发明名称 GASTROKINETISCHE BICYCLISCHE BENZAMIDE VON 3- ODER 4-SUBSTITUIERTEN 4-(AMINOMETHYL)-PIPERIDINDERIVATEN
摘要 <p>The present invention of compounds of formula (I) <CHEM> a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R<1> and R<2> taken together form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl; R<3> is hydrogen or halo; R<4> is hydrogen or C1-6alkyl; R<5> is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl, or L is a radical of formula -Alk-R<6>-, Alk-X-R<7>, -Alk-Y-C(=O)-R<9> , or -Alk-Y-C(=O)-NR<11>R<12> wherein each Alk is C1-12alkanediyl; and R<6> is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ringsystem; R<7> is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, S, SO2 or NR<8>; said R<8> being hydrogen or C1-6alkyl; R<9> is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR<10> or a direct bond; said R<10> being hydrogen, or C1-6alkyl; R<11> and R<12> each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, or R<11> and R<12> 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.</p>
申请公布号 DE69809050(D1) 申请公布日期 2002.12.05
申请号 DE1998609050 申请日期 1998.07.07
申请人 JANSSEN PHARMACEUTICA N.V., BEERSE 发明人 BOSMANS, JEAN-PAUL RENE MARIE ANDRE;DE CLEYN, ANNA;SURKYN, MICHEL
分类号 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;C07D405/06;C07D405/12;C07D405/14;C07D417/14;C07D513/04;(IPC1-7):A61K31/445 主分类号 A61K31/4427
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