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    Derivatives of 4-(2-amino -1-hydroxyethyl)phenol as agonists of the Beta2 adrenergic receptor
    4.
    发明申请
    Derivatives of 4-(2-amino -1-hydroxyethyl)phenol as agonists of the Beta2 adrenergic receptor 有权
    4-（2-氨基-1-羟乙基）苯酚的衍生物作为β2肾上腺素能受体的激动剂

    公开(公告)号：US20090042933A1

    公开(公告)日：2009-02-12

    申请号：US11920561

    申请日：2006-05-17

    申请人： Carlos Puig Duran ,  Maria Isabel Crespo Crespo ,  Julio Cesar Castro Palomino Laria ,  Silvia Gual Roig ,  Eloisa Navarro Romero

    发明人： Carlos Puig Duran ,  Maria Isabel Crespo Crespo ,  Julio Cesar Castro Palomino Laria ,  Silvia Gual Roig ,  Eloisa Navarro Romero

    IPC分类号： A61K31/4704 ,  C07C215/20 ,  C07D215/22 ,  A61P25/00 ,  A61P29/00 ,  A61P27/06 ,  A61P9/00 ,  A61K31/135

    CPC分类号： C07D233/74 ,  C07C217/10 ,  C07C217/26 ,  C07C233/43 ,  C07C275/32 ,  C07D215/26

    摘要： A compound of formula (I) or a pharmaceutically-acceptable salt, solvate or stereoisomer thereof wherein R1 is a group chosen from —CH2OH and —NHC(O)H; R2 is a hydrogen atom or R1 together with R2 form the group —NH—C(O)—CH═CH—, wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R1 and the carbon atom is bound to the carbon atom in the phenyl ring holding R2; R3 is chosen from a hydrogen atom, a halogen atom and groups chosen from —SO—R5, —SO2—R5, —NH—CO—NH2, —CO—NH2, hydantoino, C1-4alkyl, C1-4alkoxy and —SO2NR5R6; R4 is chosen from a hydrogen atom, a halogen atom and a C1-4 alkyl group; R5 is chosen from a C1-4 alkyl group and a C3-8 cycloalkyl group; R6 is independently chosen from a hydrogen atom and a C1-4 alkyl group; n, p and q are independently 0, 1, 2, 3 or 4; m and s are independently 0, 1, 2 or 3; and r is 0, 1 or 2 with the provisos that at least one of m and r is not 0, the sum n+m+p+q+r+s is 7, 8, 9, 10, 11, 12 or 13, and the sum q+r+s is 2, 3, 4, 5 or 6.

    摘要翻译： 式（I）化合物或其药学上可接受的盐，溶剂合物或立体异构体，其中R 1是选自-CH 2 OH和-NHC（O）H的基团; R2是氢原子或R1与R2一起形成-NH-C（O）-CH-CH-基团，其中氮原子与保护R1的苯基中的碳原子结合，并且碳原子与 保护R2的苯环中的碳原子; R3选自氢原子，卤素原子和选自-SO-R5，-SO2-R5，-NH-CO-NH2，-CO-NH2，乙酰氧基，C1-4烷基，C1-4烷氧基和-SO2NR5R6的基团; R 4选自氢原子，卤素原子和C 1-4烷基; R5选自C 1-4烷基和C 3-8环烷基; R6独立地选自氢原子和C1-4烷基; n，p和q独立地为0,1,2,3或4; m和s独立地为0,1,2或3; 并且r为0,1或2，条件是m和r中的至少一个不为0，则和n + m + p + q + r + s为7,8,9,10,11,12或13 ，并且和q + r + s为2,3,4,5或6。

    DERIVATIVES OF 4-(2-AMINO-1-HYDROXYETHYL)PHENOL AS AGONISTS OF THE BETA2 ADRENERGIC RECEPTOR
    6.
    发明申请
    DERIVATIVES OF 4-(2-AMINO-1-HYDROXYETHYL)PHENOL AS AGONISTS OF THE BETA2 ADRENERGIC RECEPTOR 有权
    4-（2-氨基-1-羟基乙基）苯酚的衍生物作为BETA2 ADRENERGIC受体的激动剂

    公开(公告)号：US20110251166A1

    公开(公告)日：2011-10-13

    申请号：US13094163

    申请日：2011-04-26

    申请人： Carlos PUIG DURAN ,  Maria Isabel Crespo Crespo ,  Julio Cesar Castro Palomino Laria ,  Silvia Gual Roig ,  Eloisa Navarro Romero

    发明人： Carlos PUIG DURAN ,  Maria Isabel Crespo Crespo ,  Julio Cesar Castro Palomino Laria ,  Silvia Gual Roig ,  Eloisa Navarro Romero

    IPC分类号： A61K31/56 ,  A61K31/4704 ,  A61K31/17 ,  A61K31/4166 ,  A61P29/00 ,  A61P11/00 ,  A61P15/06 ,  A61P27/06 ,  A61P25/00 ,  A61P9/00 ,  A61K31/138 ,  A61K31/167

    CPC分类号： C07D233/74 ,  C07C217/10 ,  C07C217/26 ,  C07C233/43 ,  C07C275/32 ,  C07D215/26

    摘要： The present invention provides a compound of formula (I) wherein: R1 is a group selected from —CH2OH, —NHC(O)H and R7 is a hydrogen atom; or R1 together with R2 form the group —NH—C(O)—CH═CH— wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R1 and the carbon atom is bound to the carbon is atom in the phenyl ring holding R2; R3 is selected from hydrogen and halogen atoms or groups selected from —SO—R5, —SO2—R5, —NH—CO—NH2, —CO—NH2, hydantoino, C1-4alkyl, C1-4alkoxy and —SO2NR5R6; R4 is selected from hydrogen atoms, halogen atoms and C1-4alkyl groups; R5 is a C1-4alkyl group or C3-5 cycloalkyl; R6 is independently selected from hydrogen atoms and C1-4alkyl groups; n, p and q are independently 0, 1, 2, 3 or 4: m and s are independently 0, 1, 2 or 3; r is 0, 1 or 2; with the provisos that: at least one of m and r is not 0; the sum n+m+p+q+r+s is 7, 8, 9, 10, 11, 12 or 13: the sum q+r+s is 2, 3, 4, 5 or 6 or a pharmaceutically-acceptable salt, solvate or stereoisomer thereof.

    摘要翻译： 本发明提供式（I）化合物，其中：R 1为选自-CH 2 OH，-NHC（O）H，R 7为氢原子的基团; 或R 1与R 2一起形成基团-NH-C（O）-CH = CH-，其中氮原子与保护R 1的苯基中的碳原子结合，并且碳原子与碳结合是苯基中的原子 环持R2; R3选自氢和选自-SO-R5，-SO2-R5，-NH-CO-NH2，-CO-NH2，乙酰氧基，C1-4烷基，C1-4烷氧基和-SO2NR5R6的卤素原子或基团; R 4选自氢原子，卤素原子和C 1-4烷基; R5是C1-4烷基或C3-5环烷基; R 6独立地选自氢原子和C 1-4烷基; n，p和q独立地为0,1,2,3或4：m，s独立地为0,1,2或3; r为0,1或2; 条件是：m和r中的至少一个不为0; 总和n + m + p + q + r + s为7,8,9,10,11,12或13：和q + r + s为2,3,4,5或6或药学上可接受的 盐，溶剂合物或立体异构体。

    Derivatives of 4-(2-amino-1-hydroxyethyl)phenol as agonists of the β2 adrenergic receptor
    7.
    发明授权
    Derivatives of 4-(2-amino-1-hydroxyethyl)phenol as agonists of the β2 adrenergic receptor 有权
    4-（2-氨基-1-羟乙基）苯酚的衍生物作为二肾上腺素能受体的激动剂

    公开(公告)号：US07964615B2

    公开(公告)日：2011-06-21

    申请号：US11920561

    申请日：2006-05-17

    申请人： Carlos Puig Duran ,  Maria Isabel Crespo Crespo ,  Julio Cesar Castro Palomino Laria ,  Silvia Gual Roig ,  Eloisa Navarro Romero

    发明人： Carlos Puig Duran ,  Maria Isabel Crespo Crespo ,  Julio Cesar Castro Palomino Laria ,  Silvia Gual Roig ,  Eloisa Navarro Romero

    IPC分类号： A61K31/47 ,  C07D215/00

    CPC分类号： C07D233/74 ,  C07C217/10 ,  C07C217/26 ,  C07C233/43 ,  C07C275/32 ,  C07D215/26

    摘要： A compound of formula (I) or a pharmaceutically-acceptable salt, solvate or stereoisomer thereof wherein R1 is a group chosen from —CH2OH and —NHC(O)H; R2 is a hydrogen atom or R1 together with R2 form the group —NH—C(O)—CH═CH—, wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R1 and the carbon atom is bound to the carbon atom in the phenyl ring holding R2; R3 is chosen from a hydrogen atom, a halogen atom and groups chosen from —SO—R5, —SO2—R5, —NH—CO—NH2, —CO—NH2, hydantoino, C1-4alkyl, C1-4alkoxy and —SO2NR5R6; R4 is chosen from a hydrogen atom, a halogen atom and a C1-4 alkyl group; R5 is chosen from a C1-4 alkyl group and a C3-8 cycloalkyl group; R6 is independently chosen from a hydrogen atom and a C1-4 alkyl group; n, p and q are independently 0, 1, 2, 3 or 4; m and s are independently 0, 1, 2 or 3; and r is 0, 1 or 2 with the provisos that at least one of m and r is not 0, the sum n+m+p+q+r+s is 7, 8, 9, 10, 11, 12 or 13, and the sum q+r+s is 2, 3, 4, 5 or 6.

    摘要翻译： 式（I）化合物或其药学上可接受的盐，溶剂合物或立体异构体，其中R 1是选自-CH 2 OH和-NHC（O）H的基团; R2是氢原子或R1与R2一起形成-NH-C（O）-CH = CH-基团，其中氮原子与保护R1的苯基中的碳原子结合，并且碳原子与 保护R2的苯环中的碳原子; R3选自氢原子，卤素原子和选自-SO-R5，-SO2-R5，-NH-CO-NH2，-CO-NH2，乙酰氧基，C1-4烷基，C1-4烷氧基和-SO2NR5R6的基团; R4选自氢原子，卤素原子和C1-4烷基; R5选自C 1-4烷基和C 3-8环烷基; R6独立地选自氢原子和C1-4烷基; n，p和q独立地为0,1,2,3或4; m和s独立地为0,1,2或3; 并且r为0,1或2，条件是m和r中的至少一个不为0，则和n + m + p + q + r + s为7,8,9,10,11,12或13 ，并且和q + r + s为2,3,4,5或6。