申请人:Takeda Chemical Industries, Ltd.
公开号:US05180735A1
公开(公告)日:1993-01-19
The present invention relates to a compound of the formula: ##STR1## wherein A is halogen, N(O)mR.sup.1 R.sup.2, N.sup..sym. R.sup.1 R.sup.2 R.sup.3 .multidot.X.sup..crclbar., S(O)nR.sup.1 or S.sup..sym. (O)mR.sup.1 R.sup.2 .multidot.X.sup..crclbar. where R.sup.1, R.sup.2 and R.sup.3 are each optionally substituted hydrocarbon or heterocyclic group, X.sup..crclbar. is a counter anion; m is an integer of 0 or 1; n is an integer of 0 to 2; R.sup.1 and R.sup.2 may form a nitrogen-containing or a sulfur-containing heterocyclic ring, which may further form a condensed ring, with the adjacent nitrogen atom or sulfur atom, and these nitrogen-containing or sulfur-containing heterocyclic rings may have substituents, Z is O or NR.sup.4 where R.sup.4 is hydrogen or an optionally substituted lower alkyl or aryl group, D is 2-methyl-1-propenyl group or isobutyl group, and E is hydrogen, an optionally substituted hydrocarbon or an optionally substituted acyl group; provided that, when A is chlorine, E is an optionally substituted hydrocarbon or acyl excepting dinitrobenzoyl, a salt thereof, production and use thereof. The novel cyclohexanol derivatives of the present invention have angiogenesis inhibiting activity and anti-tumor activity, and they are used as antirheumatic agents, therapeutic agents of psoriasis, therapeutic agents of diabetic retinopathy and anti-tumor agents.
本发明涉及一种化合物,其化学式为:##STR1## 其中,A是卤素、N(O)mR.sup.1 R.sup.2、N.sup..sym. R.sup.1 R.sup.2 R.sup.3 .multidot.X.sup..crclbar.、S(O)nR.sup.1或S.sup..sym. (O)mR.sup.1 R.sup.2 .multidot.X.sup..crclbar.,其中R.sup.1、R.sup.2和R.sup.3分别是可选择的取代的碳氢化合物或杂环基团,X.sup..crclbar.是一个反离子;m是0或1的整数;n是0到2的整数;R.sup.1和R.sup.2可以形成含氮或含硫杂环环,这些含氮或含硫杂环环可以进一步与相邻的氮原子或硫原子形成缩环,并且这些含氮或含硫杂环环可以有取代基,Z是O或NR.sup.4,其中R.sup.4是氢或可选择的取代的低碳基或芳基,D是2-甲基-1-丙烯基基团或异丁基基团,E是氢、可选择的取代的碳氢化合物或可选择的取代的酰基团;但当A是氯时,E是除二硝基苯甲酰基或其盐以外的可选择的取代的碳氢化合物或酰基。本发明的新型环己醇衍生物具有抑制血管生成和抗肿瘤活性,可用作抗风湿药物、牛皮癣治疗药物、糖尿病视网膜病变治疗药物和抗肿瘤药物。