申请人:Ciba-Geigy Corporation
公开号:US04451471A1
公开(公告)日:1984-05-29
2,4,5-Trisubstituted thiazoles of the formula ##STR1## in which each of R.sub.1 and R.sub.2, independently of the other, represents an aryl or optionally N-oxidized heteroaryl radical each of which is unsubstituted or substituted by aliphatic hydrocarbon radicals, free, etherified or esterified hydroxy, etherified optionally S-oxidized mercapto, aliphatically substituted amino and/or trifluoromethyl, X represents thio, n represents 0, 1, or 2, and R.sub.3 represents an aliphatic hydrocarbon radical that is unsubstituted or substituted by etherified or esterified hydroxy, etherified optionally S-oxidized mercapto and/or, in a position higher than the .alpha.-position, by oxo and/or hydroxy and optionally contains, in addition to terminally bonded hydroxy, sulpho that is present in salt form, or represents an araliphatic hydrocarbon radical that is unsubstituted or substituted in the aryl moiety as indicated for R.sub.1 and R.sub.2, or represents a cycloaliphatic or cycloaliphatic-aliphatic hydrocarbon radical that is unsubstituted or substituted in a position higher than the .alpha.-position by free, etherified or esterified hydroxy, or represents a group of the formula ##STR2## in which m represents, 0, 1 or 2, R.sub.4 represents an aliphatic hydrocarbon radical that is unsubstituted or substituted by etherified or esterified hydroxy, optionally S-oxidized etherified mercapto or, in a position higher than the .alpha.-position and lower than the .omega.-position, by oxo and/or hydroxy and that is optionally interrupted by oxa or thia, which may also be S-oxidized, or, if n and m represent O, represents a direct bond, and R.sub.1 ' and R.sub.2 ' have one of the meanings given for R.sub.1 and R.sub.2, and pharmaceutically acceptable salts thereof are suitable for combating rheumatic disorders, preferably as active ingredients in anti-rheumatic medicaments. The invention relates to medicaments of this type and to non-chemical processes for their manufacture, and also to novel compounds of the formula I and to processes for their manufacture.
公式为##STR1##的2,4,5-三取代噻唑化合物,其中R.sub.1和R.sub.2中的每一个独立地代表芳基或可选择N-氧化的杂芳基基团,每个基团未取代或被脂肪烃基团、自由、醚化或酯化的羟基、醚化的可选择S-氧化巯基、脂肪烷基取代的氨基和/或三氟甲基取代,X代表硫,n代表0、1或2,R.sub.3代表未取代或被醚化或酯化的羟基、醚化的可选择S-氧化巯基和/或在比α-位置更高的位置上被酮基和/或羟基取代的脂肪烃基团,并且可能除了末端连接的羟基外,还包含以盐形式存在的磺酸基,或者代表未取代或如R.sub.1和R.sub.2所示的芳基基团取代的芳基脂肪烃基团,或者代表未取代或在比α-位置更高的位置上被自由、醚化或酯化的羟基取代的环脂肪或环脂肪-脂肪烃基团,或者代表公式##STR2##中的基团,其中m代表0、1或2,R.sub.4代表未取代或被醚化或酯化的羟基、可选择S-氧化的醚化巯基或在比α-位置和比ω-位置更低的位置上被酮基和/或羟基取代的脂肪烃基团,并且可能被氧杂环或硫杂环中断,该环也可能被S-氧化,或者如果n和m代表O,则代表直接键,R.sub.1'和R.sub.2'具有R.sub.1和R.sub.2给定的含义之一,以及其药学上可接受的盐适用于治疗风湿性疾病,优选作为抗风湿药物中的活性成分。该发明涉及这类药物以及用于其制造的非化学过程,还涉及公式I的新化合物以及其制造方法。