首页> 外国专利> DERIVATIVES OF STAUROSPINE AS INHIBITORS OF THE ACTIVITY OF THYROSINE QUINASA RECEPTORA FLT3.

DERIVATIVES OF STAUROSPINE AS INHIBITORS OF THE ACTIVITY OF THYROSINE QUINASA RECEPTORA FLT3.

机译:酪氨酸衍生物作为酪氨酸奎那沙蛋白受体FLT3活性的抑制剂。

摘要

The use of a staurosporine derivative selected from the compounds of ** formula ** wherein R1 and R2 are, independently of each other, alkyl unsubstituted or substituted by halogen, C6-C14 aryl, hydroxy, C1-C7 alkoxy, phenyl (C1-C7) alkoxy or phenyloxy, C1-C7 alkanoyloxy or benzoyloxy, amino, (C1-C7) -amino, (C1-C7) alkanoyl-amino, phenyl-(C1-C7) -amino, N , N-di-(C1-C7) -amino, N, N-di- (phenyl-C1-C7) alkyl-amino, cyano, mercapto, (C1-C7) alkyl-thio, carboxy, alkoxy ( C1-C7) -carbonyl, carbamoyl, N-mono- or N-alkyl (C1-C7) -carbamoyl or N, N-di-alkyl (C1-C7) -carbamoyl, sulfo, alkane (C1-C7) -sulfonyl or (C1-C7) alkoxy-sulfonyl, aminosulfonyl or N-mono- or N-(C1-C7) -aminosulfonyl or N, N-di-(C1-C7) -aminosulfonyl; hydrogen; halogen; hydroxyl; C1-C7 alkoxy; C8-C14 aryloxy; aryl (C6-C14) -alkoxy (C1-C7); C1-C7 alkanoyloxy; aryl (C6-C14) -carbonyloxy; Not me; amino monosubstituted or disubstituted by C1-C7 alkyl, C6-C14 aryl, (C6-C14) aryl (C1-C7) alkyl, C1-C7 alkanoyl or (C8-C12) -carbonyl; cyano; nitro; mercapto; (C1-C7) alkylthio; aryl (C8-C14) -thio; aryl (C8-C14) -alkyl (C1-C7) -thio; (C1-C7) alkanoyl-thio; aryl (C8-C14) -alkanoyl (C1-C7) -thio; carboxy; (C1-C7) alkoxycarbonyl; aryl (C8-C14) -alkoxy (C1-C7) -carbonyl, aryloxy (C6-C14) -carbonyl; carbamoyl; N-monosubstituted or N, N-disubstituted carbamoyl by C1-C7 alkyl, C8-C14 aryl or (C6-C14) aryl (C1-C7) alkyl; sulfo; aryl (C6-C14) -sulfonyl; aryl (C8-C14) -alkane (C1-C7) -sulfonyl; (C1-C7) alkane-sulfonyl; aminosulfonyl or N-monosubstituted or N, N-disubstituted by C1-C7 alkyl, C6-C14 aryl or (C6-C14) aryl (C1-C7) alkyl; n and m are, independently of each other, a number from and including 0 to and including 4; n '' and m '' are, independently of each other, a number from and including 1 to and including 4; R3, R4, R6 and R10 are, independently of each other, hydrogen, a C1-C7 alkyl, C1-C7 alkenyl, C1-C7 alkynyl or C1-C7 straight or branched chain alkynyl, saturated or unsaturated, substituted by acyclic substituents, C1-C29 carbocycle or (C1-C29) carbocycle-(C1-C7) alkyl, (C1-C29) carbocycle-C1-C7 alkenyl, a heterocycle with up to 20 carbon atoms and up to 9 heteroatoms, or heterocycle-C1-C7 alkyl with up to 20 carbon atoms and up to 9 heteroatoms.
机译:选自以下式**化合物的星形孢菌素衍生物的用途,其中R 1和R 2彼此独立地是未被取代或被卤素取代的烷基,C 6 -C 14芳基,羟基,C 1 -C 7烷氧基,苯基(C 1- C7)烷氧基或苯氧基,C1-C7烷酰氧基或苯甲酰氧基,氨基,(C1-C7)-氨基,(C1-C7)烷酰氨基,苯基-(C1-C7)-氨基,N,N-二-(C1 -C7)-氨基,N,N-二-(苯基-C1-C7)烷基-氨基,氰基,巯基,(C1-C7)烷硫基,羧基,烷氧基(C1-C7)-羰基,氨基甲酰基,N -单-或N-烷基(C1-C7)-氨基甲酰基或N,N-二烷基(C1-C7)-氨基甲酰基,磺基,烷烃(C1-C7)-磺酰基或(C1-C7)烷氧基-磺酰基,氨基磺酰基或N-单-或N-(C 1 -C 7)-氨基磺酰基或N,N-二-(C 1 -C 7)-氨基磺酰基;氢;卤素;羟; C1-C7烷氧基; C8-C14芳氧基;芳基(C6-C14)-烷氧基(C1-C7); C1-C7烷酰氧基;芳基(C6-C14)-羰氧基;不是我;被C 1 -C 7烷基,C 6 -C 14芳基,(C 6 -C 14)芳基,(C 1 -C 7)烷基,C 1 -C 7烷酰基或(C 8 -C 12)-羰基单取代或二取代的氨基;氰基;硝基巯基(C1-C7)烷硫基;芳基(C8-C14)-硫代;芳基(C8-C14)-烷基(C1-C7)-硫; (C1-C7)烷酰基硫基;芳基(C8-C14)-烷酰基(C1-C7)-硫;羧基(C1-C7)烷氧羰基;芳基(C8-C14)-烷氧基(C1-C7)-羰基,芳氧基(C6-C14)-羰基;氨基甲酰基;通过C 1 -C 7烷基,C 8 -C 14芳基或(C 6 -C 14)芳基(C 1 -C 7)烷基的N-单取代或N,N-二取代的氨基甲酰基;磺基芳基(C 6 -C 14)-磺酰基;芳基(C8-C14)-烷烃(C1-C7)-磺酰基; (C 1 -C 7)烷烃磺酰基;氨基磺酰基或被C 1 -C 7烷基,C 6 -C 14芳基或(C 6 -C 14)芳基(C 1 -C 7)烷基取代的N-单取代或N,N-二取代; n和m彼此独立地为0至4的数字; n”和m”彼此独立地为1至4之间的数字; R 3,R 4,R 6和R 10彼此独立地是氢,C 1 -C 7烷基,C 1 -C 7烯基,C 1 -C 7炔基或C 1 -C 7饱和或不饱和的直链或支链炔基,被无环取代基取代, C1-C29碳环或(C1-C29)碳环-(C1-C7)烷基,(C1-C29)碳环-C1-C7烯基,具有最多20个碳原子和最多9个杂原子的杂环或杂环-C1-具有最多20个碳原子和最多9个杂原子的C7烷基。

著录项

  • 公开/公告号ES2269793T3

    专利类型

  • 公开/公告日2007-04-01

    原文格式PDF

  • 申请/专利权人 NOVARTIS AG;DANA-FARBER CANCER INSTITUTE INC.;

    申请/专利号ES20020791654T

  • 发明设计人 GRIFFIN JAMES DOUGLAS;MANLEY PAUL WILLIAM;

    申请日2002-10-29

  • 分类号A61K31/535;C07D498/22;A61K31/155;A61K31/407;A61K31/55;A61K31/553;A61P19/08;A61P35/02;A61P43;C07D487/04;C07D487/14;C07D519;

  • 国家 ES

  • 入库时间 2022-08-21 20:54:33

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