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    �(benzodioxan, benzofuran or benzopyran) alkylamino! alkyl substituted guanidines
    5.
    发明授权
    �(benzodioxan, benzofuran or benzopyran) alkylamino! alkyl substituted guanidines 失效
    [（苯并二恶烷，苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍

    公开(公告)号：US5703115A

    公开(公告)日：1997-12-30

    申请号：US632230

    申请日：1996-04-15

    申请人： Guy Rosalia Eugene Van Lommen ,  Marcel Frans Leopold De Bruyn ,  Walter Jacobus Joseph Janssens

    发明人： Guy Rosalia Eugene Van Lommen ,  Marcel Frans Leopold De Bruyn ,  Walter Jacobus Joseph Janssens

    IPC分类号： C07D307/81 ,  C07D311/58 ,  C07D319/20 ,  C07D405/12 ,  C07D405/14 ,  A61K31/34 ,  A61K31/35

    CPC分类号： C07D405/12 ,  C07D307/81 ,  C07D311/58 ,  C07D319/20 ,  C07D405/14

    摘要： The present invention is concerned with vasoconstricive �benzodioxan, benzofuran or benzopyran)alkylamino!alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is a bivalent C.sub.1-3 alkanediyl radical; A is a bivalent radical of formula: ##STR2## wherein each R.sup.5 is hydrogen or C.sub.1-4 alkyl; wherein each R.sup.6 is hydrogen or C.sub.1-4 alkyl; Alk.sup.2 is C.sub.2-15 alkanediyl or C.sub.5-7 cycloalkanediyl; and each p is 0, 1 or 2; provided that �2-�(2,3-dihydro-1,4-benzodioxin-2-yl)methyl!amino!ethyl guanidine is excluded. Pharmaceuticals which are useful as vasoconstrictors. Compositions comprising said guanidine derivatives as active ingredients, processes for preparing said guanidine derivatives and novel N-cyano guanidine, intermediates; and a use as a medicine are described.

    摘要翻译： 本发明涉及具有下式的血管收缩性（苯并二恶烷，苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍（I）其药学上可接受的酸加成盐及其立体化学异构形式，其中X是O，CH 2或 直接债券 R1是氢或C1-6烷基; R2是氢，C1-6烷基，C3-6烯基或C3-6炔基; R3是氢或C1-6烷基; 或者R 2和R 3可以一起形成式 - （CH 2）m - 的二价基团，其中m为4或5; 或R 1和R 2一起形成式-CH = CH-或式 - （CH 2）n - 的二价基团，其中n为2,3或4; 或者当R 1和R 2一起形成式-CH = CH-CH =，-CH = CH-N =或-CH = N-CH =的二价基团时，R 3可以表示键。 R4是氢或C1-6烷基; Alk1是二价C 1-3烷二基; （a）其中每个R 5为氢或C 1-4烷基;（e）其中每个R 5为氢或C 1-4烷基;（c） 其中每个R 6是氢或C 1-4烷基; Alk2是C2-15烷二基或C5-7环烷​​二基; 每个p为0,1或2; 条件是排除[2 - [（2,3-二氢-1,4-苯并二恶英-2-基）甲基]氨基]乙基胍。 可用作血管收缩药物的药物。 包含所述胍衍生物作为活性成分的组合物，制备所述胍衍生物的方法和新的N-氰基胍，中间体; 并描述了作为药物的用途。

    �(Benzodioxan benzofuran or benzopyran) alkylamino!alkyl substituted guanidines
    6.
    发明授权
    �(Benzodioxan benzofuran or benzopyran) alkylamino!alkyl substituted guanidines 失效
    [（苯并二恶烷苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍

    公开(公告)号：US5688952A

    公开(公告)日：1997-11-18

    申请号：US632228

    申请日：1996-04-15

    申请人： Guy Rosalia Eugene Van Lommen ,  Marcel Frans Leopold De Bruyn ,  Walter Jacobus Joseph Janssens

    发明人： Guy Rosalia Eugene Van Lommen ,  Marcel Frans Leopold De Bruyn ,  Walter Jacobus Joseph Janssens

    IPC分类号： C07C279/00 ,  C07D307/78 ,  A61K31/34 ,  A61K31/343 ,  A61K31/35 ,  A61K31/352 ,  A61K31/415 ,  A61K31/443 ,  A61K31/445 ,  A61K31/505 ,  A61K31/53 ,  A61P9/00 ,  A61P9/02 ,  A61P25/04 ,  C07C277/00 ,  C07D307/81 ,  C07D311/58 ,  C07D319/08 ,  C07D319/20 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D403/02 ,  C07D403/14

    CPC分类号： C07D405/12 ,  C07D307/81 ,  C07D311/58 ,  C07D319/20 ,  C07D405/14

    摘要： The present invention is concerned with vasoconstricive �(benzodioxan, benzofuran or benzopyran)alkylamino!alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is a bivalent C.sub.1-3 alkanediyl radical; A is a bivalent radical of formula: ##STR2## wherein each R.sup.5 is hydrogen or C.sub.1-4 alkyl; wherein each R.sup.6 is hydrogen or C.sub.1-4 alkyl; Alk.sup.2 is C.sub.2-15 alkanediyl or C.sub.5-7 cycloalkanediyl; and each p is 0, 1 or 2; provided that �2-�(2,3- dihydro-1,4-benzodioxin-2-yl)methyl!amino!ethyl guanidine is excluded. Pharmaceuticals which are useful as vasoconstrictors. Compositions comprising said guanidine derivatives as active ingredients, processes for preparing said guanidine derivatives and novel N-cyano guanidine, intermediates; and a use as a medicine are described.

    摘要翻译： 本发明涉及具有下式的[（苯并二恶烷，苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍，（I）其药学上可接受的酸加成盐及其立体化学异构形式，其中X是O，CH 2 或直接债券; R1是氢或C1-6烷基; R2是氢，C1-6烷基，C3-6烯基或C3-6炔基; R3是氢或C1-6烷基; 或者R 2和R 3可以一起形成式 - （CH 2）m - 的二价基团，其中m为4或5; 或R 1和R 2一起形成式-CH = CH-或式 - （CH 2）n - 的二价基团，其中n为2,3或4; 或者当R 1和R 2一起形成式-CH = CH-CH =，-CH = CH-N =或-CH = N-CH =的二价基团时，R 3可以表示键。 R4是氢或C1-6烷基; Alk1是二价C 1-3烷二基; （a）其中每个R 5为氢或C 1-4烷基;（e）其中每个R 5为氢或C 1-4烷基;（c） 其中每个R 6是氢或C 1-4烷基; Alk2是C2-15烷二基或C5-7环烷​​二基; 每个p为0,1或2; 条件是排除[2 - [（2,3-二氢-1,4-苯并二恶英-2-基）甲基]氨基]乙基胍。 可用作血管收缩药物的药物。 包含所述胍衍生物作为活性成分的组合物，制备所述胍衍生物的方法和新的N-氰基胍，中间体; 并描述了作为药物的用途。

    (Benzodioxan, benzofuran or benzopyran) derivatives having fundic relaxation properties
    9.
    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。