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Etinilo derivatives
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
GEORG JAESCHKE,ANTONIO RICCI,DANIEL RUEHER,HEINZ STADLER,ERIC VIEIRA,LOTHAR LINDEMANN
申请号:
ARP120103716
公开号:
AR088246A1
申请日:
2012.10.05
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
Etinilo Derivatives of the formula (1), in which u is n or CH; r u2078 is Hydrogen, halogen, alkyl or alkoxy interior is lower; and (r u2074) - N -, - or - or - C (r u2075r u2075); in which r u2074 is Hydrogen or alkyl interior and r u2075 / r u2075 are independently Hydrogen or Lower alkyl, Hydroxy, alkoxy V is lower; (r u2076) - N - or C - (r u2077r u2077)In the r u2076 is Hydrogen or lower alkyl and r u2077 / r u2077 among themselves are independently Hydrogen, Lower alkyl, alkoxy or ch u2082 - Lower along with the carbon Atom to which they are United Can form a cycloalkyl c u2083 u208b u2086; r u00b9 is phenyl or heteroaryl, which are optionally. Tuidos by Halogen, alkyl or alkoxy Lower Bottom; The Number M is 0 OR 1; in the case that m is 1,R u00b3 / r u00b3 among themselves are independently Hydrogen, Lower alkyl, alkoxy or ch u2082 - Lower along with the carbon Atom to which they are United Can form a cycloalkyl c u2083 u208b u2086; n is 0 OR 1; in the case of N is 1, R u00b2 / R u00b2 among themselves are independently Hydrogen, alkyl LowerCh u2082 Lower alkoxy - or with the carbon Atom to which they are United Can form a cycloalkyl or c u2083 u208b u2086; IF m is the Number 1, and N is the number r u00b3 r u2077 0, and along with the carbon Atoms to which they are United Can form a cycloalkyl c u2084 u208b u2086; or if M and N are the Number 1 Is the Number 1,R u00b2 and r u00b3 or r u00b3 and r u2077 along with the carbon Atoms to which they are United Can form a cycloalkyl c u2084 u208b u2086; or a pharmaceutically acceptable acid Addition Salt, a racemic mixture, and / or the corresponding enantiomers or optical isomers and / or stereoisomers of the same S.It has now been found that the compounds of the General formula (1) are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).Claim 12: a process for obtaining a compound of the formula (1) described in claim 1, consisting of the following Variations: a) reacting a compo
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