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    DERIVATIVES OF 4-(2-AMINO-1-HYDROXYETHYL)PHENOL AS AGONISTS OF THE β2 ADRENERGIC RECEPTOR
    2.
    发明申请
    DERIVATIVES OF 4-(2-AMINO-1-HYDROXYETHYL)PHENOL AS AGONISTS OF THE β2 ADRENERGIC RECEPTOR 审中-公开
    4-（2-氨基-1-羟基乙基）酚的衍生物作为β2受体受体的激动剂

    公开(公告)号：WO2008046598A1

    公开(公告)日：2008-04-24

    申请号：PCT/EP2007/008992

    申请日：2007-10-17

    Applicant: LABORATORIOS ALMIRALL, S.A. ,  BACH TANA, Jordi ,  CRESPO CRESPO, Maria, Isabel ,  PUIG DURAN, Carlos ,  GUAL ROIG, Silvia ,  ORTEGA MUÑOZ, Albert

    Inventor： BACH TANA, Jordi ,  CRESPO CRESPO, Maria, Isabel ,  PUIG DURAN, Carlos ,  GUAL ROIG, Silvia ,  ORTEGA MUÑOZ, Albert

    IPC: C07D215/22 ,  C07C217/60 ,  A61K31/435 ,  A61K31/137 ,  A61P9/00 ,  A61P11/06 ,  A61P29/00 ,  A61P27/06

    CPC classification number: C07D215/227 ,  A61K31/137 ,  A61K31/167 ,  A61K31/4704 ,  A61K31/573 ,  A61K45/06 ,  C07C217/60 ,  C07C233/43

    Abstract: The present invention provides a Compound of formula (I), wherein: R 1 is a group selected from -CH 2 OH,-NH(CO)H; and R 2 is a hydrogen atom; or R 1 together with R 2 form the group -NH-C(O)-CH=CH-, wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R 1 and the carbon atom is bound to the carbon atom in the phenyl ring holding R 2 ; R 3a and R 3b are independently selected from the group consisting of hydrogen atoms and C 1-4 alkyl groups; X and Y are independently selected from the group consisting of direct bond and oxygen atom; n, m and q each independently has a value selected from 0, 1, 2 and 3; p has a value selected from 1, 2 and 3; R 4 and R 5 are independently selected from hydrogen atoms, halogen atoms, C 1-4 alkyl, C 1-4 alkoxy, -CONH 2 , -NHCONH 2 , -SR 7 , -SOR 7 , -SO 2 R 7 , -SO 2 NHR 8 and the groups (a) and (b), wherein R 7 is selected from C 1-4 alkyl and C 3-8 cycloalkyl and R 8 is selected from hydrogen atoms and C 1-4 alkyl groups; R 6 is selected from the group consisting of hydrogen atoms, halogen atoms, C 1-4 alkyl and C 1-4 alkoxy or a pharmaceutically-acceptable salt, solvate or stereoisomer thereof.

    Abstract translation: 本发明提供式（I）的化合物，其中：R 1是选自-CH 2 OH，-NH（CO）H; R 2是氢原子; 或R 1与R 2一起形成基团-NH-C（O）-CH = CH-，其中氮原子与苯基中的碳原子结合 环保持R 1，并且碳原子与保持R 2的苯环中的碳原子结合; R 3a和 R 3b独立地选自氢原子和C 1-4烷基; X和Y独立地选自直接键和氧原子; n，m和q各自独立地具有选自0,1,2和3的值; p具有选自1,2和3的值; R 4和R 5独立地选自氢原子，卤素原子，C 1-4烷基，C 1-4烷基， 烷氧基，-CONH 2，-NHCONH 2，-SR 7，-SOR 7， - SO 2，N 2，NH 2，和（b），其中（a）和（b） R 7选自C 1-4烷基和C 3-8环烷基，R 8选自： 氢原子和C 1-4烷基; R 6选自氢原子，卤素原子，C 1-4烷基和C 1-4烷氧基或药学上可接受的盐 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 ß2 ADRENERGIC RECEPTOR
    3.
    发明申请
    DERIVATIVES OF 4-(2-AMINO-1-HYDROXYETHYL)PHENOL AS AGONISTS OF THE ß2 ADRENERGIC RECEPTOR 审中-公开
    4-（2-氨基-1-羟基乙基）酚的衍生物作为β2受体受体的激动剂

    公开(公告)号：WO2008046598A8

    公开(公告)日：2009-04-30

    申请号：PCT/EP2007008992

    申请日：2007-10-17

    Applicant: ALMIRALL LAB ,  BACH TANA JORDI ,  CRESPO CRESPO MARIA ISABEL ,  PUIG DURAN CARLOS ,  GUAL ROIG SILVIA ,  ORTEGA MUNOZ ALBERTO

    Inventor： BACH TANA JORDI ,  CRESPO CRESPO MARIA ISABEL ,  PUIG DURAN CARLOS ,  GUAL ROIG SILVIA ,  ORTEGA MUNOZ ALBERTO

    IPC: C07D215/22 ,  A61K31/137 ,  A61K31/435 ,  A61P9/00 ,  A61P11/06 ,  A61P27/06 ,  A61P29/00 ,  C07C217/60

    CPC classification number: C07D215/227 ,  A61K31/137 ,  A61K31/167 ,  A61K31/4704 ,  A61K31/573 ,  A61K45/06 ,  C07C217/60 ,  C07C233/43

    Abstract: The present invention provides a Compound of formula (I), wherein: R1 is a group selected from -CH2OH,-NH(CO)H; and 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;R3a and R3b are independently selected from the group consisting of hydrogen atoms and C1-4 alkyl groups; X and Y are independently selected from the group consisting of direct bond and oxygen atom; n, m and q each independently has a value selected from 0, 1, 2 and 3; p has a value selected from 1, 2 and 3; R4 and R5 are independently selected from hydrogen atoms, halogen atoms, C1-4 alkyl, C1-4 alkoxy, -CONH2, -NHCONH2, -SR7, -SOR7, -SO2R7, -SO2NHR8 and the groups (a) and (b), wherein R7 is selected from C1-4alkyl and C3-8 cycloalkyl and R8 is selected from hydrogen atoms and C1-4alkyl groups; R6 is selected from the group consisting of hydrogen atoms, halogen atoms, C1-4 alkyl and C1-4 alkoxy or a pharmaceutically-acceptable salt, solvate or stereoisomer thereof.

    Abstract translation: 本发明提供式（I）的化合物，其中：R 1是选自-CH 2 OH，-NH（CO）H; R2为氢原子; 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，并且碳原子与苯基中的碳原子结合 环保持R2; R3a和R3b独立地选自氢原子和C1-4烷基; X和Y独立地选自直接键和氧原子; n，m和q各自独立地具有选自0,1,2和3的值; p具有选自1,2和3的值; R 4和R 5独立地选自氢原子，卤素原子，C 1-4烷基，C 1-4烷氧基，-CONH 2，-NHCONH 2，-SR 7，-SOR 7，-SO 2 R 7，-SO 2 NHR 8和（a）和（b） 其中R 7选自C 1-4烷基和C 3-8环烷基，R 8选自氢原子和C 1-4烷基; R 6选自氢原子，卤素原子，C 1-4烷基和C 1-4烷氧基或其药学上可接受的盐，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
    4.
    发明申请
    DERIVATIVES OF 4-(2-AMINO-1-HYDROXYETHYL)PHENOL AS AGONISTS OF THE β2 ADRENERGIC RECEPTOR 审中-公开
    4-（2-氨基-1-羟基乙基）酚的衍生物作为β2受体受体的激动剂

    公开(公告)号：WO2006122788A1

    公开(公告)日：2006-11-23

    申请号：PCT/EP2006/004680

    申请日：2006-05-17

    Applicant: ALMIRALL PRODESFARMA S.A. ,  PUIG DURAN, Carlos ,  CRESPO CRESPO, Maria, Isabel ,  CASTRO PALOMINO LARIA, Julio, Cesar ,  GUAL ROIG, Silvia ,  NAVARRO ROMERO, Eloisa

    Inventor： PUIG DURAN, Carlos ,  CRESPO CRESPO, Maria, Isabel ,  CASTRO PALOMINO LARIA, Julio, Cesar ,  GUAL ROIG, Silvia ,  NAVARRO ROMERO, Eloisa

    IPC: C07C217/10 ,  C07C217/26 ,  C07C233/43 ,  C07C275/32 ,  C07D215/26 ,  C07D233/74 ,  A61K31/135 ,  A61K31/415 ,  A61K31/47 ,  A61P11/00

    CPC classification number: C07D233/74 ,  C07C217/10 ,  C07C217/26 ,  C07C233/43 ,  C07C275/32 ,  C07D215/26

    Abstract: The present invention provides a compound of formula (I) wherein: R 1 is a group selected from -CH 2 OH, -NHC(O)H and R 2 is a hydrogen atom; or R 1 together with R 2 form the group -NH-C(O)-CH=CH- wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R 1 and the carbon atom is bound to the carbon atom in the phenyl ring holding R 2 ; R 3 is selected from hydrogen and halogen atoms or groups selected from -SO-R 5 , -SO 2 - R 5 , -NH-CO-NH 2 , -CO-NH 2 , hydantoino, C 1-4 alkyl, C 1-4 alkoxy and -SO 2 NR 5 R 6 ; R 4 is selected from hydrogen atoms, halogen atoms and C 1-4 alkyl groups; R 5 is a C 1-4 alkyl group or C 3-8 cycloalkyl; R 6 is independently selected from hydrogen atoms and C 1-4 alkyl 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.

    Abstract translation: 本发明提供式（I）化合物，其中：R 1是选自-CH 2 OH，-NHC（O）H和R“ 2是氢原子; 或R 1与R 2一起形成基团-NH-C（O）-CH = CH-，其中氮原子与苯环中的碳原子结合 保持R 1，并且碳原子与保持R 2的苯基中的碳原子结合; R 3选自氢和选自-SO-R 5，-SO 2 R 5的卤素原子或基团， ，-NH-CO-NH 2，-CO-NH 2，乙酰氧基，C 1-4烷基，C 1-4烷氧基和-SO 2 NR 5 R 6; R 4选自氢原子，卤素原子和C 1-4烷基; R 5是C 1-4烷基或C 3-8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和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; 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或其药学上可接受的盐，溶剂合物或立体异构体。

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