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    • 1. 发明申请
    • Novel quinuclidine derivatives and medicinal compositions containing the same
    • US20070099953A1
    • 2007-05-03
    • US11636181
    • 2006-12-08
    • Maria Fernandez FornerMaria Prat QuinonesMaria Buil Albero
    • Maria Fernandez FornerMaria Prat QuinonesMaria Buil Albero
    • A61K31/4745C07D453/02
    • A61K31/439A61K9/0073A61K9/0075A61K31/4745A61K31/56A61K45/06A61K47/26C07D453/02Y10S514/826A61K2300/00
    • 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).
    • 2. 发明申请
    • Novel quinuclidine derivatives and medicinal compositions containing the same
    • US20070129398A1
    • 2007-06-07
    • US11515335
    • 2006-08-31
    • Maria Prat QuinonesMaria Fernandez FornerMaria Buil Albero
    • Maria Prat QuinonesMaria Fernandez FornerMaria Buil Albero
    • A61K31/4745A61K31/407A61K31/4178C07D453/02
    • C07D453/02
    • 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.
    • 3. 发明申请
    • Novel quinuclidine derivatives and medicinal compositions containing the same
    • US20060106055A1
    • 2006-05-18
    • US11324919
    • 2006-01-04
    • Maria Fernandez FornerMaria Prat QuinonesMaria Buil Albero
    • Maria Fernandez FornerMaria Prat QuinonesMaria Buil Albero
    • C07D453/04A61K31/4745
    • A61K31/439A61K9/0073A61K9/0075A61K31/4745A61K31/56A61K45/06A61K47/26C07D453/02Y10S514/826A61K2300/00
    • 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).
    • 4. 发明申请
    • Novel quinuclidine derivatives and medicinal compositions containing the same
    • US20060106056A1
    • 2006-05-18
    • US11325059
    • 2006-01-03
    • Maria Fernandez FornerMaria Prat QuinonesMaria Buil Albero
    • Maria Fernandez FornerMaria Prat QuinonesMaria Buil Albero
    • C07D453/02A61K31/4745
    • A61K31/439A61K9/0073A61K9/0075A61K31/4745A61K31/56A61K45/06A61K47/26C07D453/02Y10S514/826A61K2300/00
    • 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).
    • 5. 发明申请
    • Novel quinuclidine derivatives and medicinal compositions containing the same
    • US20070105897A1
    • 2007-05-10
    • US11514590
    • 2006-08-31
    • Maria Prat QuinonesMaria Fernandez FornerMaria Buil Albero
    • Maria Prat QuinonesMaria Fernandez FornerMaria Buil Albero
    • A61K31/4745A61K31/407C07D453/02C07D487/02
    • C07D453/02
    • 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.