发明名称 ETHYNYL DERIVATIVES
摘要 The present invention relates to compounds 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 (IA) 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 to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. 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 PH12016500427(A1) 申请公布日期 2016.05.16
申请号 PH12016500427 申请日期 2016.03.04
申请人 F-HOFFMANN-LA ROCHE AG 发明人 BIEMANS, BARBARA;GUBA, WOLFGANG;JAESCHKE, GEORG;RICCI, ANTONIO;RUEHER, DANIEL;VIEIRA, ERIC
分类号 A61K31/517;A61P3/10;A61P25/10;A61P25/22;A61P25/24;C07D239/91;C07D401/04;C07D401/10;C07D405/04;C07D405/14;C07D471/04;C07D473/04;C07D487/04;C07D495/04;C07D513/04 主分类号 A61K31/517
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