SUP>3 </SUP>are each independently H, C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl, C<SUB>1-6</SUB>-alkoxycarbonyl or C<SUB>1</SUB>-C<SUB>6</SUB>-alkanoyl; R<SUP>4 </SUP>is C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl, C<SUB>3</SUB>-C<SUB>6</SUB>-cycloalkyl, C<SUB>2</SUB>-C<SUB>6</SUB>-alkenyl or unsubstituted or substituted arylC<SUB>1</SUB>-C<SUB>6</SUB>-alkyl; R<SUP>5 </SUP>is C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl, C<SUB>1</SUB>-C<SUB>6</SUB>-hydroxyalkyl, C<SUB>1</SUB>-C<SUB>6</SUB>-alkoxy-C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl, C<SUB>1</SUB>-C<SUB>6</SUB>-alkanoyloxy C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl, C<SUB>1</SUB>-C<SUB>6</SUB>-aminoalkyl, C<SUB>1</SUB>-C<SUB>6</SUB>-alkylamino-C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl, C<SUB>1</SUB>-C<SUB>6</SUB>-dialkylamino-C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl, C<SUB>1</SUB>-C<SUB>6</SUB>-alkanoylamido-C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl, HO(O)C-C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl, C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl-O-(O)C-C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl, H<SUB>2</SUB>N-C(O)-C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl, C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl-HN-C(O)-C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl, (C<SUB>1</SUB>, -C<SUB>6</SUB>-alkyl)<SUB>2</SUB>N-C(O)-C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl, C<SUB>2</SUB>-C<SUB>8</SUB>-alkenyl, C<SUB>2</SUB>-C<SUB>8</SUB>-alkynyl, cyano-C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl, halo-C<SUB>1</SUB>-C<SUB>6</SUB>-alkyl, optionally substituted aryl-C<SUB>o</SUB>-C<SUB>6</SUB>-alkyl, optionally substituted C<SUB>3</SUB>-C<SUB>8</SUB>-cycloalkyl-C<SUB>o</SUB>-C<SUB>6</SUB>-alkyl or optionally substituted heterocydyl-C<SUB>o</SUB>-C<SUB>6</SUB>-alkyl; to a process for their preparation and to the use of these compounds as medicines, especially as renin inhibitors for the treatment of hypertension.
申请公布号 US2008280895(A1) 申请公布日期 2008.11.13
申请号 US20050593460 申请日期 2005.03.17
申请人 HEROLD PETER;STUTZ STEFAN;MAH ROBERT;TSCHINKE VINCENZO;STOJANOVIC ALEKSANDAR;JOTTERAND NATHALIE;QUIRMBACH MICHAEL;BEHNKE DIRK;MARTI CHRISTIANE 发明人 HEROLD PETER;STUTZ STEFAN;MAH ROBERT;TSCHINKE VINCENZO;STOJANOVIC ALEKSANDAR;JOTTERAND NATHALIE;QUIRMBACH MICHAEL;BEHNKE DIRK;MARTI CHRISTIANE
分类号 A61K31/538;A61K31/405;A61K31/437;A61K31/4412;A61K31/519;A61P9/00;C07C237/06;C07C237/22;C07D209/12;C07D209/18;C07D209/20;C07D213/63;C07D265/36;C07D401/02;C07D401/12;C07D403/12;C07D405/12;C07D409/12;C07D417/12;C07D471/04;C07D487/04 主分类号 A61K31/538
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