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    • 2. 发明公开
    • QUINONE DERIVATIVES FOR USE IN THE MODULATION OF REDOX STATUS OF INDIVIDUALS
    • CHINONDERIVATE ZUR VERWENDUNG BEI DER REGULIERUNG DES REDOXSTATUS VON PERSONEN
    • EP2892516A1
    • 2015-07-15
    • EP13765880.3
    • 2013-09-06
    • Edison Pharmaceuticals, Inc.
    • MILLER, Guy, M.SHRADER, William, D.KHEIFETS, Viktoria
    • A61K31/045A61P39/06
    • A61K31/122A61K31/05A61K31/198C07C66/00
    • Disclosed herein are compounds and methods of using such compounds for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging, or for modulating one or more energy biomarkers, normalizing one or more energy biomarkers, or enhancing one or more energy biomarkers, wherein the compound is a compound of Formula I or Formula II: wherein: R1 and R2 are independently hydrogen, (C1-C6)alkyl or —O(C1-C6)alkyl; or R1 and R2 together represent —CH═CH—CH═CH—; R3 is (C1-C6)alkyl; X is —CH═CH— or —C≡C—; m is 1-10; n is 1-5; k is 1-3, with the proviso that when k is an integer of 2 or 3, n is independently 1-5 in each occurrence of the —X—(CH2)n— group; Y is —OR4, —CN, —C(=0)OR5, —C(=0)R5, or —C(=0)N(R6)2; R4 and R5 are independently selected from the group consisting of hydrogen, —(C1-C6)alkyl, —(C1-C6)haloalkyl, —C(=0)-(C1-C6)alkyl, —C(=0)-(C1-C6)haloalkyl, —C(=0)-NH(C1-C6)alkyl, —C(=0)-N((C1-C6)alkyl)2, —C(=0)-NH2, and phenyl, wherein the phenyl group may optionally be substituted with a substituent selected from the group consisting of —(C1-C6)alkyl, -0-(C1-C6)alkyl, —(C1-C6)haloalkyl, and halo; each R6 is independently hydrogen or —(C1-C6)alkyl; and M is —H, —C(0)—R7 or —C(0)0-R7, wherein R7 is —(C1-C6)alkyl or phenyl; or a stereoisomer, mixture of stereoisomers, pharmaceutically acceptable salt, crystalline form, non-crystalline form, hydrate or solvate thereof.
    • 本文公开了使用这些化合物治疗或抑制氧化应激障碍(包括线粒体病症,受损能量加工障碍,神经退行性疾病和衰老疾病)或用于调节一种或多种能量生物标志物,使一种或多种能量生物标志物正常化的化合物和方法, 或增强一种或多种能量生物标志物,其中所述化合物是式I或式II的化合物:其中:R 1和R 2独立地是氢,(C 1 -C 6)烷基或-O(C 1 -C 6)烷基; 或者R1和R2一起表示-CH = CH-CH = CH-; R3是(C1-C6)烷基; X是-CH = CH-或-C≡C-; m为1-10; n为1-5; k为1-3,条件是当k为2或3的整数时,每个出现的-X-(CH 2)n - 基团,n独立地为1-5。 Y是-OR 4,-CN,-C(= O)OR 5,-C(= O)R 5或-C(= O)N(R 6)2; R4和R5独立地选自氢, - (C1-C6)烷基, - (C1-C6)卤代烷基,-C(= O) - (C1-C6)烷基,-C(= O) (C 1 -C 6)烷基,-C(= O)-NH(C 1 -C 6)烷基,-C(= O)-N((C 1 -C 6)烷基)2,-C(= O)-NH 2, 苯基,其中苯基可以任选被选自 - (C 1 -C 6)烷基,-O-(C 1 -C 6)烷基, - (C 1 -C 6)卤代烷基和卤素的取代基取代; 每个R 6独立地是氢或 - (C 1 -C 6)烷基; 并且M是-H,-C(O)-R7或-C(O)0-R7,其中R7是 - (C1-C6)烷基或苯基; 或立体异构体,立体异构体的混合物,药学上可接受的盐,结晶形式,非结晶形式,水合物或溶剂化物。
    • 3. 发明公开
    • BENZOQUINONE DERIVATIVES FOR TREATING OXIDATIVE STRESS DISORDERS
    • BENZOCHINONDERIVATE ZUR BEHANDLUNG VON氧化应变片
    • EP2892515A1
    • 2015-07-15
    • EP13762705.5
    • 2013-09-06
    • Edison Pharmaceuticals, Inc.
    • SHRADER, William, D.HINMAN, Andrew, W.KHEIFETS, Viktoria
    • A61K31/045A61K31/16A61K31/19A61K31/277C07C33/02C07C33/04C07C255/01C07C53/126C07C233/11A61P39/06
    • A61K31/122A61K31/05A61K31/198C07C66/00
    • Disclosed herein are compounds and methods of using such compounds for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging, or for modulating one or more energy biomarkers, normalizing one or more energy biomarkers, or enhancing one or more energy biomarkers, wherein the compound is a compound of Formula I or Formula II: wherein: R1 and R2 are independently hydrogen, (C1-C6)alkyl or —O(C1-C6)alkyl; or R1 and R2 together represent —CH═CH—CH═CH—; R3 is (C1-C6)alkyl; X is —CH═CH— or —C≡C—; m is 1-10; n is 1-5; k is 1-3, with the proviso that when k is an integer of 2 or 3, n is independently 1-5 in each occurrence of the —X—(CH2)n— group; Y is —OR4, —CN, —C(=0)OR5, —C(=0)R5, or —C(=0)N(R6)2; R4 and R5 are independently selected from the group consisting of hydrogen, —(C1-C6)alkyl, —(C1-C6)haloalkyl, —C(=0)-(C1-C6)alkyl, —C(=0)-(C1-C6)haloalkyl, —C(=0)-NH(C1-C6)alkyl, —C(=0)-N((C1-C6)alkyl)2, —C(=0)-NH2, and phenyl, wherein the phenyl group may optionally be substituted with a substituent selected from the group consisting of —(C1-C6)alkyl, -0-(C1-C6)alkyl, —(C1-C6)haloalkyl, and halo; each R6 is independently hydrogen or —(C1-C6)alkyl; and M is —H, —C(0)—R7 or —C(0)0-R7, wherein R7 is —(C1-C6)alkyl or phenyl; or a stereoisomer, mixture of stereoisomers, pharmaceutically acceptable salt, crystalline form, non-crystalline form, hydrate or solvate thereof.
    • 本文公开了使用这些化合物治疗或抑制氧化应激障碍(包括线粒体病症,受损能量加工障碍,神经退行性疾病和衰老疾病)或用于调节一种或多种能量生物标志物,使一种或多种能量生物标志物正常化的化合物和方法, 或增强一种或多种能量生物标志物,其中所述化合物是式I或式II的化合物:其中:R 1和R 2独立地是氢,(C 1 -C 6)烷基或-O(C 1 -C 6)烷基; 或者R1和R2一起表示-CH = CH-CH = CH-; R3是(C1-C6)烷基; X是-CH = CH-或-C≡C-; m为1-10; n为1-5; k为1-3,条件是当k为2或3的整数时,每个出现的-X-(CH 2)n - 基团,n独立地为1-5。 Y是-OR 4,-CN,-C(= O)OR 5,-C(= O)R 5或-C(= O)N(R 6)2; R4和R5独立地选自氢, - (C1-C6)烷基, - (C1-C6)卤代烷基,-C(= O) - (C1-C6)烷基,-C(= O) (C 1 -C 6)烷基,-C(= O)-NH(C 1 -C 6)烷基,-C(= O)-N((C 1 -C 6)烷基)2,-C(= O)-NH 2, 苯基,其中苯基可以任选被选自 - (C 1 -C 6)烷基,-O-(C 1 -C 6)烷基, - (C 1 -C 6)卤代烷基和卤素的取代基取代; 每个R 6独立地是氢或 - (C 1 -C 6)烷基; 并且M是-H,-C(O)-R 7或-C(O)O-R 7,其中R 7是 - (C 1 -C 6)烷基或苯基; 或立体异构体,立体异构体的混合物,药学上可接受的盐,结晶形式,非结晶形式,水合物或溶剂化物。