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AssigneeFuji Yakuhin Kogyo Kabushiki Kaisha
InventorsTetsunori Fujisawa, Shinjiro Odake, Yasuo Morita, Tomoko Hongo, Hajime Ito, Junko Yasuda, Eiko Suda, Katsuhiro Igeta, Tadanori Morikawa
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New compounds of the general formula (I) ##STR1## (wherein R.sup.1 is a hydrogen atom, or a hydroxyl, aryl (C.sub.1 -C.sub.6)alkylene or --A--SOn--B group (A is a (C.sub.1 -C.sub.6) alkylene group; B is a (C.sub.1 -C.sub.6) alkyl, (C.sub.1 -C.sub.6) acyl, aryl or heterocyclyl group; n is 0, 1 or 2), R.sup.2 is a hydrogen atom, or a (C.sub.1 -C.sub.6) alkyl, (C.sub.1 -C.sub.6) alkyloxy 10 or (C.sub.1 -C.sub.6) alkylthio group, R.sup.3 and R.sup.4 are identical or different, representing a hydrogen atom, or a (C.sub.1 -C.sub.6) alkyl, aryl or aryl(C.sub.1 -C.sub.6)alkylene group, R.sup.5 is a --Y--C or C group (Y is a (C.sub.1 -C.sub.6) alkylene group, an oxygen atom, an imino group or a (C.sub.1 -C.sub.6) alkyleneimino group, C is a sulfonic acid, phosphonic acid, amidino, (C.sub.1 -C.sub.6) acyl, acylimidoyl, diphosphonomethine or dicarboxymethine group), and R.sup.6 is a hydrogen atom, or a nonsubstituted or substituted benzyl, trialkylsilyl, tert-butyldiphenylsilyl, tetrahydropyranyl or tert-butyl group) or stereoisomers thereof, and pharmaceutically acceptable salts thereof and solvates thereof, and the process for the preparation thereof, and metalloproteinase inhibitors which comprise one or more compounds selected from those compounds as effective ingredients and inhibit matrix metalloproteinases (MMPs) and/or TNF-.alpha. converting enzyme. Furthermore, the preparation intermediates to obtain the compounds of the formula (I) and the process for the preparation.
Compounds of the general formula (I) ##STR6## (wherein R.sup.1 is a hydrogen atom, or a hydroxyl, aryl (C.sub.1 -C.sub.6)alkylene or --A--SOn--B group (A is a (C.sub.1 -C.sub.6) alkylene group;
A metalloproteinase inhibitor, characterized in that it contains one or more compounds selected from the compounds of the general formula (I) ##STR7## (wherein R.sup.1 is a hydrogen atom, or a hydroxyl, aryl(C.sub.1 -C.sub.6)alkylene or --A--SOn--B group (A is a (C.sub.1 -C.sub.6) alkylene group;
Process for the preparation of the compounds of the general formula (I) or stereoisomers thereof, and pharmaceutically acceptable salts thereof or solvates thereof, characterized in that in the process of the preparation of the compounds of the general formula (I), a succinic acid derivative of the general formula (II) and an amine derivative of the general formula (III) are reacted to obtain an ester compound of the general formula (IV), followed by, if desired, converting D to R.sup.5, which is the aimed functional group, whereby the ester part is converted to the amide:
Process for the preparation of the compounds of the general formula (I) or stereoisomers thereof, and pharmaceutically acceptable salts thereof or solvates thereof, characterized in that in the process of the preparation of the compounds of the general formula (I), a compound of the general formula (V) and hydroxylamine or its salt, if desired, whose hydroxyl group is protected, are reacted to obtain a compound of the general formula (VI), followed by the process of the addition reaction and, if desired, of the deprotection:
Compounds of the general formula (VI) ##STR10## (wherein R.sup.1 is a hydrogen atom, or a hydroxyl, aryl (C.sub.1 -C.sub.6) alkylene or --A--SOn--B group (A is a (C.sub.1 -C.sub.6) alkylene group;
Compounds of the general formula (VII) ##STR11## (wherein R.sup.1 is a hydrogen atom, or a hydroxyl, aryl (C.sup.1 -C.sub.6)alkylene or --A--SOn--B group (A is a (C.sub.1 -C.sub.6) alkylene group;
Dependencies are inferred from the claim text.