A novel benzoquinone derivative of the general formula:
[wherein R, and R2 are the same or different and each is methyl or methoxy; n is an integer of 0 to 21; m is 0 or 1, Z is a group of the formula:
(wherein R3 and R4 are the same or different and each is hydrogen or an alkyl group which may optionally be substituted or, R3 and R. together with the adjacent nitrogen atom form a morpholino group), a group of the formula: -COR5 (wherein R, is an a-amino acid residue or a substituted or unsubstituted glucosamine residue), a group of the formula:
(wherein R6 is a divalent hydrocarbon group of 1 to 3 carbon atoms), a group of the formula:
(wherein R6 has the same meaning as defined above) or a group of the formula: (-CH=CH),-COR7 (wherein I is an integer of 1 to 4 and R7 is hydroxy, methoxy or methyl)] has protocollagen-proline hydroxylase inhibiting activity, collagen biosynthesis inhibiting activity and 5-lipoxygenase suppressant activity, and is useful for the prevention and treatment of such diseases as pulmonary fibrosis, hepatocirrhosis, nephrosclerosis, arteriosclerosis, scleroderma, myelofibrosis and chronic arthritis or for the prevention and treatment of asthma, allergic rhinitis, urticaria, etc.
一种通式如下的新型苯醌衍
生物:
[其中 R 和 R2 相同或不同,各自为甲基或甲氧基;n 为 0 至 21 的整数;m 为 0 或 1;Z 为式中的基团:
(其中 R3 和 R4 相同或不同,且各自为氢或可任选被取代的烷基,或 R3 和 R.与相邻的氮原子一起形成吗啉基),一个式基团:-COR5(其中 R 是 a-
氨基酸残基或取代或未取代的
葡糖胺残基)、式中的基团
(其中 R6 为 1 至 3 个碳原子的二价烃基)、式中的基团
(其中 R6 的含义与上文所定义的相同)或式中的基团:(-CH=CH),-COR7(其中 I 为 1 至 4 的整数,R7 为羟基、甲氧基或甲基)]具有原胶原-脯
氨酸羟化酶抑制活性、胶原
生物合成抑制活性和 5-脂氧合酶抑制活性、可用于预防和治疗肺纤维化、肝硬化、肾硬化、动脉硬化、硬皮病、骨髓纤维化和慢性关节炎等疾病,或用于预防和治疗哮喘、过敏性鼻炎、荨麻疹等。