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DÉRIVÉS D'ÉTHYNYLE
专利权人:
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
申请号:
EPEP2015/053785
公开号:
WO2015/128307A1
申请日:
2015.02.24
申请国别(地区):
EP
年份:
2015
代理人:
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.La présente invention concerne des composés de formule I, dans laquelle Y est N ou C-R1' ; R1' est un hydrogène ou F ; R1 est un hydrogène, un halogène ou un alkyle inférieur substitué par un halogène ; R2 est un hydrogène ou un alkyle inférieur ; ou R2 forme avec R4 un cycle hétérocyclique à 6 chaînons contenant -CH2-CH2-O-CH2- ou -CH2-CH2-NR-C(O)- ; R est un
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