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ПОХІДНІ ЕТИНІЛУ
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
Biemans, Barbara,Guba, Wolfgang,Jaeschke, Georg,Ricci, Antonio,Rueher, Daniel,Vieira, Eric
申请号:
UAA201604513
公开号:
UA116277C2
申请日:
2014.09.22
申请国别(地区):
UA
年份:
2018
代理人:
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)i-, R3 is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be in different positions; or to a pharmaccutically 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.Дана сполука стосується сполук формули І , I де Y позначає N або C-R1'; G позначає 5- або 6-членне ароматичне або гетероароматичне кільце, що містить 0, 1, 2 або 3 гетероатоми, вибране з групи, що включає феніл, піридиніл з різними N-позиціями, імідазоліл, піразиніл, піримідиніл, тіофеніл, тіазоліл, пір
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