发明名称 INDOL-AMIDE COMPOUNDS AS BETA-AMYLOID INHBITORS
摘要 The present invention provides compounds of formula (I), wherein Z, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of Alzheimer's disease.;
申请公布号 US2015274661(A1) 申请公布日期 2015.10.01
申请号 US201314436583 申请日期 2013.10.15
申请人 Hoffmann-La Roche Inc. 发明人 Baumann Karlheinz;Flohr Alexander;Jolidon Synese;Knust Henner;Luebbers Thomas;Nettekoven Matthias
分类号 C07D209/42;C07D405/14;C07D401/14;C07D403/04;C07D401/04 主分类号 C07D209/42
代理机构 代理人
主权项 1. Compounds of formula (I) wherein Z is a bond, alkylene, or alkenylene, wherein alkylene and alkenylene are optionally substituted with one, two or three substituents selected independently from the list of halo, cyano, hydroxy, and alkoxy; R1 is aryl or heteroaryl, wherein each is optionally substituted with one, two or three substituents selected independently from the list of halo, cyano, alkyl, haloalkyl, hydroxyalkyl, alkoxy and haloalkoxy; R2 is hydrogen, alkyl, haloalkyl, cyanoalkyl, or hydroxyalkyl; R3 is saturated or partially unsaturated heterocycloalkyl which is substituted with one, two, three or four R4; R4 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, hydroxy, alkoxy, oxo, —C(O)—R5, or —S(O)2—R6; wherein alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, and alkoxy are optionally substituted by one, two or three R7; R5 is hydrogen, alkyl, haloalkyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, aryl, hydroxy, or alkoxy; R6 is hydrogen, alkyl, haloalkyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, aryl, haloaryl, heteroaryl or alkylheteroaryl; R7 is halo, haloalkyl, cyano, hydroxy, alkoxy, cycloalkyl, heterocycloalkyl, aryl or —C(O)O-alkyl; and pharmaceutically acceptable salts and esters thereof.
地址 Little Falls NJ US