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    NOVEL QUINUCLIDINE DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME
    3.
    发明申请
    NOVEL QUINUCLIDINE DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME 有权

    公开(公告)号：US20100234333A1

    公开(公告)日：2010-09-16

    申请号：US12787772

    申请日：2010-05-26

    申请人： Maria Dolors Fernandez Forner ,  Maria Prat Quiñones ,  Maria Antonia Buil Albero

    发明人： Maria Dolors Fernandez Forner ,  Maria Prat Quiñones ,  Maria Antonia Buil Albero

    IPC分类号： A61K31/56 ,  A61P11/06 ,  A61P11/08 ,  A61P11/02

    CPC分类号： A61K31/439 ,  A61K9/0073 ,  A61K9/0075 ,  A61K31/4745 ,  A61K31/56 ,  A61K45/06 ,  A61K47/26 ,  C07D453/02 ,  Y10S514/826 ,  A61K2300/00

    摘要： A compound according to formula (I) wherein: {circle around (C)} is a phenyl ring, a C4 to C9 heteroaromatic compound containing one or more heteroatoms, or a naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl or biphenyl group; R1, R2 and R3 each independently represent a hydrogen or halogen atom, or a hydroxy group, or a phenyl, —OR4, —SR4, —NR4R5, —NHCOR4, —CONR4R5, —CN, —NO2, —COOR4 or —CF3 group, or a straight or branched lower alkyl group which may optionally be substituted, for example, with a hydroxy or alcoxy group, wherein R4 and R5 each independently represent a hydrogen atom, straight or branched lower alkyl group, or together form an alicyclic ring; or R1 and R2 together form an aromatic, alicyclic or heterocyclic ring; n is an integer from 0 to 4; A represents a —CH2—, —CH═CR6, —CR6═CH—, —CR6R7—, —CO—, —O—, —S—, —S(O)—, SO2 or —NR6— group, wherein R6 and R7 each independently represent a hydrogen atom, straight or branched lower alkyl group, or R6 and R7 together form an alicyclic ring; m is an integer from 0 to 8; provided that when m=0, A is not —CH2—; p is an integer from 1 to 2 and the substitution in the azoniabicyclic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; B represents a group of formula i) or ii): wherein R10 represents a hydrogen atom, a hydroxy or methyl group; and R8 and R9 each independently represents wherein R11 represents a hydrogen or halogen atom, or a straight or branched lower alkyl group and Q represents a single bond, —CH2—, —CH2—CH2—, —O—, —O—CH2—, —S—, —S—CH2— or —CH═CH—, and when i) or ii) contain a chiral centre they may represent either configuration; X represents a pharmaceutically acceptable anion of a mono or polyvalent acid, which shows high affinity for muscarinic M3 receptors (Hm3).

    Quinuclidine derivatives and medicinal compositions containing the same
    7.
    发明授权
    Quinuclidine derivatives and medicinal compositions containing the same 失效

    公开(公告)号：US07122558B2

    公开(公告)日：2006-10-17

    申请号：US10250447

    申请日：2001-12-20

    申请人： Maria Prat Quinones ,  Maria Dolors Fernandez Forner ,  Maria Antonia Buil Albero

    发明人： Maria Prat Quinones ,  Maria Dolors Fernandez Forner ,  Maria Antonia Buil Albero

    IPC分类号： A61K31/46 ,  C07D453/02

    CPC分类号： C07D453/02

    摘要： A compound of formula (I), wherein B is a phenyl ring, a 5 to 10 membered heteroaromatic group containing one or more heteroatoms, or a naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl, benzo[1,3]dioxolyl, or biphenyl group; R1, R2 and R3 each independently represent a hydrogen or halogen atom, or a hydroxy group, a phenyl group, —OR7, —SR7, —NR7R8, —NHCOR7, —CONR7R8, —CN, —NO2, —COOR7 or CF3 group, or a strait or branched, substituted or unsubstituted lower alkyl group, wherein R7 and R8 each independently represent a hydrogen atom, a straight or branched lower alkyl group, or together form an alicyclic ring; or R1 and R2 together form an aromatic or alicyclic ring or a heterocyclic group. n is an integer from 0 to 4; A represents a group selected from —CH2—, —CH═CR9—, —CR9═CH—, —CR9R10—, —CO—, —O—, —S—, —S(O)—, —S(O)2— and NR9, wherein R9 and R10 each independently represent a hydrogen atom, a straight or branched lower alkyl group, or together form an alicyclic ring; m is an integer from 0 to 8, provided that when m=0, A is not —CH2—; p is an integer from 1 to 2 and the substitution in the azonia bicyclic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; R4 represents a group of structure: (Formulae II) wherein R11 represents a hydrogen or halogen atom, a hydroxy group, an alkoxy group, a nitro group, a cyano group, —CO2R12 or —NR12R13, wherein R12 and R13 are identical or different and are selected from hydrogen and straight or branched lower alkyl groups, or a straight or branched, substituted or unsubstituted lower alkyl group; R5 represents an alkyl group of 1 to 7 carbon atoms, an alkenyl group containing 2 to 7 carbon atoms, or a group of formula (III) wherein q=1 or 2 and R11 iss a defined above; R6 represents a hydrogen atom, a hydroxy group, a methyl group or a —CH2OH group; and X− represents a pharmaceutically acceptable anion of a mono or polyvalent acid .

    Quinuclidine derivatives and medicinal compositions containing the same
    8.
    发明授权
    Quinuclidine derivatives and medicinal compositions containing the same 有权
    奎宁环衍生物和含有它们的药物组合物

    公开(公告)号：US07109210B2

    公开(公告)日：2006-09-19

    申请号：US10740264

    申请日：2003-12-17

    申请人： Maria Dolors Fernandez Forner ,  Maria Prat Quiñones ,  Maria Antonia Buil Albero

    发明人： Maria Dolors Fernandez Forner ,  Maria Prat Quiñones ,  Maria Antonia Buil Albero

    IPC分类号： A61K31/439 ,  C07D453/02

    CPC分类号： A61K31/439 ,  A61K9/0073 ,  A61K9/0075 ,  A61K31/4745 ,  A61K31/56 ,  A61K45/06 ,  A61K47/26 ,  C07D453/02 ,  Y10S514/826 ,  A61K2300/00

    摘要： Compounds of the formula wherein: {circle around (C)} is phenyl, C4 to C9 heteroaromatic, naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl or biphenyl; R1, R2 and R3 are hydrogen or a substituent; n is 0 to 4; A represents —CH2—, —CH═CR6, —CR6═CH—, —CR6R7—, —CO—, —O—, —S—, —S(O)—, SO2 or —NR6—, wherein R6 and R7 are hydrogen or lower alkyl, or R6 and R7 together form an alicyclic ring; m is 0 to 8; (when m=0, A is not —CH2—); p is 1 or 2; B represents a group of the formula ii): wherein R10 is hydrogen, hydroxy or methyl; and Q represents a single bond, —CH2—, —CH2—CH2—, —O—, —O—CH2—, —S—, —S—CH2— or —CH═CH—, and x represents an anion and wherein the compounds show high affinity for muscarinic M3 receptors (Hm3).

    摘要翻译： 下式的化合物其中：{环绕（C为苯基，C 4至C 9 - 杂芳基，萘基，5,6,7,8-四氢萘基或联苯基; R R 1，R 2和R 3是氢或取代基; n是0-4; A代表-CH 2， CH 3，-CH-CR 6，-CR 6 -CH-，-CR 6，R 7， - ， - CO - ， - O - ， - S - ， - S（O） - ，SO 2 - 或-NR 6 - ，其中R 6， R 1和R 2分别为氢或低级烷基，或R 6和R 7一起形成脂环族; m为0至8 ;（当m = 0时，A不是-CH 2 - ）; p为1或2; B表示式II）的基团：其中R 10为 氢，羟基或甲基; 且Q表示单键，-CH 2 - ， - CH 2 -CH 2 - ， - O - ， - O-CH -S-，-S-CH 2 - 或-CH-CH-，x表示阴离子，并且其中所述化合物对毒蕈碱M 3受体（Hm3）。