PYRRAZOLOPYRIDINE DERIVATIVES

专利名称：PYRRAZOLOPYRIDINE DERIVATIVES发明人：JABLONSKI, Philippe,NETTEKOVEN,

Matthias,PATINY-ADAM, Angelique,RATNI,Hasane,STADLER, Heinz

申请号：EP11714558.1申请日：20110415公开号：EP2560974A1公开日：20130227

摘要：The present invention relates to a compound of formula (I), wherein R is

hydrogen, lower alkyl, lower alkyl substituted by halogen, benzyl, -C(0)-lower alkyl, -C(0)-CH-lower alkoxy, -C(0)-C-cycloalkyl, -(CH)-C(0)-NR,R', -(CH)S(0)- lower alkyl or -S(0)-NR,R';o is 0 or 1; R,R' are independently from each other hydrogen or lower alkyl, or may formtogether with the N atom to which they are attached a 5 or 6 membered

heterocycloalkyl ring; R is hydrogen or lower alkyl; R is halogen, lower alkoxy, lower alkylsubstituted by halogen or lower alkoxy substituted by halogen; and may be the same ordifferent in case n is 2; n is 1 or 2; Ar is phenyl optionally substituted by one or twosubstituents selected from lower alkyl, halogen, lower alkoxy, lower alkyl substituted byhydroxy or cyano, or is a five or six membered heteroaryl group, selected from

thiophenyl or pyridinyl which are optionally substituted by lower alkyl or halogen; or to apharmaceutically active acid addition salt. It has surprisingly been found that the

compounds of formula I show a high affinity simultaneously to both the NK1 and the NK3receptors (dual NK1/NK3 receptor antagonists), useful in the treatment of schizophrenia.

申请人：F.Hoffmann-La Roche AG

地址：Grenzacherstrasse 124 4070 Basel CH

国籍：CH

代理机构：Poppe, Regina

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