发明名称 HETEROCYCLYLALKYNE DERIVATIVES AND THEIR USE AS MODULATORS OF mGluR5 RECEPTORS
摘要 This invention relates to compounds of formula I,;;their use as allosteric modulators of mGluR5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for the treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction, such as schizophrenia or cognitive decline, dementia or cognitive impairment, or other pathologies that can be related directly or indirectly to glutamate dysfunction.
申请公布号 US2016185798(A1) 申请公布日期 2016.06.30
申请号 US201514983277 申请日期 2015.12.29
申请人 Recordati Ireland Ltd. 发明人 Riva Carlo;De Toma Carlo;Angelico Patrizia;Poggesi Elena;Graziani Davide
分类号 C07D498/04 主分类号 C07D498/04
代理机构 代理人
主权项 1. A compound of Formula I; or an enantiomer, diastereomer, N-oxide, or a pharmaceutically acceptable salt thereof, wherein: R1 is chosen from the group consisting of an alkyl group, an optionally substituted mono-, bi- or tricyclic C1-C13 heterocyclic group containing 1 to 5 heteroatoms selected from N, O, and S; an optionally substituted mono-, bi- or tricyclic C6-C14 aryl group, an optionally substituted C3-C6 cycloalkyl group, or an optionally substituted C3-C6 cycloalkenyl group; a bond, CO, CS, CH, CH2 and an SO2 group optionally substituted by one or more R2 groups or substituents; R2 is absent or is chosen from the group consisting of an optionally substituted mono- or bicyclic C1-C9 heterocyclic group containing from 1 to 3 heteroatoms selected from nitrogen, oxygen and sulfur, an optionally substituted mono-, bi- or tricyclic C6-C14 aryl group, or an optionally substituted group chosen from alkyl, cycloalkyl, alkoxy, cycloalkyloxy, aryloxy, heteroaryloxy, alkylthio, amino, N-alkylamino, N,N-dialkylamino, and N-alkyl-N-alkoxyamino; R3 is chosen from the group consisting of an optionally substituted alkyl group, an optionally substituted mono-, bi- or tricyclic C1-C13 heterocyclic group containing 1 to 5 heteroatoms selected from N, O, and S; an optionally substituted mono-, bi- or tricyclic C6-C14 aryl group, an optionally substituted C3-C6 cycloalkyl group, and an optionally substituted C3-C6 cycloalkenyl group; and n is 1-3.
地址 Co. Cork IE