PHELLODENDRINE ANALOGS AND ALLERGY TYPE IV SUPPRESSOR CONTAINING THE SAME AS ACTIVE INGREDIENT
申请人:TSUMURA & CO.
公开号:EP0613879A1
公开(公告)日:1994-09-07
Phellodendrine analogs represented by general formula (I), wherein A represents the group (a); B represents hydrogen, lower alkyl or lower acyl, or alternatively A and B together with the adjacent nitrogen atom form a substituted 1,2,3,4-tetrahydroisoquinoline ring represented by general formula (II), R₁₁, R₁₂, R₂₁, R₂₂, R₃₁ and R₃₂ represent each hydrogen, hydroxyl or lower alkoxy; n₁ represents a number of 0 to 2; n₂ represents a number of 1 and 2; and m₁ represents a number of 0 to 1, provided tsat when A represents the group (b), and n₂ is 2, B is lower acyl, and that when A and B together form a substituted 1,2,3,4-tetrahydroisoquinoline ring, n₁ is 1 and m₁ is not 0. These analogs (I) and related compounds have an excellent activity of suppressing allergy type IV and hence are utilizable as a medicine efficacious against diseases wherein allergy type IV participates, such as chronic hepatitis, intractable asthma, nephrotic syndrome or rheumatism.
通式(I)代表的黄柏碱类似物,其中 A 代表基团(a);B 代表氢、低级烷基或低级酰基,或者 A 和 B 与相邻的氮原子一起形成取代的 1,2,3,4-四氢异喹啉环、R₁₁、R₁₂、R₂₁、R₂₂、R₃₁ 和 R₃₂ 分别代表氢、羟基或低级烷氧基;n₁ 代表 0 至 2;n₂ 代表 1 和 2;m₁ 代表 0 至 1,条件是当 A 代表基团(b),且 n₂ 为 2 时,B 为低级酰基,且当 A 和 B 共同形成取代的 1,2,3,4-四氢异喹啉环时,n₁ 为 1,m₁ 不是 0。这些类似物(I)和相关化合物具有抑制 IV 型过敏的优异活性,因此可用作对 IV 型过敏参与的疾病(如慢性肝炎、难治性哮喘、肾病综合征或风湿病)有效的药物。