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    • 1. 发明授权
    • Synthesis and anticancer activity of aryl and heteroaryl-quinolin derivatives
    • 芳基和杂芳基 - 喹啉衍生物的合成和抗癌活性
    • US08524740B2
    • 2013-09-03
    • US13181978
    • 2011-07-13
    • Sheng-Chu KuoKuo-Hsiung LeeLi-Jiau HuangLi-Chen ChouTian-Shung WuTzong-Der WayJing-Gung ChungJai-Sing YangChi-Hung HuangMeng-Tung Tsai
    • Sheng-Chu KuoKuo-Hsiung LeeLi-Jiau HuangLi-Chen ChouTian-Shung WuTzong-Der WayJing-Gung ChungJai-Sing YangChi-Hung HuangMeng-Tung Tsai
    • A61K31/04C07D215/04
    • C07D493/04C07D215/22C07D215/233C07D215/38C07D401/04C07F9/60C07F9/65583C07F9/6561
    • A compound of Formula I is disclosed as follows: or a pharmaceutically acceptable salt, prodrug, solvate, or metabolite thereof, wherein R is hydrogen, P(═O)(OH)2, P(═O)(O(C1-C18)alkylene(C6-C20)aryl)2, P(═O)(OH)(OM), P(═O)(OM)2, P═O(O2M), S(═O)(OH)2, S(═O)(O(C1-C18)alkylene(C6-C20)aryl)2, S(═O)(OH)(OM), S(═O)(OM)2; M is a monovalent or divalent metal ion, or alkylammonium ion; W is (C6-C20)aryl, (C6-C20)heteroaryl, (C1-C18)alkyl(C6-C20)aryl, (C1-C18)alkyl(C6-C20)heteroaryl, hydroxy(C6-C20)aryl, hydroxy(C6-C20)heteroaryl, (C1-C18)alkoxy(C6-C20)aryl, (C1-C18)alkoxy(C6-C20)heteroaryl, (C1-C18)alkylenedioxy(C6-C20)aryl, (C1-C18)alkylenedioxy(C6-C20)heteroaryl, halo(C6-C20)aryl, halo(C6-C20)heteroaryl, (C1-C18)alkylamino(C6-C20)aryl, (C1-C18)alkylamino(C6-C20)heteroaryl, (C1-C18)cycloalkylamino(C6-C20)aryl, or (C1-C18)cycloalkylamino(C6-C20)heteroaryl, and their OR8 substutes; R5 is (C1-C18alkoxy, hydrogen, hydroxyl, O—(C1-C18)alkyl(C6-C20)aryl, halo or OR8, or R5 and R6 are (C1-C18)dioxy provided that R7 is hydrogen; R6 is hydroxyl, O—(C1-C18)alkyl(C6-C20)aryl, halo or OR8, (C1-C18)alkoxy, (C1-C18)alkylamino, or (C1-C18)cycloalkylamino, or R6 and R7 are (C1-C18)dioxy provided that R5 is hydrogen; R7 is hydrogen, halo or OR8, hydroxyl, or O—(C1-C18)alkyl(C6-C20)aryl; and R8 is P(═O)(OH)2, P(═O)(O(C1-C18)alkyl(C6-C20)aryl)2, P(═O)(OH)(OM), or P(═O)(OM)2, P═O(O2M).
    • 式I化合物公开如下:或其药学上可接受的盐,前药,溶剂合物或代谢物,其中R是氢,P(= O)(OH)2,P(= O)(O(C 1 -C 18) )亚烷基(C 6 -C 20)芳基)2,P(= O)(OH)(OM),P(= O)(OM)2,P = O(O 2 M) S(= O)(O(C1-C18)亚烷基(C6-C20)芳基)2,S(= O)(OH)(OM),S(= O)(OM) M是一价或二价金属离子或烷基铵离子; W是(C 6 -C 20)芳基,(C 6 -C 20)杂芳基,(C 1 -C 18)烷基(C 6 -C 20)芳基,(C 1 -C 18)烷基(C 6 -C 20) 羟基(C 6 -C 20)杂芳基,(C 1 -C 18)烷氧基(C 6 -C 20)芳基,(C 1 -C 18)烷氧基(C 6 -C 20)杂芳基,(C 1 -C 18)亚烷基二氧基 C 1 -C 20烷基氨基(C 6 -C 20)芳基,(C 1 -C 20)芳基,(C 1 -C 20)芳基, 杂芳基,(C1-C18)环烷基氨基(C6-C20)芳基或(C1-C18)环烷基氨基(C6-C20)杂芳基及其OR8分子; R5是(C1-C18烷氧基,氢,羟基,O-(C1-C18)烷基(C6-C20)芳基,卤素或OR8或R5和R6是(C1-C18)二氧基,条件是R7是氢; R6是羟基 ,(C 1 -C 18)烷基(C 6 -C 20)芳基,卤素或OR 8,(C 1 -C 18)烷氧基,(C 1 -C 18)烷基氨基或(C 1 -C 18)环烷基氨基或R 6和R 7为 (C 1 -C 18)烷基(C 6 -C 20)芳基; R 8为P(= O)(OH)2,P(= O) = O)(O(C 1 -C 18)烷基(C 6 -C 20)芳基)2,P(= O)(OH)(OM)或P(= O)(OM)2,P = O(O 2 M)。
    • 2. 发明申请
    • SYNTHESIS AND ANTICANCER ACTIVITY OF ARYL AND HETEROARYL-QUINOLIN DERIVATIVES
    • 芳基和喹啉衍生物的合成和反应活性
    • US20120015908A1
    • 2012-01-19
    • US13181978
    • 2011-07-13
    • Sheng-Chu KuoKuo-Hsiung LeeLi-Jiau HuangLi-Chen ChouTian-Shung WuTzong-Der WayJing-Gung ChungJai-Sing YangChi-Hung HuangMeng-Tung Tsai
    • Sheng-Chu KuoKuo-Hsiung LeeLi-Jiau HuangLi-Chen ChouTian-Shung WuTzong-Der WayJing-Gung ChungJai-Sing YangChi-Hung HuangMeng-Tung Tsai
    • A61K31/675A61K31/47C07D491/056A61K31/4741C07F9/60A61P35/00A61K31/5377C07D405/14A61K31/4709C07D413/10C07D401/10C07D215/233C07D413/14
    • C07D493/04C07D215/22C07D215/233C07D215/38C07D401/04C07F9/60C07F9/65583C07F9/6561
    • A compound of Formula I is disclosed as follows: or a pharmaceutically acceptable salt, prodrug, solvate, or metabolite thereof, wherein R is hydrogen, P(═O)(OH)2, P(═O)(O(C1-C18)alkylene(C6-C20)aryl)2, P(═O)(OH)(OM), P(═O)(OM)2, P═O(O2M), S(═O)(OH)2, S(═O)(O(C1-C18)alkylene(C6-C20)aryl)2, S(═O)(OH)(OM), S(═O)(OM)2; M is a monovalent or divalent metal ion, or alkylammonium ion; W is (C6-C20)aryl, (C6-C20)heteroaryl, (C1-C18)alkyl(C6-C20)aryl, (C1-C18)alkyl(C6-C20)heteroaryl, hydroxy(C6-C20)aryl, hydroxy(C6-C20)heteroaryl, (C1-C18)alkoxy(C6-C20)aryl, (C1-C18)alkoxy(C6-C20)heteroaryl, (C1-C18)alkylenedioxy(C6-C20)aryl, (C1-C18)alkylenedioxy(C6-C20)heteroaryl, halo(C6-C20)aryl, halo(C6-C20)heteroaryl, (C1-C18)alkylamino(C6-C20)aryl, (C1-C18)alkylamino(C6-C20)heteroaryl, (C1-C18)cycloalkylamino(C6-C20)aryl, or (C1-C18)cycloalkylamino(C6-C20)heteroaryl, and their OR8 substutes; R5 is (C1-C18alkoxy, hydrogen, hydroxyl, O—(C1-C18)alkyl(C6-C20)aryl, halo or OR8, or R5 and R6 are (C1-C18)dioxy provided that R7 is hydrogen; R6 is hydroxyl, O—(C1-C18)alkyl(C6-C20)aryl, halo or ORR, (C1-C18)alkoxy, (C1-C18)alkylamino, or (C1-C18)cycloalkylamino, or R6 and R7 are (C1-C18)dioxy provided that R5 is hydrogen; R7 is hydrogen, halo or OR8, hydroxyl, or O—(C1-C18)alkyl(C6-C20)aryl; and R8 is P(═O)(OH)2, P(═O)(O(C1-C18)alkyl(C6-C20)aryl)2, P(═O)(OH)(OM), or P(═O)(OM)2, P═O(O2M).
    • 式I的化合物公开如下:或其药学上可接受的盐,前药,溶剂合物或代谢物,其中R是氢,P(= O)(OH)2,P(= O)(O(C 1 -C 18) )亚烷基(C 6 -C 20)芳基)2,P(= O)(OH)(OM),P(= O)(OM)2,P = O(O 2 M) S(ΟO)(O(C1-C18)亚烷基(C6-C20)芳基)2,S(═0)(OH)(OM),S(ΟO)(OM) M是一价或二价金属离子或烷基铵离子; W是(C 6 -C 20)芳基,(C 6 -C 20)杂芳基,(C 1 -C 18)烷基(C 6 -C 20)芳基,(C 1 -C 18)烷基(C 6 -C 20) 羟基(C 6 -C 20)杂芳基,(C 1 -C 18)烷氧基(C 6 -C 20)芳基,(C 1 -C 18)烷氧基(C 6 -C 20)杂芳基,(C 1 -C 18)亚烷基二氧基 C 1 -C 20烷基氨基(C 6 -C 20)芳基,(C 1 -C 20)芳基,(C 1 -C 20)芳基, 杂芳基,(C1-C18)环烷基氨基(C6-C20)芳基或(C1-C18)环烷基氨基(C6-C20)杂芳基及其OR8分子; R5是(C1-C18烷氧基,氢,羟基,O-(C1-C18)烷基(C6-C20)芳基,卤素或OR8或R5和R6是(C1-C18)二氧基,条件是R7是氢; R6是羟基 ,(C 1 -C 18)烷基(C 6 -C 20)芳基,卤素或ORR,(C 1 -C 18)烷氧基,(C 1 -C 18)烷基氨基或(C 1 -C 18)环烷基氨基或R 6和R 7为 其中R 5为氢,R 7为氢,卤素或OR 8,羟基或O-(C 1 -C 18)烷基(C 6 -C 20)芳基; R 8为P(= O)(OH)2,P (O)(O(C1-C18)烷基(C6-C20)芳基)2,P(= O)(OH)(OM)或P(= O)(OM)2,P = O(O2M)。