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    Aminoalkyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
    6.
    发明授权
    Aminoalkyl substituted (benzodioxan, benzofuran or benzopyran) derivatives 有权
    氨基烷基取代的（苯并二恶烷，苯并呋喃或苯并吡喃）衍生物

    公开(公告)号：US06864273B1

    公开(公告)日：2005-03-08

    申请号：US09980452

    申请日：2000-05-23

    申请人： Kristof Van Emelen ,  Marcel Frans Leopold De Bruyn

    发明人： Kristof Van Emelen ,  Marcel Frans Leopold De Bruyn

    IPC分类号： A61K31/4164 ,  A61K31/4178 ,  A61K31/513 ,  A61P1/14 ,  A61P9/00 ,  A61P9/08 ,  C07D405/12 ,  C07D417/12

    CPC分类号： C07D405/12 ,  C07D417/12

    摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R6 is hydrogen or phenylmethyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. 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 impaired fundic relaxation.

    摘要翻译： 本发明涉及式（I）化合物，其立体化学异构形式，其N-氧化物形式或其药学上可接受的酸加成盐，其中-Z 1 -Z 2 - 是二价基团; R 1，R 2和R 3各自独立地选自氢，C 1-6烷基，羟基，卤素等; 或当R 1和R 2在相邻的碳原子上时，R 1和R 2一起可以形成式的二价基团; Alk 1和Alk 2是任选取代的C 1-6烷二基; R 6是氢或苯基甲基; R 5是脯氨酸的基团，n是1或2; p <1>为0，p <2为1或2; 或p <1>为1或2，p <2为0; X是氧，硫或= NR 9; Y是氧或硫; R 7是氢，C 1-6烷基，C 3-6环烷基，苯基或苯基甲基; R 8是C 1-6烷基，C 3-6环烷基苯基或苯基甲基; R 9是氰基，C 1-6烷基，C 3-6环烷基，C 1-6烷氧基羰基或氨基羰基; R 10是氢或C 1-6烷基; 而Q是二价基团。 公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗与减退的放松有关的病症。

    (Benzodioxan, benzofuran or benzopyran) derivatives having fundic relaxation properties
    8.
    发明授权
    (Benzodioxan, benzofuran or benzopyran) derivatives having fundic relaxation properties 有权
    （苯并二恶烷，苯并呋喃或苯并吡喃）衍生物

    公开(公告)号：US06495547B1

    公开(公告)日：2002-12-17

    申请号：US09641485

    申请日：2000-08-18

    申请人： Piet Tom Bert Paul Wigerinck ,  Wim Gaston Verschueren ,  Marc Francis Josephine Schroven ,  Marcel Frans Leopold De Bruyn

    发明人： Piet Tom Bert Paul Wigerinck ,  Wim Gaston Verschueren ,  Marc Francis Josephine Schroven ,  Marcel Frans Leopold De Bruyn

    IPC分类号： C07D40514

    CPC分类号： C07D405/12 ,  C07D405/14

    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, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6—Alk2— (b-1), or —Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen. sulfur or ═NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. 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 impaired fundic relaxation.

    摘要翻译： 式（I）化合物的本发明是其立体化学异构形式，其N-氧化物形式或其药学上可接受的酸加成盐，其中Alk1是任选被羟基，C 1-4烷氧基或C 1-4烷基羰基氧基取代的C 1-6烷二基; -Z1-Z2-是二价基团; R 1，R 2和R 3各自独立地选自氢，C 1-6烷基，羟基，卤素等; 或当R 1和R 2在相邻碳原子上时，R 1和R 2一起可以形成二价基; R4是氢或C1-6烷基; A是式-NR6-Alk2-（b-1）或-N-哌啶基 - （CH2）m（b-2）的二价基团，其中m是0或1; R5是一种基团，其中n是1或2; p1为0，p2为1或2; 或p1为1或2，p2为0; X是氧。 硫或= NR9; Y是氧或硫; R7是氢，C1-6烷基，C3-6环烷基，苯基或苯基甲基; R8是C1-6烷基，C3-6环烷基苯基或苯基甲基; R9是氰基，C1-6烷基，C3-6环烷基，C1-6烷氧基羰基或氨基羰基; R 10是氢或C 1-6烷基; 而Q是二价基团。 公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗与减退的放松有关的病症。