发明名称 1,2,3-triazole-4-amine derivatives for the treatment of sigma receptor related diseases and disorders
摘要 The present invention relates to new 1,2,3-triazole-amine derivatives, having affinity for sigma receptors, especially sigma-1 receptor, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments for the treatment of sigma receptor related diseases and disorders.
申请公布号 US9611229(B2) 申请公布日期 2017.04.04
申请号 US201414759280 申请日期 2014.01.07
申请人 LABORATORIOS DEL DR. ESTEVE S.A. 发明人 Torrens-Jover Antoni;Christmann Ute;Diaz-Fernández Josè-Luis;Almansa-Rosales Carmen
分类号 C07D249/04;C07D249/06;C07D295/185;C07F7/10;C07D401/12 主分类号 C07D249/04
代理机构 Hueschen and Sage 代理人 Hueschen and Sage
主权项 1. A 1,2,3-triazole-4-amine derivative of general formula (I): wherein: G1 is selected from the group consisting of a hydrogen atom; a linear or branched, saturated or unsaturated, substituted or unsubstituted aliphatic radical; a substituted or unsubstituted aryl group which is optionally condensed to other, substituted or unsubstituted, mono- or polycyclic ring systems; a —(C═O)—R5 group; a —(SO)2—R6 group; and a —C═Z—NH—R8 group; R1 and R2, which may be identical or different, are selected from the group consisting of a hydrogen atom; and a linear or branched, saturated or unsaturated, substituted or unsubstituted aliphatic radical; or R1 and R2 together with the bridging nitrogen atom to which they are attached form an at least mono-cyclic, substituted or unsubstituted, at least one heteroatom containing heterocyclyl group which is optionally condensed with a substituted or unsubstituted mono- or polycyclic ring system; R4 is selected from the group consisting of a hydrogen atom; a linear or branched, saturated or unsaturated, substituted or unsubstituted aliphatic radical; a substituted or unsubstituted cycloalkyl group which is optionally condensed to other, substituted or unsubstituted, mono- or polycyclic ring systems; a substituted or unsubstituted aryl group which is optionally condensed to other, substituted or unsubstituted, mono- or polycyclic ring systems; a branched or unbranched, saturated or unsaturated, substituted or unsubstituted alkyl-cycloalkyl group in which the cycloalkyl group may be substituted or unsubstituted and/or condensed with a mono- or polycyclic ring system; and a branched or unbranched, saturated, substituted or unsubstituted alkyl-aryl group in which the aryl group may be substituted or unsubstituted and/or condensed with a mono- or polycyclic ring system; R5 is selected from the group consisting of a linear or branched, saturated or unsaturated, substituted or unsubstituted aliphatic radical; a substituted or unsubstituted cycloalkyl group which is optionally condensed to other, substituted or unsubstituted, mono- or polycyclic ring systems; a substituted or unsubstituted aryl group which is optionally condensed to other, substituted or unsubstituted, mono- or polycyclic ring systems; a substituted or unsubstituted heterocyclyl group which is optionally condensed to other, substituted or unsubstituted, mono- or polycyclic ring systems; a branched or unbranched, saturated or unsaturated, substituted or unsubstituted alkyl-cycloalkyl group in which the cycloalkyl group may be substituted or unsubstituted and/or condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated, substituted or unsubstituted alkyl-aryl group in which the aryl group may be substituted or unsubstituted and/or condensed with a mono- or polycyclic ring system; and a branched or unbranched, saturated, substituted or unsubstituted alkyl-heterocyclyl group in which the heterocyclyl group may be substituted or unsubstituted and/or condensed with a mono- or polycyclic ring system; R6 is selected from the group consisting of a linear or branched, saturated or unsaturated, substituted or unsubstituted aliphatic radical; a substituted or unsubstituted aryl group which is optionally condensed to other, substituted or unsubstituted, mono- or polycyclic ring systems; and a branched or unbranched, saturated or unsaturated, substituted or unsubstituted alkyl-cycloalkyl group in which the cycloalkyl group may be substituted or unsubstituted and/or condensed with a mono- or polycyclic ring system; Z is S or O; R8 is a linear or branched, saturated or unsaturated, substituted or unsubstituted aliphatic radical; n is 1, 2, 3, or 4; optionally as a stereoisomer, including enantiomers and diastereomers, a racemate or as of a mixture of at least two stereoisomers, including enantiomers and/or diastereomers, in any mixing ratio, or a salt thereof, or a solvate thereof.
地址 Barcelona ES