公开(公告)号：EP1558577B1

公开(公告)日：2009-12-30

申请号：EP03762615.7

申请日：2003-07-02

申请人： GLAXO GROUP LIMITED

发明人： ALVARO, Giuseppe, GlaxoSmithKline ,  CARDULLO, Francesca, GlaxoSmithKline ,  DI FABIO, Romano, GlaxoSmithKline ,  GIOVANNINI, Riccardo, GlaxoSmithKline ,  PIGA, Elisabetta, GlaxoSmithKline ,  TRANQUILLINI, Maria, Elvira, GlaxoSmithKline

IPC分类号： C07D211/34 ,  C07D211/64 ,  C07D223/04 ,  C07D223/06

CPC分类号： C07D211/34 ,  C07D211/64 ,  C07D223/04 ,  C07D223/06

摘要： The present invention relates to cyclic amine derivatives of formula(I) (I)whereinR represents halogen, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy;R1 represents hydrogen, halogen, C3-7cycloalkyl, hydroxy, nitro, cyano or C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy;R2 represents hydrogen or C1-4 alkyl;R3 and R4 independently represent hydrogen, cyano, C1-4 alkyl or R3 together with R4 represents C3-7 cycloalkyl;R5 represents trifluoromethyl, S(O)t C 1-4 alkyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy, halogen or cyano;R6 represents hydrogen or (CH2)rR7;R7 represents hydrogen, C3-7 cycloalkyl, NH(C1-4alkylOC1-4alkoxy), NH(C1-4alkyl), N(C1-4alkyl)2 , OC(O)NR9R8 , NR8C(O)R9 or C(O)NR9R8;R9 and R8 independently represent hydrogen, C1-4 alkyl or C3-7 cycloalkyl; m represents zero or an integer from 1 to 4;n represents 1 or 2;p is zero or an integer from 1 to 3;q is an integer from 1 to 3;r is an integer from 1 to 4;t is 0 , 1 or 2 ;provided that when m is 0, p is 2, q , r and n represent 1, R1, R2,R3, R4, R5 and R7 are hydrogen and R is chlorine, R5 is not iodine; and pharmaceutically acceptable salts and solvates thereof; process for their preparation and their use in the treatment of conditions mediated by tackykinins and/or by selective inhibition of serotonin reuptake transporter protein .

公开(公告)号：EP1517894B1

公开(公告)日：2006-09-06

申请号：EP03740413.4

申请日：2003-07-02

申请人： GLAXO GROUP LIMITED

发明人： ALVARO, Giuseppe, GlaxoSmithKline ,  CARDULLO, Francesca, GlaxoSmithKline ,  D'ADAMO, Lucilla, GlaxoSmithKline ,  PIGA, Elisabetta, GlaxoSmithKline ,  SERI, Catia, GlaxoSmithKline

IPC分类号： C07D211/14 ,  C07D211/38 ,  C07D207/20 ,  C07D211/70 ,  C07D207/06 ,  C07D265/30 ,  C07D213/16 ,  A61K31/40 ,  A61K31/445 ,  A61K31/44 ,  A61K31/535 ,  A61P25/00 ,  A61P29/00 ,  A61P1/08

CPC分类号： C07D207/08 ,  A61K31/40 ,  A61K31/44 ,  A61K31/445 ,  A61K31/535 ,  C07D207/20 ,  C07D211/34 ,  C07D211/38 ,  C07D211/70 ,  C07D213/56 ,  C07D265/30

摘要： The present invention relates to heterocyclic derivatives of formula (1) wherein R1 represents a 5 or 6 membered heteroaryl group, in which the 5-membered heteroaryl group contains at least one heteroatom selected from oxygen, sulphur or nitrogen and the 6-membered heteroaryl group contains from 1 to 3 nitrogen atoms, or R1 represents a 4,5 or 6 membered heterocyclic group, wherein saids 5 or 6 membered heteroaryl or the 4,5 or 6 membered heterocyclic group may optionally be substituted by one to three substituents, which may be the same or different, selected from (CH2)pR6, wherein p is zero or an integer from 1 to 4 and wherein R and R2- R6 are each as defined in the description and pharmaceutically acceptable salts and solvates thereof; process for their preparation and their use in the treatment of conditions mediated by tachykinins and/or by selective inhibition of serotonin reuptake transporter protein.