发明名称 SUBSTITUTED PYRIDINE AZOLOPYRIMIDINE-5-(6H)-ONE COMPOUNDS
摘要 Described herein are compounds and chemical entities of Formula I, methods of their synthesis, compositions comprising them, and their use in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders.
申请公布号 US2015158885(A1) 申请公布日期 2015.06.11
申请号 US201314408942 申请日期 2013.06.18
申请人 DART NEUROSCIENCE (CAYMAN) LTD. 发明人 Allan Amy;Branstetter Bryan;Gomez Laurent;Dyck Brian;Marrone Tami Jo;Peters Marco;Weinhouse Michael I.
分类号 C07D519/00;C07D487/14;C07D471/14 主分类号 C07D519/00
代理机构 代理人
主权项 1. A chemical entity of Formula I: wherein: Y and Z are each independently —CH— or —N—, with the proviso that at least one Y or Z member is —N—; M is 0-5; R1 is each independently selected from H, halo, —CN, —C1-6alkyl, —C1-6alkynyl —C1-6haloalkyl, —C1-6thioalkyl, —C1-6thiohaloalkyl, —C1-6alkoxy, —C1-6haloalkoxy, —SO2C1-6alkyl, aryl, pyrazole, and 2-oxopyrrolidine; or two R1 members are on adjacent carbons and taken together with the carbons to which they are attached form a 5-6 member saturated or unsaturated monocylic ring system comprising one or more oxygen or nitrogen atoms, wherein the ring system is optionally substituted with one or more groups selected from halo, —C1-6alkyl, —C1-6alkoxy, and —C1-C6haloalkoxy; R3 and R4 are each independently selected from the group consisting of H, halo, —CN, —OH, —C1-6alkyl, —C1-6haloalkyl, —C1-6alkenyl, —CH2O-aryl, —C1-6alkoxy, —C1-6haloalkoxy, —C(O)CH3, —CH(OH)(CF3), —(CR10R11)0-3NR12R13, aryl, heteroaryl, heterocycloalkyl, wherein each aryl, heteroaryl and heterocycloalkyl is optionally unsubstituted or substituted with a member each independently selected from the group consisting of —CH3 and —OCH3; R10 and R11 are each independently selected from the group consisting of: —H, —F, —C1-6alkyl, —CF3, and —OH; R12 and R13 are each independently selected from the group consisting of —H, —C1-6alkyl, —CO2-benzyl, —C1-6alkyl(aryl), —C1-6alkyl(heterocycloalkyl), optionally unsubstituted or substituted aryl, —C3-6cycloalkyl, heteroaryl, and heterocycloalkyl; or R12 and R13 are taken together with the nitrogen to which they are attached form an optionally substituted heterocycloalkyl; and wherein the chemical entity is selected from the group consisting of compounds of Formula (I), pharmaceutically acceptable salts of compounds of Formula (I), pharmaceutically acceptable prodrugs of compounds of Formula (I); and pharmaceutically active metabolites of compounds of Formula (I).
地址 Grand Cayman KY