发明名称 Bicyclic benzamides of 3- or 4-substituted 4-(aminomethyl)-piperidine derivatives
摘要 The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R<SUP>1 </SUP>and R<SUP>2 </SUP>taken together form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C<SUB>1-6</SUB>alkyl; R<SUP>3 </SUP>is hydrogen or halo; R<SUP>4 </SUP>is hydrogen or C<SUB>1-6</SUB>alkyl; R<SUP>5 </SUP>is hydrogen or C<SUB>1-6</SUB>alkyl; L is C<SUB>3-6</SUB>cycloalkyl, C<SUB>5-6</SUB>cycloalkanone, C<SUB>2-6</SUB>alkenyl, or L is a radical of formula -Alk-R<SUP>6</SUP>-, Alk-X-R<SUP>7</SUP>, -Alk-Y-C(-O)-R<SUP>9</SUP>, or -Alk-Y-C(-O)-NR<SUP>11</SUP>R<SUP>12 </SUP>wherein each Alk is C<SUB>1-12</SUB>alkanediyl; and R<SUP>6 </SUP>is hydrogen, cyano, C<SUB>1-6</SUB>alkylsulfonylamino, C<SUB>3-6</SUB>cycloalkyl, C<SUB>5-6</SUB>cycloalkanone, or a heterocyclic ringsystem; R<SUP>7 </SUP>is hydrogen, C<SUB>1-6</SUB>alkyl, hydroxyC<SUB>1-6</SUB>alkyl, C<SUB>3-6</SUB>cycloalkyl, or a heterocyclic ringsystem; X is O, S, SO<SUB>2 </SUB>or NR<SUP>8</SUP>; said R<SUP>8 </SUP>being hydrogen or C<SUB>1-6</SUB>alkyl; R<SUP>9 </SUP>is hydrogen, C<SUB>1-6</SUB>alkyl, C<SUB>3-6</SUB>cycloalkyl, C<SUB>1-6</SUB>alkyloxy or hydroxy; Y is NR<SUP>10 </SUP>or a direct bond; said R<SUP>10 </SUP>being hydrogen, or C<SUB>1-6</SUB>alkyl; R<SUP>11 </SUP>and R<SUP>12 </SUP>each independently are hydrogen, C<SUB>1-6</SUB>alkyl, C<SUB>3-6</SUB>cycloalkyl, or R<SUP>11</SUP>and R<SUP>12 </SUP>combined with the nitrogen atom may form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
申请公布号 US2006142341(A1) 申请公布日期 2006.06.29
申请号 US20060355326 申请日期 2006.02.16
申请人 BOSMANS JEAN-PAUL RENE MARIE A;CLEYN MICHEL ANNA JOZEF DE;SURKYN MICHEL 发明人 BOSMANS JEAN-PAUL R.M.;DE CLEYN MICHEL A.J.;SURKYN MICHEL
分类号 A61K31/452;A61K31/4427;A61K31/443;A61K31/445;A61K31/4523;A61K31/4525;A61K31/453;A61K31/454;A61K31/4545;A61K31/497;A61K31/501;A61K31/502;A61P1/00;A61P1/10;A61P1/14;A61P43/00;C07C229/60;C07D211/42;C07D211/44;C07D401/06;C07D405/02;C07D405/06;C07D405/12;C07D405/14;C07D417/14;C07D513/04 主分类号 A61K31/452
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