发明申请
US20060058348A1 N-benzyl-3-phenyl-3-heterocyclyl-propionamide compounds as tachykinin and/or serotonin reuptake inhibitors
审中-公开
N-苄基-3-苯基-3-杂环基 - 丙酰胺化合物作为速激肽和/或5-羟色胺再摄取抑制剂
- 专利标题: N-benzyl-3-phenyl-3-heterocyclyl-propionamide compounds as tachykinin and/or serotonin reuptake inhibitors
- 专利标题(中): N-苄基-3-苯基-3-杂环基 - 丙酰胺化合物作为速激肽和/或5-羟色胺再摄取抑制剂
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申请号: US10521159申请日: 2003-07-02
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公开(公告)号: US20060058348A1公开(公告)日: 2006-03-16
- 发明人: Giuseppe Alvaro , Francesca Cardullo , Lucilla D'Adamo , Elisabeth Piga , Catia Seri
- 申请人: Giuseppe Alvaro , Francesca Cardullo , Lucilla D'Adamo , Elisabeth Piga , Catia Seri
- 优先权: GB0215392.2 20020703
- 国际申请: PCT/EP03/07126 WO 20030702
- 主分类号: C07D211/26
- IPC分类号: C07D211/26 ; A61K31/445
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.
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