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DERIVATIVES OF ETHYNES
专利权人:
Ф. ХОФФМАНН-ЛЯ РОШ АГ
发明人:
Биманс, Барбара,Губа, Вольфганг,Ешке, Георг,Риччи, Антонио,Рюхер, Даниэль,Виейра, Эрик
申请号:
EA201690408
公开号:
EA201690408A1
申请日:
2014.09.22
申请国别(地区):
EA
年份:
2016
代理人:
摘要:
This compound refers to compounds of the formula I, where Y is N or C — R; G is a 5- or 6-membered aromatic or heteroaromatic ring containing 0, 1, 2 or 3 heteroatoms selected from the group comprising phenyl, pyridinyl with different N-positions, imidazolyl, pyrazinyl, pyrimidinyl, thiophenyl, thiazolyl, pyrazolyl or thiadiazolyl, which is optionally substituted with 1, 2 or 3 substituents selected from the group consisting of halogen, lower alkyl, lower alkoxy, lower alkoxy, substituted with halogen or NRR '; R and R 'independently of one another represent hydrogen or lower alkyl or can 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; R 5 is hydrogen, halogen, or lower alkyl substituted with halogen; R 5 is hydrogen, halogen, or lower alkyl substituted with halogen; R4 is hydrogen, lower alkyl, lower alkoxyalkyl, cycloalkyl or heterocycloalkyl; or R together with the nearest carbon atom in group G may form a group; this A represents -CH-, -CHCHH-or -C (CH) -, R represents phenyl or pyridinyl, where the N atom in the pyridinyl group may be in different positions; or a pharmaceutically acceptable acid or acid addition salt thereof, a racemic mixture, or a corresponding enantiomer and / or optical isomer and / or stereoisomer thereof. Unexpectedly, it was found that compounds of the general formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor 4 (mGluR4), can be used to treat the diseaseДанное соединение относится к соединениям формулы Iгде Y представляет собой N или C-R; G представляет собой 5- или 6-членное ароматическое или гетероароматическое кольцо, содержащее 0, 1, 2 или 3 гетероатома, выбранное из группы, включающей фенил, пиридинил с различными N-позициями, имидазолил, пиразинил, пиримидинил, тиофенил, тиазолил, пиразолил или тиадиазолил, которое, возможно, замещено 1, 2 или 3 заместителями, выбран
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