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Pyrazine- 1,2-a indole compounds, their preparation and use in medicinal products

机译:吡嗪-[1,2-a]吲哚化合物及其制备和在医药产品中的应用

摘要

A compound of general formula (I), or a pharmaceutically acceptable enantiomer, diastereoisomer, racemate, solvate, or salt thereof: ** Formula ** wherein m is selected from 0.1, 2, 3 and 4; n is selected from 0, 1, 2, 3 and 4; represents a single or double bond; R1 represents one or more optional and independent substitutions on the benzene moiety selected from the group consisting of alkyl and halogen; R2 and R3 are independently selected from the group consisting of hydrogen, alkyl, and cycloalkyl, or R2 and R3 together form a cycloalkyl or heterocyclyl; R4 and R5 are independently selected from the group consisting of hydrogen, substituted or unsubstituted alkyl, and substituted or unsubstituted cycloalkyl, or R4 and R5 together with the bridging nitrogen atom form a substituted or unsubstituted heterocyclyl, wherein said non-substituted heterocyclyl it is a phthalimidyl; R6 is selected from the group consisting of hydrogen and alkyl; wherein the substituted groups defined above are substituted at one or more available positions by one or more suitable groups selected from OR ', = O, SR', SOR ', SO2R', OSO2R ', OSO3R', NO2, NHR ', N (R ') 2, = N-R', N (R ') COR', N (COR ') 2, N (R') SO2R ', N (R') C (= NR ') N (R' ) R ', N3, CN, halogen, COR', COOR ', OCOR', OCOOR ', OCONHR', OCON (R ') 2, CONHR', CON (R ') 2, CON (R') OR ', CON (R ') SO2R', PO (OR ') 2, PO (OR') R ', PO (OR') (N (R ') R'), C1-C12 alkyl, C3-C10 cycloalkyl, C2 alkenyl - C12, C2-C12 alkynyl, aryl and heterocyclic group, wherein each of the R 'groups is independently selected from the group consisting of hydrogen, OH, NO2, NH2, SH, CN, halogen, COH, COalkyl, COOH, C1-C12 alkyl, C3-C10 cycloalkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl and heterocyclic group.
机译:通式(I)的化合物,或其药学上可接受的对映异构体,非对映异构体,外消旋体,溶剂化物或其盐:**式**,其中m选自0.1、2、3和4; n从0、1、2、3和4中选择;代表单键或双键; R1代表选自烷基和卤素的苯部分上的一个或多个任选和独立的取代基; R2和R3独立地选自氢,烷基和环烷基,或R2和R3一起形成环烷基或杂环基; R 4和R 5独立地选自氢,取代或未取代的烷基以及取代或未取代的环烷基,或R 4和R 5与桥接的氮原子一起形成取代或未取代的杂环基,其中所述非取代的杂环基为邻苯二甲酰亚胺R6选自氢和烷基;其中上面定义的取代基在一个或多个可用位置上被一个或多个选自OR',= O,SR',SOR',SO2R',OSO2R',OSO3R',NO2,NHR',N( R')2 = N-R',N(R')COR',N(COR')2,N(R')SO2R',N(R')C(= NR')N(R') R',N3,CN,卤素,COR',COOR',OCOR',OCOOR',OCONHR',OCON(R')2,CONHR',CON(R')2,CON(R')OR',CON (R')SO2R',PO(OR')2,PO(OR')R',PO(OR')(N(R')R'),C1-C12烷基,C3-C10环烷基,C2烯基- C 12,C 2 -C 12炔基,芳基和杂环基,其中每个R'基团独立地选自氢,OH,NO 2,NH 2,SH,CN,卤素,COH,CO烷基,COOH,C1-C12烷基,C 3 -C 10环烷基,C 2 -C 12烯基,C 2 -C 12炔基,芳基和杂环基。

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