发明名称 BICYCLIC NITROGEN-CONTAINING DERIVATIVES OR THEIR SALTS WITH MINERAL AND ORGANIC ACIDS OR BASES, METHODS OF THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITION ON THEIR BASIS
摘要 FIELD: organic synthesis. SUBSTANCE: invention relates to high-efficiency angiotensin II receptor antagonists and provides compounds with general formula I: <EMI ID=0.25 HE=27 WI=42 TI=CHI> where R<SB>2B</SB> and R<SB>3B</SB>, the same or different, are hydrogen, lower alkyl, lower fluoroalkyl, and lower thioalkyl; A<SB>1B</SB>, A<SB>2B</SB>, A<SB>3B</SB> and A<SB>4B</SB> are carbon or nitrogen, one or two of them being nitrogen and at least one of them being methyne group; R<SB>3</SB> is hydrogen, hydroxyl, alkyl, hydroxyalkyl, phenyl, alkoxycarbonyl, and thioalkyl; R<SB>4</SB> hydrogen, hydroxyl, arylalkyl, arylalkoxy, aryloxy, and arylamino groups. Compound I is prepared by reaction of compound II (formula <EMI ID=0.26 HE=24 WI=24 TI=CHI>) with compound <EMI ID=0.27 HE=6 WI=45 TI=CHI> where <EMI ID=0.28 HE=6 WI=21 TI=CHI> are the same as R<SB>2B</SB> and R<SB>3B</SB> in compound I, <EMI ID=0.29 HE=6 WI=21 TI=CHI> are R<SB>4</SB> in which reactive groups can be protected, and alk is C<SB>1</SB>-C<SB>6</SB>-alkyl, to form compound III (formula <EMI ID=0.30 HE=30 WI=33 TI=CHI>) that is further subjected to cyclization. Reaction is carried out in organic solvent. EFFECT: new efficient drugs prepared. 7 cl, 38 ex
申请公布号 RU2119481(C1) 申请公布日期 1998.09.27
申请号 SU19925011269 申请日期 1992.02.06
申请人 RUSSEL' JUKLAF 发明人 FRANSUA KLEMANS;MISHEL' FORTEHN;ZHAN-LJUK AESSLEEN
分类号 A61K31/47;A61K31/498;A61K31/502;A61K31/517;A61P9/12;C07D215/06;C07D215/12;C07D215/22;C07D215/233;C07D215/36;C07D215/44;C07D237/28;C07D239/72;C07D239/74;C07D401/10;(IPC1-7):C07D215/12;A61K31/505 主分类号 A61K31/47
代理机构 代理人
主权项
地址