发明名称 DERIVATIVES OF 2-AMINOPYRAZINE-5-CARBOXAMIDE, A METHOD OF THEIR SYNTHESIS AND A DRUG AND A PHARMACEUTICAL COMPOSITION CONTAINING SAID
摘要 FIELD: organic chemistry and chemical technology, pharmacy. SUBSTANCE: invention relates to synthesis of compounds showing antagonistic activity with respect to alpha<SB>1</SB>--adrenoreceptors at the level of lower urinary way. Derivatives of 2-aminopyrazine-5-carboxamide of the general formula (I) <EMI ID=0.704 HE=27 WI=57 TI=CHI> where n = 0 or 1; R means methyl-group and in this case R means phenoxy-(C<SB>1</SB>-C<SB>4</SB>)-alkyl-group where phenoxy-group is substituted in turn with methoxy- or ethoxy-group; or R and R in combination with nitrogen atom to which they are bound form 4-(phenoxymethyl)piperide-1-yl-group where phenoxy-group is substituted with one or two (C<SB>1</SB>-C<SB>4</SB>)-alkyl groups, or 4-phenylpiperazine-1-yl-group where phenyl-group is substituted with one or two substituents taken from halogen, methoxy-, ethoxy- or (C<SB>1</SB>-C<SB>4</SB>)--alkyl-group; R means hydrogen atom or methyl-group; R means hydrogen atom; R means hydrogen atom or a group of the general formula <EMI ID=0.705 HE=12 WI=18 TI=CHI> where R means hydrogen atom, tert.-butylhydroxycarbonyl-group, 4-carbamoylpyrimidine-2-yl-group or 5-carbamoylpyrazine-2-yl-group in the form of base or acid-additive salt. Invention describes also a method of synthesis of compounds of the formula (I) and drug and a pharmaceutical composition containing compounds of the formula (I) exhibiting the above indicated activity. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 5 cl, 1 dwg, 2 tbl, 8 ex
申请公布号 RU2128176(C1) 申请公布日期 1999.03.27
申请号 RU19940016363 申请日期 1994.05.16
申请人 SINTELJABO 发明人 PASKAL' ZHORZH;BENUA MARABU;ZHAK FRUASAN
分类号 A61K31/495;A61K31/4965;A61P13/02;A61P13/08;A61P15/00;C07D241/26;C07D241/28;C07D401/12;C07D403/12;C07D403/14;(IPC1-7):C07D241/26;A61K31/505 主分类号 A61K31/495
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