首页> 外国专利> 2-Thioindoles, 2-indolinethiones and polysulfides, their analogues (2-indolineselenone) (selenide), and pharmaceutical compositions based on them

2-Thioindoles, 2-indolinethiones and polysulfides, their analogues (2-indolineselenone) (selenide), and pharmaceutical compositions based on them

机译:2-硫吲哚,2-吲哚啉硫酮和多硫化物,它们的类似物(2-吲哚硒酮)(硒化物)以及基于它们的药物组合物

摘要

2-Thioindoles, 2-indolinethiones and polysulfides, their selen analogues of formula (A), wherein one or two groups -CH= of benzene ring in the formula (A) can be replaced by -N=; R1 is C-bounded substituent selected from the group comprising H, halogen, R, OH, OCOR, OR, CF3, NO2, NH2, NHR, COOH, CONHR, (CH2)nOH, (CH2)nOR, (CH2)nNH2, (CH2)nNHR or (CH2)nNRR; R2 is alkyl with 2 to 4 C or (CH2)nCOOH, (CH2)nCOOR, (CH2)nCOR, (CH2)nSO2R, (CH2)nSO2NRR, (CH2)nSO2NHR, CH=CHCOOH, (CH2)nCH(OH)COOH, (CH2)nCH(NH2)COOH, (CH2)nCONH2, (CH2)nCONHR, (CH2)nCONRR, (CH2)nCONHCH2Ph, CONHR, CONRR, CONHPh, COY, COPhCOOH, COPhCOOR, (CH2)nCONHPh, (CH2)nCONHPhR or SO2Y; n is integral number 1 to 4; R is alkyl with 1 to 4 C; R3 is H, alkyl with 1 to 4 C or benzyl; Y is cyclic residual derived from benzene, pyridine, thiophene, furane, thiazole or imidazole, which is optionally substituted by alkyl with 1 to 4 C or COOH, OH, OCOR, NH2, CONHR, CONRR, OR or NHR; R4 is S, SH, SOX or SOQ, wherein o is an integral number 1, 2 or 3 and X is H, alkyl with 1 to 4 C, benzyl or cyclic residual derived from benzene, pyridine, thiophene, furane, thiazole or imidazole and Q is another 2-thioindole residual of general formula (A); or R4 is Se, SeH, SeOX or SeOQ, wherein o is a number with the value 1, 2 or 3 and X is H, alkyl with 1 to 4 atoms C, benzyl or cyclic residual derived from benzene, pyridine, thiophene, furane, thiazole or imidazole and Q is another 2-selenoindole residual of general formula (A); and dashed lines represent additive bonds, from which is present always only one, whist the occurred double bond is endocyclic, if the residual R4 is univalent and exocyclic, if the residual R4 is bivalent; and their pharmaceutically acceptable salts, which are protein tyrosine kinases inhibitors; pharmaceutical compositions based on them.
机译:式(A)的2-硫吲哚,2-二氢吲哚硫酮和多硫化物,它们的硒类似物,其中式(A)中苯环的一个或两个-CH =基团可以被-N =取代; R1是选自以下的C键合的取代基:H,卤素,R,OH,OCOR,OR,CF3,NO2,NH2,NHR,COOH,CONHR,(CH2)nOH,(CH2)nOR,(CH2)nNH2, (CH2)nNHR或(CH2)nNRR; R 2是具有2至4个碳的烷基或(CH2)nCOOH,(CH2)nCOOR,(CH2)nCOR,(CH2)nSO2R,(CH2)nSO2NRR,(CH2)nSO2NHR,CH = CHCOOH,(CH2)nCH(OH) COOH,(CH2)nCH(NH2)COOH,(CH2)nCONH2,(CH2)nCONHR,(CH2)nCONRR,(CH2)nCONHCH2Ph,CONHR,CONRR,CONHPh,COY,COPhCOOH,COPhCOOR,(CH2)nCONHPh,(CH2 )nCONHPhR或SO2Y; n是整数1到4; R为具有1至4个碳的烷基; R3是H,具有1-4个碳的烷基或苄基; Y是衍生自苯,吡啶,噻吩,呋喃,噻唑或咪唑的环状残基,其任选地被1-4个碳的烷基或COOH,OH,OCOR,NH 2,CONHR,CONRR,OR或NHR取代; R4为S,SH,SOX或SOQ,其中o为整数1、2或3,X为H,具有1-4个碳的烷基,苄基或衍生自苯,吡啶,噻吩,呋喃,噻唑或咪唑的环状残基Q是通式(A)的另一个2-硫代吲哚残基;或R4为Se,SeH,SeOX或SeOQ,其中o为值为1、2或3的数字,X为H,具有1-4个原子的烷基C,苄基或衍生自苯,吡啶,噻吩,呋喃的环状残基,噻唑或咪唑,Q为通式(A)的另一个2-硒代吲哚残基;虚线表示加成键,如果残基R4为一价,则总是仅存在一个,而发生的双键为内环,如果残基R4为二价,则为外环。及其药学上可接受的盐,它们是蛋白质酪氨酸激酶抑制剂;基于它们的药物组合物。

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