首页> 外国专利> 1-SUBSTITUTED -4-PIPERIDINYL HYDRO-BENZOFURAN, PYRAN AND BENZOXEPINE AND BENZODIOXOLANE, DIOXAN AND DIOXEPINE CARBOXAMIDE DERIVATIVES: PREPARATORY PROCESSES, INTERMEDIATES AND PHARMACEUTICAL COMPOSITIONS

1-SUBSTITUTED -4-PIPERIDINYL HYDRO-BENZOFURAN, PYRAN AND BENZOXEPINE AND BENZODIOXOLANE, DIOXAN AND DIOXEPINE CARBOXAMIDE DERIVATIVES: PREPARATORY PROCESSES, INTERMEDIATES AND PHARMACEUTICAL COMPOSITIONS

机译:1-取代的-4-哌啶基苯并呋喃,吡喃和苯并西庚因和苯并二恶烷,二恶英和二恶英的羧酰胺衍生物:制备方法,中间体和药物组合物

摘要

N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives of formula CHEM wherein A is -CH2-CH2-, -CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-, -CH2-O-, -CH2-CH2-O- or -CH2-CH2-CH2-O-, R1 is hydrogen, halo, C1-6alkylsulfonyl or aminosulfonyl; R2 is hydrogen, amino, mono or di(C1-6alkyl)amino, arylC1-6alkylamino or C1-6alkylcarbonylamino; R3 and R4 are hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C3-6alkenyl optionally substituted with aryl, or L is -Alk-R5, -Alk-X-R6, -Alk-Y-C(=O)-R8 or -Alk-Y-C(=O)-NR10R11; the N-oxides, the pharmaceutically acceptable acid addition salts and possible stereochemically isomeric forms thereof. Said compounds have gastrointestinal stimulating activity. Pharmaceutical compositions containing such compounds as an active ingredient; methods of preparing said compounds and pharmaceutical compositions.
机译:的N-(3-羟基-4-哌啶基)(二氢苯并呋喃,二氢-2H-苯并吡喃或二氢苯并二恶英)羧酰胺衍生物,其中A为-CH2-CH2-,-CH2-CH2-CH2-,-CH2-CH2 -CH 2 -CH 2-,-CH 2 -O-,-CH 2 -CH 2 -O-或-CH 2 -CH 2 -CH 2 -O-,R 1为氢,卤素,C 1-6烷基磺酰基或氨基磺酰基; R 2为氢,氨基,单或二(C 1-6烷基)氨基,芳基C 1-6烷基氨基或C 1-6烷基羰基氨基; R 3和R 4为氢或C 1-6烷基; L为C 3-6环烷基,C 5-6环烷酮,任选地被芳基取代的C 3-6烯基,或L为-Alk-R 5,-Alk-XR 6,-Alk-YC(= O)-R 8。或-Alk-YC(= O)-NR <1> <0> R <1> <1>; N-氧化物,药学上可接受的酸加成盐及其可能的立体化学异构形式。所述化合物具有胃肠刺激活性。含有这类化合物作为有效成分的药物组合物;所述化合物和药物组合物的制备方法。

著录项

  • 公开/公告号NZ232964A

    专利类型

  • 公开/公告日1991-07-26

    原文格式PDF

  • 申请/专利权人 JANSSEN PHARMACEUTICA NV;

    申请/专利号NZ19900232964

  • 申请日1990-03-16

  • 分类号C07D405/12;C07D405/14;C07D471/12;C07D513/06;C07D513/16;C07D487/02;C07D487/12;C07D317/46;C07D319/08;C07D319/16;C07D321/10;A61K31/445;A61K31/495;A61K31/50;A61K31/505;A61K31/53;C07D211/42;C07D307/79;

  • 国家 NZ

  • 入库时间 2022-08-22 05:57:43

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