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 MX2016002717(A) 申请公布日期 2016.06.08
申请号 MX20160002717 申请日期 2014.09.22
申请人 F. HOFFMANN-LA ROCHE AG 发明人 ANTONIO RICCI;GEORG JAESCHKE;ERIC VIEIRA;DANIEL RUEHER;WOLFGANG GUBA;BARBARA BIEMANS
分类号 C07D405/14;A61K31/517;A61P3/10;A61P25/10;A61P25/22;A61P25/24;C07D239/91;C07D401/04;C07D401/10;C07D405/04;C07D471/04;C07D473/04;C07D487/04;C07D495/04;C07D513/04 主分类号 C07D405/14
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