首页> 外国专利> DERIVATIVES OF ARYL (HETARIL) -3-AMINOMETHYLINOLONE-2 AS INHIBITORS OF NO-SYNTHETIZE AND CYCLOXYGENASE-2, METHODS OF THEIR PRODUCTION, BIOLOGICALLY ACTIVE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS BASED ON THEIR BASIS

DERIVATIVES OF ARYL (HETARIL) -3-AMINOMETHYLINOLONE-2 AS INHIBITORS OF NO-SYNTHETIZE AND CYCLOXYGENASE-2, METHODS OF THEIR PRODUCTION, BIOLOGICALLY ACTIVE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS BASED ON THEIR BASIS

机译:作为合成抑制剂和环氧化酶-2抑制剂的芳基(氨基)-3-氨基噻吩-2-酮衍生物,其生产方法,生物活性化合物和基于其成分的药物组合物

摘要

1. Amino derivatives of aryl-3-aminomethylquinolone-2 of general formula (1): R1, R2, R3, R4 are independently the same or different and at least one of R1, R2, R3, R4 is selected from the group consisting of Alk, OAlk , Ar, OAr, CHCH, SAlk, F, Cl, Br, OCF, NO, NH, NHAlk, N (Alk); the other or other of R1, R2, R3, R4 are H, or R2 and R3 are taken together and are selected from (CH2) -, - (CH2) -, -OCO-, -OSCON-, for R1 and R4 being the same or different and selected independently from H, Alk, OAlk, Hal; R5 is independently selected from H or Alk; R6 is independently selected from H, Alk, CHNO; R7, R8, R10, R11 are independently the same or different and at least one, one of R7, R8, R10, R11 is selected from Alk, OAlk, CHOH, SAlk, Ar, OAr, F, Cl, Br, CF, OCF, COOR, COONRR, NRR, NHCOR, SONRR, NO; where R14, R15, R16, R17, R18, R19, R20, R21 are the same or different and are independently selected from H or Alk; the other or the other of R7, R8, R10, R11 are H; R9 is independently selected from H or from the following substituents: where (*) corresponds to the place of attachment of the bond of the substituent R9 to the phenyl moiety in formula (I); n = 1, 2 , 3 or 4; X is independently selected from OH or Alk; Y is independently selected from Alk, OAlk, Ar or Het; R22, R23 are independently selected from H, Alk, OAlk, SAlk, Hal, COOH, COOAlk, SOAlk, NO, CN ; R24, R25 are the same or different and are independently selected from H, Alk; R26 is independently selected from H or Alk; R27, R28 are independently selected from H, Alk, OAlk, Hal, NO, CN; or R8 and R9 are taken together and are selected from - (CH) -, - (CH) -, -OCHO-, -OCH2CH2-, with this R7, R11 are independently the same or different and are selected from H, Hal, NO; and R10 is H.R12, R13 are independently the same or different and are selected from the group consisting of H, Alk, Bz.2. The amino derivatives of aryl-3-aminomethylquinolone-2 according to claim 1, characterized in that they are selected from the group consisting of 3 - [(4-dimethylamino-phenylamino) methyl] -5,6,7-trimethoxy-1H-quinolin-2-one ; 3 - [(4-dimethylamine
机译:1.通式(1)的芳基-3-氨基甲基喹诺酮-2的氨基衍生物:R 1,R 2,R 3,R 4独立地相同或不同,并且R 1,R 2,R 3,R 4中的至少一个选自下组: Alk,OAlk,Ar,OAr,CHCH,SAlk,F,Cl,Br,OCF,NO,NH,NHAlk,N(Alk)的含量; R1,R2,R3,R4的另一个或另一个是H,或R2和R3并在一起并选自(CH2)-,-(CH2)-,-OCO-,-OSCON-,其中R1和R4为相同或不同,并且独立于H,Alk,OAlk,Hal选择; R5独立地选自H或Alk; R6独立地选自H,Alk,CHNO; R 7,R 8,R 10,R 11独立地相同或不同,并且R 7,R 8,R 10,R 11中的至少一个选自Alk,OAlk,CHOH,SAlk,Ar,OAr,F,Cl,Br,CF, OCF,COOR,COONRR,NRR,NHCOR,SONRR,NO;其中R14,R15,R16,R17,R18,R19,R20,R21相同或不同,并且独立地选自H或Alk; R7,R8,R10,R11中的另一个为H。 R9独立地选自H或以下取代基:其中(*)对应于取代基R9的键与式(I)中的苯基部分的连接位置; n = 1、2、3或4; X独立地选自OH或Alk; Y独立地选自Alk,OAlk,Ar或Het; R22,R23独立地选自H,Alk,OAlk,SAlk,Hal,COOH,COOAlk,SOAlk,NO,CN; R24,R25相同或不同,并且独立地选自H,Alk; R26独立地选自H或Alk; R27,R28独立地选自H,Alk,OAlk,Hal,NO,CN;或R8和R9合在一起并选自-(CH)-,-(CH)-,-OCHO-,-OCH2CH2-,其中R7,R11独立相同或不同,并且选自H,Hal,没有; R10为H。R12,R13独立地相同或不同,并且选自H,Alk,Bz.2。 2.根据权利要求1的芳基-3-氨基甲基喹诺酮-2的氨基衍生物,其特征在于它们选自3-[(4-二甲基氨基-苯基氨基)甲基] -5,6,7-三甲氧基-1H-喹啉-2-酮; 3-[(4-二甲胺

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