发明名称 DERIVATIVES OF ISOSORBID MONONITRATE, UTILIZATION AS VASODILATOR AGENTS WITH REDUCED TOLERANCE
摘要 1. Compounds, which are derivatives of isosorbide mononitrate, and its pharmaceutically acceptable salts, which corresponds to following general formula (I) in which A and B individually represent any of the groups wherein Z is an oxygen atom or sulphur atom, and R is an alkyl C1-C4 group, an aryl group or an aralkyl group, eventually substituted, or the group in which R is hydrogen or an alkyl C1-C4 group, an aryl group or an aralkyl group, eventually substituted; with the proviso that: (a) one of A or B is always -ONO2, but never both of them at the same time; (b) when Z is an sulphur atom R is an alkyl C1-C4 group, an aryl group or an aralkyl group, eventually substituted; and (c) when Z is an oxygen atom R is the group in which R<1> represents the groups indicated above. 2. Compounds of claim 1, characterized in that when Z is a sulphur atom, R is a short chain C1-C4 alkyl group, and when Z is an oxygen atom, R is a hydrogen atom or a short chain C1-C4 alkyl group. 3. Compounds of claims 1 or 2, characterized in that B is the -ONO2 group. 4. The compound isosorbide 2-(2'-ethylthio) nicotinate 5-mononitrate and its pharmaceutically acceptable salts. 5. The compound isosorbide 5-(2'-ethylthio)nicotinate 2-mononitrate and its pharmaceutically acceptable salts. 6. The compound isosorbide 2-(2'-mercapto)nicotinate 5-mononitrate and its pharmaceutically acceptable salts. 7. The compound isosorbide 5-(2'-mercapto)nicotinate 2-mononitrate and its pharmaceutically acceptable salts. 8. The compound 2-acetylmercaptoisosorbide 5-mononitrate. 9. The use of the compounds of any of the claims 1 to 8 for the manufacture of a medicament with vasodilating effect for the treatment of dysfunctions of the circulatory system. 10. The use, according to claim 8, of the compounds of any of the claims 1 to 8, for the manufacture of a medicament for the treatment of cardiovascular and coronary dysfunctions.
申请公布号 EA003360(B1) 申请公布日期 2003.04.24
申请号 EA20010000422 申请日期 1999.10.04
申请人 LACER, C.A. 发明人 REPOLLES MOLINER, JOSE;PUBILL COY, FRANCISCO;CABEZA LLORENTE, LYDIA;CARBO BANUS, MARCEL;NEGRIE ROFES, CRISTINA;CERDA RIUDAVETS, JUAN ANTONIO;FERRER SISO, ALICIA;RADOMSKI, MAREK;SALAS PEREZ-RASILLA, EDUARDO;MARTINEZ BONNIN, JUAN
分类号 A61K31/34;A61P9/10;C07D493/04;(IPC1-7):C07D493/04;A61P9/00 主分类号 A61K31/34
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