发明名称 TRIAZOLO COMPOUNDS AS PDE10 INHIBITORS
摘要 The present invention provides compounds of formula (Ia) and (Ib);;wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
申请公布号 US2015148332(A1) 申请公布日期 2015.05.28
申请号 US201414552837 申请日期 2014.11.25
申请人 HOFFMANN-LA ROCHE INC. 发明人 Flohr Alexander;Groebke Zbinden Katrin;Kuhn Bernd;Lerner Christian;Rudolph Markus;Schaffhauser Herve
分类号 C07D487/04;C07D471/04;C07D403/06 主分类号 C07D487/04
代理机构 代理人
主权项 1. A compound of formula (Ia) or (Ib) wherein B is C1-C4-alkylene, C2-C4-alkenylene, C2-C4-alkynylene, C3-C5-cycloalkyl, R1 and R2, are independently selected from hydrogen, C1-C7-alkyl optionally substituted by C3-C5-cycloalkyl; C1-C7-hydroxyalkyl, C1-C7-alkoxyalkyl, C1-C7-haloalkyl, C3-C5-cycloalkyl, R1 and R2 together with the nitrogen atom to which they are attached, form a azaspirocycloalkyl, a bicyclic ring or heterocycloalkyl which can be substituted by 1 to 3 substituents independently selected from the group consisting of halogen, C1-C7-alkyl, C1-C7-alkoxyalkyl; C1-C7-hydroxyalkyl, C1-C7-alkoxy, C1-C7 haloalkyl, hydroxyl, —NR9R10 and oxo; R3 is selected from hydrogen, C3-C5-cycloalkyl, C1-C7-alkoxyalkyl, C1-C7-haloalkyl, heterocycloalkyl, —(CH2)0,1,2-aryl optionally substituted by C1-C7-alkoxy and C1-C7-alkyl optionally substituted by C3-C5-cycloalkyl; R4 is selected from heteroaryl optionally substituted by 1 to 3 substituents selected from halogen, C1-C7-alkyl, C1-C7-hydroxyalkyl, C1-C7-haloalkoxy, C1-C7-haloalkyl, C3-C5-cycloalkyl, cyano, amino, nitro, —O—R6—C(O)—R7, —SO2R8, C1-C2-alkoxy optionally substituted by C1-C2-alkoxy, heterocycloalkyl, R6 and R8 are selected from C1-C7-alkyl, R7 is selected from heterocycloalkyl, R9 and R10 are independently selected from hydrogen, C1-C7-alkyl, C(O)—O— C1-C7-alkyl.
地址 Little Falls NJ US