发明名称 |
1,3-DISUBSTITUTED UREAS AS ACAT INHIBITORS,AND METHOD OF PREPARING THEREOF |
摘要 |
The invention relates to 1,3-disubstituted ureas of general formula (I) where R1 is an aryl, R2 is nitro and/or amino, and X is oxygen and/or sulfur, and the method of preparing thereof which consists in treating aromatic amines with isocyanates. Isocyanates may be formed in situ and the reaction carried out in toluene, at 80°C. If the nitro group is formed, it is reduced with hydrogen in the presence of palladium catalyst to the amino group. The obtained 1,3-disubstituted ureas are inhibitors of the activity of the acyl co-enzyme A: cholesterol acyltransferase (ACAT) enzyme, and may be used to inhibit cholesterol esterification and absorption in hypercholesterolemia. |
申请公布号 |
YU35100(A) |
申请公布日期 |
2002.10.18 |
申请号 |
YU20000000351 |
申请日期 |
1998.12.16 |
申请人 |
SLOVAKOFARMA A.S. |
发明人 |
OREMUS, VLADIMIR;SMAHOVSKY, VENDELIN;FABEROVA, VIERA;KAKALIK, IVAN;SCHMIDTOVA, LUDMILA;ZEMANEK, MARIAN |
分类号 |
C07D213/74;A61K31/17;A61K31/44;A61K31/4402;A61K31/4406;A61K31/4409;A61P1/00;A61P3/06;A61P9/00;A61P43/00;C07C275/30;C07C275/34;C07C275/36;C07C323/44;C07D213/75 |
主分类号 |
C07D213/74 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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