公开(公告)号：US20060058348A1

公开(公告)日：2006-03-16

申请号：US10521159

申请日：2003-07-02

申请人： Giuseppe Alvaro ,  Francesca Cardullo ,  Lucilla D'Adamo ,  Elisabeth Piga ,  Catia Seri

发明人： Giuseppe Alvaro ,  Francesca Cardullo ,  Lucilla D'Adamo ,  Elisabeth Piga ,  Catia Seri

IPC分类号： C07D211/26 ,  A61K31/445

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 (I) wherein R represents halogen, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy; 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 R6 is selected from: halogen, C1-4alkoxy, C1-4alkyl, C3-7cycloalkyl, C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy, hydroxy, cyano, nitro, trifluoromethyl, carboxy, NH(C1-4 alkyl), N(C1-4 alkyl)2 NH(C3-7 cycloalkyl), N(C1-4 alkyl)(C3-7 cycloalkyl); NH(C1-4alkylOC1-4alkoxy), OC(O)NR7R8, NR8C(O)R7 or C(O)NR7R8; R2 represents hydrogen, or C1-4 alkyl; R3 and R4 independently represent hydrogen, C1-4 alkyl or R3 together with R4 represents C3-7 cycloalkyl; R5 represents trifluoromethyl, S(O)qC1-4 alkyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy, halogen or cyano; R7 and R8 independently represent hydrogen, C1-4 alkyl or C3-7 cycloalkyl; L is a single or a double bond; n is an integer from 1 to 3; m is zero or an integer from 1 to 3; q is zero or an integer from 1 to 2; provided that a) when L is a double bond, R1 is not an optionally substituted 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; b) the group R1 is linked to the carbon atom shown as * via a carbon atom; and c) when the heteroatom contained in the group R1 is substituted, p is not zero; 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.

摘要翻译： 本发明涉及式（I）的杂环衍生物，

公开(公告)号：US20060128752A1

公开(公告)日：2006-06-15

申请号：US10520143

申请日：2003-07-02

申请人： Giuseppe Alvaro ,  Francesca Cardullo ,  Romano Di Fabio ,  Riccardo Giovannini ,  Elisabeth Piga ,  Maria Tranquillini

发明人： Giuseppe Alvaro ,  Francesca Cardullo ,  Romano Di Fabio ,  Riccardo Giovannini ,  Elisabeth Piga ,  Maria Tranquillini

IPC分类号： A61K31/445 ,  C07D211/06

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

摘要： The present invention relates to cyclic amine derivatives of formula(l) wherein R 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 C1-4 alkyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy, halogen or cyano; R6 represents hydrogen or (CH2)rR7; R7 represents hydrogen, C37 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.