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公开(公告)号：US20070099953A1
公开(公告)日：2007-05-03
申请号：US11636181
申请日：2006-12-08
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).
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公开(公告)号：US20060106056A1
公开(公告)日：2006-05-18
申请号：US11325059
申请日：2006-01-03
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).
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公开(公告)号：US20050282875A1
公开(公告)日：2005-12-22
申请号：US10510680
申请日：2003-04-11
IPC分类号： A61P1/00 , A61P11/00 , A61P13/10 , C07D207/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14 , A61K31/428 , A61K31/4025 , A61K31/4178 , C07D417/02 , C07D47/02
CPC分类号： C07D409/14 , C07D207/12 , C07D405/12 , C07D405/14 , C07D417/14
摘要： New pyrrolidinium derivatives having the chemical structure of general formula (I) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as antagonists of M3 muscarinic receptors.
摘要翻译： 公开了具有通式（I）化学结构的新的吡咯烷鎓衍生物; 以及其制备方法，包含它们的药物组合物及其在治疗中作为M3毒蕈碱受体的拮抗剂的用途。
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公开(公告)号：US20070129398A1
公开(公告)日：2007-06-07
申请号：US11515335
申请日：2006-08-31
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.
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公开(公告)号：US20060106055A1
公开(公告)日：2006-05-18
申请号：US11324919
申请日：2006-01-04
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).
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公开(公告)号：US20100234332A1
公开(公告)日：2010-09-16
申请号：US12785345
申请日：2010-05-21
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 is 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.
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公开(公告)号：US20070105897A1
公开(公告)日：2007-05-10
申请号：US11514590
申请日：2006-08-31
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.
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8.发明申请公开(公告)号：US20060094751A1
公开(公告)日：2006-05-04
申请号：US10518496
申请日：2003-06-18
IPC分类号： C07D453/04 , A61K31/4745 , A61K31/407 , C07D453/02 , C07D487/02
CPC分类号： C07D453/02
摘要： Carbamates of formula (I) or pharmaceutically acceptable salts thereof, including quaternary ammonium salts of formula (II) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as antagonists of M3 muscarinic receptors.
摘要翻译： 公开了式（I）的氨基甲酸酯或其药学上可接受的盐，包括式（II）的季铵盐： 以及其制备方法，包含它们的药物组合物及其在治疗中作为M3毒蕈碱受体的拮抗剂的用途。
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9.发明申请公开(公告)号：US20080021060A1
公开(公告)日：2008-01-24
申请号：US11806927
申请日：2007-06-05
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）。
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公开(公告)号：US20050209272A1
公开(公告)日：2005-09-22
申请号：US11116777
申请日：2005-04-28
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).
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