发明名称 1,4-DIHYDRO-NAPHTHYRIDINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION AND USE THEREOF
摘要 Disclosed are 1,4-dihydro-naphthyridine derivatives and pharmaceutical composition and uses thereof. The 1,4-dihydro-naphthyridine derivatives are a compound capable of inhibiting acetylcholinesterase activity and preventing extracellular calcium from flowing into a cell via a calcium channel, i.e., having a dual-activity, which are of potential importance as a pharmaceutical and can be used to prepare the drugs for treating cardiovascular diseases, cerebrovascular diseases and dementia.
申请公布号 US2014364443(A1) 申请公布日期 2014.12.11
申请号 US201214362735 申请日期 2012.12.07
申请人 Chen Rong;Feng Lin;Zhang Zhengping;Fang Fang;Dong Qingli;Li Fulong;Wang Lei;Hua Yao;Yang Shibao;Wang Peng 发明人 Chen Rong;Feng Lin;Zhang Zhengping;Fang Fang;Dong Qingli;Li Fulong;Wang Lei;Hua Yao;Yang Shibao;Wang Peng
分类号 C07D495/14;C07D471/14;C07D471/04 主分类号 C07D495/14
代理机构 代理人
主权项 1. A type of compounds of formula I or the pharmaceutically acceptable salts thereof, wherein, R is selected from the group consisting of aryl and heteroaryl, and said aryl or heteroaryl is optionally substituted on the ring by halogen atom, hydroxy, sulfhydryl, amino, nitro, cyano, trihaloalkyl, carboxyl, acyl, alkoxyl, aryl, heteroaryl, heteroalicyclic group, C1-C10 alkyl, C3-C8 cycloalkyl, C2-C8 alkenyl or C2-C8 alkynyl, wherein the substituents on any two positions can be combined to form aliphatic ring, heterocyclic ring, aromatic ring, or heteroaromatic ring, and —CH2— on said C1-C10 alkyl, C3-C8 cycloalkyl, C2-C8 alkenyl or C2-C8 alkynyl can be optionally replaced by one or two or more of —O—, —S—, —SO2—, —C(O)— or/and —NR6—, and said C1-C10 alkyl, C3-C8 cycloalkyl, C2-C8 alkenyl or C2-C8 alkynyl can be optionally substituted by one or two or more of halogen atom, cyano, nitro, aryl, heteroaryl, aryloxy, heteroalicyclic group, amino, hydroxyl and —NR4R5; X is selected from the group consisting of —O— and —NR7—; R4 and R5 are independently selected from the group consisting of hydrogen, aryl, heteroaryl, C1-C8 alkyl, C3-C8 cycloalkyl, C2-C8 alkenyl and C2-C8 alkynyl, or R4 and R5 are combined to form a heteroalicyclic group; R6 and R7 are independently selected from the group consisting of hydrogen, aryl, heteroaryl, C1-C8 alkyl, C3-C8 cycloalkyl, C2-C8 alkenyl and C2-C8 alkynyl; R1 is selected from the group consisting of hydrogen, hydroxy, aryl, heteroaryl, C1-C8 alkyl, C3-C8 cycloalkyl, C2-C8 alkenyl and C2-C8 alkynyl, and optional —CH2— on said C1-C8 alkyl, C3-C8 cycloalkyl, C2-C8 alkenyl or C2-C8 alkynyl can be replaced by one or two or more of —O—, —S—, —SO2—, —C(O)— or/and —NR6—, and any position on said C1-C8 alkyl, C3-C8 cycloalkyl, C2-C8 alkenyl or C2-C8 alkynyl can be optionally substituted by one or two or more of halogen atom, cyano, nitro, aryl, heteroaryl, amino and —NR4R5; R2 is selected from the group consisting of hydrogen, halogen atom, nitro, amino, hydroxy, trihaloalkyl, C1-C8 alkyl, C3-C8 cycloalkyl, C2-C8 alkenyl and C2-C8 alkynyl, and optional —CH2— on said C1-C8 alkyl, C3-C8 cycloalkyl, C2-C8 alkenyl or C2-C8 alkynyl can be replaced by one or two or more of —O—, —S—, —SO2—, —C(O)— or/and —NR6—, and any position on said C1-C8 alkyl, C3-C8 cycloalkyl, C2-C8 alkenyl or C2-C8 alkynyl can be optionally substituted by one or two or more of halogen atom, cyano, nitro, aryl, heteroaryl, amino and —NR4R5; R3 is selected from the group consisting of hydrogen, C1-C8 alkyl and C3-C8 cycloalkyl, and —CH2— on said C1-C8 alkyl or C3-C8 cycloalkyl can be optionally replaced by one or two or more of —O—, —S—, —SO2—, —C(O)— or/and —NR6—, and any position on said C1-C8 alkyl or C3-C8 cycloalkyl can be optionally substituted by one or two or more of halogen atom, cyano, nitro, aryl, heteroaryl, amino and —NR4R5; Y is selected from the group consisting of C2-C8 alkenylene, C2-C8 alkynylene and non-hydrogen substituted C2-C8 alkylene, and optional —CH2— on said C2-C8 alkenylene, C2-C8 alkynylene or non-hydrogen substituted C2-C8 alkylene can be optionally replaced by one or two or more of —O—, —S—, —C(O)— or/and —NR6—, and any position on said replaced or unreplaced C2-C8 alkenylene, C2-C8 alkynylene or non-hydrogen substituted C2-C8 alkylene can be optionally substituted by one or two or more of halogen atom, hydroxy, sulfhydryl, amino, cyano, nitro, aryl, heteroaryl, heteroalicyclic group, —NR4R5, C1-C8 alkyl, C3-C8 cycloalkyl, C2-C8 alkenyl and C2-C8 alkynyl, wherein substituents on two adjacent positions can be combined to form aliphatic ring, heterocyclic ring, aromatic ring or heteroaromatic ring.
地址 Jiangsu CN