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    • 4. 发明授权
    • Use of purine derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells
    • 使用嘌呤衍生物生产用于治疗粘液性疾病的药物和与细胞中的蛋白质寻址错误有关的疾病
    • US08492420B2
    • 2013-07-23
    • US11786754
    • 2007-04-12
    • Frédéric BecqLaurent Meijer
    • Frédéric BecqLaurent Meijer
    • A01N43/50A61K31/415
    • A61K31/52
    • The invention relates to the use of purine derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells, said derivatives being of formula (I): where R2, R6 and R9, independently=halogen, a R—NH—, R—NH—NH—, NH2—R′—NH or R—NH—R′—NH— group, where R=straight or branched chain saturated or unsaturated alkyl, aryl, cycloalkyl, or heterocyclyl group, R′=straight or branched chain, saturated or unsaturated alkylene, arylene or cycloalkylene, R and R′ each include 1 to 8 carbon atoms optionally substituted with one or more —OH, halogen, amino or alkyl groups, R2 furthermore may be a heterocycle optionally with a straight or branched chain saturated or unsaturated alkyl, aryl or cycloaryl or a heterocycle optionally substituted by one or more —OH, halogen, amino or alkyl groups, R9 furthermore may be a straight or branched chain saturated or unsaturated alkyl, aryl or cycloalkyl and R2 and R9 furthermore may be hydrogen with the exception of 2-(2-hydroxyethylamino)-6-benzylamino-9-methylpurine.
    • 本发明涉及嘌呤衍生物用于生产药物用于治疗粘液性疾病和与细胞中蛋白质寻址错误相关的疾病的用途,所述衍生物具有式(I):其中R2,R6和R9独立地为卤素, R-NH-,R-NH-NH-,NH2-R'-NH或R-NH-R'-NH-基,其中R =直链或支链饱和或不饱和的烷基,芳基,环烷基或杂环基, R'=直链或支链,饱和或不饱和的亚烷基,亚芳基或亚环烷基,R和R'各自包含任选被一个或多个-OH,卤素,氨基或烷基取代的1至8个碳原子,此外,R 2也可以是杂环 任选地具有直链或支链饱和或不饱和的烷基,芳基或环芳基或任选被一个或多个-OH,卤素,氨基或烷基取代的杂环,R 9还可以是直链或支链饱和或不饱和的烷基,芳基或 环烷基,R2和R9另外可以是氢 除了2-(2-羟乙基氨基)-6-苄氨基-9-甲基嘌呤外。
    • 6. 发明授权
    • Use of paullone derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells
    • 使用paullone衍生物生产用于治疗粘液性疾病的药物和与细胞中蛋白质寻址错误有关的疾病
    • US07605153B2
    • 2009-10-20
    • US11786784
    • 2007-04-12
    • Frédéric BecqLaurent MeijerConrad Kunick
    • Frédéric BecqLaurent MeijerConrad Kunick
    • A61K31/55A61P11/00
    • A61K31/55
    • The invention relates to paullone derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells, said derivatives being of general formula (1): wherein X═C═O, C—S—CH3, C—S, —C—NHOH, Z—C or N, Y— with the adjacent ring, a phenyl or thienyl group, the ring(s) of said derivatives being optionally substituted with one or more halogen atoms, hydroxy, alkylenehydroxy, alkynealkylenehydroxy, alkynehydroxycyclohexyl, alkyl, alkoxy, alkylenealkoxy, or alkylenecyano groups where the alkylene group is either saturated or unsaturated, the groups having a straight or branched chain with C1 to C18, said chain being optionally substituted with one or more hydroxy or amino groups, or one or more trifluoromethyl, —COM, —COOM, or —CH2COOM groups (where M=H, C1 to C18 straight or branched chain alkyl, optionally substituted with one or more hydroxy and/or amino groups) nitroso, or cyano, R5═H, or C1 to C5 alkyl and R12═H, or —C—CO2—(CH3)3 and the physiologically-acceptable salts and derivatives thereof.
    • 本发明涉及用于生产用于治疗粘液性疾病的药物的paullone衍生物和与细胞中的蛋白质寻址错误有关的疾病,所述衍生物为通式(1):其中XCO,CS-CH3,CS,-C-NHOH, ZC或N,Y-与相邻的环,苯基或噻吩基,所述衍生物的环任选被一个或多个卤素原子取代,羟基,亚烷基羟基,亚炔基亚烷基羟基,炔羟基环己基,烷基,烷氧基,亚烷基烷氧基或 亚烷基基团,其中亚烷基是饱和或不饱和的,该基团具有C1至C18的直链或支链,所述链任选被一个或多个羟基或氨基取代,或一个或多个三氟甲基-COM,-COOM 或-CH 2 COOM基团(其中M = H,C1至C18直链或支链烷基,任选被一个或多个羟基和/或氨基取代)亚硝基或氰基,R 5 -H或C 1至C 5烷基和R 12 - H或 - C-CO 2 - (CH 3)3及其生理学上可接受的盐和衍生物。