ALEXANDER FLOHR,EMMANUEL PINARD,HERVE SCHAFFHAUSER,KATRIN GROEBKE ZBINDEN,THERESA MARIA BALLARD,THOMAS RYCKMANS
申请号：
BR112015032637
公开号：
BR112015032637A2
申请日:
2014.08.27
申请国别(地区):
BR
年份:
2017
代理人:
摘要：
The present invention relates to compounds of formula I wherein R1 is halogen, lower alkyl, lower alkoxy, cyano, phenyl, c (o) nhch3, c (o) nh2, halogen substituted lower alkyl or a group. five membered heteroaryl optionally substituted by lower alkyl； y1 is n or ch； y2 is ch； and if y1 is ch, y1 and y2 may form, together with the atoms of c to which they are attached, a ring containing -ch = n-n (ch3) -, -ch = n-n (h) -； x is ch or n； r is (ch 2) m -cycloalkyl, optionally substituted by hydroxy, lower alkoxy or lower alkyl, or is tetrahydropyran, optionally substituted by hydroxy or is lower alkoxy, substituted by hydroxy, or is lower alkyl substituted by a or two hydroxy, or is (ch 2) m -pyridinyl, optionally substituted by hydroxy, lower alkyl or hydroxy substituted lower alkyl, or is 1-phenyl, optionally substituted by hydroxy, lower alkyl or lower alkyl substituted by hydroxy, el is a bond, -ch (ch2oh) - or –ch2ch (oh) -； n is 0, 1 or 2； m is 0 or 1； or to a pharmaceutically acceptable acid addition salt, a racemic mixture or its enantiomer and / or corresponding optical isomers thereof. The compounds of the present invention are m1 muscarinic receptor positive allosteric (pam) modulators and thus are useful in the treatment of m1 muscarinic receptor mediated diseases such as alzheimer's disease, cognitive dysfunction, schizophrenia, pain or disorders. sleepa presente invenção refere-se a compostos de fórmula i em que r1 é halogênio, alquila inferior, alcóxi inferior, ciano, feni-la, c(o)nhch3, c(o)nh2, alquila inferior substituída por halogênio ou é um grupo heteroarila de cinco membros, opcionalmente substituído por alquila inferior； y1 é n ou ch； y2 é ch； e se y1 for ch, y1 e y2 podem formar, junto com os átomos de c aos quais eles estão ligados, um anel, contendo –ch=n-n(ch3)-, -ch=n-n(h)-； x é ch ou n； r é (ch2)m-cicloalquila, opcio-nalmente substituída por hidróxi, alcóxi inferior ou alquila inferior, ou é tetra-hidropirano, opcionalmente substituído por
