申请人:Banyu Pharmaceutical Co., Ltd.
公开号:US05306728A1
公开(公告)日:1994-04-26
Substituted amine derivatives represented by the general formula ##STR1## wherein Q is -C-D-E- F-G-M- or -N-H-I-J-K-L- [C, D, E, F, G, H, I, J, K and L are each O, S, a carbonyl group, -CHR.sup.2 -, -R.sup.b = or -NR.sup.c - (R.sup.a, R.sup.b and R.sup.c are each H or a lower alkyl group), M and N are each an aromatic ring of 5-6 members optionally having a halogen, OH, LN, a lower alkyl group or a lower alkoxy group, provided that L is not O, S, or -NR.sup.c -]; R is a heterocyclic ring of 5-6 members; R.sup.1 is H, a lower alkyl group, a lower haloalkyl group, a lower alkenyl group, a lower alkynyl group or a cycloalkyl group; R.sup.2, R.sup.3, R.sup.4, R.sup.5 R.sup.6 and R.sup.7 are each H, a halogen or a lower alkyl group or two of them denote a single bond; R.sup.8 and R.sup.9 are each F, CF.sub.3 or a lower alkyl group or are a cycloalkane in combination thereof; and R.sup.10 is H, F, CF.sub. 3 an acetoxy group, a lower alkyl group or a lower alkoxy group. These compounds inhibit biosynthesis of cholesterol in mammals by inhibiting their squalene epoxidase, and thereby lower their blood cholesterol values. Therefore, these compounds are expected to be effective as an agent for treatment and prophylaxis of diseases caused by excess of cholesterol, for example, obesity, hyperlipemia and arteriosclerosis and heart and encephalic diseases accompanying them.
通式为##STR1##的取代胺衍生物,其中Q为-C-D-E-F-G-M-或-N-H-I-J-K-L- [C,D,E,F,G,H,I,J,K和L分别为O,S,羰基,-CHR.sup.2-,-R.sup.b=或-NR.sup.c-(R.sup.a,R.sup.b和R.sup.c分别为H或较低的烷基),M和N分别为5-6个成员的芳香环,可选地具有卤素,OH,LN,较低的烷基或较低的烷氧基,前提是L不是O,S或-NR.sup.c-];R为5-6个成员的杂环环;R.sup.1为H,较低的烷基,较低的卤代烷基,较低的烯基,较低的炔基或环烷基;R.sup.2,R.sup.3,R.sup.4,R.sup.5,R.sup.6和R.sup.7分别为H,卤素或较低的烷基或其中两个表示单键;R.sup.8和R.sup.9分别为F,CF.sub.3或较低的烷基或它们的环烷烃组合;R.sup.10为H,F,CF.sub.3乙酰氧基,较低的烷基或较低的烷氧基。这些化合物通过抑制它们的角鲨烷环氧化酶抑制哺乳动物的胆固醇生物合成,从而降低它们的血液胆固醇值。因此,这些化合物被预计作为治疗和预防由胆固醇过多引起的疾病的药物是有效的,例如肥胖症,高脂血症和动脉硬化以及伴随它们的心脏和脑疾病。