公开(公告)号：EP1745040B9

公开(公告)日：2010-06-02

申请号：EP05707610.1

申请日：2005-02-21

申请人： Glaxo Group Limited

发明人： ARISTA, Luca GlaxoSmithKline SpA ,  BONANOMI, Giorgio GlaxoSmithKline SpA ,  CAPELLI, Anna Maria GlaxoSmithKline SpA ,  DAMIANI, Federica GlaxoSmithKline SpA ,  DI FABIO, Romano GlaxoSmithKline SpA ,  GENTILE, Gabriella GlaxoSmithKline SpA ,  HAMPRECHT, Dieter GlaxoSmithKline SpA ,  MICHELI, Fabrizio GlaxoSmithKline SpA ,  TARSI, Luca GlaxoSmithKline SpA ,  TEDESCO, Giovanna GlaxoSmithKline SpA ,  TERRENI, Silvia GlaxoSmithKline SpA

IPC分类号： C07D403/12 ,  A61K31/403 ,  A61P25/00

CPC分类号： C07D495/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08

摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, -CH2-N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, p is 1; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency or as antipsychotic agents.

公开(公告)号：EP1745040B1

公开(公告)日：2009-12-09

申请号：EP05707610.1

申请日：2005-02-21

申请人： Glaxo Group Limited

发明人： ARISTA, Luca GlaxoSmithKline SpA ,  BONANOMI, Giorgio GlaxoSmithKline SpA ,  CAPELLI, Anna Maria GlaxoSmithKline SpA ,  DAMIANI, Federica GlaxoSmithKline SpA ,  DI FABIO, Romano GlaxoSmithKline SpA ,  GENTILE, Gabriella GlaxoSmithKline SpA ,  HAMPRECHT, Dieter GlaxoSmithKline SpA ,  MICHELI, Fabrizio GlaxoSmithKline SpA ,  TARSI, Luca GlaxoSmithKline SpA ,  TEDESCO, Giovanna GlaxoSmithKline SpA ,  TERRENI, Silvia GlaxoSmithKline SpA

IPC分类号： C07D403/12 ,  A61K31/403 ,  A61P25/00

CPC分类号： C07D495/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08

摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, -CH2-N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, p is 1; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency or as antipsychotic agents.

公开(公告)号：EP1745040A1

公开(公告)日：2007-01-24

申请号：EP05707610.1

申请日：2005-02-21

申请人： GLAXO GROUP LIMITED

发明人： ARISTA, Luca GlaxoSmithKline SpA ,  BONANOMI, Giorgio GlaxoSmithKline SpA ,  CAPELLI, Anna Maria GlaxoSmithKline SpA ,  DAMIANI, Federica GlaxoSmithKline SpA ,  DI FABIO, Romano GlaxoSmithKline SpA ,  GENTILE, Gabriella GlaxoSmithKline SpA ,  HAMPRECHT, Dieter GlaxoSmithKline SpA ,  MICHELI, Fabrizio GlaxoSmithKline SpA ,  TARSI, Luca GlaxoSmithKline SpA ,  TEDESCO, Giovanna GlaxoSmithKline SpA ,  TERRENI, Silvia GlaxoSmithKline SpA

IPC分类号： C07D403/12 ,  A61K31/403 ,  A61P25/00

CPC分类号： C07D495/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08

摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, -CH2-N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, p is 1; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency or as antipsychotic agents.

公开(公告)号：EP1472256B1

公开(公告)日：2005-11-02

申请号：EP03702621.8

申请日：2003-02-10

申请人： GLAXO GROUP LIMITED

发明人： ALVARO, Giuseppe GlaxoSmithKline SpA ,  DI FABIO, Romano GlaxoSmithKline SpA ,  TRANQUILLINI, Maria Elvira GlaxoSmithKline SpA ,  SPADA, Simone GlaxoSmithKline SpA

IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61P25/00 ,  C07D498/04 ,  C07D471/04

CPC分类号： C07D487/04 ,  A61K31/445

摘要： The present invention relates to piperidine derivatives of formula (I): R represents halogen or C1-4 alkyl; R1 represents C1-4 alkyl; R2 or R3 independently represent hydrogen or C1-4 alkyl; R4 represents trifluoromethyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy or halogen; R5 represents hydrogen , C1-4 alkyl or C3-7 cycloalkyl; R6 is hydrogen and R7 is a radical of formula (W): R6 is a radical of formula (W) and R7 is hydrogen; X represents CH2, NR5 or O; Y represents Nitrogen and Z is CH or Y represents CH and Z is Nitrogen; A represents C(O) or S(O)q, provided that when Y is nitrogen and Z is CH, A is not S(O)q; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; p and q are independently an integer from 1 to 2; and pharmaceutically acceptable salts and solvates thereof. The process for their preparation and their use in the treatment of condition mediated by tachykinins.