发明名称 Pyrrolidino heterocycles
摘要 The invention relates to compounds of formula I;wherein A1, A2, A3, B, 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 US9540384(B2) 申请公布日期 2017.01.10
申请号 US201414554484 申请日期 2014.11.26
申请人 Hoffmann-La Roche, Inc. 发明人 Flohr Alexander;Zbinden Katrin Groebke;Koerner Matthias;Lerner Christian
分类号 C07D487/04;C07D213/68;C07D401/06;C07D401/12;C07D401/14;A61K31/4427;A61K31/4439;A61K31/444;C07D405/14;C07D213/74;C07D413/06;C07D473/30 主分类号 C07D487/04
代理机构 代理人
主权项 1. A compound of formula (I) wherein A1, A2 and A3 are C; B is C1-C4-alkylene, C2-C4-alkenylene, —O—C1-C4 alkyl or —NH—C1-C4alkyl; R1 and R2 together with the nitrogen atom to which they are attached, form a azetidinyl, morpholinyl, pyrrolidinyl, piperidinyl or pyrazolidinyl ring which can be substituted by 1 to 3 substituents independently selected from the group consisting of halogen, C1-C7-alkyl, C1-C7-hydroxyalkyl, C1-C7 alkoxy, C1-C7-haloalkyl, hydroxyl and oxo; R3 is selected from the group consisting of: R8, R9 and R10 are independently selected from hydrogen, C1-C7 alkyl or NR5R6; R11 is selected from hydrogen, halogen, C1-C7 alkyl or C1-C7 alkoxy; R12 is selected from hydrogen or C1-C7 alkyl; R13 is selected from hydrogen, C1-C7-alkyl optionally substituted by halogen, C3-C8 cycloalkyl, or —C(O)—NH2; R4 is selected from hydrogen, C1-C7-alkyl or C3-C8-cycloalkyl; R5 and R6 are independently selected from hydrogen or C1-C7-alkyl, or R5 and R6 together with the nitrogen atom to which they are attached, form a heterocycloalkyl which can be substituted by 1 to 3 substituents independently selected from the group consisting of halogen, C1-C7-alkyl, C1-C7-hydroxyalkyl, C1-C7 alkoxy, C1-C7-haloalkyl and oxo; or a pharmaceutically acceptable salts or pharmaceutically acceptable esters thereof.
地址 Little Falls NJ US