发明名称 CYCLIC ETHER DERIVATIVES OF PYRAZOLO[1,5-A]PYRIMIDINE-3-CARBOXYAMIDE
摘要 The invention relates to Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxyamide of general formula (I) which are inhibitors of phosphodiesterase 2, useful in treating central nervous system diseases and other diseases.;In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.
申请公布号 US2017101411(A1) 申请公布日期 2017.04.13
申请号 US201615291316 申请日期 2016.10.12
申请人 Boehringer Ingelheim International GmbH 发明人 HOENKE Christoph;BERTANI Barbara;FERRARA Marco;FOSSATI Giacomo;FRATTINI Sara;GIOVANNINI Riccardo;HOBSON Scott
分类号 C07D487/04 主分类号 C07D487/04
代理机构 代理人
主权项 1. A compound of formula (I) wherein A is selected from the group Aa consisting of wherein above mentioned groups are substituted with one R5 and one R6; R1 is selected from the group R1a consisting of halogen, C1-3-alkyl- and C3-6-cycloalkyl- wherein the above mentioned C1-3-alkyl-, and C3-6-cycloalkyl-groups may optionally be substituted with 1 to 5 substituents independently selected from the group consisting of halogen, NC— and HO—; R2 is selected from the group R2a consisting of aryl and heteroaryl, wherein the above mentioned aryl and heteroaryl-groups may optionally be substituted with 1 to 5 substituents R4; R3 is selected from the group R3a consisting of H— and C1-3-alkyl-, wherein the above mentioned C1-3-alkyl-groups may optionally be substituted with 1 to 7 substituents independently from each other selected from the group consisting of halogen; R4 is independently from each other selected from the group R4a consisting of halogen, NC—, HO—, C1-4-alkyl- and C1-3-alkyl-O— wherein the above mentioned C1-4-alkyl- and C1-3-alkyl-O-groups may optionally be substituted with 1 to 5 substituents independently selected from the group consisting of HO— and F—; R5 is selected from the group R5a consisting of H—, halogen, NC—, HO— and C1-3-alkyl-, wherein the above mentioned C1-3-alkyl-group may optionally be substituted with 1 to 5 substituents independently selected from the group consisting of HO— and F—or R5 and R6 together form an group O═; R6 is selected from the group R6a consisting of H—, halogen, NC—, HO— and C1-3-alkyl-, wherein the above mentioned C1-3-alkyl-group may optionally be substituted with 1 to 5 substituents independently selected from the group consisting of HO— and F—or R5 and R6 together form a group O═; or a salt thereof.
地址 Ingelheim am Rhein DE