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QUINAZOLINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS
专利权人:
发明人:
申请号:
EP09744414.5
公开号:
EP2346848B1
申请日:
2009.11.04
申请国别(地区):
EP
年份:
2013
代理人:
摘要:
The present invention relates to a compounds of formula I wherein R1 is hydroxy or NRR" R and R" are independently from each other hydrogen, lower alkyl, cycloalkyl, or may form together with the N-atom to which they are attached a heteroalkyl ring R2 is hydrogen, lower alkyl, lower alkoxy, halogen, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cyano or S(O)2-Iower alkyl R3 is lower alkyl, -(CH2)m-aryl, optionally substituted by halogen, or is -(CH2)m-cycloalkyl R4 and R5 are independently from each other hydrogen or lower alkyl substituted by halogen, or are -(CR2)m-aryl or -(CR2)m-heteroaryl, wherein the rings may be substituted by one or more substituents, selected from halogen, lower alkyl, lower alkyl substituted by halogen, cyano, hydroxy, NRR" or by lower alkoxy substituted by halogen, or are -(CR2)m-cycloalkyl, optionally substituted by hydroxy or by aryl, or are a heteroalkyl ring, optionally substituted by =O or -(CR2)m-aryl, or R4 and R5 are together with the N-atom to which they are attached a heterocyclic ring system, optionally substituted by lower alkyl, aryl or halogen-substituted aryl, and R may be independently from each other hydrogen, lower alkyl or lower alkyl substituted by hydroxyl n is 1 or 2 m is 0, 1 or 2 or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinsons disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).La présente invention porte sur des composés de formule I dans laquelle R1 représente hydroxy ou NRR R et R représentent chacun, indépendamment lun de lautre, hydrogène, alkyle inférieur, cycloalkyle, ou peuvent former conjointement avec latome dazote auquel ils sont attachés un noyau hétéroalkyle R2 représente hydrogène, alkyle inférieur, alcoxy inférieur, halog
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