发明名称 ETHYNYL DERIVATIVES
摘要 The present invention relates to compounds of formula I, wherein Y is N or C-R1'; R1' is hydrogen or F; R1 is hydrogen, halogen or lower alkyl substituted by halogen; R2 is hydrogen or lower alkyl; or R2 forms together with R4 a 6 membered heterocyclic ring containing -CH2-CH2-O-CH2- or -CH2-CH2-NR-C(O)-; R is hydrogen, lower alkyl, phenyl or benzyl; R3 is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be in different positions; R4' is hydrogen, lower alkyl or lower alkoxyalkyl; R4 is hydrogen, lower alkyl, phenyl optionally substituted by halogen or lower alkoxy, or is cycloalkyl, or is pyridinyl optionally substituted by halogen, lower alkyl, lower alkoxy or =0, or is pyrimidinyl optionally substituted by lower alkyl, lower alkoxy or =0, or is 1 -lower alkyl-pyridinyl, or is pyrazinyl, or is pyridazinyl optionally substituted by lower alkyl, lower alkoxy or =0, or is l-methylpyrrolo[2,3-b]pyridine-5-yl, or is 6-imidazo[l,2- b]pyridazin-6-yl; or R4 forms together with R4' a 4, 5 or 6 membered heterocyclic ring containing -(CH2)5-, -CH2-CH2-O-CH2-CH2-, -CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-, -CH2-O-CH2-CH2- or CH2-CH2-CH2-O-CH2; R5 and R5' are hydrogen or lower alkyl; or R4 forms together with R5 a saturated 5- membered ring containing -CH2-CH2-CH2-; 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. The compounds may be used 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 WO2015128307(A1) 申请公布日期 2015.09.03
申请号 WO2015EP53785 申请日期 2015.02.24
申请人 F. HOFFMANN-LA ROCHE AG;HOFFMANN-LA ROCHE INC. 发明人 VIEIRA, ERIC;JAESCHKE, GEORG;GUBA, WOLFGANG;RICCI, ANTONIO;RUEHER, DANIEL;BIEMANS, BARBARA;PLANCHER, JEAN-MARC;O`HARA, FIONN
分类号 C07D401/14;A61K31/505;A61K31/506;A61K31/519;A61K31/527;A61P25/16;A61P25/22;C07D239/22;C07D401/04;C07D401/10;C07D403/04;C07D471/04;C07D487/04;C07D491/107;C07D498/04 主分类号 C07D401/14
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