发明名称 ETHYNYL DERIVATIVES
摘要 It has been surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4), useful for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
申请公布号 US2017114028(A1) 申请公布日期 2017.04.27
申请号 US201615283010 申请日期 2016.09.30
申请人 Hoffmann-La Roche Inc. 发明人 Biemans Barbara;Guba Wolfgang;Jaeschke Georg;Ricci Antonio;Rueher Daniel;Vieira Eric
分类号 C07D239/96;C07D473/04;C07D487/06;C07D475/02;C07D405/14;C07D513/04;C07D401/10;C07D401/04;C07D405/04;C07D487/04;C07D495/04 主分类号 C07D239/96
代理机构 代理人
主权项 1. A compound of formula I wherein Y is N or C—R1′; G is a 5 or 6-membered aromatic or heteroaromatic ring containing 0, 1, 2 or 3 heteroatoms, selected from the group consisting of phenyl, pyridinyl with different N-positions, imidazolyl, pyrazinyl, pyrimidinyl, thiophenyl, thiazolyl, pyrazolyl or thiadiazolyl, which are optionally substituted by 1, 2 or 3 substituents, selected from the group consisting of halogen, lower alkyl, lower alkoxy, lower alkoxy substituted by halogen or NRR′; R and R′ are independently from each other hydrogen or lower alkyl, or may form together with the N atom to which they are attached a five or six membered saturated heterocyclic group which may contain an additional oxygen, NH, or N-lower alkyl group; R1 is hydrogen, halogen or lower alkyl substituted by halogen; R1′ is hydrogen, halogen or lower alkyl substituted by halogen; R2 is hydrogen, lower alkyl, lower alkoxyalkyl, cycloalkyl or heterocycloalkyl; or R2 may form together with the closest carbon atom in group G a group  for A being —CH2—, —CH2CH2, or —C(CH3)2—, R3 is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be in different positions; or a pharmaceutically acceptable salt or acid addition salt, a racemic mixture, or its corresponding enantiomer, optical isomer, or stereoisomer thereof.
地址 Little Falls NJ US