发明名称 ISOINDOLOINDOLONE DERIVATIVES, METHOD OF PREPARATION THEM AND PHARMACEUTICAL COMPOSITIONS, COMPRISING THEM
摘要 1. A compound of formula (I) : wherein: R1, R2, R3, R4, R5, R6, and R8, which can be similar or different, each means hydrogen atom or linear or branched (C1-C6) alkyl group, aryl (C1-C6) alkyl group, where alkyl can be linear or branched, hydroxyl group, linear or branched (C1-C6) alkoxy group, aryl (C1-C6) alkoxy group, in which alkoxy residue can be linear or branched, linear or branched (C1-C6) acyl group, arylcarbonyloxy group, carboxy (C1-C6) alkyl group, in which alkyl can be linear or branched or carboxy group, R7 is hydrogen atom or hydroxyl group, linear or branched (C1-C6) alkoxy group, aryl (C1-C6)alkoxy group, in which alkoxy residue can be linear or branched, linear or branched (C1-C6) acyloxy group or arylcarbonyloxy group, or one of groups R1-R8 together with one of other groups R1-R8, placed near of it, forms (C1-C2) alkylenedioxy group, its optical isomers, if exist, or its additive salts with pharmaceutically acceptable acid or base, with proviso: that minimum one of groups R1-R8 means hydroxy group, linear or branched (C1-C6) alkoxy group, linear or branched (C1-C6) acyloxy group or arylcarbonyloxy group and that compounds of formula (I) are different, and not 1,3-dimethoxy-6H isoindolo[2,1-a]indole-6-on. 2. Compound of formula (I), according to claim 1, which represents 2-hydroxy-8,9-dimethoxy-isoindolo[2,1-a]indole-6-on. 3. Method of preparation of compounds of formula (I), characterized in that the compound of formula (II): wherein R1, R2, R3 and R4 are such as said for formula (I), is subjected for reaction with N-bromesuccinimide with forming of compound of formula (III) wherein R1, R2, R3 and R4 are such as said above, which is reacted with triphenylphosphine with forming of compound of formula (IV): wherein R1, R2, R3 and R4 are such as said above, which compound is reacted with compound of formula (V): wherein R5, R6, R7and R8 are such as said for formula (I), with the forming of compound of formula (IV): wherein R1, R2, R3, R4 R5, R6, R7and R8 are such as said above, compound of formula (VI) is subjected to the reaction of regeneration agent with the resulting compound of formula (VIII): wherein R1, R2, R3, R4 R5, R6, R7and R8 are such as said above, which is subjected after to cyclization with the forming of compound of formula (I), which is, if necessary purified in accordance with normal purification method and separated, if desirable, on optical isomers according to normal separation method, and transformed, is desirable, in to additive salt with pharmaceutically acceptable acid or base. 4. Pharmaceutical compositions, comprising as an active ingredient a compound of formula (I) according to claim 1 or 2, in combination with one or more pharmaceutically acceptable inert non-toxic carriers. 5. Pharmaceutical compositions according to claim 4 for using at receiving of drugs for treating of melatoninergic system.
申请公布号 EA004035(B1) 申请公布日期 2003.12.25
申请号 EA20020000241 申请日期 2002.03.11
申请人 LES LABORATOIRES SERVIER 发明人 VERZHBINSKI, MICHEL;BOUSSAR, MARIE-FRANCOISE;ROUSSEAU, ANNE;BOUTEN, JEAN-ALBERT;DELAGRANGE, PHILIPPE
分类号 C07D487/06;A61K31/407;A61P3/04;A61P3/10;A61P9/00;A61P15/00;A61P25/00;A61P25/04;A61P25/16;A61P25/18;A61P25/20;A61P25/22;A61P25/24;A61P25/28;A61P35/00;A61P43/00;C07D487/04;(IPC1-7):C07D487/04 主分类号 C07D487/06
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