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    Indole derivatives
    2.
    发明公开
    Indole derivatives 失效
    吲哚衍生物

    公开(公告)号：EP0429257A3

    公开(公告)日：1992-01-29

    申请号：EP90312489.9

    申请日：1990-11-16

    申请人： GLAXO GROUP LIMITED

    发明人： Ross, Barry Clive ,  Middlemiss, David ,  Scopes, David Ian Carter ,  Jack, Torquil Iain Maclean ,  Cardwell, Kevin Stuart ,  Dowle, Michael Dennis

    IPC分类号： C07D403/06 ,  C07D403/14 ,  C07D521/00 ,  A61K31/415 ,  C07D209/30

    CPC分类号： C07D249/08 ,  C07D209/10 ,  C07D209/26 ,  C07D209/30 ,  C07D231/12 ,  C07D233/56 ,  C07D403/06 ,  C07D403/14

    摘要： The invention provides compounds of the general formula (I):

    or a physiologically acceptable salt or a solvate (e.g. hydrates) thereof in which
    R¹ represents a hydrogen atom or a halogen atom or a group selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, fluoroC₁₋₆alkyl, -CHO, -CO₂H or -COR⁴;
    R² represents a hydrogen atom or a halogen atom or the group Ar;
    R³ represents a hydrogen atom or a group selected from C₁₋₆ alkyl, C₃₋₆alkenyl, C₁₋₆alkoxy, -COR⁴, -SO₂R⁴ or the group Ar;
    R⁴ represents a group selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₁₋₆ alkoxy or the group -NR¹²R¹³;
    Ar represents the group

    R⁵ represents a group selected from -CO₂H, -NHSO₂CF₃ or a C-linked tetrazolyl group;
    R⁶ and R⁷ which may be the same or different each independently represent a hydrogen atom or a halogen atom or a C₁₋₆alkyl group; Het represents an N-linked imidazolyl group substituted at the 2-position by a C₁₋₆alkyl, C₂₋₆alkenyl or a C₁₋₆alkylthio group, the imidazolyl group optionally being substituted by one or two further substituents selected from a halogen atom or a group selected from cyano, nitro, C₁₋₆alkyl, C₂₋₆alkenyl, fluoroC₁₋₆alkyl, -(CH₂) m R⁸, -(CH₂) n COR⁹, or -(CH₂) p NR¹⁰COR¹¹;
    or Het represents an N-linked benzimidazolyl group substituted at the 2-position by a C₁₋₆alkyl, C₂₋₆alkenyl or a C₁₋₆alkylthio group;
    R⁸ represents a hydroxy or C₁₋₆alkoxy group;
    R⁹ represents a hydrogen atom or a group selected from hydroxy, C₁₋₆alkyl, C₁₋₆alkoxy, phenyl, phenoxy or the group -NR¹²R¹³;
    R¹⁰ represents a hydrogen atom or a C₁₋₆alkyl group;
    R¹¹ represents a hydrogen atom or a group selected from C₁₋₆alkyl, C₁₋₆alkoxy, phenyl, phenoxy or the group -NR¹²R¹³;
    R¹² and R¹³ which may be the same or different each independently represent a hydrogen atom or a C₁₋₄alkyl group or -NR¹²R¹³ forms a saturated heterocyclic ring which has 5 or 6 ring members and may optionally contain in the ring one oxygen atom;
    m represents an integer from 1 to 4;
    n represents an integer from 0 to 4; and
    p represents an integer from 1 to 4;
    provided that one of R² and R³ represents the group Ar, and that when R² represents the group Ar, R³ represents a hydrogen atom or a group selected from C₁₋₆ alkyl, C₃₋₆ alkenyl, C₁₋₆alkoxy -COR⁴ or -SO₂R⁴, and that when R³ represents the group Ar, R² represents a hydrogen atom or a halogen atom. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

    摘要翻译： 本发明提供了通式（I）的化合物：或其生理上可接受的盐或溶剂合物（例如水合物），其中R 1代表氢原子或卤素原子或选自C 1-6烷基，C 2-6链烯基 ，氟代C 1-6烷基，-CHO，-CO 2 H或-COR 4; R 2代表氢原子或卤素原子或基团Ar; R 3代表氢原子或选自C 1-6烷基，C 3-6链烯基，C 1-6烷氧基，-COR 4，-SO 2 R 4或基团Ar的基团; R 4代表选自C 1-6烷基，C 2-6链烯基，C 1-6烷氧基或-NR 12 R 13的基团; Ar代表基团R 5代表选自-CO 2 H，-NHSO 2 CF 3或C-连接的四唑基的基团; 可以相同或不同的R 8和R 8各自独立地代表氢原子或卤素原子或C 1-6烷基; Het代表在2-位被C 1-6烷基，C 2-6链烯基或C 1-6烷硫基取代的N-连接的咪唑基，该咪唑基任选地被一个或两个选自卤素原子或基团 选自氰基，硝基，C 1-6烷基，C 2-6链烯基，氟C 1-6烷基， - （CH 2）mR 9， - （CH 2）n COR 9或 - （CH 2）p NR 10 COR 11; 或Het代表在2-位被C 1-6烷基，C 2-6链烯基或C 1-6烷硫基取代的N-连接的苯并咪唑基; R 6代表羟基或C 1-6烷氧基; R 6代表氢原子或选自羟基，C 1-6烷基，C 1-6烷氧基，苯基，苯氧基或基团-NR 12 R 13的基团; R 10代表氢原子或C 1-6烷基; R 11代表氢原子或选自C 1-6烷基，C 1-6烷氧基，苯基，苯氧基或基团-NR 12 R 13的基团; R 12和R 13可以相同或不同，各自独立地代表氢原子或C 1-4烷基或-NR 12 R 13形成饱和杂环，其具有5或6个环成员并且可以任选地在该环中含有一个氧原子; m表示1至4的整数; n表示0至4的整数; 并且p表示1至4的整数; 条件是R 2和R 3中的一个代表基团Ar，当R 2代表基团Ar时，R 3代表氢原子或选自C 1-6烷基，C 3-6链烯基，C 1-6烷氧基-COR 4或-SO 2 R 4的基团， 当R 3代表基团Ar时，R 2代表氢原子或卤素原子。 这些化合物可用于治疗或预防高血压和与认知障碍相关的疾病。

    Benzthiophen derivatives
    4.
    发明公开
    Benzthiophen derivatives 失效
    Benzothiophenderivate。

    公开(公告)号：EP0430709A2

    公开(公告)日：1991-06-05

    申请号：EP90313061.5

    申请日：1990-11-30

    申请人： GLAXO GROUP LIMITED

    发明人： Ross, Barry Clive ,  Middlemiss, David ,  Scopes, David Ian Carter ,  Jack, Torquil Iain Maclean ,  Cardwell, Kevin Stuart ,  Dowle, Michael Dennis

    IPC分类号： C07D409/06 ,  C07D409/14 ,  A61K31/41 ,  C07D333/52

    CPC分类号： C07D249/08 ,  C07C47/565 ,  C07D231/12 ,  C07D233/56 ,  C07D409/06 ,  C07D409/14

    摘要： The invention provides compounds of the general formula (I)
    or a physiologically acceptable salt, solvate or non-toxic metabolically labile ester thereof wherein

    R 1 represents a hydrogen atom or a halogen atom or a group selected from C 1-6 alkyl, C 2 - 6 alkenyl, fluoroC 1-6 alkyl, C 1-6 alkoxy, -CHO, -C0 2 H or ―COR 2 ; Ar represents the group

    R 2 represents a group selected from C 1-6 alkyl, C 2-6 alkenyl, C 1-6 alkoxy or the group ―NR 10 R11 ;
    R 3 represents a group selected from ―CO 2 H, -NHS0 2 CF3 or a C-linked tetrazolyl group ;
    R 4 and R 5 , which may be the same or different, each independently represent a hydrogen atom or a halogen atom or a C 1-6 alkyl group ;
    Het represents an N-linked imidazolyl group optionally substituted at the 2-position by a C 1-6 alkyl, C 2-6 alkenyl or a C 1 - 6 alkylthio group, the imidazolyl group optionally being substituted at the 4- and 5- positions by one or two further substituents selected from a halogen atom or group selected from cyano, nitro, C 1-6 alkyl, C 2-6 alkenyl, fluoroC 1-6 alkyl, ―(CH 2 ) m R 6 , ―(CH 2 )nCOR 7 or ―(CH 2 ) p NR 8 COR 9 ;
    R 6 represents a hydroxy or C 1 - 6 alkoxy group ;
    R 7 represents a hydrogen atom or a group selected from hydroxy, C 1-6 alkyl, C 1-6 alkoxy, phenyl, phenoxy or the group -NR 10 R 11 ;
    R 8 represents a hydrogen atom or a C 1-6 alkyl group ;
    R 9 represents a hydrogen atom or a group selected from C 1-6 alkyl,C 1-6 alkoxy, phenyl, phenoxy or the group -NR 10 R 11 ;
    R 10 and R 11 , which may be the same or different, each independently represent a hydrogen atom or a C I - 4 alkyl group or -NR 10 R 11 forms a saturated heterocyclic ring which has 5 or 6 ring members and may optionally contain in the ring one oxygen atom;
    m represents an integer from 1 to 4 ;
    n represents an integer from 0 to 4; and
    p represents an integer from 1 to 4.
    The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

    摘要翻译： 本发明提供通式（I）化合物或其生理上可接受的盐，溶剂合物或无毒代谢不稳定的酯，其中R 1表示氢原子或卤原子或选自C 1-6烷基 ，C 2-6烯基，氟C 1-6烷基，C 1-6烷氧基，-CHO，-CO 2 H或-COR 2; Ar表示基团 R 2表示选自C 1-6烷基，C 2-6烯基，C 1-6烷氧基或基团-NR 1 R 1 1的基团。 R 3表示选自-CO 2 H，-NHSO 2 CF 3或C连接的四唑基的基团; R 4和R 5可以相同或不同，各自独立地表示氢原子或卤素原子或C 1-6烷基; Het表示任选在2-位被C 1-6烷基，C 2-6烯基或C 1-6烷硫基任意取代的N-连接的咪唑基，咪唑基任选在4-和5-位被取代一个或两个进一步 选自氰基，硝基，C 1-6烷基，C 2-6烯基，氟C 1-6烷基， - （CH 2）m R 6， - （CH 2）n CROR 7或 - （CH 2）p NR 8> COR <9>; R 6表示羟基或C 1-6烷氧基; R 7表示氢原子或选自羟基，C 1-6烷基，C 1-6烷氧基，苯基，苯氧基或基团-NR 1 R 1的基团。 R 8表示氢原子或C 1-6烷基; R 9表示氢原子或选自C 1-6烷基，C 1-6烷氧基，苯基，苯氧基或基团-NR 1 R 1的基团。 R 1和R 1可以相同或不同，各自独立地表示氢原子或C1-4烷基或-NR 1 R 1， 1>形成饱和杂环，其具有5或6个环成员，并且可以任选地在环中含有一个氧原子; m表示1〜4的整数， n表示0〜4的整数， p表示1〜4的整数。该化合物可用于治疗或预防与认知障碍相关的高血压和疾病。

    Benzofuran derivatives
    6.
    发明公开
    Benzofuran derivatives 失效
    BENZOFURAN衍生物

    公开(公告)号：EP0434249A3

    公开(公告)日：1992-02-12

    申请号：EP90313051.6

    申请日：1990-11-30

    申请人： GLAXO GROUP LIMITED

    发明人： Ross, Barry Clive ,  Middlemiss, David ,  Scopes, David Ian Carter ,  Jack, Torquil Iain Maclean ,  Cardwell, Kevin Stuart ,  Dowle, Michael Dennis

    IPC分类号： C07D405/06 ,  C07D405/14 ,  A61K31/41 ,  C07D307/78 ,  C07D405/10

    CPC分类号： C07D249/08 ,  C07C45/45 ,  C07C45/54 ,  C07C45/68 ,  C07C47/565 ,  C07C49/825 ,  C07D231/12 ,  C07D233/56 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14

    摘要： The invention provides compounds of the general formula (I)

    or a physiologically acceptable salt, solvate or non-toxic metabolically labile ester thereof
    wherein
       R¹ represents a hydrogen atom or a halogen atom or a group selected from C₁₋₆alkyl, C₂₋₆alkenyl, fluoroC₁₋₆alkyl, C₁₋₆alkoxy, ―CHO, ―CO₂H or ―COR²;
       Ar represents the group
       R² represents a group selected from C₁₋₆alkyl, C₂₋₆alkenyl, C₁₋₆alkoxy or the group ―NR¹⁰R¹¹;
       R³ represents a group selected from ―CO₂H, ―NHSO₂CF₃ or a C-linked tetrazolyl group;
       R⁴ and R⁵, which may be the same or different, each independently represent a hydrogen atom or a halogen atom or a C₁₋₆alkyl group;    Het represents an N-linked imidazolyl group optionally substituted at the 2-position by a C₁₋₆alkyl, C₂₋₆alkenyl or a C₁₋₆alkylthio group, the imidazolyl group optionally being substituted at the 4- and 5- positions by one or two further substituents selected from a halogen atom or group selected from cyano, nitro, C₁₋₆alkyl, C₂₋₆alkenyl, fluoroC₁₋₆alkyl, ―(CH₂) m R⁶, ―(CH₂) n COR⁷ or ―(CH₂) p NR⁸COR⁹;
       R⁶ represents a hydroxy or C₁₋₆alkoxy group;
       R⁷ represents a hydrogen atom or a group selected from hydroxy, C₁₋₆alkyl, C₁₋₆alkoxy, phenyl, phenoxy or the group ―NR¹⁰R¹¹;
       R⁸ represents a hydrogen atom or a C₁₋₆alkyl group;
       R⁹ represents a hydrogen atom or a group selected from C₁₋₆alkyl, C₁₋₆alkoxy, phenyl, phenoxy or the group ―NR¹⁰R¹¹;
       R¹⁰ and R¹¹ which may be the same or different, each independently represent a hydrogen atom or a C₁₋₄alkyl group or ―NR¹⁰R¹¹ forms a saturated heterocyclic ring which has 5 or 6 ring members and may optionally contain in the ring one oxygen atom;
       m represents an integer from 1 to 4;
       n represents an integer from 0 to 4; and
       p represents an integer from 1 to 4. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

    Benzthiophen derivatives
    7.
    发明公开
    Benzthiophen derivatives 失效
    苯并噻吩衍生物

    公开(公告)号：EP0430709A3

    公开(公告)日：1992-02-12

    申请号：EP90313061.5

    申请日：1990-11-30

    申请人： GLAXO GROUP LIMITED

    发明人： Ross, Barry Clive ,  Middlemiss, David ,  Scopes, David Ian Carter ,  Jack, Torquil Iain Maclean ,  Cardwell, Kevin Stuart ,  Dowle, Michael Dennis

    IPC分类号： C07D409/06 ,  C07D409/14 ,  A61K31/41 ,  C07D333/52

    CPC分类号： C07D249/08 ,  C07C47/565 ,  C07D231/12 ,  C07D233/56 ,  C07D409/06 ,  C07D409/14

    摘要： The invention provides compounds of the general formula (I)
    or a physiologically acceptable salt, solvate or non-toxic metabolically labile ester thereof wherein
    R 1 represents a hydrogen atom or a halogen atom or a group selected from C 1-6 alkyl, C 2 - 6 alkenyl, fluoroC 1-6 alkyl, C 1-6 alkoxy, -CHO, -C0 2 H or ―COR 2 ; Ar represents the group
    R 2 represents a group selected from C 1-6 alkyl, C 2-6 alkenyl, C 1-6 alkoxy or the group ―NR 10 R11 ; R 3 represents a group selected from ―CO 2 H, -NHS0 2 CF3 or a C-linked tetrazolyl group ; R 4 and R 5 , which may be the same or different, each independently represent a hydrogen atom or a halogen atom or a C 1-6 alkyl group ; Het represents an N-linked imidazolyl group optionally substituted at the 2-position by a C 1-6 alkyl, C 2-6 alkenyl or a C 1 - 6 alkylthio group, the imidazolyl group optionally being substituted at the 4- and 5- positions by one or two further substituents selected from a halogen atom or group selected from cyano, nitro, C 1-6 alkyl, C 2-6 alkenyl, fluoroC 1-6 alkyl, ―(CH 2 ) m R 6 , ―(CH 2 )nCOR 7 or ―(CH 2 ) p NR 8 COR 9 ; R 6 represents a hydroxy or C 1 - 6 alkoxy group ; R 7 represents a hydrogen atom or a group selected from hydroxy, C 1-6 alkyl, C 1-6 alkoxy, phenyl, phenoxy or the group -NR 10 R 11 ; R 8 represents a hydrogen atom or a C 1-6 alkyl group ; R 9 represents a hydrogen atom or a group selected from C 1-6 alkyl,C 1-6 alkoxy, phenyl, phenoxy or the group -NR 10 R 11 ; R 10 and R 11 , which may be the same or different, each independently represent a hydrogen atom or a C I - 4 alkyl group or -NR 10 R 11 forms a saturated heterocyclic ring which has 5 or 6 ring members and may optionally contain in the ring one oxygen atom; m represents an integer from 1 to 4 ; n represents an integer from 0 to 4; and p represents an integer from 1 to 4. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

    Ethanolamine derivatives
    8.
    发明公开
    Ethanolamine derivatives 失效

    公开(公告)号：EP0220054A3

    公开(公告)日：1987-12-02

    申请号：EP86307974

    申请日：1986-10-15

    申请人： GLAXO GROUP LIMITED

    发明人： Finch, Harry ,  Lunts, Lawrence Henry Charles ,  Naylor, Alan ,  Skidmore, Ian Frederick ,  Campbell, Ian Baxter ,  Middlemiss, David ,  Willbe, Charles

    IPC分类号： C07D213/38 ,  C07C143/75 ,  C07C93/00 ,  C07C93/08 ,  C07C127/17 ,  C07C93/14 ,  C07C125/065 ,  C07C103/76 ,  C07C103/38 ,  C07D295/08 ,  A61K31/135

    CPC分类号： C07D295/096 ,  C07D213/65 ,  Y10S514/826

    摘要： The present invention provides compounds of the general formula (I)
    wherein
    Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms, or the groups C 1-6 alkyl, nitro, -(CH 2 )qR, [where R is hydroxy, C 1-6 alkoxy, -NR3R4 (where R3 and R 4 each represents a hydrogen atom, or a C 1-4 alkyl group, or -NR 3 R 4 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from -O- or -S-or a group -NH- or -N(CH 3 )-), -NR 5 COR 6 (where R 5 represents a hydrogen atom or a C 1-4 alkyl group, and R 6 represents a hydrogen atom or a C 1-4 alkyl, Ci- 4 alkoxy, phenyl or -NR 3 R 4 group), -NR S S0 2 R 7 (where R 7 represents a C 1-4 alkyl, phenyl or -NR3R4 group), -COR 8 (where R 8 represents hydroxy, C 1-4 alkoxy or-NR 3 R 4 ), -SR 9 (where R 9 is a hydrogen atom, or a C 1-4 alkyl or phenyl group), -SOR 9 , -S0 2 R 9 , or -CN, and q represents an integer from 0 to 3], or -O(CH 2 ) 1 R 10 [where R 10 represents a hydroxy or C 1-4 alkoxy group, and t is an integer 2 or 3], or Ar is a phenyl group substituted by an alkylenedioxy group of formula -O(CH 2 )pO-, where p represents an integer 1 or 2: R 1 and R 2 each represents a hydrogen atom or a C 1-3 alkyl group with the proviso that the sum total of carbon atoms in R 1 and R 2 is not more than 4; X represents a bond or a C 1-7 alkylene, C 2 - 7 alkynylene or C 2 - 7 alkenylene chain and Y represents a bond or a C 1-6 alkylene, C 2-6 alkenylene or C 2-6 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is 2-10; Q represents the group
    [where Q 1 represents C 1-3 alkoxy, methanesulphonyl or cyano) or the group -CH 2 NHR 11 (where R 11 represents R 12 CO-. R 12 NHCO-. R 12 R 13 NSO 2 - or R 14 SO 2 -, where R 12 and R 13 each represent a hydrogen atom or a C 1-3 alkyl group, and R 14 represents a C 1-3 alkyl group), or the group -NR 15 R 16 (where R 15 represents a hydrogen atom or a C 1-4 alkyl group, and R 16 represents a hydrogen atom or a C 1-4 alkyl group or, when R 15 is a hydrogen atom. R 16 also represents a C 1-4 alkoxycarbonyl group)]. or Q represents the group
    or Q represents a phenyl group substituted by a hydroxy group and optionally also by a halogen atom; and physiologically acceptable salts and solvates (e.g. hydrates)thereof. The compounds have a stimulant action at β2-adrenorecep- tors and may be used in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.

    Ethanolamine derivatives
    9.
    发明公开
    Ethanolamine derivatives 失效
    乙醇胺衍生物

    公开(公告)号：EP0220054A2

    公开(公告)日：1987-04-29

    申请号：EP86307974.5

    申请日：1986-10-15

    申请人： GLAXO GROUP LIMITED

    发明人： Finch, Harry ,  Lunts, Lawrence Henry Charles ,  Naylor, Alan ,  Skidmore, Ian Frederick ,  Campbell, Ian Baxter ,  Middlemiss, David ,  Willbe, Charles

    IPC分类号： C07D213/38 ,  C07C311/00 ,  C07C217/00 ,  C07C275/00 ,  C07C273/00 ,  C07C233/00 ,  C07D295/08 ,  A61K31/135

    CPC分类号： C07D295/096 ,  C07D213/65 ,  Y10S514/826

    摘要： The present invention provides compounds of the general formula (I)
    wherein

    Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms, or the groups C 1-6 alkyl, nitro, -(CH 2 )qR, [where R is hydroxy, C 1-6 alkoxy, -NR3R4 (where R3 and R 4 each represents a hydrogen atom, or a C 1-4 alkyl group, or -NR 3 R 4 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from -O- or -S-or a group -NH- or -N(CH 3 )-), -NR 5 COR 6 (where R 5 represents a hydrogen atom or a C 1-4 alkyl group, and R 6 represents a hydrogen atom or a C 1-4 alkyl, Ci- 4 alkoxy, phenyl or -NR 3 R 4 group), -NR S S0 2 R 7 (where R 7 represents a C 1-4 alkyl, phenyl or -NR3R4 group), -COR 8 (where R 8 represents hydroxy, C 1-4 alkoxy or-NR 3 R 4 ), -SR 9 (where R 9 is a hydrogen atom, or a C 1-4 alkyl or phenyl group), -SOR 9 , -S0 2 R 9 , or -CN, and q represents an integer from 0 to 3], or -O(CH 2 ) 1 R 10 [where R 10 represents a hydroxy or C 1-4 alkoxy group, and t is an integer 2 or 3], or Ar is a phenyl group substituted by an alkylenedioxy group of formula -O(CH 2 )pO-, where p represents an integer 1 or 2:
    R 1 and R 2 each represents a hydrogen atom or a C 1-3 alkyl group with the proviso that the sum total of carbon atoms in R 1 and R 2 is not more than 4;
    X represents a bond or a C 1-7 alkylene, C 2 - 7 alkynylene or C 2 - 7 alkenylene chain and
    Y represents a bond or a C 1-6 alkylene, C 2-6 alkenylene or C 2-6 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is 2-10;
    Q represents the group
    [where Q 1 represents C 1-3 alkoxy, methanesulphonyl or cyano) or the group -CH 2 NHR 11 (where R 11 represents R 12 CO-. R 12 NHCO-. R 12 R 13 NSO 2 - or R 14 SO 2 -, where R 12 and R 13 each represent a hydrogen atom or a C 1-3 alkyl group, and R 14 represents a C 1-3 alkyl group), or the group -NR 15 R 16 (where R 15 represents a hydrogen atom or a C 1-4 alkyl group, and R 16 represents a hydrogen atom or a C 1-4 alkyl group or, when R 15 is a hydrogen atom. R 16 also represents a C 1-4 alkoxycarbonyl group)]. or Q represents the group
    or Q represents a phenyl group substituted by a hydroxy group and optionally also by a halogen atom;
    and physiologically acceptable salts and solvates (e.g. hydrates)thereof.

    The compounds have a stimulant action at β2-adrenorecep- tors and may be used in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.

    摘要翻译： 本发明提供了通式（I）的化合物，其中Ar代表任选被一个或多个选自卤素原子，或基团C 1-6烷基，硝基， - （CH 2）q R的取代基取代的苯基，其中R是羟基 ，C 1-6烷氧基，-NR 3 R 4（其中R 3和R 4各自表示氢原子或C 1-4烷基，或者-NR 3 R 4形成饱和杂环氨基，其具有5-7个环成员且任选地在环中包含一个 或更多选自-O-或-S-或基团-NH-或-N（CH 3） - 的原子，-NR 5 COR 6（其中R 5表示氢原子或C 1-4烷基，并且R 6表示氢原子 （其中R 7代表C 1-4烷基，苯基或-NR 3 R 4基团），-COR 8（其中R 8代表羟基，C 1-4烷氧基或C 1-4烷氧基，苯基或-NR 3 R 4基团） -NR 3 R 4）， - SR 9（其中R 9为氢原子或C 1-4烷基或苯基），-SOR 9，-SO 2 R 9或-CN，并且q表示0至3的整数]或-O（ CH2）1R10 [其中R10代表羟基或C 1-4烷氧基，并且t是整数2或3]或Ar是被式-O（CH 2）p -O-的亚烷基二氧基取代的苯基，其中p表示整数1或2：R 1和R 2各自为 表示氢原子或C 1-3烷基，条件是R 1和R 2中的碳原子总数不超过4; X表示键或C1-7亚烷基，C2-7亚炔基或C2-7亚烯基链，并且Y表示键或C1-6亚烷基，C2-6亚烯基或C2-6亚炔基链，条件是总和 X和Y中的碳原子数为2-10; Q表示基团[其中Q1表示C1-3烷氧基，甲磺酰基或氰基）或基团-CH2NHR11（其中R11表示R12CO- .R12NHCO- .R12R13NSO2-或R14SO2-，其中R12和R13各自表示氢原子或C1 -3烷基，R14表示C1-3烷基）或基团-NR15R16（式中，R15表示氢原子或C1-4烷基，R16表示氢原子或C1-4烷基，或者在 R15是氢原子，R16也表示C1-4烷氧基羰基）]。 或Q代表基团或Q代表被羟基和任选还被卤素原子取代的苯基; 和其生理学上可接受的盐和溶剂化物（例如水合物）。 这些化合物对β2-肾上腺素受体具有刺激作用，可用于治疗与可逆性气道阻塞有关的疾病，如哮喘和慢性支气管炎。

    1H-Imidazol-1-yl-methyl benzofuran derivatives with the imidazolyl moiety being substituted by a cycloalkyl group
    10.
    发明公开
    1H-Imidazol-1-yl-methyl benzofuran derivatives with the imidazolyl moiety being substituted by a cycloalkyl group 失效
    1H-咪唑-1-基 - 甲基 - 苯并呋喃酮，bei denen die Imidazolyleinheit durch eine Cycloalkylgruppe取代物。

    公开(公告)号：EP0514198A1

    公开(公告)日：1992-11-19

    申请号：EP92304420.0

    申请日：1992-05-15

    申请人： GLAXO GROUP LIMITED

    发明人： Ross, Barry Clive ,  Middlemiss, David ,  Scopes, David Ian Carter ,  Jack, Torquil Iain MacLean ,  Cardwell, Kevin Stuart ,  Dowle, Michael Dennis ,  Judd, Duncan Bruce ,  Watson, Stephen Paul

    IPC分类号： C07D405/14 ,  C07D405/06 ,  A61K31/415

    CPC分类号： C07D249/08 ,  C07B59/00 ,  C07D231/12 ,  C07D233/56 ,  C07D405/06 ,  C07D405/14

    摘要： The invention provides compounds of the general formula (I):

    or a physiologically acceptable salt, solvate or metabolically labile ester thereof wherein the definition of R¹ and Ar are as given in the claims, het represents the group

    R⁶ represents a hydrogen atom or a group selected from C1-6alkyl, C2-6alkenyl, C1-6alkylthio, C1-6alkoxy, C3-7cycloalkyl or C3-7cycloalkylC1-4alkyl;
    R⁷ represents among others and as shown in the examples a group selectedfrom C3-7cycloalkyl or C3-7cycloalkylC1-4alkyl;
    R⁸ represents a hydrogen atom or a halogen atom or a group selected from cyano, nitro, C1-6alkyl, C2-6alkenyl, fluoroC1-6alkyl, -(CH₂)mR⁹, -(CH₂)nCOR¹⁰ or -(CH²)pNR¹¹COR¹²; and
    R⁹, R¹⁰, R¹¹, R¹², R¹³ and R¹⁴ are a variety of groups and substituents;
    with the proviso that when R⁶ represents a hydrogen atom or a group selected from C1-6alkyl, C2-6alkenyl or C1-6alkylthio, R⁷ represents a group selected from C3-7cycloalkyl or C3-7cycloalkylC1-4alkyl.
    The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

    摘要翻译： 本发明提供了通式（I）的化合物：其中R 1和Ar的定义如权利要求书中所给出，其代表基团或其生理上可接受的盐，溶剂化物或代谢不稳定的酯 R 6表示氢原子或选自C 1-6烷基，C 2-6烯基，C 1-6烷硫基，C 1-6烷氧基，C 3-7环烷基或C 3-7环烷基C 1-4烷基的基团。 R 7表示，并且如实施例中所示，选自C 3-7环烷基或C 3-7环烷基C 1-4烷基的基团; R 8表示氢原子或卤素原子或选自氰基，硝基，C 1-6烷基，C 2-6烯基，氟C 1-6烷基， - （CH 2）m R 9， - （CH 2）n COOR 1 0或 - （CH 2）pNR 1 COR 1 <2>; 和R 9，R 1，R 1，R 1，R 1，R 2，R 3和R 4是各种基团 和取代基; 条件是当R 6表示氢原子或选自C 1-6烷基，C 2-6烯基或C 1-6烷硫基时，R 7表示选自C 3-7环烷基或C 3-7环烷基C 1-4烷基的基团。 该化合物可用于治疗或预防与认知障碍相关的高血压和疾病。