Substituted pyrazolo[1,5-A]pyridines, their preparation and use as medicaments,申请号US201314379844-传众专利搜索

Substituted pyrazolo[1,5-A]pyridines, their preparation and use as medicaments

申请公布号：US9487513(B2)

申请号：US201314379844

申请日期：2013.02.21

申请公布日期：2016.11.08

申请人：

LABORATORIOS DE DR. ESTEVE S.A.

发明人：Diaz Fernández José Luis;Cuberes Altisent Ma Rosa

分类号：C07D471/04;C07D519/00;C07D491/107

主分类号：C07D471/04

代理机构：

Hueschen and Sage

代理人：Hueschen and Sage

地址：Barcelona ES

摘要：The present invention relates to new substituted pyrazolo[1,5-a]pyridine having a great 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.

主权项：1. A compound of general formula (I):wherein R1 and R2 independently represent hydrogen; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, aliphatic radical C1-10; a substituted or unsubstituted aryl radical; a substituted or unsubstituted heteroaryl radical; a substituted or unsubstituted C3-9 cycloalkyl radical optionally containing at least one heteroatom as ring member selected from N, O or S; a cycloalkylalkyl radical C1-10; an arylalkyl radical C1-10; or an heteroarylalkyl radical C1-10; or R1 and R2 together with the bridging nitrogen form a C3-9 cycloalkyl optionally having at least one additional heteroatom as a ring member selected from N, O or S and optionally substituted by one or more substituents selected from the group consisting of a C1-6 alkyl group, a linear or branched C1-6 alkoxy group, —F, —Cl, —I, —Br, —CF3, —CH2F, —CHF2, —CN, —OH, —SH, —NH2, oxo, —(C═O)R′, —SR′, —SOR′, —SO2R′, —NHR′, —NR′R″, wherein R′ and R″ at each occurrence independently represents a linear or branched C1-6-alkyl group; or R1 and R2 together with the bridging nitrogen form C3-9 cycloalkyl optionally having at least one additional heteroatom as a ring member selected from N, O or S, which may be condensed to form a ring system with another C3-9 cycloalkyl optionally having at least one heteroatom as a ring member selected from N, O or S; or which may be condensed to form a ring system with an aryl radical; or which may be spirofused to an aryl or heteroaryl group; R3 represents hydrogen or halogen; n is 0, 1 or 2; m is 1, 2, 3 or 4; and - - - - - represents an optional double bond, with the proviso that when R1 and R2 together with the bridging nitrogen form a piperidine, R3 is hydrogen, n is 0, and m is not 3; or a pharmaceutically acceptable salt, stereoisomer, or solvate thereof.