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    NOVEL QUINUCLIDINE DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME
    1.
    发明申请
    NOVEL QUINUCLIDINE DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME 有权

    公开(公告)号：US20150246026A1

    公开(公告)日：2015-09-03

    申请号：US14712866

    申请日：2015-05-14

    Applicant: ALMIRALL, S.A.

    Inventor： Maria Dolors FERNANDEZ FORNER ,  Maria PRAT QUINONES ,  Maria Antonia BUIL ALBERO

    IPC: A61K31/439 ,  A61K9/00 ,  A61K31/56 ,  A61K47/26 ,  A61K45/06

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

    Abstract: A compound according to formula (I) wherein z© 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—, —CR6122—, —CO—, —O—, —S—, —S(O)—, SO2 or NR6— group, wherein R6 and R2 each independently represent a hydrogen atom, straight or branched lower alkyl group, or R6 and 122 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 formulae (a), (b), (c), (d) and 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).

    NOVEL QUINUCLIDINE DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME
    5.
    发明申请
    NOVEL QUINUCLIDINE DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME 有权

    公开(公告)号：US20140303126A1

    公开(公告)日：2014-10-09

    申请号：US14311102

    申请日：2014-06-20

    Applicant: ALMIRALL, S.A.

    Inventor： Maria Dolors FERNANDEZ FORNER ,  Maria PRAT QUINONES ,  Maria Antonia BUIL ALBERO

    IPC: C07D453/02 ,  A61K45/06 ,  A61K31/439

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

    Abstract: A compound according to formula (I) wherein z© 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; in 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 formulae (a), (b), (c), (d) and 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).

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