2-aryl-4-quinazolinones and their pharmaceutical compositions
    1.
    发明授权
    2-aryl-4-quinazolinones and their pharmaceutical compositions 有权
    2-芳基-4-喹唑啉酮及其药物组合物

    公开(公告)号:US08710064B2

    公开(公告)日:2014-04-29

    申请号:US13277520

    申请日:2011-10-20

    IPC分类号: A61K31/517

    摘要: Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof: wherein Ar represents R5, R6, R7, R8, R1′, R2′, R3′, R4′, R5′, R6′, R7′, R8′ independently represent H, OH, F, Cl, Br, C1 to C6 alkyl group, C1 to C6 alkoxy group, C2 to C6 alkenyl group, C2 to C6 alkenoxy group, C2 to C6 alkynyl group, C2 to C6 alkynoxy group, amine group, mono- or di-substituted amino group, cyclic C1 to C5 alkylamino group, imidazolyl group, morpholino group, piperazinyl group, optionally substituted with one or more hydroxy or halo; and X represents NH, O or S. The present invention also provides a composition comprising the compound of formula I. The compound and the composition in accordance with the present invention are effective on treating or alleviating a disease or disorder, such as malignant glioma.

    摘要翻译: 提供式I化合物或其药学上可接受的盐,溶剂合物或立体异构体:其中Ar表示R5,R6,R7,R8,R1',R2',R3',R4',R5',R6',R7' ,R8'独立地表示H,OH,F,Cl,Br,C1至C6烷基,C1至C6烷氧基,C2至C6烯基,C2至C6链烯氧基,C2至C6炔基,C2至C6炔氧基 ,胺基,单取代或二取代氨基,环C1至C5烷基氨基,咪唑基,吗啉代基,哌嗪基,任选被一个或多个羟基或卤素取代; 并且X表示NH,O或S.本发明还提供包含式I化合物的组合物。根据本发明的化合物和组合物可有效治疗或减轻疾病或病症,例如恶性胶质瘤。

    2-Aryl-4-Quinazolinones And Their Pharmaceutical Compositions
    2.
    发明申请
    2-Aryl-4-Quinazolinones And Their Pharmaceutical Compositions 有权
    2-芳基-4-喹唑啉酮及其药物组合物

    公开(公告)号:US20130102602A1

    公开(公告)日:2013-04-25

    申请号:US13277520

    申请日:2011-10-20

    摘要: Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof: wherein Ar represents R5, R6, R7, R8, R1′, R2′, R3′, R4′, R5′, R6′, R7′, R8′ independently represent H, OH, F, Cl, Br, C1 to C6 alkyl group, C1 to C6 alkoxy group, C2 to C6 alkenyl group, C2 to C6 alkenoxy group, C2 to C6 alkynyl group, C2 to C6 alkynoxy group, amine group, mono- or di-substituted amino group, cyclic C1 to C5 alkylamino group, imidazolyl group, morpholino group, piperazinyl group, optionally substituted with one or more hydroxy or halo; and X represents NH, O or S. The present invention also provides a composition comprising the compound of formula I. The compound and the composition in accordance with the present invention are effective on treating or alleviating a disease or disorder, such as malignant glioma.

    摘要翻译: 提供式I化合物或其药学上可接受的盐,溶剂合物或立体异构体:其中Ar表示R5,R6,R7,R8,R1',R2',R3',R4',R5',R6',R7' ,R8'独立地表示H,OH,F,Cl,Br,C1至C6烷基,C1至C6烷氧基,C2至C6烯基,C2至C6链烯氧基,C2至C6炔基,C2至C6炔氧基 ,胺基,单取代或二取代氨基,环C1至C5烷基氨基,咪唑基,吗啉代基,哌嗪基,任选被一个或多个羟基或卤素取代; 并且X表示NH,O或S.本发明还提供包含式I化合物的组合物。根据本发明的化合物和组合物可有效治疗或减轻疾病或病症,例如恶性胶质瘤。

    Synthesis and anticancer activity of aryl and heteroaryl-quinolin derivatives
    4.
    发明授权
    Synthesis and anticancer activity of aryl and heteroaryl-quinolin derivatives 有权
    芳基和杂芳基 - 喹啉衍生物的合成和抗癌活性

    公开(公告)号:US08524740B2

    公开(公告)日:2013-09-03

    申请号:US13181978

    申请日:2011-07-13

    IPC分类号: A61K31/04 C07D215/04

    摘要: 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).

    摘要翻译: 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)。

    SYNTHESIS AND ANTICANCER ACTIVITY OF ARYL AND HETEROARYL-QUINOLIN DERIVATIVES
    7.
    发明申请
    SYNTHESIS AND ANTICANCER ACTIVITY OF ARYL AND HETEROARYL-QUINOLIN DERIVATIVES 有权
    芳基和喹啉衍生物的合成和反应活性

    公开(公告)号:US20120015908A1

    公开(公告)日:2012-01-19

    申请号:US13181978

    申请日:2011-07-13

    摘要: 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).

    摘要翻译: 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)。