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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 失效

    公开(公告)号：US20070099953A1

    公开(公告)日：2007-05-03

    申请号：US11636181

    申请日：2006-12-08

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

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

    IPC分类号： A61K31/4745 ,  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： A compound according to formula (I) wherein: Ĉ 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).

    Novel quinuclidine derivatives and medicinal compositions containing the same
    2.
    发明申请
    Novel quinuclidine derivatives and medicinal compositions containing the same 失效

    公开(公告)号：US20070129398A1

    公开(公告)日：2007-06-07

    申请号：US11515335

    申请日：2006-08-31

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

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

    IPC分类号： A61K31/4745 ,  A61K31/407 ,  A61K31/4178 ,  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)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.

    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：US20060106055A1

    公开(公告)日：2006-05-18

    申请号：US11324919

    申请日：2006-01-04

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

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

    IPC分类号： C07D453/04 ,  A61K31/4745

    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).

    Novel quinuclidine derivatives and medicinal compositions containing the same
    4.
    发明申请
    Novel quinuclidine derivatives and medicinal compositions containing the same 有权

    公开(公告)号：US20060106056A1

    公开(公告)日：2006-05-18

    申请号：US11325059

    申请日：2006-01-03

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

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

    IPC分类号： C07D453/02 ,  A61K31/4745

    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, —NR4R51—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).

    Novel quinuclidine derivatives and medicinal compositions containing the same
    5.
    发明申请
    Novel quinuclidine derivatives and medicinal compositions containing the same 失效

    公开(公告)号：US20070105897A1

    公开(公告)日：2007-05-10

    申请号：US11514590

    申请日：2006-08-31

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

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

    IPC分类号： A61K31/4745 ,  A61K31/407 ,  C07D453/02 ,  C07D487/02

    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 carbamate derivatives and their use as M3 antagonists
    7.
    发明申请
    Quinuclidine carbamate derivatives and their use as M3 antagonists 失效
    奎宁环氨基甲酸酯衍生物及其作为M3拮抗剂的用途

    公开(公告)号：US20080021060A1

    公开(公告)日：2008-01-24

    申请号：US11806927

    申请日：2007-06-05

    申请人： Maria Buil Albero ,  Maria Fernandez Forner ,  Maria Quinones

    发明人： Maria Buil Albero ,  Maria Fernandez Forner ,  Maria Quinones

    IPC分类号： A61K31/439 ,  A61P1/00 ,  A61P11/00 ,  A61P13/00 ,  C07D453/02

    CPC分类号： C07D471/08 ,  C07D453/02

    摘要： A carbamate of formula (I), wherein R1 represents wherein R2 represents a benzyl, phenethyl, furan-2-ylmethyl, furan-3-ylmethyl, thiophen-2-ylmethyl or thiophen-3-ylmethyl group or a straight or branched alkyl group having 3 or 8 carbon atoms, an alkenyl group having 3 to 8 carbon atoms, or a cycloalkyl group of 3 to 6 carbon atoms; p is 1 or 2 and the substitution in the azoniabicylic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; or a pharmaceutically acceptable salt thereof. The pharmaceutically acceptable salt may be of formula (II).

    摘要翻译： 式（I）的氨基甲酸酯，其中R 1表示其中R 2表示苄基，苯乙基，呋喃-2-基甲基，呋喃-3-基甲基，噻吩-2-基甲基或噻吩-3-基甲基或直链或支链烷基 具有3或8个碳原子，具有3至8个碳原子的烯基或3至6个碳原子的环烷基; p是1或2，并且在氮杂烷环中的取代可以在2,3或4位，包括不对称碳的所有可能的构型; 或其药学上可接受的盐。 药学上可接受的盐可以是式（II）。

    Novel quinuclidine derivatives and medicinal compositions containing the same
    8.
    发明申请
    Novel quinuclidine derivatives and medicinal compositions containing the same 有权

    公开(公告)号：US20050209272A1

    公开(公告)日：2005-09-22

    申请号：US11116777

    申请日：2005-04-28

    申请人： Maria Fernandez Forner ,  Maria Quinones ,  Maria Buil Albero

    发明人： Maria Fernandez Forner ,  Maria Quinones ,  Maria Buil Albero

    IPC分类号： A61K31/435 ,  A61K31/439 ,  A61K31/4745 ,  A61P1/00 ,  A61P1/04 ,  A61P1/06 ,  A61P1/12 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P11/08 ,  A61P11/14 ,  A61P13/00 ,  A61P13/02 ,  A61P13/06 ,  A61P13/10 ,  A61P27/16 ,  A61P43/00 ,  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： A compound according to formula (I) wherein: {circle over (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).