发明名称 PYRIMIDIN-2,4,6-TRION DERIVATIVES AND THEIR USE AS METALLOPROTEASE-INHIBITORS
摘要 The invention relates to substances of general formula (I), where R1 and R2, independently of each other, can be H, alkenyl or alkyl, R3 is a W-V group, where W is a bond or a linear or branched alkyl group, which is optionally interrupted by oxygen, sulphur or nitrogen and can be substituted with hydroxy-, amino-, mercapto-, alkoxy-, oxo-, carboxy-, acyl-, alkyl-, aralkyl-, aryl- or heteroaryl groups, and in which V is H, a monocyclic or bicyclic, saturated or unsaturated ring, which can possibly contain between 1 and 4 nitrogen, oxygen or sulphur atoms and can be optionally substituted with hydroxy-, amino-, mercapto-, alkoxy-, oxo-, carboxy-, acyl-, acylamido-, alkyl-, aralkyl-, aryl- or heteroaryl groups; R4 is an -N(R13)-C(O)-R5, -N(R13)-C(O)-OR5, -N(R13)-SO2-R5, -N(R13)-C(S)-R5, -N(R13)-C(S)-OR5, -N(R13)-C(O)-CR14R15(-CR16R17)n -C(O)-R5, or -N(R13)-CR14R15(-CR16R17)n-C(O)-R18 rest, which in each case is linked by the nitrogen atom to the central pyrimidin ring; n is 0 or 1; R13 has the meaning given above for R3 or with R14 or R16 possibly forms a heterocycle having between 4 and 7 members; and R5 is an alkyl-, cycloalkyl-, aralkyl-, aryl- or heteroaryl rest, whereby these rests can be substituted with hydroxy-, amino groups or halogen. R14, R15, R16 and R17, independently of each other, are hydrogen, the C alpha radical of a proteinogenic amino acid, alkyl, cycloalkyl, aryl, heteroaryl, aralkyl or heteroaralkyl, and R14 and R15 or alternatively R16 and R17 can together form a carbocycle having between 3 and 7 members; R18 is OH or N(R6R7), where R6 can be H, alkyl, cycloalkyl, aralkyl, aryl or heteroaryl and R7 is a group which, together with the N atom, represents a proteinogenic or non-proteinogenic alpha or beta amino acid or amino acid amide. In addition, R6 and R7 can together form a ring having between 4 and 7 members, which optionally contains heteroatoms such as oxygen, sulphur or nitrogen and is optionally substituted with alkyl, aralkyl, aryl or heteroaryl. The invention further relates to pharmacologically compatible salts and esters of general formula I and the use of these compounds for manufacturing medicinal products.
申请公布号 WO9858915(A3) 申请公布日期 1999.05.14
申请号 WO1998EP03740 申请日期 1998.06.19
申请人 ROCHE DIAGNOSTICS GMBH;GRAMS, FRANK;ZIMMERMANN, GERD 发明人 GRAMS, FRANK;ZIMMERMANN, GERD
分类号 A61K31/505;A61K31/506;A61P9/00;A61P9/12;A61P43/00;C07D239/60;C07D239/62;C07D403/04;C07D403/12 主分类号 A61K31/505
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